SOLID STATE CHARACTERIZATION AND IN VITRO DISSOLUTION

www.wjpps.com Vol 7, Issue 5, 2018.

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Yadav et al. World Journal of Pharmacy and Pharmaceutical Sciences

SOLID STATE CHARACTERIZATION AND IN VITRO DISSOLUTION

ENHANCEMENT OF IRBESARTAN BY SOLID DISPERSION

ADSORBATE TECHNIQUE

Dipak R. Yadav* and Dr. S. K. Shah1

*Saraswati Institute of Pharmaceutical Sciences, Dhanap, Gandhinagr-382355, Gujarat.

1Department of Pharmaceutics, Principal, Saraswati Institute of Pharmaceutical Sciences,

Dhanap, Gandhinagr-382355, Gujarat.

ABSTRACT

Various processes were used for the solubility enhancement of

Irbesartan, solid dispersion adsorbate technique is one of them. The

improvement in solubility and in-vitro drug release were observed. The

in-vitro drug release of solid dispersion adsorbate of PEG 4000 and

Poloxamer 188 prepared by fusion method was significantly improved

the dissolution compared to solid dispersion of PVP K-30 and pure

drug. The in-vitro release studies showed 90% of drug release in 30

minutes. Solid-state characterization based on FT-IR spectroscopy,

DSC and in vitro dissolution study was carried out to investigate the

mechanisms of carrier dissolution enhancement. Enhanced Solubility

and dissolution rate of Irbesartan show dissolution rate limited absorption and the onset of

action is beneficial to treat hypertensive patients. Overall, the formulations FENPEG (1:3)

and FENPOL (1:3) which showed better in-vitro dissolution profile, lower MDT and f2

values. Tablets of FENPEG (1:3) prepared and compared with pure drug tablets and marketed

formulation. Tablets of FENPEG (1:3) gives highest drug release 99% in 60 min. additionally

the prepared tablets checked for stability study and found stable after 1 month. Hence, based

on above results it concluded that the FENPEG (1:3) was optimized formulation.

KEYWORDS: Solid Dispersion, Adsorbate, Irbesartan.

INTRODUCTION[1,4]

Solid Dispersion Adsorbates were ready like that of Solid Dispersion, however solely

WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES

SJIF Impact Factor 7.421

Volume 7, Issue 5, 1137-1155 Research Article ISSN 2278 – 4357

Article Received on

04 March 2018,

Revised on 24 March 2018,

Accepted on 14 April 2018

DOI: 10.20959/wjpps20185-11538

*Corresponding Author

Dipak R. Yadav

Saraswati Institute of

Pharmaceutical Sciences,

Dhanap, Gandhinagr-

382355, Gujarat.


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distinction was Neusilin US2 (selected adsorbent) was more once the preparation of

homogeneous suspension as that in Solid Dispersion formulation. The co-melt of carrier and

also the drug was adsorbable singly on to the surface of Neusilin US2 to arrange free flowing

granules of solid dispersion adsorbates. Dissolution rates for Solid Dispersion Adsorbates

were bigger than Solid Dispersion. the improved dissolution rates of Solid Dispersion

Adsorbates is also because of several factors like diminished particle size of drug, specific

style of drug in these Solid Dispersion Adsorbates, additionally to the rise in drug wettability

and preventing of drug aggregation by every compound.

Neusilin ® was employed in this investigation as associate degree adsorbent. It exhibits high

specific space, enlarged surface sorption, porosity, anti-caking and flow enhancing properties.

The H bonding potential of silanol within the native surroundings on oxide surfaces is well

documented. Within the gift investigation, a mixture of solid dispersion and soften sorption

technology was used to arrange Solid Dispersion Adsorbate. The solid dispersions adsorbates

were characterised by fourier remodel infrared spectroscopic analysis (FTIR), differential

scanning measure (DSC) and diffraction study (XRD). The Solid Dispersion Adsorbate could

be a promising and a unique approach for the dissolution enhancement and will be used for

the event of appropriate solid dose kind for commercialisation.

The aim of present study is to prepare solid dispersion adsorbate of Irbesartan by solid

dispersion adsorbate technique. Preparation, Evaluation and optimization of Solid dispersion

adsorbate tablets to achieve more than 80% drug release after 30 min in drug release study.

