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1A-1FormulAtion And EvAluAtion oF PhytosomE loAdEd drug dElivEry
oF gingErol For thE trEAtmEnt oF rEsPirAtory inFEction
Singh RudRa PRataP, gangadhaRaPPa h. V.Department of
pharmaceutics, Jeypore college of pharmacy, Jeypore – 764002,
oDisha, inDia
[email protected]
ABstrActrespiratory tract infection (rti) is a well-known
issues
and influence the working of the lungs and other respiratory
organs in winter season, especially in kids and adults. the
phyto-constituent antibacterial drug [gingerol] was used to treat
rti but it exhibits pharmacological issues. to overcome these
issues and make home grown treatment more viably for the treatment
of rti, novel drug delivery (nanoparticle) based phytosome loaded
complex approach was adopted. the phytosome (gp) was prepared by
mixing of gingerol and soya lecithin using anti-solvent
precipitation technique. the phytosome loaded complex (lpc) was
prepared by loading of phytosome (glpc) in chitosan aqueous
solution and characterized & evaluated. the physical
compatibility studies demonstrated the confirmation of glpc with
soya lecithin and chitosan. the optimized glpc and gp were
irregular particle & spherical structures, with a mean particle
size of 254.01±0.05 nm (-13.11 mV) and 431.21±0.90 nm (-17.53 mV),
respectively. the % entrapment efficiency and % drug loading of
glpc (86.02±0.18 %, 08.26±0.72%) and gp (84.36±0.42%, 08.05±0.03%)
was found, respectively. the in vitro release rate of gp
(86.03±0.06%) was slower than glpc (88.93±0.33%) in ph 7.4
phosphate buffer up to 24 h by diffusion process (Korsmeyer peppas
model). glpc has shown the potent antioxidant activity, susceptible
antibacterial activity and significant anti-inflammatory activity
as compared to gp. glpc has improved the significant
bioavailability and also correlate the hematological values of glpc
on rabbit blood against the incubation of microorganisms (S. aureus
& E. coli). the prepared nanoparticle based complex of
phytosome loaded of phyto-constituent drug has the combined effect
of chitosan and phytosome which shown better sustained-release
profile and also prolonging the oral absorption rate of gingerol
with effective antibacterial activity in a better stable way at
different storage conditions than phytosome or drug with
chitosan.
Keywords: respiratory tract infection
(rti), complex of phytosome loaded (lpc), phytosome (p),
GinGerol (G).
1A-2FormulAtion And IN VIVO EvAluAtion oF FluvAstAtin
microsPhErEs
daminEni SaRithaDepartment of pharmaceutics, sultan-ul-uloom
college of pharmacy, BanJara hills, hyDeraBaD.
[email protected]
ABstrActfluvastatin sodium is a cholesterol lowering agent,
a
freely soluble and poorly bioavailable drug, frequent dosing is
required in case of conventional dosage form. the microspheres were
formulated by emulsion solvent evaporation method, using the
eudragit rs100, eudragit rl100 and also by their combination.
microspheres were characterized for the micromeritic properties,
drug loading, ftir, Dsc and scanning electron microscopy.
microparticles formed were discrete and free flowing in nature.
ftir and Dsc showed stable character of drug in microparticles and
absence of drug polymer interaction. scanning electron microscopy
revealed the surface morphology. percentage yield for the
formulations observed that for f1 to f8 is varied from 68.4 to
87.05. percentage drug entrapment efficiency was observed for the
formulations of f1 to f8 are varied from 37 to 61.3. mean particle
size ranged from 112 to 132 µm. microspheres showed a sustained
delivery for 12 hours and the mechanism of drug release was
non-fickian type diffusion. the pharmacokinetic parameters were
also evaluated for optimized formulation in rabbits and it was
found that fluvastatin microspheres showed increased t1/2 and auc
values. Ke value was less than that of pure drug. this confirms
sustained release of the drug from microspheres leading to more
residence time of the drug in the body with in therapeutic range
providing longer duration of action.
Key words: fluvastatin sodium, scanninG electron microscopy,
auc, entrapment efficiency
1A-3FormulAtion, chArActErizAtion And EvAluAtion oF FAst
dissolving Films (FdF) contAining comBinAtion oF lisinoPril And
cArvEdilol
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RudRa PRataP Singh, SoumyaShREE tRiPathy, SnigdhaRani
BEhERaJeypore college of pharmacy, Jeypore – 764002, oDisha,
inDia
[email protected]
ABstrActlisinopril (lp) is angiotensin converting enzyme
(ace)
inhibitor that is primarily used in treatment of hypertension,
congestive heart failure, heart attacks and also in preventing
renal and retinal complications of diabetes. carvedilol (cr) is a
non-selective β-adrenergic blocking agent with α-1 blocking
activity and is indicated for the management of congestive heart
failure (chf), commonly as an adjunct to ace inhibitor and
diuretics. the present investigation is aimed at formulation and
evaluation of fast dissolving films containing combination of lp
and cr. the films were prepared by solvent casting method using
combination of different polymers like hpmc e3, hpmc e5 lV, pVp and
peg as plasticizer. ft-ir studies were carried out for determining
any interaction between drug/s and polymers. the films were
evaluated for physiochemical characteristics such as weight,
thickness, surface ph, folding endurance, tensile strength, and
uniformity of drug content, kinetic release study and stability
studies. ft-ir studies indicated that no interaction between drug/s
and polymers. among all the formulations, polymers hpmc e3, hpmc e5
lV and pVp produced satisfactory results with respect of in vitro
disintegration time, percentage drug release after 5 seconds. the
mechanism of the drug release of fast release of oral films was
found to be first order kinetics. short term stability studies of
selected strips indicated that there is no significant change with
respect to drug content, percentage drug release and disintegration
of strips.
Keywords: fast dissolvinG films (fdf), lisinopril, carvedilol,
in vitro druG release.
1A-4 FormulAtion And EvAluAtion oF AtEnolol liquisolid
comPActs
RudRa PRataP Singh, diBya Ranjan, Snigdha Rani BEhERaJeypore
college of pharmacy, Jeypore – 764002, oDisha
[email protected]
ABstrActthe main objective of the present study was to
enhance
dissolution rate of atenolol. atenolol is drug of choice in
treatment of hypertension and angina pectoris. the liquisolid
tablets of atenolol were prepared by direct compression method
using peg 400, propylene glycol and tween 80 as non-volatile
solvents and sodium starch glycolate, crosspovidone and
crosscarmellose sodium as superdisintegrants. the drug
compatibility study with excipients was checked by ft-ir studies.
the granules were subjected to pre-compression and post-compression
evaluation parameters such as angle of repose, bulk density, tapped
bulk density, and weight variation, hardness, friability, drug
content, in-vitro disintegration, in-vitro dissolution and
stability studies respectively. results showed that the drug was
compatible with all excipients. the granules exhibited good flow
properties and compressibility. the tablets were subjected to
in-vitro drug release in 6.8 ph phosphate buffer. formulations ls7
and ls9 showed good dissolution profile. short-term stability
studies on promising formulations ls7 and ls9 indicated that there
were no significant changes in hardness, drug content and in-vitro
drug release. from this study, it can be concluded that dissolution
rate of atenolol liquisolid tablets can be enhanced by using
non-volatile solvents and super disintegrates.
Keywords: liquisolid compacts, atenolol, in vitro disinteGration
and dissolution.
1A-5PrEPArAtion And dEvEloPmEnt oF DOmperIDONe orAl thin Films:
A nEw gloBAl APProAch
uRaVi PatEl, ShaRBaRi mohanty, akankSha Sa, SuBhEndu SEkhaR
miShRa gayatri college of pharmacy, Department of pharmaceutics,
JamaDarpali, samBalpur, 768200
[email protected]
thin-film drug delivery has emerged as an advanced alternative
to the traditional tablets, capsules and liquids often associated
with prescription and otc medications. the oral route is most
popular route for the administration of the therapeutic agents. in
some general inconvenient cases the swallowing of tablet or
capsules may become difficult. to avoid these difficulties, several
fast dissolving drug delivery
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systems have been developed. thin films have been identified as
an alternative approach to conventional dosage forms. these are
considered to be convenient to swallow, self-administrable and fast
dissolving dosage form, which make it as a versatile platform for
drug delivery. By keeping the views of above facts our present
study is approached for preparation of oral thin films (mouth
dissolving film of Domperidone) by solvent casting method. in this
method aqueous solution was prepared by dissolving hpmc in 25ml
distilled water and was kept for 1hour to remove all the air
bubbles entrapped. then domperidone and peg were added to that
polymeric solution. to that solution, menthol and ethyl-alcohol
were added. then the mixture solution was casted as a film on petri
dish and it was dried at room temperature for 24 hours. after
drying the film was carefully removed out of the petri dish and cut
into strips of 2x2 sq cm and kept in desiccator. oral thin film of
domperidone is one such novel approach to increase consumer
acceptance by virtue of rapid dissolution, self administration
without water, % of drug content and it’s mucoadhesion time
etc.
KEy words: oral thin film, domPERidonE, solvent castinG,
hpmc, peG
1A-6dEvEloPmEnt And EvAluAtion oF BuccAl Film oF niFEdiPinE
RudRa PRataP Singh, alok mohaPatRaJeypore college of pharmacy,
Jeypore – 764002, oDisha, inDia
[email protected]
ABstrActthe present study was aimed to formulate
mucoadhesive
drug delivery system to enhance bioavailability and avoid pre
systemic metabolism. the key to develop successful buccal film by
the solvent casting technique is to select the right compatible
excipients depending on ftir studies. in this method the
mucoadhesive film was fabricated by solvent casting method with
base polymer chitosan and a combination of hydrophilic polymer like
gelatin or pVp. the prepared batches of films were evaluated for
film weight & thickness, folding endurance, drug content
uniformity of films, surface ph, swelling index, determination of
in vitro residence time, in vitro drug permeation studies, in vitro
bioadhesive strength, in vitro release study. Based on in vitro
drug release pattern (in ph 6.8 phosphate buffer), the formulations
were tested for short-term stability (at 40±75% relative humidity)
and drug-excipient
interaction (ir spectroscopy). among the formulations, the
formulation Bf2 with chitosan and gelatin in the ratio 1:1.5 showed
drug release of 90.08% in 7 hours. the sole purpose of this work is
to adhere the buccal film with the mucosa, hence formulation Bf2
was selected as best formulation. the surface ph was found to be in
the range of 6-6.5 which makes the film suitable for buccal
administration. the ph near to the neutral region decreases the
chances of mucosal irritation. the proposed work showed that the
prepared film were extent the drug release without any discomfort
in the mouth.
