DESIGN, DEVELOPMENT AND OPTIMIZATION OF OLMESARTAN MEDOXOMIL LIQUISOLID TABLETS USING CENTRAL COMPOSITE DESIGN

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CONCLUSION:
The Liquisolid technique is a promising alternative for improvement of dissolution property of water-insoluble drugs, such as OLM. The higher dissolution rate showed by Liquisolid compacts may imply enhanced oral bioavailability due to the increased wetting properties and surface of drug available for dissolution. The Liquisolid compact of OLM made in PEG 400 showed better dissolution rate than marketed tablet (olmezest) based upon solubility and molecular fraction (FM) of the drug in their liquid medication. From this technique solubility of pure drug (0.12µg/ml) increases upto the 25µg/ml.

ACKNOWLEDGEMENTS:
Authors would like to express sincere thanks to SICART lab, V.V. Nagar for providing instruments.  We also thank to CTX lifescience, Surat to provide gratis sample of expensive Olmesartan medoxomil.

Table 1- Solubility study of OLM in different non-volatile solvents.

Sr no

Solvents

Solubility (mg/ml)

1.

Propylene glycol

2.253333 ± 0.041096

2.

PEG-200

6.15 ± 0.122474

3.

PEG-400

20.52 ± 0.384014

4.

PEG-600

10.76667 ± 0.262467

5.

GLYCERIN

4.756667 ± 0.316263

6.

Cremophore® EL

3.553333 ± 0.294882

7.

Tween 20

19.1 ± 0.348807

8.

Tween 80

9.653333 ± 0.192585

9.

Span 80

2.746667 ±0.373661

10.

Span 20

15.41333 ±0.083799

11.

Liq.paraffin

0.883333 ±0.041096

12.

Castor oil

14.14333 ±0.20822

Table 2: Factors and their different levels for Central composite design for preparation liquisolid tablets.

Independent Variables

Levels

Lowest(-α)

Low(-1)

Medium(0)

High(+1)

Highest(+α)

Ratio of carrier to coating material (R) (X1)



5


10


15


20


25

Drug concentration(Cd)

(X2)

10%

15%

20%

25%

30%

Dependent Variables

Goal

Angle of Repose (Y1)

Minimize

Hardness (kg/cm2) (Y2)

Maximize

Saturation solubility study(Y3)

Maximize

Cumulative percentage release at 10 min CPR10 min (Y4)

Maximize

Table 3- Formulation of liquisolid compact-

FORMULA

DRUG(mg)

WEIGHT OF SOLVENT (mg)

DRUG CONC

(%)

[X2]

R=Q/q

[X1]

Lf=W/Q

Avicel PH 102

Q=W/Lf

(mg)

Aerosil 200

q= Q/R(mg)

CCS

10%

(mg)

TOTAL

WEIGHT

(mg)

F1






      10

66.6

15

10

0.693

96.10

9.61

18.23

208.56

F2

66.6

15

20

0.609

109.35

5.4675

19.14

218.97

F3

40

25

10

0.693

57.72

5.77

11.34

129.82

F4

40

25

20

0.609

65.68

3.28

11.89

136.084

F5

50

20

5

0.861

58.07

11.61

12.96

148.64

F6

50

20

25

0.592

84.43

3.377

14.78

169.08

F7

100

10


 

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