Literature Review LITERATURE REVIEW - Shodhgangashodhganga.inflibnet.ac.in/bitstream/10603/8952/8/09_chapter 2.pdf · as a model drug. The tablet formulation containing polyvinyl

_____________________________________________________________Literature Review

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LITERATURE REVIEW

2.1 Fast Dissolving Tablet of Anti-Emetic Drugs

Gudas GK et al., (2010), prepared FDT of chlorpromazine. The tablets were prepared

with sodium starch glycolate, crospovidone, croscarmellose, L-HPC, pre-gelatinised

starch. The blends were examined for angle of repose, bulk density, tapped density,

compressibility index and Hausner’s ratio. The tablets were evaluated for hardness,

friability, disintegration time, dissolution rate and drug content.1

Kumar DN et al., (2010), prepared fast dissolving tablets of granisetron HCl using

novel coprocessed superdisintegrants consisting of crospovidone and sodium

starchglycolate in the different ratios (1:1, 1:2 & 1:3). The developed

superdisintegrants were evaluated for angle of repose, carr’s index and Hausner’s

ratio in comparison with physical mixture of superdisintegrants. The angle of repose

of the developed excipients was found to be < 250, carr’s index in the range of 10-

15% and Hausner’s ratio in the range of 1.11-1.14. Short-term stability studies on

promising formulation indicated that there were no significant changes in drug

content and in vitro dispersion time (p<0.05).2

Randale SA et al., (2010), masked the intensely bitter taste of metoclopramide and

formulated a rapid disintegrating tablets of the taste masked drug. Taste masking was

done by complexing metoclopramide with Eudragit in different ratio by the extrusion-

precipitation method. Drug-polymer complexes (DPCs) were tested for drug content,

in vitro taste in simulated salivary fluid, taste evaluation in oral cavity. The complex

having drug-polymer ratio of 1 : 2 shows significant taste masking, confirmed by

drug. Prepared tablets were evaluated for various parameters like tensile strength,

wetting time, water absorption ratio, in vitro disintegration time and disintegration in

oral cavity.3

Goel H et al., (2010), developed a disintegrating system that could be used for

preparing fast disintegrating tablets of highly water soluble drug metoclopramide

without compromising on the mechanical strength. For this purpose disintegrating

system consisting of chitosan-alginate (CTN-ALG) complex (1:1): glycine and chitin

was developed. The results revealed that when CTN-ALG and glycine were mixed in

the ratio of 30:70, the granules exhibited a minimum water sorption time and

maximum effective pore radius. The results suggested incorporation of chitin (5-10%


16

w/w) while preparing FDTs of metoclopramide to enhanced the disintegration without

compromising their mechanical strength.4

Shirshand SB et al., (2010), developed fast disintegrating tablets of proclorperazine

maleate with a view to enhance patient compliance by direct compression method. In

this method, crospovidone and croscarmellose sodium in combination were used as

superdisintigrant.5

Dahima R and Sharma R, (2010), masked the intensely bitter taste of

metoclopramide hydrochloride and to formulate orodispersible tablets of taste mask

drug. Drug-resin complex were optimize by considering parameters such as

optimization of resin concentration, optimization of swelling time, optimization of

stirring time, optimization of pH and optimization of temperature on maximum drug

loading. In vitro drug release study of taste masked tablets showed that more than 85%

of the drug release within 10 min. Thus, results conclusively demonstrated successful

masking of taste and rapid disintegration of the formulated tablets in the oral cavity.6

Mahamuni SB et al., (2009), prepared fast dissolving tablets, which can rapidly

disintegrate in the saliva using taste-masked granules of drugs with a bitter taste,

Promethazine HCl. The taste masked granules were prepared using gastro erodible

Eudragit E-100 by extrusion method. Fast dissolving tablets were prepared using

taste-masked granules and a mixture of excipients containing optimized level of

microcrystalline cellulose and starch. The effect of various superdisintegrants

crospovidone, sodium starch glycolate, croscarmellose sodium was also studied. The

prepared tablets were evaluated for taste, crushing strength, disintegration time and

dissolution.7

Singh SK et al., (2009), prepared fast disintegrating combination tablets of

omeprazole and domperidone by using pertinent disintegrant. The tablets were

prepared using mannitol as diluent and sodium saccharin as sweetening agent along

with three different levels of disintegrant. The superdisintegrant used in this study

were Kollidon CL, Ac-di-sol and SSG. The tablets were evaluated for weight

variation, hardness, friability, wetting time, water absorption ratio, disintegration time

and dissolution study. Using the same excipients, the tablets were prepared by direct

compression and were evaluated in the similar way. Drug content was estimated by

using HPLC. Tablet formulation prepared with 4.76% Ac-di-sol i.e. 10 mg showed


17

disintegration time 15 s. Also the hardness, friability, dissolution rate and assay of

prepared tablets were found to be acceptable according to standard limits.8

Shirsand SB et al., (2009), designed fast disintegrating tablets of prochlorperazine

maleate by direct compression method. Mucilage of plantago ovata and crospovidone

were used as superdisintegrants (2-8% w/w) along with microcrystalline cellulose

(20-60% w/w) and directly compressible mannitol to enhance mouth feel. The

prepared batches of tablets were evaluated for hardness, friability, drug content

uniformity, wetting time, water absorption ratio and in vitro dispersion time.