KEywords: mucoadhesive druG delivery system, Buccal film,
nifedipine, chitosan, Gelatin or pvp
1A-7FormulAtion And EvAluAtion oF novEl mEtFormin tABlEt to
rEducE gAstritic Acidosis on its chronic usE
RudRa PRataP Singh, uttam ChoudhuRy, SnigdhaRani BEhERaJeypore
college of pharmacy, Jeypore – 764002, oDisha, inDia
[email protected]
ABstrActpharmaceutical materials science being a fundamental
branch that continuously provides important insights, theories,
and technologies to formulation sciences. the present investigation
involves formulation of metformin tablet and to reduce gastric
acidosis caused on chronic usage of metformin. metformin is one of
the most widely used drug in the treatment of type-2 Diabetes
mellitus and it causes acidosis by gastric erosion. the objective
is to formulate an immediate release tablet of metformin with
various excipients. firstly tablets are prepared by direct
compression method and wet granulation method and prepared tablets
are subjected to preliminary characterization such as hardness
test, weight variation, friability, disintegration test, acid
neutralizing capacity and in vitro dissolution studies. Dsc and
ftir confirm the formation of molecular complex. stability study
was carried out for 15 days according to ich guidelines. the
prepared metformin tablet has shown acid neutralizing capacity
similar to marketed antacid tablet.
Keywords: taBlet dosaGe form, Gastric acidosis, in vitro druG
release, staBility study.
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1A-8dEsign And EvAluAtion oF colon sPEciFic drug dElivEry systEm
oF curcumin
RudRa PRataP Singh, SamEER kumaR BiSSoi, SnigdhaRani
BEhERaJeypore college of pharmacy, Jeypore – 764002, oDisha,
inDia
[email protected]
ABstrActcolon cancer is the development of malignant tumours
in the inner wall of the colon. research has proved that
curcumin has therapeutic potential in the management of colon
cancer. the present study is based on development of compression
coated tablet containing curcumin for colon cancer. the colon
specific drug delivery system (cDDs) should be capable of
protecting the drug in route to the colon i.e. drug release and
absorption should not occur in the stomach as well as the small
intestine, and neither the bioactive agent should be degraded in
either of the dissolution sites but only released and absorbed once
the system reaches the colon. curcumin is a poorly soluble api.
therefore in the present study cyclodextrin is used to form an
inclusion complex with curcumin to enhance the solubility. to
prepare cDDs, further this core was compressed between the layers
of polymer blend of pectin and eudragit protecting it from the
stomach and intestinal environment. total 9 formulations were
prepared to achieve solubility and site specificity. total nine
formulations are prepared by direct compression and compression
coating method. f1-f4 are formulated with various ratios of
curcumin and cyclodextrin. f5-f9 tablets are formulated with
various ratios of biodegradable polymer pectin and ph dependent
polymer eudragit. the results revealed that higher coat weight and
optimized ratio of pectin and eudragit ratio protected the curcumin
tablet till ascending colon. f9 formulation containing curcumin
& cyclodextrin in 1:2 ratio coated with eudragit & pectin
in 80:20 showed an optimum release of drug protecting it from
acidic environment. optimized formulation f9 was subjected to
accelerated stability studies by storing at 40oc/75% rh as per ich
guidelines for 3 months. it was observed that there was no
significant physical or chemical.
Keywords: colon specific druG delivery system (cdds), curcumin,
cyclodextrin pectin and eudraGit.
1A-9FormulAtion And EvAluAtion oF nAnostructurEd liPid cArriErs
oF gliPizidE For orAl dElivEry
RudRa PRataP Singh, ShaRmila daS, Snigdha Rani BEhERaJeypore
college of pharmacy, Jeypore – 764002, oDisha
gulguli41/[email protected]
ABstrActthe present study is aimed at formulating the nano
structured lipid carriers (nlc) of glipizide with the aim of
increasing the drug loading capacity and prolonging the duration of
action, there by improving the stability of conventional dosage
forms. nlc of glipizide was prepared by hot melt micro-emulsion and
hot melt probe sonication based methods. the hot melt was prepared
by heating the drug with blend of solid and liquid lipids: stearic
acid and oleic acid with and without cholesterol. the prepared hot
melt was poured into the hot aqueous surfactant solution and
subjected to rapid cooling in case of micro-emulsion method, and in
case of sonication method, is subjected to prob sonication method.
the sem photographs showed that the glipizide nlc was spherical in
shape with the average particle size of 2985.41 ± 0.08 nm and 762.1
± 0.02 nm prepared by micro-emulsion and probe sonication methods
respectively. the surface charge of the unsonicated nlc and
sonicated nlc was found to be -17.02 ± 0.03 mV and -22.0 ± 0.00 mV
respectively. the pDi index value remained approximately around
0.483 ± 0.06. all the formulations followed the higuchi model drug
release profile. the Dsc thermograms for the drug and formulation
indicated that the drug was in an amorphous form in the nlc.
stability studies indicated that the formulations stored at
refrigeration temperature and room temperature showed no
significant changes in the drug content and in vitro drug release,
after a period of 4 weeks, indicated good stability of nlc. the
method of preparation of nlc of glipizide was found to be more
simple, economical with a potential of overcoming the drawbacks
associated with conventional dosage forms of the drug.
Keywords: nanostructured lipid carriers, Glipizide, in vitro
druG release, staBility study.
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1A-10FormulAtion And oPtimizAtion oF gAstrorEtEntivE BioAdhEsivE
FloAting tABlEts oF orAl hyPogysEmic AgEnts.
dhaRmajit Pattanayak 1,2, C. m. hoSSain1, RamESh adEPu21Bengal
school of technology, suganDha hooghly, WB, 2 ViKas college of
pharmaceutical sciences, suryapet, telangana
[email protected]
the purpose of present investigation was to develop and
characterize a novel gastroretentive drug delivery system (grDDs)
for oral hypoglycemic agents possessing a unique combination of
floatation and bioadhesive properties. it was aimed to prepare for
prolonged residence in the stomach over conventional
gastroretentive approaches. the tablets are produced by direct
compression method by using hpmc K15m as hydrophilic rate retarding
polymer and carbopol 934 and carbopol 940 as Bioadhesive polymer
along with other requisite excipients in different combinations and
proportions. in this research two model anti-diabetic drugs,
glipizide & rosiglitazone are used. glipizide is an oral, rapid
and short acting hypoglycemic agent belongs to sulfonylurea class.
rosiglitazone is an antidiabetic drug in the
thiazolidinedione class. Both are prescribed to treat type-ii
diabetes and have short biological half-life. hence they are to be
administered in 2 or 3 doses in a day. moreover, stomach is the
site of absorption of both drugs. thus, the development of
gastroretentive dosage forms would clearly be advantageous. tablets
containing different ratios of polymer were designed and evaluated
for different parameters. the prepared tablets exhibited
satisfactory physical parameters and good in-vitro buoyancy. the
modified in-vitro assembly was used to measure the bioadhesive
strength of tablets with fresh gastric mucosa of a goat as model
tissue. the tablets were evaluated for in-vitro release in 1.2 ph
buffer 0.1 n hcl. it can be concluded that, hpmc K15m and carbopol
940 combination can be used to design effective and stable floating
and bioadhesive tablets for better retention in stomach.
Key words: Glipizide,rosiGlitazone, hpmc K15m, carBopol 934,
carBopol 940
1A-11study oF FormulAtion And EvAluAtion oF FAst disintEgrAting
tABlEt oF BisoProlol
SidhaRtha SankaR Padhy, VikRam ViSwajit.B.k miShRa, S.B
BhanjaDepartment of pharmaceutics, Jeypore college of pharmacy,
Jeypore, Koraput (oDisha)- 764002
[email protected]
ABstrActThe oral route of administration is considered as
the
most preferably route because of its easy of
self-administration, compactness and easy manufacturing. The
objective of the present investigation was to prepare the fast
disintegrating tablet of for respiratory disorders in case of
pediatrics. The present examination was to attempt with a view to
develop a fast disintegrating tablet so that it will offers a new
range of products which shows desired characteristics and proposed
benefits. DSc and IR spectroscopy data showed the characterization
of drug, excipient, compatibility of drug and solid dispersion with
excipients, gave evidence of solid dispersion formation and UV
absorption spectra shows enhancement of solubility. Various
pre-formulation batches (f1-f10) formulated by direct compression
method using different concentration of polymer such as ac-di-sol
and it was studied for pre and post compression evaluation.
Formulation with ac-di-sol Batch no. F9 shows excellent result with
disintegration time of 105 sec, drug content of 99.35%, and greater
dissolution rate 98.32%at 40 min. Fast disintegrating tablets are
used by a most of the populations who find it difficulty in
swallowing. It has been investigated for their potential in
improving bioavailability of most poorly soluble drug. It shows its
effect by enhancing the dissolution profile of the drug as well as
hepatic metabolism of drugs.
Key words: fdt, Bisoprolol, disinteGration, lyophilization,
dimethylsulphoxide
1A-12FormulAtion And EvAluAtion oF nicArdiPinE sustAinEd
rElEAsEd tABlEts
guidEd By: C Soujanya PRESEnting authoR: S.SuPRitha REddy
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Dept. of pharmaceutics, Vishnu institute of pharmaceutical
eDucation anD research, narsapur meDaK, telanagana,
inDia-502313
ABstrActthe purpose of this research was to develop
nicardipine
sustained release (30 mg) matrix tablets, which is an calcium
channel blocker drug it is designed to attain the gastric residence
time , good oral bioavailiblity and thus prolonging the drug
release by comparing with marketed product (cardene sr 30 mg)
tablets. in the present study the tablets were formulated by direct
compression technique using different hydrophilic polymer grades
such as cmec, xantham gum, ethyl cellulose with granulating agent
as mcc and lactose, as the other ingredients before formulation,
the granules were evaluated by pre-compression studies. the
obtained tablets were evaluated with different parameters like
hardness, friability, thickness, weight variation , drug content,
in vitro dissolution studies. the tablets containing nicardipine
released from 1:2 ratio to 93% of the drug at the end of 16th hour
by in vitro released study. the formulation f7 was selected as an
optimised formulation because it gives the best results in terms of
required in vitro drug release in a sustained released manner and
best fitted to first order model with r^2 value as 0.989. short
term stability studies indicated no. appreciable changes in drug
content and in vitro drug release of optimised formula f7.