MATERIALS AND METHODS

Instruments and Apparatus

Digital weighing balance (Reptech weighing balance Ltd, Ahmadabad), Tablet punching

machine (Hardik Engineering work, Ahmadabad), Hardness tester (Monsanto Hardness

tester, Ahmadabad), Disintegrator apparatus (Electrolab Ltd, Mumbai) Dissolution apparatus

(Electrolab Ltd, Mumbai), Friabilator apparatus (Electrolab Ltd, Mumbai), Bulk density

apparatus (Electrolab Ltd, Mumbai.)UV spectrophotometer (Shimadzu 1601, Kroyoto,

Japan.), FTIR (FTIR 8400S, Shimadzu, Kroyoto, Japan.)

DSC(DSC TA-60WS, Kroyoto, Japan.)

Ingredients and Excipients

Irbesartan (Torrent Pharmaceutical LTD), Neusilin US2 (Gangwal Chemicals, Mumbai,


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India), PVP K-30 (ACS chemicals, Ahmedabad), Poloxamer 188 (ACS chemicals,

Ahmedabad), PEG 4000, (ACS chemicals, Ahmedabad) Talc, Lactose, Magnisum stearate

(ACS chemicals, Ahmedabad).

Pre-Formulation Study[5,8]

Characterization of Drug (Irbesartan)

Organoleptic Characteristics

Colour of Drug was characterized and recorded using descriptive terminology.

Flow Properties

1) Bulk density and tapped density

An accurately weighed quantity of the blend (W), was carefully poured into the graduated

cylinder and the volume (Vo) was measured. Then the graduated cylinder with lid, set into the

density determination apparatus (Tapped Density Apparatus) the density apparatus was set for

100 taps and after that the volume (Vf) was measured which was tapped volume. The bulk

density and tapped density were calculated by using the following formulas.

Bulk density = W/ V0 Tapped density = W/ Vf

2) Compressibility index (CI) / Carr’s index

It was obtained from bulk and tapped densities. It was calculated by using the following

formula.

% Carr’s index = (T.D. - B.D. ÷ T.D.) × 100

3) Hausner’s ratio

Hausner’s ratio is a number that is correlated to the flow ability of a powder. It is measured

by ratio of tapped density to bulk density.

Hausner’s ratio = (Tapped density ÷ Bulk Density)

4) Angle of repose

Angle of repose of powder was determined by the funnel method. Accurately weight powder

blend were taken in the funnel. Height of the funnel was adjusted in such a way the tip of the

funnel just touched the apex of the powder blend. Powder blend was allowed to flow through

the funnel freely on to the surface. Diameter of the powder cone was measured and angle of

repose was calculated using the following equation.

Tan θ= h/r


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Identification of drug by FTIR[9]

The Fourier transform infrared spectrum of moisture free powdered sample of Drug was

recorded on IR spectrophotometer. The range of spectra was found to be 600 to 4000cm-1

The

characteristics peaks of different functional group were compared with reported standard

peak.

DSC Study of Irbesartan[9]

Differential Scanning Calorimeter allows the fast evaluation of possible incompatibilities,

because it shows changes in the appearance, shift of melting endotherms and isotherms’,

and/or variations in the corresponding enthalpies of reaction. The DSC thermograms of pure

drug recorded.

Calibration Curve[10,14]

Preparation of standard calibration curve of Irbesartan.

Principle: The Irbesartan exhibits peak absorbance at 250 nm in Water and Methanol in ratio

of (9:1).

Instrument used: Shimadzu, UV Spectrophotometer, Japan.

Procedure

Preparation of standard solution: 10 mg of Irbesartan was accurately weighed in to 100 ml

volumetric flask and dissolved in small quantity of water: methanol (90:10).

Preparation of working standard solutions: From standard solution of 100 ml, aliquots of

1ml, 2ml, 3ml, 4ml and 5ml were pipetted into 10ml volumetric flasks. The volume was

made up distilled water get the final concentration of 10μg/ml, 20 μg/ml, 30μg/ml,

40μg/ml and 50μg/ml respectively. The absorbance of each concentration was measured

at 250 nm. The Beer’s range is 10-50μg/ml.