Formulation prepared by using 8% w/w of plantago ovata mucilage and 60% w/w of

microcrystalline cellulose emerged as the overall best formulation.9

Fars KA, (2007), formulated metoclopramide FDT with sufficient mechanical

strength and fast disintegration from bases prepared by both spray and freeze drying

techniques. Different disintegration accelerators were utilized to prepare the proper

FDT using various superdisintegrants (Ac-di-sol, kollidon and sodium starch

glycolate), a volatilizing solvent (ethanol) and an amino acid (glycine).10

2.2 Fast Dissolving Tablet of Other Drugs

Khemariya P et al., (2010), developed mouth dissolving tablet of meloxicam by

sublimation technology. The tablets were prepared by wet granulation procedure. The

tablets were evaluated for friability, wetting and disintegration time. Sublimation of

camphor from tablets resulted in better tablets as compared to the tablets prepared

from granules that were exposing to vacuum.11

Bhardwaj S et al., (2010), developed fast disintirating tablets of accelofenac. Tablets

were prepared by sodium starch glycolate following by direct compression technique.

The tablets were evaluated for hardness, friability, weight variation, disintegration

time, water absorption ratio and wetting time. All the formulation showed

disintegration time in range of 12.2 to 27.5 s along with rapid in vitro dissolution.12

Abed KK et al., (2010), prepared orodispersible tablets of diazepam using different

types of superdisintegrants (Ac-di-sol, sodium starch glycolate and crospovidone and

different types of subliming agents camphor and ammonium bicarbonate at different

concentrations and two methods of tablets preparations (wet granulation and direct

compression methods). The formulations were evaluated for flow properties, wetting

time, hardness, friability, content uniformity, in vivo disintegration time, release


18

profiles and buccal absorption tests. All formulations showed satisfactory mechanical

strength except formulation which contains camphor and formulation which was

prepared by direct compression method. The results revealed that the tablets

containing crospovidone as a superdisintegrant had good dissolution profile with

shortest disintegration time.13

Chandira RM et al., (2010), prepared FDT of etoricoxib using variety of super

disintegrants like primogel, kollidone, Ac-di-sol, L-HPMC, L-HPC. The prepared

tablets were evaluated for weight variation, hardness, friability, in vitro disintegration

time, wetting time and in vitro dissolution study. Formulation contain L-HPC 8%

shows the lowest disintegration time (44 s) and wetting time (52 s).14

El-Massik MA et al., (2010), utilized a maltodextrin to prepare orally disintegrating

tablets of meclizine. Tablets were prepared by both direct compression and wet

granulation techniques. The effect of maltodextrin concentrations on ODT

characteristics-manifested as hardness and disintegration time-was studied. The effect

of conditioning as a post-compression treatment on ODT characteristics was also

assessed. Maltodextrin-pronounced hardening effect was investigated using

differential scanning calorimetry (DSC) and X-ray analysis.15

Keny RV et al., (2010), developed mouth disintegrating tablets of rizatriptan benzoate

to produce the intended benefit. Mouth dissolving tablets of rizatriptan benzoate were

prepared using superdisintigrant crospovidone, carboxymethylcellulose calcium,

indion 414 and indion 234 using direct compression method. The tablets prepared

were evaluated for thickness, uniformity of weight, content uniformity, hardness,

friability, wetting time, in vivo and in vitro disintegration time, mouth feel, in vitro

drug release and assay by high performance liquid chromatography.16

Parikh BN et al., (2010), developed solid oral formulations of telmisartan which can

be prepared using less complicated and expensive processes and fulfill all prerequisites

for pharmaceutical use, i.e. long-lasting stability of the formulation under different

climatic conditions and sufficient solubility of the active substance for sufficient

gastrointestinal absorption in the slightly acidic and neutral pH region. Preferably, the

formulations should have immediate release characteristics and a dissolution showing

no essential pH dependency within the physiological relevant pH interval of the

gastrointestinal tract. Tablets were evaluated for various parameters like, weight


19

variation, content uniformity, in-vitro dissolution studies were performed using United

States Pharmacopeia (USP) apparatus type II.17

Shid SL et al., (2010), prepared orodispersible tablets of flurbiprofen using various

superdisintegrants such as croscarmellose sodium, sodium starch glycolate,

crospovidone and camphor (as subliming agent) in different ratio and subjected for

evaluation. Results revealed that the tablets of all formulations have acceptable

physical parameters.18

Rajalakshmi G et al., (2010), formulated pheniramine maleate a selective H1 receptor

antagonist into orodispersible tablets. The tablets were prepared by direct compression

method using superdisintegrants like croscarmellose sodium, crospovidone, sodium

starch glycolate, low hydroxylpropyl cellulose and pre-gelatinized starch in different

ratios. The blends examined for various pre compression parameters. Tablets were

evaluated by measuring hardness, friability, content uniformity, weight variation and

drug release pattern.19

Kalia A et al., (2009), prepared mouth dissolving tablets of oxcabazepine using two

different technologies, direct compression method and solid dispersion technology.