Keywords: nicardipine, hydrophilic, and natural polymers,
sustained release.
1A-13FormulAtion And chArActErizAtion oF KEtAconAzolE
microsPongEs using vArious PolymErs For toPicAl drug dElivEry
systEm
PaRimalakRiShnan. S, anton Smith. a, muRali. R, muRalikRiShna,
ajithkumaR, jaCoBDepartment of pharmacy, annamalai uniVersity,
annamalai nagar – 608002, tamilnaDu.
[email protected]
ABstrActmicrosponges (ms) are polymeric delivery systems
composed of porous microspheres. they are small similar to
sponge and spherical particles with a big porous surface. ms may
improve stability and drug release. the aim of the present study is
to formulate and evaluation of ketoconazole microsponges
using various polymers by liquid – liquid suspension
polymerization method. ms incorporated ketoconazole (msK) with six
different proportions with polymers like eudragit rs 100 (msK i to
iii) and ethyl cellulose (msK iV to Vi) were formulated by liquid –
liquid suspension polymerization method. these formulations were
evaluated for their particle size and physical properties. the
physical properties showed that msK formulations ii and Vi have
good production yield and loading efficiency. msK ii and Vi
formulations were prepared as gel in 1.25 %w/w eudragit rs 100 and
ethyl cellulose evaluated for ph, viscosity, spreadability, drug
content and in vitro release. msK ii and Vi exhibited 3900 &
3750, 20.58 & 21.38, 85.68 & 87.81 and 92.75% & 94.69%
of viscosity (cps), spreadability (g cm/s), assay (%) and
cumulative drug release respectively. from the above findings it is
to conclude that the percentage of increase in polymer
concentration the physical properties get altered. out of six
formulations msK ii and Vi was exhibited good drug release
pattern.
Keywords: microsponGes, Ketoconazole, druG release pattern
1A-14dEsign And in vitro EvAluAtion oF gAstro rEtEntivE orAl
mAtrix tABlEt FormulAtions oF KEtorolAc tromEthAminE
ABstrActKetorolac tromethamine floating tablets were
prepared
by using combination of hydrophilic polymers such as hydroxy
propyl methyl cellulose 4000 cps grade and 100000 cps grade. eight
set of formulations were prepared by gradual increasing and
decreasing concentrations of above two polymers. the floating
pattern was found to be instant for all the formulations and best
controlled release profile was achieved for few set of
formulations. the drug content, tablet weight, friability and
weight variation were found to be within the limits. Validated uV
spectrophotometric method was developed and standard linear
regression was used to determine the concentration of released drug
during the course of dissolution. the release studies were
subjected to zero order, first order, higuchi and ritger-peppas
kinetics and the parameters for controlled release were
calculated.
KEywords:Ketorolac tromethamine, floatinG taBlets, Gastro
retentive druG delivery, hydroxy propyl methyl cellulose, uv
method.
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1A-15FormulAtion And EvAluAtion oF sumAtriPtAn orAl
disintEgrAting tABlEts By using hiBiscus rosA sinEsis
t SnEha REddy guidEd, PRaSanna kumaR dESu Vishnu institute of
pharmaceutical eDucation anD research, Vishnupur, narsapur, meDaK,
anDhrapraDesh-502313 corresponDing author
[email protected]
ABstrActoDts may be used to deliver drugs to the oral cavity,
for
local action or, in some cases, absorption across the oral
mucosa, thereby avoiding first-pass hepatic metabolism and
potentially increasing the rate and extent of uptake, and reducing
undesirable metabolites. the objectives of the research work is to
formulate oral disintegrating tablets of sumatriptan by using
natural super disintegrate i.e, hibiscus rosa sinesis in different
ratio by direct compression technique and tablets were evaluated
for precompressional parameters such as angle of repose, bulk
density, tapped density, compressabilit index and postcompressional
parameters like drug content and in-vitro drug release study,
hardness, friability, wetting time and invitro dispersion time,
invitro disintegration time and invitro dissolution time. the
physical interactions of the individual drug and optimized
formulations were studied by the using of ftir spectroscopy.
KEy words: sumAtriPtAn, hiBiscus rosA mucilAgE, dirEct
comPrEssion mEthod
1A-16chitosAn-gliclAzidE mucoAdhEsivE microPArticlEs:
PrEPArAtion And INVItrO And INVIVO EvAluAtion
P.VEERa lakShmi , k.P.R ChowdaRy, a.PRamEEla Rani,
S.V.u.m.PRaSadschool of pharmacy, JntuK KaKinaDa
ABstrActthe objective of the present study is to prepare
and evaluate microparticles of gliclazide using chitosan, a
mucoadhesive polymer for oral controlled release. a new technique
namely emulsification-desolvation-crosslinking method was tried for
the preparation of chitosan microparticles.
the chitosan- gliclazide microparticles prepared were evaluated
for various physical and drug release characteristics. the new
method developed was reproducible with regard to size and size
distribution and drug content. about 68-75 % of microparticles in
each batch were in the size range 35/50 mesh (398.5µm). the
chitosan-gliclazide microparticles prepared exhibited good
muoadhesive property. encapsulation efficiency was in the range
97.1-99.5 % in the preparation of microparticles. gliclazide
release from the chitosan microparticles was slow and spread over
longer periods of time. the drug release depended on the proportion
of core: coat in the microparticles. a good linear relationship (r²
= 0.874) between percent coat and release rate (k0) was observed.
gliclazide release from the chitosan microparticles prepared was by
diffusion mechanism. fickian diffusion was observed in the case of
microparticles which gave relatively rapidly release (f1 and f2)
and the release was by non-fickian diffusion in the case of
microparticles which gave slow release of gliclazide ( f3 and
f4).microparticles (f3) prepared using a core: coat ratio of 8:2
gave slow and controlled release of gliclazide over 12 hours
similar to that of commercial gliclazide sr tablets. in the in vivo
evaluation, gliclazide gave a rapid reduction in serum gluclose
levels and the reduced gluclose levels are also recovered rapidly.
Whereas the gliclazide microparticles (f3) gave a slower reduction
in serum glucose levels and the reduced gluclose levels were
sustained over longer periods of time.
1A-17titlE: FormulAtion And oPtimizAtion oF vAlsArtAn sustAinEd
rElEAsE FloAting tABlEts
k. SRiniVaSa REddy 1 , SuRya kanta Swain2, k. P. R. ChowdaRy 3
JaWarharlal nehru technological uniVersity, KaKinaDa
ABstrActthe objective of the present study is optimization
of
valsartan controlled release floating tablet formulation by 23
factorial design. controlled release floating tablets of valsartan
(80 mg) were formulated employing hpmcK100m (factor a) as matrix
forming polymer, sodium bicarbonate (factor B) as gas generating
agent and ethyl cellulose (factor c) and beeswax as floating
enhancers.eight formulations of Valsartan floating tablets using
the selected combinations of the three factors were prepared by wet
granulation method and were evaluated. optimization of valsartan
controlled release floating tablet
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8
formulation was done taking release rate (K0) as the parameter
for optimization. for optimization, release rate (K0) was taken as
response (y) and level of hpmcK100m as (X1); level of sodium
bicarbonate as (X2) and level of ethyl cellulose as (X3). the
polynomial equation describing the relationship between the
response, y and the variables, X1, X2 and X3 based on the observed
data obtained by multiple regression was found to be y = 7.75 -
1.25 (X1) + 0.75 (X2) – 0.25 (X1 X2) – 0.3 (X3). Based on the
polynomial equation developed, the optimized valsartan controlled
release floating tablet formulation with the desired release rate
(K0) of 7.4 mg/hr could be formulated employing hpmcK100m (240
mg/tablet), sodium bicarbonate (76 mg/tablet) and ethyl cellulose
(21 mg/tablet). the optimized formulation (fopt) exhibited a
floating time of > 12 h with a lag time of 18 seconds and gave a
release rate (K0) of 7.65 mg/hr fulfilling the target release rate
(K0) set indicating validity of the optimization technique
employed.
1A-18FormulAtion And EvAluAtion oF immEdiAtE rElEAsE tABlEts oF
nEvirAPinE solid disPErsions
PRESEnting authoR:n.haRShitha, guidEd By: PRaSanna kumaR
dESuDepartment of pharmaceutics, Vishnu institute of pharmaceutical
eDucation anD research, Vishnupur, narsapur, meDaK(Dt), telangana,
inDia – 502313
[email protected]
ABstrActthe objective of the present study was to develop
immediate release tablets of nevirapine in order to achieve
rapid release in git which might result in enhanced absorption and
thereby improved bioavailability. six batches of solid dispersions
of nevirapine were prepared by using different ratios urea and peg
6000 as carriers. Drug–excipients interaction was carried out for
pure drug and optimized formulations by using ftir studies.
nevirapine tablets were formulated employing different synthetic
polymers fusion dispersions by direct compression method. all the
batches of immediate release tablets were evaluated with reference
to different pre-compression and post-compression parameters. Based
evaluation of different parameters it was concluded that
formulation of immediate release tablets of nevirapine was
successfully done and f4 shows 100% at 60 min.
KEy words: nevirapine, urea, peG 6000, croscarmallose sodium and
starch Glycolate
1A-19FormulAtion And EvAluAtion oF sustAinEd rElEAsE BuccAl
tABlEts oF lABEtAlol hydrochloridE
V.RajaRam, V.udhayakumaR, l.SaSikumaR, V.kalVimooRthi
aaDhiBhagaWan college of pharmacy, rantham, thiruVannamalai,
tamilnaDu
ABstrActthe buccal tablets preparation appears to be an
attractive
approach for achieving better drug product effectiveness, many
anti-hypertensive tablets available in oral dosage form. the
rationale of the study is to design a sustained - mucoadhesive
buccal tablets for labetalol hydrochloride which is having a short
biological half-life (6-8 hrs). the labetolol having less bio
availability (25%) and due to its dose requirement labetolol favors
the traditional approach to sustained release delivery. the buccal
sustained release tablets of labetalol were prepared by the direct
compression method. the prepared tablets were evaluated for
uniformity of weight, hardness, friability, content uniformity,
disintegration time and in vitro drug release. the results
experiment shows that % drug release of all formulations are in
range 85.1%-99.39% after 8 hrs formulation-7 having high % drug
release up to 12 hrs to having the dose 100mg of labetolol. Based
on the result obtained the f7 considered as the optimum formulation
to design time dependent Drug Delivery system.