Phase Solubility

Phase-solubility studies were performed by the method of Higuchi and Connors. IRB, in

constant amounts (5 mg) that exceeded its solubility, was transferred to screw capped vials

containing 20 ml of aqueous solution of PVP K-30, Poloxamer 188 and PEG 4000 at various

molar concentration. The contents were stirred on rotary shaker (Remi, India) for 72 hrs. At

370C ± 0.1°C and 300 rpm. The time duration was fixed based on pilot experiment and found

to be sufficient to achieve equilibrium of mixture. After reaching equilibrium, samples were


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filtered through a 0.22 μm membrane filter, suitably diluted and analyzed

spectrophotometrically for drug content at 230 nm. Solubility studies were performed in

triplicate. The solubility of Irbesartan in pure water is 0.0084 mg/ml.

Solid Dispersion of Irbesartan

As we know that Irbesartan belongs from BCS class II which have low solubility. So first of

all we are going to enhance solubility of Irbesartan.

A) Physical mixture

Physical mixture (PM) of PVP K-30, PEG 4000 and Poloxamer 188 with Irbesartan was

prepared by geometric mixing of Irbesartan respectively without applying pressure. The

required quantities of Irbesartan with PVP K-30, PEG 4000 and Poloxamer 188 respectively

were taken in a glass mortar and mixed for 15 minutes. Each carrier was taken in drug: carrier

ratio of 1:1, 1:2 and 1:3.

Drug polymer ratio for solid dispersion

Formulation Code Drug : Carrier ratio Carrier

PMPVP(1:1) 1:1 PVP K 30

PMPVP(1:2) 1:2 PVP K 30

PMPVP(1:3) 1:3 PVP K 30


PMPEG(1:1) 1:1 PEG 4000

PMPEG(1:2) 1:2 PEG 4000

PMPEG(1:3) 1:3 PEG 4000


PMPOL(1:1) 1:1 POLOXAMER 188



B) Solvent Evaporation Method

Irbesartan and PVP K-30 were taken in ratio of 1:1, 1:2 and 1:3. The polymer was dissolved

in an adequate amount of methanol. Then add Irbesartan in to the solution under continuous

stirring. The solvent was then rapidly evaporated then sized into different sieve fractions and

stored.


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Formulation of Irbesartan solid dispersion


SEPVP(1:1) 1:1 PVP K 30

SEPVP(1:2) 1:2 PVP K 30

SEPVP(1:3) 1:3 PVP K 30

Evaluation of Solid Dispersion of Irbesartan

Physical Appearance

All the ratios of Irbesartan solid dispersions were evaluated for colour and appearance.

Drug Content

A quantity, which was equivalent to 80 mg of drug, was accurately weighed and transferred

to 100 ml volumetric flask. Then the volume was made up with water and Methanol (9:1) and

shaken for 10 min to ensure complete solubility of the drug. Then the solution was filtered

and filtrate was diluted suitably and Assayed for drug content at 250 nm by using UV-Visible

spectrophotometer.

In vitro dissolution study

The prepared solid dispersions were subjected to in vitro dissolution. Dissolution test was

carried out using USP Paddle method [apparatus 2]. The stirring rate was 50 rpm, pH-0.1 N

HCl was used as dissolution medium and dissolution medium was 0C.

Samples of 5 ml was withdrawn at regular intervals of time, filtered and replaced with 5 ml

of fresh dissolution medium, dilutions were made and analyzed for Irbesartan at 250 nm by

using UV-visible spectrophotometer.

Solid Dispersion Adsorbate of Irbesartan

Solid dispersion adsorbate by fusion method

Solid dispersions were prepared by weighed quantities of Irbesartan and Poloxamer 188 and

PEG4000. The Poloxamer 188 and PEG were molten in a porcelain dish at different

processing temperatures. Once homogeneous slurry was obtained, it was cooled rapidly at

different cooling temperatures and passed through number 22 sieves to obtain a uniform

particle size and stored in a desiccator at room temperature and evaluated. SDAs were

prepared similar to that of SD, but only difference was NUS was added after the preparation

of homogeneous slurry as that in SD.


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Formulation of Irbesartan solid dispersion with PEG4000 (Without Neusilin).