Tablets produced by direct compression method contain crospovidone as a

superdisintegrant and aspartame as a sweetener. Solid dispersions of oxcarbazepine

with polyvinylpyrrolidone K-30 and polyethylene glycol 6000 in different weight

ratios were prepared with a view to increase its water solubility. Oxcarbazepine solid

dispersions with polyvinylpyrrolidone K-30 in 1:2 ratios of drug: carrier showed

maximum drug release and hence, compressed along with other excipients into mouth

dissolving tablet. The results compared for both the technologies showed that the

oxcarbazepine tablets prepared using solid dispersion technology was found to have

good technological properties and satisfying and reproducible drug dissolution

profiles.20

Rao NG et al., (2009), developed rapidly disintegrating oral tablets by direct

compression using cogrinding and solid dispersion methods by using chlorthalidone

as a model drug. The tablet formulation containing polyvinyl pyrrolidone K-12 solid

dispersion showed maximum drug release than the chlorthalidone polyvinyl

pyrrolidone K-12 co-grinding method. The prepared tablets were evaluated for

hardness, friability, wetting time, disintegration time and in vitro drug release. DSC


20

and FTIR studies revealed that no chemical interaction between the drug and the

carrier. The stability studies were conducted as per the ICH guidelines and the

formulations were found to be stable with insignificant change in the hardness, and

disintegration time.21

Kumar DN et al., (2009), prepared fast dissolving tablets of fexofenadine by

effervescent method with a view to enhance patient compliance. Three super-

disintegrants viz., crospovidone, croscarmellose sodium and sodium starch glycolate

along with sodium bicarbonate and anhydrous citric acid in different ratios were used

and directly compressible mannitol to enhance mouth feel property of tablets. The

prepared batches of tablets were evaluated for hardness, friability, drug content

uniformity and in vitro dispersion time. Among the three promising formulations, the

formulation containing 8% w/w of crospovidone and mixture of 24% w/w sodium

bicarbonate, 18% w/w of anhydrous citric acid emerged as the best based on the in

vitro drug release characteristics compared to conventional commercial tablet

formulation. Short-term stability studies on the formulations indicated that there were

no significant changes in drug content and in vitro dispersion time (P<0.05).22

Swamy PV et al., (2009), designed orodispersible tablets of pheniramine maleate by

effervescent method. Mixture of sodium bicarbonate and tartaric acid were used along

with superdisintegrants pregelatinized starch, sodium starch glycolate, croscarmellose

sodium and crospovidone. The prepared batches of tablets were evaluated for

hardness, friability, drug content uniformity and in vitro dispersion time. Formulation

containing 4% w/w crospovidone and mixture of sodium bicarbonate and tartaric acid

emerged as the overall best formulation.23

Devireddy SR et al., (2009), formulated orally disintegrating tablets of levocetirizine

dihydrochloride with different superdisintegrants (sodium starch glycollate,

croscarmellose sodium, and crospovidone) using mannitol as a diluent. Tulsion-335,

Indion-204 and poly kyron T-134 cation exchange resins were used as taste-masking

agents. The drug and resin complex was prepared by the kneading method. Ten

formulations were prepared with varying combinations of superdisintegrants and ion-

exchange resins by the wet granulation technique, using polyvinylpyrrolidone K-30 as

the binder. The prepared tablets were evaluated for degree of taste masking, weight

variation, hardness, friability, in vitro and in vivo disintegration time, content

uniformity and water absorption ratio.24


21

Okuda Y et al., (2009), designed a new orally disintegrating tablet that has high

tablet hardness and a fast oral disintegration rate using a new preparation method. To

obtain rapid disintegration granules (RGD), a saccharide, such as trehalose, mannitol,

or lactose, was spray-coated with a suspension of corn starch using a fluidized-bed

granulator. As an additional disintegrant, crospovidone, light anhydrous silicic acid,

or hydroxypropyl starch was also included in the suspension. The RDGs obtained

possessed extremely large surface areas, narrow particle size distribution, and

numerous micro-pores. When tabletting these RDGs, it was found that the RDGs

increased tablet hardness by decreasing plastic deformation and increasing the contact

frequency between granules. In all tablets, a linear relationship was observed between

tablet hardness and oral disintegration time.25

Giri TK and Sa B, (2009), described the formulation of rapidly disintegrating,

diazepam tablets. The tablets were prepared by the conventional wet granulation

method using solid dispersion of the drug with PEG-4000 and/or PEG-6000. A 32

factorial design was used to reduce the number of experimental runs and to obtain

several formulations by which tablets disintegrated within 3 min and released 85% of

the drug in less than 30 min. Several tablet formulations prepared with different

amounts of PEGs in solid dispersion met the above two criteria. However, tablets

which were prepared with PEG-4000 alone at the lowest concentration disintegrated

in the shortest time (32.12 s) and released 85% of the drug most rapidly (11.03 min).26

Gupta A et al., (2009), investigated correlation between disintegration and

dissolution for immediate release tablets containing a high solubility drug and to

identify formulations where disintegration test, instead of the dissolution test, may be

used as the acceptance criteria based on International Conference on Harmonization

Q6A guidelines. A statistical design of experiments was used to study the effect of

filler, binder, disintegrating agent and tablet hardness on the disintegration and

dissolution of verapamil hydrochloride tablets. All formulation variables, i.e., filler,

binder and disintegrating agent were found to influence tablet dissolution and

disintegration, with the filler and disintegrating agent exerting the most significant

influence.27

Jacob S et al., (2009), prepared fast dissolving effervescent tablets were prepared by

the modification of nonreactive liquid based wet granulation technique. Citric acid

was coated with plastic materials such as polyethylene glycol (PEG), which provide a