1A-20conjugAtion oF Acyclovir to Poly (EthylEnE glycol) through
Amino Acid And diPEPtidE sPAcErs And IN VItrO drug rElEAsE
EvAluAtion
dEBaPRotim daSguPta , Sikhamoni duttagiriJananDa choWDhury
institute of pharmaceutical science (gips), azara, hathKhoWapara,
guWahati -781017, state- assam
[email protected]
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9
ABstrActimproving the therapeutic index of drugs is a major
impetus for innovation in many therapeutic areas such as cancer
and infective diseases. the purpose of the present study is to
conjugate acyclovir to poly (ethylene glycol) through amino acid
and dipeptide spacers and study the in vitro drug release
evaluation. the study was done with the preparation of chloro
derivatives of peg (peg-cl2) followed by covalent binding of
glycine and leucine to (peg-cl2), and dipeptide glycine – leucine
to peg – cl2. acyclovir drug was incorporated in all the above
matrix. the estimation of drug content of the above formulation was
done at λmax of 254 nm in a double beam spectrophotometer (model uV
160 a). the in vitro drug release from the polymeric pro-drug was
evaluated using usp XXiii ,nmr and ir. the in vitro release profile
of acyclovir from (peg-[(glycine) – acyclovir]2), (peg-[(leucine) –
acyclovir]2), peg-[(leucine-glycine) – acyclovir]2 and
peg-[(glycine-leucine) – acyclovir]2 , shows that at ph 7.4 a
maximum of 56.24 ± 0.032% , 58.34 ± 0.019% , 89 ± 0.022% and 80 ±
0.027% was released and the time taken for 50% of the drug release
(t50) was 8hrs, 10 hrs, 5hrs and 3 hrs respectively. the drug
release study of four prodrugs of acyclovir revels that the drug
release is slower at ph 1.2 and 5.5 and higher at ph 6.8 and 7.4.
further, the drug release also takes place in a sustained
manner.
KEywords – polymer , conjuGation , prodruG , spacer molecule ,
in vitro in vivo.
1A-21FormulAtion And EvAluAtion oF sustAinEd rElEAsE tABlEts oF
mErcAPtoPurinE
maRaPuR SC1, PattanShEtty dS 1
Dept. of pharmaceutics, BlDea’s college of pharmacy, BlDe
uniVersity campus, ViJayapur-586103, KarnataKa, inDia.
[email protected]
ABstrActin the present study, an attempt was made to develop
and evaluate the sustained release tablets of mercaptopurine
using polymers like pectin and hydroxy propyl methylcellulose 4Km
in different ratios individually and in combination of above
polymer. Wet granulation technique has employed for the preparation
of tablets. the granules were evaluated for pre compressional
evaluation parameters like angle of repose,
bulk density tap density, carr’s index, hausner’s ratio. the pre
compression evaluation result suggested that all the granules are
good flowing. the tablets were evaluated for post compression
evaluation parameters like hardness, thickness, friability, drug
content, weight variation, Dsc, XrD, ftir, stability studies and
invitro drug release. all the prepared tablets were uniformity in
weight and thickness were observed with their low sD values with
good mechanical strength. ftir and Dsc study showed compatible in
drug and polymers.XrD was conducted to know the nature of the drug
in the formulation. stability studies on all formulation showed
that, there are no considerable changes in drug content.
the tablets were performed for in-vitro drug release study using
0.1n hcl of ph 1.2 for 2 hours and after that in ph7.4 phosphate
buffer for up to 12 hours in standard dissolution apparatus. zero
order, first order, higuchi and peppas models are used for
determination of mode of drug release. the formulated sustain
released matrix tablet of mercaptopurine drug has showed drug
release upto 12 hours. this concludes that sustained release matrix
tablets of mercaptopurine can overcome the disadvantage associated
with conventional tablets.
Keywords: mercaptopurine, sustained release, hpmc 4Km, pectin,
wet Granulation technique
1A-22 AdditivE mAnuFActuring: A Boon to PhArmAcEuticAl
FormulAtions
akankSha Singh, RuPa mazumdER, aVijit mazumdER, PRaVEEn
PaChauRinoiDa institute of engineering anD technology (pharmacy
institute), greater noiDa, inDia -201306
[email protected]
ABstrActadditive manufacturing is an emerging technology
that
involves layer by layer fabrication of materials or drugs in the
dosage forms, as required. this technology forms the basis of 3D
printing or 3Dp, rapid prototyping and solid free form technology,
which rely on computer aided design (caD) for non parallel
flexibility and time efficient manufacturing capability of drug
products. 3Dp is an additive manufacturing method, in which objects
are made by depositing or fusing materials in layers to prepare 3D
objects. the various advantages and applications of 3Dp include
bioprinting of tissues, organs,
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10
anatomical models for surgical preparations, fabrication of
customized drug delivery devices, personalized medicines and in
situ bioprinting of external organs like skin and so on. presently
various dosage forms of a single api and also multiple medications
in a unit dosage form to control multiple diseases are 3D printed.
Quality products can be obtained by optimization and improvement of
software performance, printing rate, printing press, print heads
line velocity and distances between two nozzles of the 3D printer
in use. Different 3D printers are available to perform multitasking
and modify different types of dosage forms of drugs. solvent
extrusion and fused disposition methods are amongst the most widely
used methods of additive manufacturing technique in the form of
3Dp. We hope that in the advancement of pharmaceutical
formulations, additive manufacturing technique will work as a boon
to lead to major breakthrough in treatment modules in the coming
days.
KEywords: BioprintinG, solvent extrusion, fused disposition,
personalized medicines, anatomical model.
1A-23FormulAtion And chArActErizAtion oF oncE dAily thEoPhyllinE
tABlEts By wEt grAnulAtion mEthod
PallaVi, S. mohaPatRaschool of pharmaceutical sciences, siKsha o
anusanDhan DeemeD to Be uniVersity, BhuBanesWar, oDisha-750003
ABstrActchronic obstructive pulmonary disease (copD) is a
class
of chronic respiratory disease, and need long term medication.
theophylline, 1, 3-dimethylxanthine, is a methylxanthine drug used
in therapy for chronic obstructive pulmonary disease. extended
release formulations are prepared to make the contained drug
available over a prolonged period of time following administration.
the purposes of the research work is to prepare the extended
release tablets of theophylline by wet granulation method using
different grades of hydroxy propyl methyl cellulose (hpmc) as a
retardant polymer. furthermore different evaluation parameters like
weight variation, hardness test, friability, tablet thickness,
disintegration time, drug content and XrD studies were
investigated. in vitro dissolution studies were done to found the
release pattern of drug. observation of all formulations complies
with specification of official pharmacopoeias and standard
references. in vitro release profile
indicated formulations showed release pattern for an extended
period of 24 hour as compared to marketed formulation. XrD study
showed no change in physical form. hence a stable extended release
tablet formulation of theophylline was developed to achieve best
therapeutic efficacy.
Key words: copd, theophylline, hydroxy propyl methyl cellulose,
wet Granulation
1A-24FormulAtion And EvAluAtion oF microBAllons oF ondAnsEtron
hydrochloridE
SuBham Pattnaik, ShaRBaRi mohanty, PRaSant kumaR, SuBhEndu
SEkhaR miShRa gayatri college of pharmacy, Department of
pharmaceutics, JamaDarpali, samBalpur, 768200
[email protected]
ABstrActmicroballons delivery systems are uniform,
spherical,
porous polymeric microspheres having myriad of interconnected
voids of particle size range 5-300μm. these microballons have the
capacity to entrap a wide range of active ingredients such as
emollients, fragrances, essential oils, sunscreens and
anti-infective, etc. and then release them onto skin over a time
and in response to trigger. ondansetron hydrochloride, a 5 ht3
antagonist is a powerful antiemetic drug. microballons offers
numerous advantages for releasing one of the drugs or part of the
same drug immediately while remaining drug or parts of the same can
be sustained release. these are useful where drug-excipients and
drug-drug interactions are predictable with single type dosage
form. By keeping the views of above facts our present study is
approached for preparation of microballons of ondansetron
hydrochloride by Quasi-emulsion diffusion method. for prepare the
inner phase, eudragit rs 100 was dissolved in 3 ml of methanol and
triethylcitrate (tec) was added at an amount of 20% of the polymer
in order to facilitate the plasticity. the drug was then added to
the solution and dissolved under ultrasonication at 35°c. for
preparing the outer phase pVa dissolved in 200 ml of water in a
separate container. then the inner phase was poured into the pVa
solution in 200 ml of water (outer phase). the resultant mixture
was stirred for 60 min, and filtered to separate the microballons.
the microballons were washed with distilled water and dried at 40°c
for 24h.
Key words: microBallons, quasi-emulsion diffusion, ondansetron
hydrochloride, tec
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1A-25FormulAtion And oPtimizAtion oF EFAvirEnz tABlEts to
AchiEvE thE dEsirEd dissolution rAtE
m.PRiyadaRSini, k.P.R.ChowdhaRyDepartment of pharmaceutical
sciences, JntuK, KaKinaDa, inDia-533003.