Formulation code Drug: carrier ratio Polymer

FEPEG (1:1) 1:1 PEG 4000

FEPEG (1:2) 1:2 PEG 4000

FEPEG (1:3) 1:3 PEG 4000

Formulation of Irbesartan solid dispersion adsorbate with PEG4000 (with Neusilin).


FENPEG (1:1) 1:1 PEG 4000

FENPEG (1:2) 1:2 PEG 4000

FENPEG (1:3) 1:3 PEG 4000

Formulation of Irbesartan solid dispersion with Poloxamer 188 (without Neusilin).


FEPOL(1:1) 1:1 Poloxamer 188



Formulation of Irbesartan solid dispersion adsorbate with poloxamer 188 (with

Neusilin).


FENPOL1:1 1:1 Poloxamer 188



Formulation Table for all batches.

BATCHES IRBESARTAN PVPK30 PEG4000 POLOXAMER 188 NEUSILIN

PMPVP(1:1) 100 100 - - -

PMPVP(1:2) 100 200 - - -

PMPVP(1:3) 100 300 - - -

PMPEG (1:1) 100 - 100 - -

PMPEG (1:2) 100 - 200 - -

PMPEG (1:3) 100 - 300 - -

PMPOL(1:1) 100 - - 100 -

PMPOL(1:2) 100 - - 200 -

PMPOL(1:3) 100 - - 300 -

SEPVP(1:1) 100 100 - - -

SEPVP(1:2) 100 200 - - -

SEPVP(1:3) 100 300 - - -

FEPEG (1:1) 100 - 100 - -

FEPEG (1:2) 100 - 200 - -

FEPEG (1:3) 100 - 300 - -

FENPEG (1:1) 100 - 100 - 100

FENPEG (1:2) 100 - 200 - 200

FENPEG (1:3) 100 - 300 - 300

FEPOL(1:1) 100 - - 100 -

FEPOL(1:2) 100 - - 200 -

FEPOL(1:3) 100 - - 300 -

FENPOL(1:1) 100 - - - 100

FENPOL(1:2) 100 - - - 200

FENPOL(1:3) 100 - - - 300


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Note:-All weight is in mg.

Characterization of Solid Dispersion Adsorbate of Irbesartan

Drug content

In vitro dissolution studies.

Fourier transform infrared spectroscopy

Differential scanning calorimetry

Statistical analysis

The U.S. FDA’s guidance for industry on dissolution testing of immediate release (IR) solid

oral dose forms (1997), as well as SUPAC-IR (1995), SUPACMR (1997) and bioavailability

and bioequivalence study guidance for oral dosage forms, describes the model independent

mathematical approach proposed by Moore and Flanner for calculating a dissimilarity factor

f1 and a similarity factor f2 of dissolution across a suitable time interval. The similarity factor

f2 is a measure of similarity in the percentage dissolution between two dissolution curves and

is defined by following equation,

f2=50×log {[1+ (1/n) Σt=1n (Rt-Tt) 2]-0.5 ×100}

Where,

n is the number of withdrawal points,

Rt is the percentage dissolved of reference at the time point t And

Tt is the percentage dissolved of test at the time point t.

MDT (mean Dissolution time)

A higher MDT value indicates a greater drug retarding ability. To understand the extent of

improvement in dissolution rate of FUR from its PMs and SDs with PEG and PVP, the

obtained dissolution data of all samples were fitted into the equation;

Where i is the dissolution sample number, n is the number of dissolution times, tmid is time at

the midpoint between times ti and ti-1, and ∆M is the amount of FUR dissolved (µg) between

times ti and ti-1.


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Formulation of the Tablet

Drug, SD of PEG (FEPEG 1:3) and Solid dispersion adsorbate of FENPEG (1:3) along with

all the excipients were accurately weighed and passed through 22 number sieves. Then the

powder was uniformly mixed in polybag. The resulting powder mixture was directly

compressed in to tablet using rotary tablet machine.

Formulation table of Tablet preparation from SD.