22

physical barrier to the reaction. The inherent hygroscopic nature of PEG could

decrease the affinity for moisture of effervescent mixtures and can provide a

stabilizing effect. Sodium bicarbonate was blended with sugar alcohol like mannitol,

which would give a protective coating. PEG 1000 melts at body temperature and

thereby does not delay the reaction between the acid source and base.28

Singh J and Singh R, (2009), formulated and optimized orodispersible tablets of

meloxicam using a 22 factorial design for enhanced bioavailability. The tablets were

made by non-aqueous wet granulation using crospovidone and mannitol. A 22 factorial

design was used to investigate the amount of crospovidone and taste masking,

soothening hydrophilic agent (mannitol), as independent variables and disintegration

time as dependent response.29

Madan J et al., (2009), prepared fast dissolving tablets of the nutraceutical, freeze-

dried aloe vera gel by dry granulation method. The tablets were evaluated for crushing

strength, disintegration time, wetting time, friability, drug content and drug release. A

32 full factorial design was applied to investigate the combined effect of two

formulation variables - amounts of microcrystalline cellulose and mannitol. The results

of multiple regression analysis revealed that in order to obtain fast dissolving tablets of

the aloe vera gel, an optimum concentration of mannitol and a higher content of

microcrystalline cellulose should be used.30

Late SG et al., (2009), investigated effects of calcium silicate (disintegration-

promoting agent) and various lubricants on an optimized cyclodextrin-based fast

disintegrating tablets formulation. Effects of moisture treatment were also evaluated at

75, 85 and 95% relative humidities. A two factors at three levels (32) full factorial

design were used to optimize concentrations of calcium silicate and lubricant.

Magnesium stearate, being commonly used lubricant, was used to optimize lubricant

concentration in optimization study. Results of multiple linear regression analysis

revealed that concentration of calcium silicate had no effect; however concentration of

lubricant was found to be important for tablet disintegration and hardness.31

Fujii M et al., (2009), investigated the factors affecting disintegration time in the

mouth (DTM) of rapidly disintegrating tablets. The relation between DTM and

stationary time of upper punch displacement (STP) was examined using a tabletting

process analyzer. Results indicated that the bulk density of mixed excipient powder


23

used for tablet preparation affects both DTM and STP. As the value of bulk density

increased, STP became longer and DTM shorter. The results of a combination of

granules and powder with or without drug showed linear relation between apparent

volume and DTM (r2 = 0.7332). For a DTM less than 60 s, a formulation with a bulk

density greater than 0.5 g/mL should be chosen with a compression force of 5 kN. The

hardness of tablets could be greater than 3 kg if at least one high-compressibility

excipient was used in the formulation.32

Madgulkar et al., (2009), developed novel taste masked mouth-dissolving tablets of

tramadol that overcomes principle drawback of such formulation which was

inadequate mechanical strength. In this work, the bitter taste of tramadol HCl was

masked by forming a complex with an ion exchange resin Tulsion335. The novel

combination of a superdisintegrant and a binder that melts near the body temperature

was used to formulate mechanically strong tablets that showed fast disintegration. A 32

full factorial design and statistical models were applied to optimize the effect of two

factors, i.e., superdisintegrant (crospovidone) and a mouth-melting binder (gelucire

39/01). It was observed that the responses, i.e., disintegration time and percent

friability were affected by both the factors. The statistical models were validated and

can be successfully used to prepare optimized taste masked mouth-dissolving tablets

of tramadol HCl with adequate mechanical strength and rapid disintegration.33

Zade PS et al., (2009), prepared bitterless fast dissolving tablet of tizanidine

hydrochloride using Eudragit E 100 as a taste masking agent. Mass extrusion was the

technique used for preparing taste masked granules. The tablets were prepared with

three superdisintegrants e.g. sodium starch glycolate, crosscarmellose sodium and

crospovidone.34

Chaulang G et al., (2009), prepared solid dispersion of furosemide in SSG in ratios of

1:1 and 1:2 by kneading method. The solid dispersion was characterized FTIR, DSC

and XRD to ascertain if there were any physicochemical interactions between drug

and carrier that could affect dissolution. Tablets containing the solid dispersion were

formulated and their dissolution characteristics compared with commercial furosemide

tablets.35

Furtado S et al., (2008), prepared orodispersible tablets of famotidine using camphor

as subliming agent and sodium starch glycollate together with crosscarmellose sodium


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as superdisintegrants. The formulations were evaluated for weight variation, hardness

and friability, drug content, wetting time, in vitro and in vivo dispersion time, mouth

feel and in vitro dissolution. The results revealed that the tablets containing subliming

agent had a good dissolution profile.36

Mohapatra A et al., (2008), prepared the tablets of metformin using starch RX1500

and microcrystalline cellulose by direct compression. The tablets showed erosion

behavior rather than disintegration. Then lactose was incorporated which created

pores to cause burst release of drug. But these tablets did not give good mouth feel.

Thus, Pearlitol SD 200 (spray dried mannitol) was used to prepare tablets by wet

granulation (10% polyvinylpyrrolidone in Isopropyl alcohol as binder). The optimized

batches of tablets not only exhibited desired mouth feel but also disintegration time, in

vitro dispersion time, water absorption ratio and in vitro drug release. All the batches

contained 15% starch and 4% of croscarmellose sodium.37

Kuno Y et al., (2008), evaluated the effect of lubricants on the characteristics of

orally disintegrating (OD) tablets manufactured using the phase transition of sugar

alcohol. OD tablets were produced by directly compressing a mixture containing

lactose–xylitol granules, disintegrant, glidant and lubricant and subsequent heating.