[email protected]
ABstrAct the objective of the present study is to enhance
the
dissolution rate of efavirenz by solid dispersion in starch 1500
and soluplus in its tablet formulation development and to optimise
the efavirenz tablet formulation employing starch 1500(factor a)
and soluplus(factor B) by 22 factorial design to achieve nlt 85%
dissolution in 10 min. four efavirenz tablet formulations were
prepared using selected combinations of the two factors as per 22
factorial design. efavirenz tablets were prepared by direct
compression method and evaluated.the individual and combined
effects of the two factors, starch 1500 and soluplus are highly
significant (p < 0.01) in influencing the dissolution rate of
efavirenz tablets. efavirenz tablet formulations fab and fa
disintegrated rapidly within one min and gave very rapid
dissolution of efavirenz 96.1% and 88.6% in 10 min respectively.
the increasing order of dissolution rate (K1) of various
formulations was f1< fb< fa
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12
drug delivery systems. in the present study, an attempt was made
to sustain the release of ciprofloxacin hydrochloride from matrix
tablets by sintering technique. this has been an evolving one in
the study of effect of heating on mechanical properties of
pharmaceutical powders that is used in the formulation of sustained
release matrix tablet. the tablets were formulated by direct
compression method. the punched tablets were subjected to sintering
process and exposed to three different durations of sintering (1.5,
3.0 and 4.5 h). this type of system provides an important and
suitable method for acheving controlled release in oral dosage
forms. the release of the drug from un-sintered matrix tablets
containing 100mg polymer was 100% within 90minutes. for a
particular sintering time, the release rate decreased with
increasing polymer concentration. for 1.5, 3.0 and 4.5h sintering
durations the least retardation is offered by least polymer
concentration. the highest retardation was offered by matrixes with
highest polymer concentration.
KEywords:ciprofloxacin hydrochloride, sinterinG technique,
matrix taBlets, direct compression.
1A-28FormulAtE And EvAluAtion oF thE controllEd rElEAsE
microsPhErE using PolymEthAcrylAtEs (EudrAgits) is rElEAsE
rEtArding PolymErs.
PRaShant joRaPuR1, SomaShEkhaR m21Department of pharmaceutics,
2Department of pharmaceutical chemistry, BlDea’s ssm college of
pharmacy anD research centre ViJayapur-586103, KarnataKa
ABstrActin the present investigation an attempt has been
made
to formulate and evaluate the controlled release microsphere
using polymethacrylates (eudragits) are release retarding polymers.
in the present study 9 formulations were formulated by using
polymethacrylates (eudragits) in different ratios. all the
formulations were subjected for various evaluation parameters. the
results of preformulations studies, particle size analysis, flow
properties, micomeritic properties, drug content and entrapment
efficiency showed the acceptable result. the in vitro dissolution
of formulations showed the amount of drug release decreases with
increase in polymer concentration and particle size. further the
release kinetics of all formulation was done were the optimized
formulation showed good fit value for
hixon-crowell model. the study of optimized formulation f1 is
viewed through sem and shows uniform matrix formulation with dense
nature and rough surface. further the optimized formulation f1was
subjected to accelerated stability, and was found to be stable as
there was no drastic change in drug content as well as drug release
profile.
Keywords: controlled release, polymethacrylates, hixon-crowell
model.
1A-29dEvEloPmEnt And invitro chArActErizAtion oF risEdronAtE
sodium FloAting microBAlloons
munija PanChEddula, ShayEda Department of pharmaceutics,
uniVersity college of pharmaceutical sciences,KaKatiya uniVersity,
Warangal - 506 009, telangana, inDia.
[email protected]
ABstrActin the present research work, floating microballoons
of risedronate sodium using eudragit rs 100, eudragit s
100, hpmc K4m, ethylcellulose as polymers were formulated to
deliver risedronate sodium via oral route. the
objective behind the research work is to develop the
gastroretentive drug delivery system of the drug to prolong the
drug release to enhance its action time for longer
duration.prepared microballoons were evaluated for particle
size,percentage yield, entrapment efficiency,percentage buoyancy
and percentage drug release. the results of this investigation
indicate that, solvent evaporation method can be successfully
employed to formulate risedronate sodium microballoons. the
in-vitro release studies demonstrated that microballoons of
risedronate sodium prepared using eudragit rs 100 along with
eudragit s 100 in 1:1 ratio shown maximum amount of drug release,
hence it is considered as the optimized formulation. the in vitro
release kinetics revealed that the optimized formulation release
the drug in zero order manner based on the regression values of
kinetic models.thus it can be concluded that risedronate sodium
loaded floating microballoons are proven to be potential
pharmaceutical dosage forms for prolonging the gastric retention
time of dosage form.
Key words : risedronate sodium, floatinG microBalloons, solvent
evaporation method, Gastric residence time, Gastroretentive druG
delivery systems.
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1A-303 (2) tAguchi FActoriAl dEsign AssistEd hydrodynAmicAlly
BAlAncEd systEm oF mEtoProlol succinAtE
dEEPankaR Bahuguna, BiSwanath ChaudhaRy, ShaShank SoniDepartment
of pharmaceutics, school of pharmaceutical sciences anD technology,
sarDar BhagWan singh uniVersity, DehraDun, uttaraKhanD, inDia,
248161.
[email protected]
ABstrActmetoprolol succinate (ms) is a highly selective β1
adrenergic receptor which is used for the treatment of
hypertension, chronic heart failure, and arrhythmia. in the present
experimental investigation, an attempt has been made to assess the
utility of medium molecular Weight chitosan (mWch), high molecular
Weight chitosan (hWch) and hpmc K15 as a polymeric carrier for the
sustained stomach delivery of ms. a total of nine formulations were
prepared by using 3 (2) taguchi factorial design. Briefly, hBs
capsules formulation were prepared by encapsulating manually
blended drug-polymer mixture in hard gelatin capsules, where
polymer used were cationic hWch and mWch in combination with
hydrophilic polymer hpmc K 15m is anionic. the main intention to
select the hWch and mWch was that it shows both mucoadhesive and
swelling tendency when comes in contact with dissolution media (0.1
m hcl). however, it has been observed that hBs formulation remained
buoyant up to the time span of 7.5 hours in dissolution media when
a higher level of hWch and mWch was incorporated including 98.07%
release drug sustained manner. from the conducted experiment it was
observed that formulation f1-f6 followed non-fickian diffusion and
on the other hand formulation f7-f9 followed super case 2 transport
mechanism. the data gained from the conducted experiment suggests
that a higher level of chitosan in addition with hpmc K15m has the
ability to be constituted as a carrier for stomach specific
delivery of ms.
KEywords: hydrodynamically Balanced system, taGuchi factorial
desiGn, hiGh molecular weiGht chitosan, medium molecular weiGht
chitosan, hpmc K15m.
1A-31hiBiscus EsculEntus: A rEviEw oF sustAinEd rElEAsE Action
oF ProPAnolol hydrochloridE in solid orAl dosAgE Form
aVinandan aSh, SuBhEndu BikaSh jana, SwaRnajit duttaDepartment
of pharmaceutical chemistry, calcutta institute of pharmaceutical
technology anD, allieD health sciences, uluBeria, hoWrah, West
Bengal, inDia-711316.
[email protected]
ABstrActsustained release is a type of dosage form which is
designed to release a drug at predetermined rate in order to
maintain a constant drug concentration for specific period of time
with minimum side effects. after dosing with sustained release
propanolol, plasma levels begin to rise almost immediately. the
main objective is to evaluate the properties of okra gum & it’s
applicability in the design of floating tablets. the principal
property of polysaccharide gums is their easy hydration to produce
aqueous solutions possessing high viscosity of low gum
concentration. okra gum is extracted from the pods of hibiscus
esculentus using acetone as a drying agent. Dried okra gum was made
into powder form and it’s physical and chemical characteristics
such as solubility, ph , moisture content, viscosity, morphology
study using sem, infrared study using ftir, crystalline study using
XrD and thermal study using Dsc and tga were carried out. the
activity of okra gum as a binder was compared in formulation of
propanolol tablets using a synthetic and a semisynthetic binder
which are hydroxy propyl methyl cellulose (hpmc) and sodium
algenate respectively and evaluate the drug release kinetics which
was attained from dissolution studies to show okra gum release up
to 24 hours and exhibit the longer release compared to hpmc and
sodium algenate. hence okra gum was testified to produce favourable
sustained release tablets with strong tensile.
Keywords: hiBiscus esculentus, sustained release, hpmc, sodium
alGenate.
1A-32dEvEloPmEnt And EvAluAtion oF hydrodynAmicAlly BAlAncEd
systEm
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oF trAmAdol hydrochloridE By using chitosAn And locust BEAn
Sandhya SEmwal, PRaVjot kauR, ShaShank SoniDepartment of
pharmaceutics, school of pharmaceutical sciences anD technology,
sarDar BhagWan singh uniVersity, BalaWala, DehraDun, uttaraKhanD,
inDia. 248161.
[email protected]
ABstrActthe study was performed to develop and evaluate
hydrodynamically balanced capsule of tramadol hcl (th) by using
chitosan and locust bean gum as a natural polymer that prolongs the
gastric residence time. chitosan with different grade (low
molecular weight, medium and high molecular weight) and locust bean
gum were used as a drug release retarding agents. the
hydrodynamically balanced capsule of tramadol hcl were prepared by
ordered mixing technique. the concentration of both the polymers
was optimized in order to achieve the sustained release of drug
(th) for 10 hours. then the prepared capsules were evaluated for
buoyancy test and in vitro drug release were performed. and other
characterization analysis was also considered like ftir study,
Dsc/Dtg/tga study and interaction study were also performed on the
basis of characterization analysis. from these studies it was
confirmed that there is no interaction observed between drug and
excipient. the drug release studies show that the retarding drug
release pattern is dependent on the concentration and molecular
weight of polymer as the concentration /molecular weight increases
the retarding drug release pattern was also improved. and the
synergistic action of retarding drug release was observed by the
addition of another polymer i.e. locust bean gum. release pattern
was fitted with the different kinetic model like zero order, first
order, higuchi model and Korsmeyer peppas and it was concluded from
the models that the drug release pattern obeys zero order model
which signifies high therapeutic efficacy and minimum side
effects.
Keywords: hiGuchi model, Korsmeyer-peppas, Buoyancy, Gastric
residence time.