Ingredients (mg) Tablets of Pure

Drug

Tablets of

FEPEG (1:3)

Tablets of

FENPEG (1:3)

Irbesartan 150.00 -- --

SD of Irbesartan Eq. to 150 mg of Drug -- 600.00 600.00

MCC (Avicel 102) 579.00 129.00 129.00

Talc 7.00 7.00 7.00

Magnesium Stearate 14.00 14.00 14.00

Total 750.00 750.00 750.00

Characterization of Tablet

The prepared tablets were evaluated for weight variation, thickness, hardness, friability,

disintegration time, drug content analysis, and in vitro dissolution.

A. Weight Variation

B. Thickness

C. Hardness

D. Friability

E. Drug Content

F. Drug release study

G. Stability studies

RESULTS AND DISCUSSION

Preformulation Studies

Characterization of Drug

Results of Irbesartan characterization are given in below table.


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Characterization of Irbesartan.

Sr. No. Characteristic Properties Observation/Result

1 Organoleptic

Characteristics

Colour white to practically white fine

powder

2 Odour Characteristic odour

4

Flow Properties

Bulk density (g /ml) 0.45

5 Tapped density (g /ml) 0.51

6 Carr’s index (%) 16.48

7 Hausner’s ratio 1.07

8 Angle of repose (θ°) 58.08

9 Solubility Solubility Soluble in Methanol

Insoluble in water.

Based on above results it concluded that the API itself having good flow property because

Hausner ratio is 1.07. Further solubility found in methanol and water.

Ftir Study of Drug

The IR spectra of the drug showed their characteristic absorption bands which was given in

figure.

DSC Study of Irbesartan

The differential scanning calorimetric thermograms of the irbesartan are shown in below

figure 6.1.3. Irbesartan shows sharp endothermic peak at 189.12ºC which supports literature

data.

https://pubchem.ncbi.nlm.nih.gov/compound/water


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Calibration Curve of Drug

Calibration Curve of Irbesartan

Overlay graph of Irbesartan at 210 nm in water:methnol (9:1).

Calibration curve of Irbesartan in water and methanol (1:9) at 210 nm.


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Phase Solubility

Phase solubility analysis has been among the preliminary requirements towards the

optimization of the development into inclusion complexes of the drugs as it permits the

evaluation of the affinity between different carriers and drug molecule in water. This process

has been used by many researchers for the determination of the exact molar ratios in which

the drugs could make complexes with different carriers.

Comparison of solubility for ratio of drug and different polymer.

Polymer Drug : Carrier ratio Increased solubility

PVPK-30 1:1 13 fold

PVPK-30 1:2 18 fold

PVPK-30 1:3 25 fold


Poloxamer 188 1:1 6 fold




PEG 4000 1:1 10 fold

PEG 4000 1:2 16 fold

PEG 4000 1:3 23 fold

Characterization of Solid Dispersion

Differential Scanning Calorimetry (Dsc) Analysis

DSC thermo gram of pure drug Irbesartan and solid dispersion of Irbesartan with PVPK 30,

Poloxamer 188 and PEG 6000 shown in below figure.6.5. Pure drug melting point was

observed 189.12°C. Different solid dispersion of Irbesartan with carriers shows melting point

of drug at 247.51°C in PVPK 30, 264.63°C in Poloxamer 188 and 256.35°C in PEG 4000.

Increased in melting point indicates that in such systems the drug has basically maintained its

original crystallinity.


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DSC thermogram of A. Drug, B. PMPVP, C. PMPEG and D.PMPOL.

Infrared (IR) Spectroscopic Analysis

Fourier transform infrared spectroscopy (FT-IR) has been used to assess the interaction

between drug and polymer in the solid state. The chemical interaction between the drug and

the carrier often leads to identifiable changes in the infrared (IR) profile of SD’s. However,

some of the changes are very subtle requiring careful interpretation of the spectrum.

The FTIR spectra of A. Drug, B. SD with PVPK 30, C. SD with Poloxamer 188 SD with

PEG 4000 and E. SD with Poloxamer 188 with Neusilin are shown in Figure 6.6.

FTIR of A. Drug, B. PMPVP, C. PMPEG and D. PMPOL E. FENPEG.