The effect of the type of lubricant on the tablet characteristics was evaluated using

magnesium stearate, sodium stearyl fumarate (SSF) and talc as lubricants.38

Seong HJ and Kinam P, (2008), investigated complex formation between drugs and

ion-exchange resins and the effects of coating by various aqueous polymeric

dispersions on the complexes were evaluated for developing new sustained-release

fast-disintegrating tablets. Complexes of ion-exchange resin and dextromethorphan, a

model drug, were prepared using different particle sizes of the resins. Based on drug

loading, release profiles and scanning electron microscopy images, the coated

particles were granulated with suitable tablet excipients and then compressed into the

tablets. As the particle size of resins increased, the drug loading and release rate

decreased due to the reduced effective diffusion coefficient and surface area.39

Patel IM and Patel MM, (2008), developed fast dissolving tablets of etoricoxib.

Granules containing etoricxib, crospovidone, aspartame and menthol prepared by wet

granulation technique. Menthol was sublimed from the granules by exposing the

granules to vacuum. The porous granules were then compressed into tablets.


25

Alternatively, the tablets were prepared and later exposed to vacuum. The tablets were

evaluated for percentage friability and disintegration time. A 32 full factorial design

was applied to investigate the combined effect of two formulation variables; amount

of menthol and crospovidone. The result of multiple regression analysis indicated that

for obtaining for fast dissolving tablet optimum amount of menthol and higher

percentage of crospovidone should be used.40

Masareddy RS et al., (2008), studied two different methods direct compression and

sublimation in formulation of mouth dissolving tablets of clozapine. Total four

formulations using various superdisintegrants and subliming agents were prepared. All

prepared formulations were evaluated for physico-chemical parameters. The

formulations exhibited good disintegration properties with total disintegration time in

the range of 25 to 35 s. Comparative evaluation of two methods showed direct

compression method was a better alternative to sublimation method as its formulations

rapidly disintegrate in oral cavity. Kinetic studies indicated that all the formulations

followed first order release with diffusion mechanism.41

Shen YC et al., (2007), designed an orally disintegrating tablet formulation of

olanzapine to dissolve rapidly upon contact with saliva also described a manic patient

who has an esophageal stricture and chronic pharyngitis, two conditions that impede

the swallowing of medications. She was successfully treated for her mania with this

orally disintegrating formulation.42

Mohammad BJ et al., (2007), prepared carbamazepine solid dispersions by the co-

grinding technique using an insoluble but highly hydrophilic crospovidone and

soluble hydroxypropylmethylcellulose (HPMC) as the carriers. The ratios of drug to

carrier were 1:1, 1:5 and 1:10. Comparison of the dissolution of the drug from its

cogrounds with that of the unground drug, its ground form and the corresponding

physical mixtures revealed considerable differences. The percentage of drug dissolved

during the first 30 min (% D30), for the ground and coground drug was 75-95, whereas

the % D30 for ungrounded drug and its physical mixtures ranged from 41-62.43

Malke S et al., (2007), prepared fast dissolving tablets of oxycarbazepine containing

Avicel PH 102 as a diluent and Ac-di-sol as a superdisintegrant by wet granulation

process. All the formulations were evaluated for characteristics such as hardness,

friability, weight variation, wetting ability, disintegration time and dissolution rate.44


26

Pandey PV and Amarnath R, (2007), investigated performance of three

disintegrants, sodium starch glycolate, croscarmellose sodium and crospovidone using

intragranular and extragranular methods, both in the same quantity of 2% w/w.

Chloroquine phosphate was the drug of choice for the present study. Other excipients

used in the formulation of tablets were lactose monodehydrate, polyvinylpyrolidone

K-30 (PVP K-30), aerosil and magnesium stearate.45

Modi A and Tayade P, (2006), investigated enhancement of the dissolution profile of

valdecoxib using solid dispersion with polyvinylpyrrolidine. They also described the

preparation of fast-dissolving tablets of valdecoxib by using a high amount of

superdisintegrants. A phase solubility method was used to evaluate the effect of

various water-soluble polymers on aqueous solubility of valdecoxib.46

Ahmed IS et al., (2006), developed ketoprofen tablets which dissolve rapidly in the

mouth. The solubility and dissolution rate of poorly water-soluble ketoprofen was

improved by preparing a lyophilized tablet of ketoprofen using freeze-drying

technique.47

Cirri M et al., (2006), developed a tablet formulation based on an effective

flurbiprofen-cyclodextrin system, able to allow a rapid and complete dissolution of

this practically insoluble drug. Three different cyclodextrins were evaluated the parent

beta-cyclodextrin (previously found to be the best partner for the drug among the

natural cyclodextrins) and two amorphous, highly soluble beta-cyclodextrin

derivatives, i.e., methyl-beta-cyclodextrin and hydroxyethyl-beta-cyclodextrin.48

Shishu and Bhatti A, (2006), formulated compressed tablets of diazepam using

microcrystalline cellulose as directly compressible filler and sodium starch glycolate

as superdisintegrant. The taste masked microspheres were prepared using amino alkyl

methacrylate copolymer (Eudragit E-100) by solvent evaporation technique. Taste

evaluation of these microspheres was done by both spectrophotometric taste

evaluation technique and panel testing.49

Takagi H et al., (2005), established a pharmaceutical composition useful for rapid

disintegration, which comprises of a sparingly soluble medicament held on a gel-

forming water-soluble polymer as a solid dispersion.50

Francesco C, (2005), studied the feasibility of preparing fast-dissolving

mucoadhesive microparticulate delivery systems containing amorphous piroxicam to

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Search&itool=pubmed_AbstractPlus&term=%22Modi+A%22%5BAuthor%5D