1A-33novEl gAstrorEtEntivE orAl in situ gElling systEm oF
niFEdiPinE – FormulAtion, oPtimizAtion And EvAluAtion
akankSha tomaR, aShiSh tiwaRi, nayan gujaRathi, anil
jadhaVDepartment of pharmaceutics, sanDip institute of
pharmaceutical sciences, mahiraVani, nashiK - 422213, maharashtra,
inDia
[email protected]
ABstrActhe objective of present study was to develop
nifedipine
gastroretentive in situ gel which provides sustained release of
the drug for the management of hypertension and angina pectoris.
gastroretentive in situ gelling system helps to increase
bioavailability of drug compared to conventional oral dosage form.
accurately weighed quantity of calcium carbonate along with
sorbitol, ethyl paraben and propyl paraben was dissolved in
purified water. in another beaker accurately weighed quantity of
calcium chloride and 0.25% sodium citrate was dissolved in
deionized water. sodium alginate was then added to the resulting
mixture with continuous stirring and heated upto 70˚c followed by
cooling back to 40˚c. accurately weighed quantity of drug was
initially dissolved in small quantity of methanol and added slowly
to the above sodium alginate solution while stirring on a magnetic
stirrer. at 40˚c, both solutions were mixed and subjected to
stirring for 30 min. preformulation studies proved absence of any
drug polymer interaction between the drug, polymer and the other
excipients used in the formulations. the drug content and swelling
index of all (f1-f9) formulations ranges in between 97.99%-101.97%
and 80.1% - 82.6% respectively. formulation f7 exhibited the least
buoyancy lag time (26 s) while formulation f3 exhibited the highest
lag time (57 s). the prepared gastroretentive oral in situ gel of
nifedipine formulation proved that, 76.86% drug get released from
the formulation in stomach hence increases bioavailabilty by about
20% and retained in the stomach for >12 h for sustained effect
in git.
Keywords: nifedipine, in situ Gel, sustained release,
Gastroretentive
1A-34EvAluAtion oF in VitRo And in ViVo EFFicAcy oF PrussiAn
BluE AlginAtE BEAds For rEmovAl oF cEsium in micE
Pooja ShaRma, mahEndRa yadaV, nidhi Sandal, a k Singh
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15
institute nuclear meDicine anD allieD sciences, Defence research
anD DeVelopment organization Brig s K mazumDar roaD, timarpur,
Delhi 11005
[email protected]
ABstrActprussian blue (pB) is a dark blue synthetic
pigment
produced by oxidation of ferrous ferrocyanide salts.
it is indicated for treatment of patients with known internal
contamination with radioactive cesium and/or radioactive thallium
to increase their rate of elimination. the aim of the present study
is to determine the in vitro and in vivo efficiency of pB-alginate
beads for the removal of cesium. the prussian blue encapsulated in
alginate beads were prepared and characterized as described in
literature. to evaluate the in vitro efficacy of pB-alginate beads,
100 mg of prussian blue and pB-alginate beads (encapsulation
efficiency∼30%) were incubated with 600 ppm solution of cesium
chloride in water for 3 hrs and supernatant samples were analyzed
by atomic absorption spectroscopy. prussian blue and pB-alginate
beads were found to have cs adsorption efficiency of 4997ppm/gm and
4916ppm/gm respectively. in vivo efficacy of pB-alginate beads was
compared with prussian blue in male swiss albino mice, of 8 week
old. mice were given 1mg cesium chloride orally and then Divided
into three groups: the mice of first group were administered orally
a dose of prussian blue equivalent to 2mg , mice of second group
were administered a dose of pB-alginate beads equivalent to 4mg in
twice a day, for 5 days,starting 1h after administration of cesium
chloride on day 1. the third group was kept as a control. on 6th
day mice were sacrificed. the cesium content in each organ was
measured using atomic absorption spectrophotometer having graphite
furnace. the data was subjected to statistical analysis using
graphpad prism 5.0. treatment with pB and pB-alginate beads showed
significant decreased (p
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16
designed to increase its residence time in the stomach without
contact with the tablets was achieved through the preparation of
floating tablets by the direct compression method. in the present
study attempt has been made to develop sustained released drug
delivery system by formulating the floating tablets of losartan
potassium using psyllium husk powder as a natural polymer which is
biodegradable, biocompatible, nontoxic, economically cheap cost,
devoid of adverse and side effects and easily availability.
losartan potassium chemically
Butyl-4chloro-1-[(2-(1hetrazol-5-yl)[11-biphenyl]-4-yl] methyl]–1h–
imidazole–5–methanol potassium used as an anti-hypertensive agent.
the 14 batches of floating tablets (lf1 to lf14) were formulated by
direct compression method using different ratio of polymers like
psyllium husk power, hpmc K4m, hpmc K100 and carbopal. the
formulated tablets were evaluated by means of different parameters
like shape and density of tablet, hardness, friability, weight
variation, drug content uniformity, invitro buoyancy, swelling
index, invitro dissolution studies. the formulation lf8 has better
sustained release when compared other formulations, hence we
conclude that the combination of psyllium husk powder, hpmc K4m and
hpmc K100 shows better gastric retention time which sustains the
release of the dosage form.
1A-38FormulAtion And EvAluAtion oF dicloFEnAc mEdicAtEd
lolliPoPs By hEAting And congEAling mEthod
daya Ratnam madugula, Raghu VamSi kidamBiDepartment of
pharmaceutics, sims college of pharmacy, mangalDas nagar, guntur,
anDhra praDesh, inDia – 522001.
[email protected]
ABstrAct-the objective of the work was to prepare diclofenac
sodium medicated lollipop using mucoadhesive polymers like
sodium carboxy methyl cellulose and methyl cellulose in different
ratios. in the current research work is to formulate sugar based
medicated lollipops of using diclofenac sodium has a model drug is
used as an analgesic, antipyretic and anti-inflammatory. now-a-days
it is difficult to manage pediatrics for parents to administer a
conventional dosage form like tablets, capsules and liquid dosage
forms. the prepared lollipops were evaluated for weight variation,
hardness, thickness drug content. infra red analysis of diclofenac
sodium lollipops showed no interaction between drug and polymer
during the formulation process. therefore diclofenac sodium of
medicated
lollipops have been successfully formulated as it was observed
good results to prolong dissolution time and drug release in
salivary ph condition for a period of 30min. thus, it can be
calculated this study can be comfortness in applications and
transportations with effective better patient compliance to
lollipops over conventional dosage forms. the stability studies
proved that the prepared lollipops were found to be stable when
stored at air tight containers or twist strips. hence the present
work of investigation will be used for industry, research and
development division.
Key words: - diclofenac sodium, lollipops, sodium cmc,
mucoadhesive polymers.
1A-38FormulAtion And EvAluAtion oF dicloFEnAc mEdicAtEd
lolliPoPs By hEAting And congEAling mEthod
daya Ratnam madugula, Raghu VamSi kidamBiDepartment of
pharmaceutics, sims college of pharmacy, mangalDas nagar, guntur,
anDhra praDesh, inDia – 522001.
[email protected]
ABstrAct-the objective of the work was to prepare diclofenac
sodium medicated lollipop using mucoadhesive polymers like
sodium carboxy methyl cellulose and methyl cellulose in different
ratios. in the current research work is to formulate sugar based
medicated lollipops of using diclofenac sodium has a model drug is
used as an analgesic, antipyretic and anti-inflammatory. now-a-days
it is difficult to manage pediatrics for parents to administer a
conventional dosage form like tablets, capsules and liquid dosage
forms. the prepared lollipops were evaluated for weight variation,
hardness, thickness drug content. infra red analysis of diclofenac
sodium lollipops showed no interaction between drug and polymer
during the formulation process. therefore diclofenac sodium of
medicated lollipops have been successfully formulated as it was
observed good results to prolong dissolution time and drug release
in salivary ph condition for a period of 30min. thus, it can be
calculated this study can be comfortness in applications and
transportations with effective better patient compliance to
lollipops over conventional dosage forms. the stability studies
proved that the prepared lollipops were found to be stable when
stored at air tight containers or twist strips. hence the present
work of investigation will be used for industry, research and
development division.
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17
Key words: - diclofenac sodium, lollipops, sodium cmc,
mucoadhesive polymers.
1A-39FoEmulAtion And in-vitroEvAluAtion oF orAl FAst dissolving
tABlEts using AntimigrAnE drug
SaRita a. ukEy, a. t. Patil, d. R. tElangE, m. j. umEkaR
Department of Quality assurance smt. Kishoritai Bhoyar college of
pharmacy Kamptee, BehinD railWay station Kamptee, Dist: nagpur,
maharashtra (inDia) -441002
[email protected]
ABstArct: in the current research, we formulate and evaluate
oral
fast dissolving tablet using anti-migraine drug zolmitriptan
(zlp). the objective behind the research was, to prepare the fast
dissolving tablet(fDt) containing anti-migraine drug by using the
suitable method and the fDt containing anti-migraine drug which are
dissolve or disperse in the oral cavity within second of matter.
the prepared tablets were evaluated for pre-compression parameters
i.e. Bulk density, tapped density, hausner’sratio, angle of repose,
carr”s index and post compression parameters i.e. hardness test,
friability test, weight variation test, thickness and diameter,
disintegration time, in-vitro dissolution study, stability studies.
the formulation containing croscarmelleose sodium(60mg) and micro
crystalline cellulose(20mg) showed good disintegration time highest
cumulative drug release and highest drug content. Best formulation
ff7 found to be stable. ftir studies concluded that drug and
excipients were compatible with each other. the formulated tablets
were satisfactory in terms of hardness, thickness, friability,
weight variation, drug content uniformity, wetting time,
disintegration time and in-vitro drug release. the final optimized
formulation(ff7) of zlp containing super disintegrants and results
was revealed that formulated ofDt of zlp were effective and better
to meet patient compliance.
Key words: zolmitriptan, oral fast dissolvinG taBlets, fast
dissolvinG taBlet
1A-40ABstrAct
the aim of the present research work was to develop
delayed release mini tablets in capsule of drug lenalidomide
similar to reference listed drug (rlD) in terms of dissolution and
stability. Drug lenalidomide is an immune-modulator and belongs to
Bcs class-i compound displaying high solubility across the
physiological ph range. mini-tablets are small tablets with a
diameter equal to or less than 3 mm that are filled into a capsule.
mini tablets were prepared by direct compression method using
multi-tip punch and coated with eudragit l100 as a seal coating
material and with eudragit l30 D55 as an enteric coating material.
five formulations (Batch 1-5) were prepared and subjected for
evaluation like weight variation, hardness, friability,
disintegration, drug release and stability studies to select the
best formulation among the five. Batch-1 was dropped due to low
hardness and failure in dissolution profile. Batch 2, 3 and 4
failed to give the requisite dissolution similar to that of rlD.
evaluation results for batch-5 were found well within the limits.
hence, batch-5 has been considered as an optimized formulation and
recommended for the scale up batch for further development.