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X-Ray Powder Diffraction (Xrd)

The XRD spectra of pure drug Irbesartan and solid dispersion of Irbesartan with PVPK 30,

Poloxamer 188 and PEG 6000 are depicted in Figure 6.7. The diffraction spectrum of pure

Irbesartan indicated its crystalline nature as demonstrated by numerous peaks observed at 2θ

of 4.7, 12.5, 13.3, 17.1, 19.4, 21.2, 22.6, 23.2 and 27.3. Crystalline properties of PEG were

also confirmed by two peaks with the highest intensity at 2θ of 19.3 and 23.4.

XRD of A. Drug, B. PMPVP, C. PMPEG and D. PMPOL.

In-Vitro Dissolution Study

Drug release data of pure drug Irbesartan and prepared SD with PVPK 30, Poloxamer 188

and PEG 4000 shows in table 6.5. Based on that results, pure drug release only 9.40% after

60 min which was lowest drug release profile in all. Further in SD which was prepared by

physical method, no any significant improvement observed in drug release in all SD e.g.

PVPK 30, Poloxamer 188 and PEG 4000. Only 28% drug release observed in SD with PEG

by physical method. SD of solvent evaporation method and fusion method gives drastic

change in drug release after 60 min which was more than 80% in all SD’s. SD by fusion

method without neusilin gives 60% drug release in 30 min where with neusilin gives more

than 90% drug release in 30 min. So the neusilin gives significant impact on drug release with

SD’s.


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Comparison of Different solid dispersion of drug with PVPK 30, PEG 4000 and Poloxamer

188 gives in figures.

Drug Release of Irbesartan solid dispersion and solid dispersion adsorbate in 1 hour.

Batches 10 min 20 min 30 min 40 min 50 min 60 min

IRB 3.40 4.91 5.79 7.70 8.06 9.40

PMPVP(1:1) 4.40 5.92 6.03 8.70 9.20 10.15

PMPVP(1:2) 5.15 6.25 8.25 14.23 16.23 18.2

PMPVP(1:3) 5.65 7.49 10.90 17.91 18.97 21.64

PMPEG (1:1) 5.65 6.10 7.85 9.20 12.25 13.68

PMPEG (1:2) 5.76 8.34 12.64 15.65 20.11 23.22

PMPEG (1:3) 8.23 10.21 14.25 20.21 25.65 28.23

PMPOL(1:1) 5.42 6.01 7.42 8.25 11.25 12.01

PMPOL(1:2) 6.28 7.56 9.25 10.25 13.22 14.78

PMPOL(1:3) 7.00 8.25 11.20 12.59 15.99 17.76

SEPVP(1:1) 10.15 23.65 38.8 55.65 76.95 91.36

SEPVP(1:2) 16.68 25.74 42.36 57.73 81.05 92.49

SEPVP(1:3) 20.59 45.95 59.12 78.20 93.78 95.36

FEPEG (1:1) 15.69 26.46 41.87 57.73 78.14 90.96

FEPEG (1:2) 25.9 29.18 43.24 59.67 81.47 91.95

FEPEG (1:3) 27.75 39.17 57.32 65.18 89.7 91.30

FENPEG (1:1) 31.36 52.84 69.95 78.45 93.7 96.54

FENPEG (1:2) 38.79 64.67 81.85 89.49 90.54 92.65

FENPEG (1:3) 40.78 72.6 93.63 99.12 99.52 99.79

FEPOL(1:1) 13.15 24.95 39.68 55.35 76.34 89.50

FEPOL(1:2) 17.85 27.61 42.8 71.49 87.15 90.98

FEPOL(1:3) 22.45 39.19 69.64 84.41 91.74 96.10

FENPOL(1:1) 18.3 48.95 67.21 79.63 92.45 94.65

FENPOL(1:2) 24.5 54.59 82.78 91.37 93.65 96.47

FENPOL(1:3) 38.2 68.3 87.9 92.32 95.12 97.18



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Statistical Analysis

From the table 6.6 it is evident the release profile of IRB from all batches were different from

release profile of pure IRB. All batches showed difference in release profile of IRB compared

to Physical mixture method and solvent evaporation of IRB, respectively. FENPEG (1:3) and

FENPOL (1:3) which showed better in-vitro dissolution profile, lower MDT and f2 values.