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Search&itool=pubmed_AbstractPlus&term=%22Ahmed+IS%22%5BAuthor%5D

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Search&itool=pubmed_AbstractPlus&term=%22Cirri+M%22%5BAuthor%5D


27

improve drug residence time on sublingual mucosa and drug dissolution rate. The two

new mucoadhesive carriers Eudragit L 100 and Eudragit S 100 sodium salts, both

characterized by a fast intrinsic dissolution rate, have selected.51

Rasetti EC and Grange V, (2005), developed new non-steroidal anti-inflammatory

drugs (NSAID) formulations with faster onset of analgesic action like fast dissolving

tablets. An open-label, randomized, single dose, crossover study with a 18 days

washout period was conducted in 16 healthy volunteers to compare the

pharmacokinetic profile of 20 mg piroxicam freeze-dried tablet (Proxalyoc, Cephalon)

with that of 20 mg piroxicam capsule (Feldene, Pfizer).52

Abdelbary G et al., (2005), assessed the in vitro disintegration profile of rapidly

disintegrating tablets (RDT) was very important in the evaluation and the

development of new formulations of this type. So far neither the US Pharmacopoeia

nor the European Pharmacopoeia has defined a specific disintegration test for RDT;

currently, it was only possible to refer to the tests on dispersible or effervescent

tablets for the evaluation of RDT's disintegration capacity. In the present study, they

have evaluated the disintegration profile of RDT manufactured by main

commercialized technologies, using the texture analyzer .53

Yoshio K et al., (2005), studied the properties of rapidly disintegrating (RD) tablets

manufactured by the phase transition method. RD tablets were produced by

compressing powder containing erythritol (melting point: 122°) and xylitol (melting

point: 93-95°) and then heating at about 93° for 15 min. The hardness and oral

disintegration time of the heated tablets increased with an increase of the xylitol

content.54

Kuchekar BS et al., (2004), in the present work, an attempt was made to formulated

and evaluated mouth dissolving tablets of salbutamol sulphate. Formulations were

prepared by factorial design technique. Different disintegrates were used to formulate

fast dissolving tablets.55

Abu-Izza et al., (2004), formulated tablets which dissolve rapidly in the mouth and

provide an excellent mouth feel. The tablets of the invention comprise a compound,

which melts at about 37o or lower, have a low hardness, high stability and generally

comprise few insoluble disintegrants which may cause a gritty or bulky sensation in


28

the mouth. Convenient and economically feasible processes by which the tablets of

the invention may be produced were also provided.56

Mizumoto T et al., (2004), developed a quick disintegrating tablet in buccal cavity,

comprising a mixture of drug, a sugar (A) and an amorphous sugar (B) and after

forming a tablet, it was humidified and dried. The tablet in the present invention was

to provide stability against moisture at preserved, because the amorphous sugar

changed to the crystalline state in a non-reversible reaction after it was humidified and

dried in a manufacturing process.57

Johnson ES and Lacy J, (2004), formulated a composition for oral administration

comprising a carrier and as active ingredient, an opioid (µ-receptor) agonist, such as

fentanyl or a salt thereof, characterized in that the composition was in the form of a

fast-dispersing dosage form designed to release the active ingredient rapidly in the

oral cavity.58

Luber J and Bunick FJ, (2004), studied an immediate release tablet capable of being

chewed or disintegrated in the oral cavity, which comprises a pharmaceutically active

ingredient and a matrix comprising polyethylene oxide having a weight average

molecular weight of from about 500,000 to about 10,000,000. The tablets possesses

exceptionally good mouth feel and stability.59

Hall M et al., (2004), developed a composition comprising a carrier and an active

ingredient, wherein the carrier was fish gelatin and the composition was a fast-

dispersing dosage form designed to release the active ingredient rapidly on contact

with a fluid. In one embodiment, the composition was designed for oral

administration and releases the active ingredient rapidly in the oral cavity on contact

with saliva. The fish gelatin can be obtained from cold water fish sources and was

preferably the non-gelling, non-hydrolyzed form. A process for preparing such a

composition and a method of using fish gelatin in a fast dispersing dosage form were

also provided.60

Lalla JK and Mamania HM, (2004), studied the inclusion complex of rofecoxib, an

NSAID with β-cyclodextrin using ball milling technique has been prepared and

evaluated using differential scanning calorimetry thermograph. The fast dissolving

tablet composition with 25 mg equivalent rofecoxib showed complete release of


29

rofecoxib in 12 min as compared to 20% drug release from the conventional release

marketed tablets during the same period.61

Shirwaikar AA and Ramesh A, (2004), formulated atenolol as fast disintegrating

tablets using three superdisintegrants, croscarmellose sodium (Ac-di-sol),

crospovidone (Polyplasdone XL) and sodium starch glycolate (Explotab). All the

superdisintegrants were used at different concentration levels to assess their efficiency

and critical concentration level.62

Valleri M et al., (2004), investigated the possibility of developing glyburide tablets,

allowing fast, reproducible and complete drug dissolution, by using drug solid

dispersion in polyethylene glycol. The glyburide dissolution profile from the newly

developed tablets was clearly better than those from various commercial tablets at the

same drug dosage.63

Drooge DJ et al., (2004), studied anomalous dissolution behavior of tablets consisting

of sugar glass dispersions was investigated. The poorly aqueous soluble diazepam was

used as a lipophilic model drug. The release of diazepam and sugar carrier was

determined to study the mechanisms governing dissolution behavior.64

Gohel M et al., (2004), developed mouth dissolving tablets of nimesulide. Granules