Key words: immuno-modulator, mini-taBlets, delayed-release,
taBlets in capsule
1A-41FormulAtion oF monodisPErsE (micro) sPhErEs contAin
lAmivudinE For ExtEndEd rElEAsE dosAgE Form
g.VEnkataSiVa S S kondala Rao,P. RaghuVEER, a.PRamEEla Rani, i.
haRiSh.uniVersity college of pharmaceutical sciences, acharya
nagarJuna uniVersity,guntur,ap.
ABstrActoral delivery of lamivudine as a therapeutic drug
would
significantly improve the quality of life of hiV patients who
would otherwise receive multiple daily doses. the oral delivery of
lamivudine, however, is still limited in its delivery efficiency
which could be due severe adverse effects and high dosing
frequency, in an attempt to improve the delivery efficiency, the
lamivudine loaded micro spheres for control release medication were
designed and constructed through ionic gelation technique employing
sodium alginate alone and in combination with sodium cmc and hpmc
to retard drug release by forming polymer matrix. the resulted
micro spheres of formulation f3 containing Drug and hpmc in the
ratio (1:5) with particle size ∼200 μm could easily be
reverted to discrete from aqueous solution. surface morphology of
microspheres was found to be
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18
smooth and porous. entrapment efficiency (84%) was found to be
excellent with controlled drug release (∼12 h).in vitro
kinetics reveals that drug release from formulation followed zero
order kinetics with non-fickian diffusion. these results suggested
that the lamivudine microspheres are promising and should be
investigated further in the near future as an effective oral
delivery system.
Key words: microsphers contain lamivudine,ion Gelation
technique,extended release.
1A-42FormulAtion And EvAluAtion oF gAstro-rEtEntivE systEms oF
nAtEglinidE
j. VijaRatna, ChiRRaVuRi. S. Phani kumaRDepartment of
pharmaceutical technology, ViKas institute of pharmaceutical
sciences, niDigatla, raJahmunDry, anDhra praDesh, inDia.
[email protected]
ABstrActgastro-retentive controlled drug delivery systems
(grcDDs) are majorly employed for poorly soluble drugs with
absorption window as upper part of intestine with short biological
half-life. nateglinide is a type-ii anti-diabetic agent belongs to
Bcs class ii drug, its biological half-life is 1.5 h and its
absorption window is upper part of intestine. the present research
work was aimed at designing and evaluating grcDDs of nateglinide.
four different techniques employing different polymers were used,
namely effervescent floating (ef), non-effervescent floating (nf),
raft forming (rf) and bio-adhesive (Baf) techniques using carboxy
methyl ethyl cellulose (cmec) for ef and nf, guar gum for rf and
hpmc K4m for Baf as rate drug release retardants. these
formulations were evaluated for in-vitro studies like floating lag
time, total floating time, and in-vitro drug release. and best
formulation was selected based on pharmacodynamic studies i.e.
non-effervescent system (nf3 formulation) due to its longer
duration of anti-diabetic activity on rabbit. nf3 consists of 40 %
of cmec per tablet and poly ethylene foam powder as floating agent
at 30 %. pharmacokinetic studies were conducted on nf3, 2% sodium
carboxy methyl cellulose (sod. cmc) suspension of nateglinide and
marketed product. it was found that nf3 gave the best
bioavailability among the three formulations tested. good
correlation (level a) was observed between the results of the pK
and pD studies.
Key words: nateGlinide, Gastro-retentive controlled release druG
delivery systems, floatinG system, raft forminG system and
Bio-adhesive system.
1a-43dEvEloPmEnt And EvAluAtion oF hydrodynAmicAlly BAlAncEd
systEm oF trAmAdol hydrochloridE By using chitosAn And locust
BEAn
Sandhya SEmwal, PRaVjot kauR, ShaShank SoniDepartment of
pharmaceutics, school of pharmaceutical sciences anD technology,
sarDar BhagWan singh uniVersity, BalaWala, DehraDun, uttaraKhanD,
inDia. 248161.
[email protected]
ABstrActthe study was performed to develop and evaluate
hydrodynamically balanced capsule of tramadol hcl (th) by using
chitosan and locust bean gum as a natural polymer that prolongs the
gastric residence time. chitosan with different grade (low
molecular weight, medium and high molecular weight) and locust bean
gum were used as a drug release retarding agents. the
hydrodynamically balanced capsule of tramadol hcl were prepared by
ordered mixing technique. the concentration of both the polymers
was optimized in order to achieve the sustained release of drug
(th) for 10 hours. then the prepared capsules were evaluated for
buoyancy test and in vitro drug release were performed. and other
characterization analysis was also considered like ftir study,
Dsc/Dtg/tga study and interaction study were also performed on the
basis of characterization analysis. from these studies it was
confirmed that there is no interaction observed between drug and
excipient. the drug release studies show that the retarding drug
release pattern is dependent on the concentration and molecular
weight of polymer as the concentration /molecular weight increases
the retarding drug release pattern was also improved. and the
synergistic action of retarding drug release was observed by the
addition of another polymer i.e. locust bean gum. release pattern
was fitted with the different kinetic model like zero order, first
order, higuchi model and Korsmeyer peppas and it was concluded from
the models that the drug release pattern obeys zero order model
which signifies high therapeutic efficacy and minimum side
effects.
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19
KEywords: hiGuchi model, Korsmeyer-peppas, Buoyancy, Gastric
residence time.
1A-44dEvEloPmEnt And chArActErizAtion oF novEl gAstrorEtEntivE
ExPAndABlE Films oF mEtoProlol tArtrAtE
PaREPalli SRikanth1, S. hEmalatha2, S.V.SatyanaRayana3 1research
scholar, Jntua, ananthapuramu, 515002, anDhra praDesh,
inDia2Department of pharmacognosy, sri VenKatesWara college of
pharmacy, chittoor, 517127, anDhra praDesh, inDia3Department of
chemical engineering, Jntua, ananthapuramu, 515002, anDhra praDesh,
inDia
[email protected].
ABstrActoral route is most preferable route of administration
of
drugs, but it has certain limitations for those drugs which
absorb from specific region of gastrointestinal tract. the
bioavailability of drugs can be improved by increase their
retention time in the stomach and several approaches are used to
increase the gastric retention time of the dosage, one of the
approach is expandable gastroretentive dosage forms. Bilayered
films were prepared by solvent-casting technique using ethyl
cellulose, hpmc and eudragit as polymers and dibutyl-phthalate as
the plasticizer in both layers. the film with rolled folding in the
capsule was shown to unfold in the gastric juice and provide drug
release up to 12 hrs in the acidic medium. metoprolol tartrate is
an antihypertensive drug, which has low elimination half life: 3-4
hrs. the expandable formulation of metoprolol tartrate was prepared
to increase the gastric retention and to improve the
bioavailability of the drug. metoprolol tartrate was chosen as a
model drug because it is better absorbed in the stomach than the
lower gastro intestinal tract. the prepared films were evaluated
for weight & thickness variation, mechanical properties,
in-vitro drug release and unfolding. absence of drug polymer.
interaction and uniform drug dispersion in the polymeric layers was
revealed by ftir & dSC. the dosage form location in the
gastrointestinal tract was determined by X-ray studies.
Key words: Bilayered films, unfold, antihypertensive. metoprolol
tartrate, x-ray studies.
1A-45dEsign And IN-VItrO EvAluAtion oF AtEnolol microBAllons
aRun SahaRawat, manoj joShi, nidhi nainwalDepartment of
pharmaceutics, school of pharmaceutical sciences anD technology,
sarDar BhagWan singh uniVersity, BalaWala, DehraDun, uttaraKhanD,
inDia. 248161.
[email protected]
ABstrActin the present work sustained release microballons
of
atenolol was prepared to enhance its residence time in stomach,
reduces its frequency, increment in the bioavailability (40-50%)
and half-life of atenolol. the preparation of 6 batches prepared by
solvent evaporation method by using ethyl cellulose (ec) (f1, f4,
f6), hpmc K 4 m ( f2, f4, f5) and eudragit rs 100 (ers100) f3, f5,
f6). the ratio of ec, hpmc K4m, ers 100 with the drug is 1:2, and
the ratio of drug: ethyl cellulose: hpmc K4m is 1:1:5:1:5, drug:
hpmc K4m: e rs 100 is 1:1:5:1:5 and the ratio of drug: ers 100: ec
is 1:1:5:1:5. physical characterization of microballons such as
particle size, particle shape, and surface morphology was evaluated
by scanning electron microscopy. the prepared microballons were
further evaluated for percentage yield, drug entrapment efficiency,
in- vitro buoyancy, and in vitro drug release. the prepared
microballons were free flowing, spherical and displayed a particle
size ranging from 64.0 to 96.30 µm suitable for oral delivery. the
drug entrapped in the microballons increased with the increase in
polymer content. the formulation f2 selected as optimized
formulation as it showed maximum buoyancy up to 85.60% and more
than 45% drug release in first 2 hr and more than 79% drug release
in 12 hours. the drug release from the all six batches follows
higuchi kinetics with fickian diffusion mechanism. the obtained
results indicated that atenolol microballons could be sustaining
drug release for prolonged periods of time.
Keywords: microBallons, atenolol, sustained release, Gastro
retentive
1A-46An invEstigAtion oF in-vitro rElEAsE oF rABEPrAzolE sodium
From PulsAtilE rElEAsE tABlEts contAining hPmc-Ec BlEnd As timE
lAggEd PrEss coAting
jyoti joShi, SaChin Chauhan, nidhi nainwal
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20
Department of pharmaceutics, school of pharmaceutical science
anD technology, sarDar BhagWan singh uniVersity, BalaWala,
DehraDun, inDia- 248161
[email protected]
ABstrActto develop new pulsatile release tablets of
rabeprazole
sodium (rs),that can suppress drug release in stomach and
release the drug rapidly after predetermined lag time for about 4 h
in intestine, a multiple unit dosage forms was designed that
contain, drug- containing core, a coating to achieve time lag in
drug release and an outermost acid resistant enteric coating. time
lagged press coating was performed using ethyl cellulose (ec) and
different grades of hydroxypropyl methylcellulose (hpmc) in
different ratios. the press coated tablets were optimized by the
drug release study and finally the formulation f17 containing 7:1
ratio of ec and hpmc K4m was selected as optimized formulation.
this press coated tablet was further enteric coated with cellulose
acetate phthalate (cap). the weight gain of the enteric coating was
optimized based on the integrity of coating in an acidic solution
for about 2 h. formulation f21 was finally selected with 10% weight
gain and rupture time of 120 minutes in 0.1n hcl. further, the drug
release from f21 formulation started after 270 minutes (4.5 h). the
results indicate that the drug release was successfully suppressed
till 4.5 hrs as per the need of pulsatile dosing of rs as the drug
concentration needed between 12 am to 6 am. By considering the
dosing time of 8:00 pm, the formulation release only 15:1% of the
drug till 1 am (after 5 hrs) and 90% of the drug release after 7.25
h.