% Drug dissolved within 30 minutes (DP30 min), f2 and mean dissolution time (MDT)

for pure Irbesartan and SD. Batches DP30 MDT(min) f2

IRB 5.79 14.12 -

PMPVP(1:1) 6.03 13.12 97.96

PMPVP(1:2) 8.25 16.12 75.86

PMPVP(1:3) 10.90 15.91 68.54

PMPEG (1:1) 7.85 14.99 87.94

PMPEG (1:2) 12.64 16.54 67.3

PMPEG (1:3) 14.25 16.08 59.86

PMPOL(1:1) 7.42 14.03 92.19

PMPOL(1:2) 9.25 14.28 83.14

PMPOL(1:3) 11.20 14.5 75.26

SEPVP(1:1) 38.8 18.76 29.9

SEPVP(1:2) 42.36 17.19 28.93

SEPVP(1:3) 59.12 15.11 24.92

FEPEG (1:1) 41.87 17.91 29.39

FEPEG (1:2) 43.24 16.97 28.47

FEPEG (1:3) 57.32 14.93 26.33

FENPEG (1:1) 69.95 11.87 23.97

FENPEG (1:2) 81.85 14.56 21.88

FENPEG (1:3) 93.63 9.63 20.88

FEPOL(1:1) 39.68 18.29 30.09

FEPOL(1:2) 42.8 16.43 27.48

FEPOL(1:3) 69.64 14.62 24.47

FENPOL(1:1) 67.21 14.67 27.91

FENPOL(1:2) 82.78 12.71 25.42

FENPOL(1:3) 87.9 11.08 24.04


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Drug Content

Prepared formulations were checked for drug content analysis and the obtained results were

recorded in table 6.7. From the results it concluded that there was no any loss of drug in SD

preparation. All batches having drug content data well within acceptable range.

Drug content results.

Batches % Drug Content

IRB 99.4 ± 0.4

PMPVP(1:1) 98.5 ± 0.5

PMPVP(1:2) 99.5 ± 0.7

PMPVP(1:3) 97.8 ± 0.5

PMPEG (1:1) 99.8 ± 0.6

PMPEG (1:2) 99.4 ± 0.5

PMPEG (1:3) 98.4 ± 0.4

PMPOL(1:1) 99.4 ± 0.2

PMPOL(1:2) 98.8 ± 0.4

PMPOL(1:3) 99.7 ± 0.2

SEPVP(1:1) 99.9 ± 0.6

SEPVP(1:2) 99.8 ± 0.4

SEPVP(1:3) 99.4 ± 0.5

FEPEG (1:1) 99.7 ± 0.7

FEPEG (1:2) 98.7 ± 0.5

FEPEG (1:3) 97.9 ± 0.6

FENPEG (1:1) 98.9 ± 0.4

FENPEG (1:2) 99.7 ± 0.5

FENPEG (1:3) 99.6 ± 0.6

FEPOL(1:1) 98.7 ± 0.4

FEPOL(1:2) 99.6 ± 0.8

FEPOL(1:3) 98.7 ± 0.5

FENPOL(1:1) 99.5 ± 0.5

FENPOL(1:2) 98.9 ± 0.3

FENPOL(1:3) 99.8 ± 0.4

Evalution of Tablets.

Parameters Tablets of Pure Drug Tablets of FEPEG

(1:3)

Tablets of FENPEG

(1:3)

Hardness 3.5 ± 0.42 3.7 ± 0.34 3.9 ± 0.23

Friability 0.41± 0.05 0.40 ± 0.03 0.35 ± 0.01

Disintegration Time (min) 4.5 ± 0.62 4.1 ± 0.32 4.3 ± 0.51

% Drug Content 98.3 ± 0.45 97.5 ± 0.12 99.3 ± 0.35

% Drug release at 60 min 10.9 ± 0.10 91.5 ± 0.44 99.5 ± 0.17

Stability Study

Stability study of Optimized batch FENPEG (1:3) tablets performed for 1 month. Sample

withdrawal after 1 month; it showed no change in in-vitro drug release profile. Results of


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stability study do not show any remarkable change in the release profile of the tablet after the

stability.

ACKNOWLEDGEMENT

The authors are also thankful to Saraswati Institute of Pharmaceutical Sciences for providing

necessary equipment, facility & chemicals to complete research work.

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Documents

SOLID STATE CHARACTERIZATION AND IN VITRO DISSOLUTION