containing nimesulide, camphor, crospovidone and lactose were prepared by wet

granulation technique. Camphor was sublimed from the dried granules by exposure to

vacuum. The porous granules were then compressed. Alternatively, tablets were first

prepared and later exposed to vacuum. The tablets were evaluated for percentage

friability, wetting time, and disintegration time. In the investigation, a 32 full factorial

design was used to investigate the joint influence of 2 formulation variables: amount

of camphor and crospovidone.65

Schroeder M and Steffens K, (2003), prepared rapidly disintegrating preparations

containing at least one active pharmaceutical ingredient and at least one excipient by a

simple process in which the predominant part of the complete composition of the

ingredients was granulated, the resulting granules and where appropriate, the

remainder of the ingredients were shaped in the presence of liquid virtually without

pressure, and the resulting shaped articles were dried.66

Zakarian N et al., (2003), invented dispersible tablets containing macrolides as active

ingredients either on their own or associated with other active ingredients, in addition


30

to a method for the production thereof. The dispersible tablets were characterized in

that the macrolide was chosen from a group that was made up of pristinamycin,

azithromycin, roxithromycin, clarithromycin and spiramycin.67

Murray OJ et al., (2003), studied fast dispersing solid dosage forms that preferably

dissolve in the oral cavity within sixty, more preferably within thirty, most preferably

within ten seconds. A novel feature of the solid dosage forms according to the

invention resided in the fact that the composition was essentially free or absolutely

free of mammalian gelatin.68

Laruelle C et al., (2003), established pharmaceutical dosage forms with rapid

disintegration in the mouth and to their process of preparation. The pharmaceutical

dosage forms comprised of at least one active principle dispersed in a mixture of

excipients and were characterized in that the mixture of excipients comprised at least

one weakly compressible diluting agent other than trehalose and a copolymer of 1-

vinylpyrrolidin-2-one and of vinyl acetate.69

Murali M et al., (2002), designed nimodipine tablets with fast in vitro release rates

using nimodipine-modified gum karaya co-grinding mixtures. Co-grinding mixtures of

nimodipine and gum karaya were also prepared to highlight the efficiency of modified

gum karaya.70

El-Arini SK and Clas SD, (2002), studied in vitro disintegration behavior of fast

dissolving system, manufactured by the main commercialized technology, using the

texture analyzer instrument.71

Simone S and Peter CS, (2002), prepared two types of tablets containing coated

ibuprofen as a high dosed model drug. The properties of the water dispersible tablet,

such as porosity, hardness, disintegration time and increase in viscosity after

dispersion, were investigated. The selected tablet formulation, containing 26%

galactomannan and 5% crospovidone, disintegrated before the galactomannan started

to swell. These tablets dispersed in water within 40 s and showed a crushing strength

of 95 N.72

Sunanda H and Bi Y, (2002) developed rapidly disintegrating tablets using both

direct compression and wet compression methods. Tablet properties such as porosity,

tensile strength, wetting time and disintegration time were evaluated and the

formulation and disintegration time of the tablets were elucidated. Formulation and


31

preparation conditions were optimized using polynomial regression or artificial neural

network.73

Khankari et al., (2001), formulated a rapidly dissolving robust dosage form. The

invention was directed to a hard tablet that can be stored, packaged and processed in

bulk. The tablet dissolved rapidly in the mouth of the patient with a minimum of grit.

The tablet was created from an active ingredient mixed into a matrix of no direct

compression filler and a relatively high lubricant content.74

Gilis P and De Conde V, (2000), formulated a fast-dissolving tablets for oral

administration comprising of an active ingredient, a therapeutically effective amount

of galanthamine hydrobromide and a pharmaceutically acceptable carrier,

characterized in that the said carrier comprised a spray-dried mixture of lactose

monohydrate and microcrystalline cellulose as diluents, and a disintegrant; and direct

compression process for preparing such fast dissolving tablets was used.75

2.3 Formulations of Promethazine Theoclate

Argemi A et al., (2010), prepared and characterized of transdermal patches of

promethazine. A mixture of ethylene vinyl acetate and Eudragit ( E100) (80:20, w/w)

was used as a polymeric matrix to obtain a thin membrane. Patches synthesized in this

way were loaded with about 1% promethazine. The drug release and diffusion process

through a membrane have been studied chromatographically using a Franz diffusion

cell. Results have shown that a sustained delivery for more than 24 h was obtained.76

Bhanja S et al., (2010), formulated and evaluated of mucoadhesive buccal tablets

containing promethazine to circumvent the first pass effect and to improve its

bioavailability with reduction in dosing frequency and dose related side effects. The

tablets were prepared by direct compression method. Eight formulations were

developed with varying concentrations of polymers like carbopol 934, polyethylene

oxide and hydroxy propyl methyl cellulose. The tablets were tested for weight

variation, hardness, surface pH, drug content uniformity, swelling index and

bioadhesive strength and in-vitro drug dissolution study. The in vitro release kinetics

studies reveal that all formulations fits well with zero order kinetics followed by

korsmeyer-peppas, first order and then higuchi’s model and the mechanism of drug

release was non-fickian diffusion.77


32

Adhikari SN et al., (2010), developed buccal patches for the delivery of

promethazine using sodium alginate with various hydrophilic polymers like carbopol

934 P, sodium carboxymethyl cellulose, and hydroxypropyl methylcellulose in

various proportions and combinations were fabricated by solvent casting technique.