Keywords: pulsatil release taBlets, time laGGed press coatinG,
enteric coatinG.
1A-47FormulAtion And EvAluAtion oF tolmitin EntEric coAtEd
tABlEts And invitro EvAluAtion
P. nithin , t. Ramya kRiShna , g. laxmidEViDepartment of
pharmaceutics, talla paDmaVathi pharmacy college, B,pharmacy iV
year, Jntuh, hyDeraBaD, telangana, inDia.
[email protected]
ABstrActthe main objective of the present research work is
to formulate the tolmetin extended release tablet. tolmetin is a
non- steroidal anti- inflammatory drug(nsaiDs) that is effective in
treating fever, pain, inflammation in the body. tolmetin blocks the
enzyme that makes prostaolandins(cyclo-oxigenase), resulting in
lower concentration as a conseqenece, inflammation, pain, are
reduced at present the tablets are available in the market use as
multiunitparticulate system to deliver the drugs at acontroled rate
over 24hrs. the present research edeavor was directed towards the
development of extended release tablet to be taken twice daily. the
formulation of tolmetin extended release tablet is important to
give prolonged activity in the prolonged drug release in an
extended period of time for the long terms therapeuitic activity.
the formulation of the extended released tablet were prepared by
using suitable exceipients such as hydroxypropylmethyl cellulose,
hpmce3, hpmcK15m, hpmcK100m hydroxyehthylcellulose, povidone
colloida silicondioxide, megnesium strerate. this tolmetin extended
release tablets were prepared by using wet grannulation method they
can be also prepared by dry grannulation method. the prepared
extended release tablet is evaluated in terms of bulk density,
tapped density, angle of repose, cars index and hardness test,
weight variation test, variability test,and invitro study. the
hardness weihght varion and friability this values are within in
the pharmacopeia limit. the finalised formulation was subjected for
invitro dissolution and campared with the innovator(tolectinr 600)
to produce an equivalent product and stability studies performed at
400 c/75% for 2months. stability samples were evaluated initially
and after 2months. the result were compared with the predetermined
specification to be satisfactory.
Key word : extended release taBlets, tolmetin, and nsaids.
1A-48dEvEloPmEnt And in vitro chArActErizAtion oF PulsAtivE drug
dElivEry oF toFAcitiniB By osmotic controllEd rElEAsE orAl
systEm
introduction
With the advancement of the technologies in the pharmaceutical
field, drug delivery system have drawn an increasing interest over
the last few decades. nowadays, the emphasis of pharmaceutical
galenic research is turned towards the development of more
officious drug delivery system with already existing molecule
rather than going for new drug discovery. the oral controlled
release system show a
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21
typical pattern of drug release. in the window for a prolonged
period of time (sustained release), thereby ensuring sustained
therapeutic action.
objective
the objective of the present study is the formulation and
evaluation of tofacitinib by osmotic controlled release oral system
of pulsative delivery with better lag time and attain controlled
drug release and excellent patient acceptability.
Disease that follow chronopharmacological behavior can be
effectively treated with this system.
to enhance the patient compliance.
methodology
selection of druganalytical method development for
tofacitinibpreparation of buffersDrug excipient
compatabilitypreparation of tofacitinib core tabletspre-compression
studiespost-compression studies
rEsult:-
stAndArd Plot oF toFAcitiniB in PhosPhAtE BuFFEr Ph 6.8
absobance at 218 nm
0 0
1 0.087
2 0.174
3 0.252
4 0.342
5 0.427
6 0.513
r2 0.999
slope 0.085
conclusion:-
pulsatile drug delivery of tofacitinib tablets were
successfullyfomulated by employing oros technique and found to show
sufficient lag time and controlled drug release. from the in-vitro
dissolution studiesd the formulation f2 were found to be better
formulations and the lag phase and dissolution efficiency was
increased . ftir showed that there is no interaction between the
drug and excipients. in conclusion, the formulation and evaluation
of tofacitinib tablets using polymers is able to yield better lag
phase, controlled drug relewase and diseases that follow
chronopharmacological
behavior like rheumatoid arthritis can be treated
efficiently.the kinetic models used were zero, first order
equation,
higuchi model and peppas kinetic model. the tofacitinib pDDs
shows the zero order release and release mechanism of drug was
found to be anomalous diffusion.
1A-49co-PolymEric consEquEncEs on in vitro, Ex vivo And in situ
studiEs oFclindAmycin PhosPhAtE nAnoPArticlEs-loAdEd Films For
suB-gingivAl dElivEry
VRunda PatEl, RakESh PaRmaRparul institute of pharmacy anD
research, p.o. limDa, t.a-WaghoDia (391762), Dist-VaDoDara, guJarat
(inDia)
[email protected]
ABstrActsub-gingival delivery of anti-microbials to renovate
the
inflammatory response or eliminate or restrain the pathogenic
microbiota, thereby improving periodontitis, has highlighted
significant patient’s compliance with the purpose of enhanced
periodontal disease treatment. however, no one has previously
efforted for in-vitro weight loss, exvivo swelling study and
in-situ release study of a sustained-release preparation of
clindamycin phosphate nanoparticles to be used in the local
treatment of periodontal diseases. the present study was attempted
to prepare and evaluate chitosan nanoparticles loaded ethyl
cellulose (ec) with three different co-polymeric films and carried
out in-vitro polymeric weight loss, ex-vivo polymeric swelling
study and in-situ release profile of clindamycin phosphate.
chitosan containing clindamycin phosphate nanoparticles were
prepared using ionotropic gelation method. nanoparticles loaded ec
with different co-polymeric films were prepared using solvent
casting technique. the polymeric in-vitro weight loss, ex-vivo
swelling profile of films and the in-situ release of anti-microbial
were carried out in 15ml phosphate buffer (ph 6.8). Distinct result
profiles were demonstrated by the all formulations for a respective
total observation period. When the comparison was made between the
formulations having the three different co-polymers, low
substituted hydroxypropyl cellulose (l-hpc) and hydroxypropylmethyl
cellulose K4m (hpmc K4m) containing formulations were found to be
convenient, while the eudragit rl-100 (e rl-100) demonstrated
lowest results. in conclusion, for demonstrating an extended site
specific release of clindamycin phosphate the polymeric
combination, chitosan and ec with l-hpc or hpmc K4m as a co-polymer
may be a suitable inert excipient.
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22
Keywords: chitosan nanoparticles, ethyl cellulose films, low
sustained hydroxy propyl cellulose, hydroxypropylmethyl cellulose
K4m, eudraGit rl-100
1a-50
FormulAtion And EvAluAtion oF Bi lAyEr tABlEts oF sustAinEd
rElEAsE nsAid’s And immEdiAtE rElEAsE Proton PumP inhiBitor
ViShal CS, kiShoRi PatEl, aShwini RajEndRa
ABstrActin the current research, Bi-layer tablets of
esomeprazole
(immediate release) and Diclofenac sodium (sustained release)
was formulated. the objective behind the research is to find drug
release from bi layer tablets and determining model independent
parameters like mean dissolution time (mDt) and % Dissolution
efficiency (%De). esomeprazole layer was prepared by direct
compression method and Diclofenac sustained release tablets was
prepared by wet granulation method. the drug and excipient showed
no interaction when subjected to ft-ir studies. Drug release
studies was performed for immediate release layer using 0.1n hcl
for 120 min and for sustained release using phosphate buffer for 9
hours. formulations f1 to f12 were prepared using bi layer
technique, in formulation f2 and f3 % drug release of esomeprazole
was 44.500±0.75 to 99.801±0.52 and 52.428±0.49 to 99.461
respectively and in formulation f2 and f3% drug release of
diclofenac sodium was 11.196±1.11% to 75.474±0.66% and 11.286±1.08
to 71.275±2.14% respectively. mDt and % De of f2 were 4.64 hours
and 48.37% respectively and f3 were 4.64 and 48.80 %
respectively,f2 and f3 showed satisfactory results of % cumulative
Drug release, mean dissolution time and % Dissolution efficiency
which were prepared by bilayer technique, hence f2 and f3 were
selected as best formulations. thus it can be concluded that study
can be beneficial for formulation of bi layer tablets which is used
in treatment of arthritic diseases.
Keywords : esomeprazole, diclofenac sodium, Bi-layer taBlets
1A-51dEvEloPmEnt And in vitro
chArActErizAtion oF PulsAtilE drug dElivEry oF toFAcitiniB By
osmotic controllEd rElEAsE orAl systEm
mohammEd Faizan ali, t.RamyaDepartment of pharmaceutics,
tallapaDmaVathi pharmacy college,
KareemaBaD,Warangal,telangana.
[email protected]
ABsrtActthe study was aimed to formulate pulsatile drug
delivery of tofacitinib tablets by employing oros technique by
using various polymers like ethyl cellulose-100, eudragit l30 D55
and cellulose acetate-394-60s. Development of pulsatile drug
delivery of tofacitinib tablets found to show the sufficient lag
time and sufficient level of drug release that leads to
non-compliance and effective therapy. tofacitinib tablets were
prepared by using direct compression method and were characterized
for both pre-compression and post-compression parameters. from the
in-vitro drug release studies the optimized formulation f2 were
found to be better for formulations as the lag phase and controlled
release was produced sufficient and dissolution efficiency was
increased. ftir study was carried out to understand the
drug-polymer compatibility and revealed that there was no
interaction between them. thus, usages of polymers to develop
pulsatile drug of tofacitinib tablets may be suitable to give
controlled drug release and produce therapeutic action.
Keywords: pulsatile druG delivery, tofacitiniB, oros.
1A-52dEvEloPmEnt And chArActErisAtion oF simvAstAtin
nAnosusPEnsion
tanzEEl majEEd, ganESh n.S., VinEEth ChandyDepartment of
pharmaceutics, t. John college of pharmacy, gottigere