Various physicomechanical parameters like weight variation, thickness, folding

endurance, drug content, moisture content, moisture absorption, and various ex vivo

mucoadhesion parameters like mucoadhesive strength, force of adhesion and bond

strength were evaluated. An in vitro drug release study was designed and it was

carried out using commercial semipermeable membrane. All these fabricated patches

were sustained for 24 h and obeyed first-order release kinetics.78

Patel RS and Poddar SS, (2009), prepared and evaluated of mucoadhesive buccal

patches for the controlled systemic delivery of promethazine theoclate to avoid first

pass hepatic metabolism. The developed patches were evaluated for the

physicochemical, mechanical and drug release characteristics. The patches showed

desired mechanical and physicochemical properties to withstand environment of oral

cavity. The in vitro release study showed that patches could deliver drug to the oral

mucosa for a period of 7 h. The patches exhibited adequate stability when tested

under accelerated conditions.79

Sekhar K et al., (2008), described buccal permeation of promethazine theoclate and

its transbuccal delivery using mucoadhesive buccal patches. Permeation of drug was

calculated in vitro using porcine buccal membrane and in vivo in healthy humans.

Buccal formulations were developed with hydroxyethylcellulose and evaluated for in

vitro release, moisture absorption, mechanical properties and bioadhesion. Optimized

formulation was subjected for bioavailability studies in healthy human volunteers.80

2.4 Formulations of Prochlorperazine Maleate

Obata Y et al., (2010), developed transdermal drug delivery system for

prochlorperazine (PCPZ) and performed an in vitro skin permeation study with

hairless mouse skin. When the concentration of L-menthol in the hydrogel was

0-0.5%, the PCPZ flux was small; on the other hand, the flux was increased

remarkably when the L-menthol concentration was higher than 1%. The optimal

formulation of hydrogel would be contained 20% isopropanol (IPA), 10% N-methyl-

2-pyrrolidone (NMP), 2% L-menthol and 1% PCPZ. The strong inhibitory effects to


33

stereotyped behavior were observed at 4 h after administration of PCPZ hydrogel, and

the efficacy was sustained for at least 8 h after the administration in mice in vivo.

Thus, it was considered that PCPZ was delivered to brain via systemic circulation by

the administration of PCPZ hydrogel.81

Suresh S et al., (2010), designed fast disintegrating tablets of prochlorperazine

maleate with crospovidone (upto 3% w/w) and croscarmellose sodium (upto 5% w/w)

in combination were used as superdisintegrants. The prepared formulations were

evaluated for hardness, friability, drug content uniformity, dispersion time, wetting

time and water absorption ratio. Among the formulations tested, formulation

containing 5% w/w of croscarmellose sodium and 3% w/w of crospovidone as

superdisintegrant emerged as the overall best based on drug release characteristics in

pH 6.8 phosphate buffer compared to commercial conventional tablet formulation.82

Misao N et al., (2009), developed oral disintegrating film

containing prochlorperazine using microcrystalline cellulose, polyethlene glycol and

hydroxypropylmethyl cellulose as the base materials. The uniformity of dosage units

of the preparation was acceptable according to the criteria of JP15 or USP27. The

film showed an excellent stability at least for 8 weeks when stored at 40° and 75% in

humidity. The dissolution test revealed a rapid disintegration property, in which most

of prochlorperazine dissolved within 2 min after insertion into the medium.83

Finn A et al., (2005), developed buccal dosage form of prochlorperazine and also

conducted two clinical studies to characterize the single-dose and multiple-dose

pharmacokinetics of prochlorperazine and its metabolites after buccal administration.

The results of these studies demonstrate that buccal administration of

prochlorperazine produces plasma concentrations more than twice as high as an oral

tablet, with less than half the variability. In addition to the metabolites, N-desmethyl

prochlorperazine and prochlorperazine sulfoxide, 2 new metabolites, prochlorperazine

7-hydroxide and prochlorperazine sulfoxide 4-N-oxide, were identified and

quantitated. Exposure to metabolites after the buccal prochlorperazine formulation

was approximately half that observed after the oral tablet. Buccal administration of

prochlorperazine, twice daily, should enhance the therapeutic role of prochlorperazine

in preventing and treating nausea and vomiting.84


34

Singh S et al., (1999), prepared and evaluated buccal prochlorperazine (Bukatel) for

its efficacy and tolerability with commonly used metoclopramide. Bukatel was well

tolerated and well rated by both patients and investigators with no adverse effects on

buccal mucosa and causing less drowsiness and sedation. Results indicated that

Bukatel was safe and effective for the treatment of nausea and/or vomiting in patients

suffering from vertiginous disorders and could be safely and strongly recommended

as an alternative to less bioavailable and indiscriminately used oral metoclopramide

tablets.85

Nagarsenker MS et al., (1998), prepared coevaporates of prochlorperazine maleate

(PCPM) by using different polymers by solvent evaporation technique. Ethyl

cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose phthalate were

used in preparation of coevaporates. The coevaporates were characterized by X-ray

diffraction studies, IR spectrophotometry and Differential scanning calorimetry.

Dissolution behavior of coevaporates was studied using buffer solution with pH 1.2

and 6.8 by half change method. A two level, two factor factorial design was used to

quantitate effect of polymers on dissolution profile of PCPM. Dissolution of drug in

pH 6.8 buffer improved with increasing content of hydroxypropyl methylcellulose

phthalate in coevaporates.86


35

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