ABSTRACT

In the present study an attempt was made to formulate fast dissolving tablets of
Valsartan by direct compression method. The tablets were prepared using
superdisintegrants such as Kyron T-314, Crospovidone and Emcosoy.
Valsartan is an antihypertensive drug belongs to the category of Angiotension II
receptor antagonist. It suppresses the effects of angiotensin II at its receptors,
thereby blocking the rennin-angiotensin system. Due to its first pass metabolism,
metabolized mainly in the liver. Keeping all these factors in mind, it was
considered appropriate to formulate FDTs of Valsartan. The literature survey
reveals that Valsartan is a promising drug candidate for FDTs formulation. Precompression parameters such as angle of repose, bulk density, and carrs index
were carried out to study the flow properties of powder to achieve uniformity of
tablet weight and the values were within permissible limits. In present study
the tablets were prepared using various superdisintegrants in different
concentrations. The prepared tablets were evaluated for hardness, thickness,
weight variation, friability, drug content, wetting time, water absorption ratio,
and in vitro disintegration time, the results were found satisfactory. The
formulation containing 6% crospovidone (CP3) showed 97.58% of drug release
with in 10 mins. Overall, 9 formulations showed more than 98% of drug release
within 12 minutes.
Key words: Valsartan, Fast dissolving tablets, superdisintegrant, Kyron T-314,
Emcosoy, Crospovidone.

TABLE OF CONTENTS

Sl.No

Description

Page No.

Introduction

Aim & Objectives

Plan of Work

Literature Review

18 34

Drug and Excipients Profile

35 - 45

5.
6

Materials & Methods

Results & Discussion

Summary & Conclusion

Bibliography

1 13
14 15
16 17

46 57
58 77
78 - 80
81 87

LIST OF TABLES
Number

Description

Page.no

Table 1

List of materials

47

Table 2

List of equipments

47

Table 3
Table 4
Table 5

Formulations of Valsartan FDTs with superdisintegrant

KYRON T-314
Formulations of Valsartan FDTs with superdisintegrant
CROSPOVIDONE
Formulations of Valsartan FDTs with superdisintegrant
EMCOSOY

49
49
50

Table 6

Drug Excipient compatibility studies

52

Table 7

Percentage deviations allowed for tablets

54

Table 8

Concentration and absorbance obtained for calibration curve of

Valsartan 6.8 pH phosphate buffer

59

Table 9

FT-IR spectral data of Valsartan, KY, CP, EM. Physical mixture 61

Table 10

Pre compression Parameters of developed formulations

62

Table 11

Post compression Parameters of developed formulations

63

Table 12

Post compression Parameters of developed formulations

65

Table 13
Table 14

Table 15
Table 16

In vitro drug release profile of Valsartan FDT's with KYRON T314

In vitro drug release profile of Valsartan FDTs with
CROSPOVIDONE
In vitro drug release profile of Valsartan FDTs with
EMCOSOY
Treatment of dissolution data of KY1 with first order kinetics

67
68

69
70

Table 17

Treatment of dissolution data of KY2 with first order kinetics

70

Table 18

Treatment of dissolution data of KY3 with first order kinetics

70

Table 19

Treatment of dissolution data of CP1 with first order kinetics

71

Table 20

Treatment of dissolution data of CP2 with first order kinetics

71

Table 21

Treatment of dissolution data of CP3 with first order kinetics

71

Table 22

Treatment of dissolution data of EM1 with first order kinetics

72

Table 23

Treatment of dissolution data of EM2 with first order kinetics

72

Table 24

Treatment of dissolution data of EM3 with first order kinetics

72

LIST OF FIGURES
Number

Name of figures

Page No.

Fig 1

Various steps involved in sublimation process

Fig 2

Mechanism of super disintegrants by wicking and swelling

Fig 3

Mechanism of super disintegrants by deformation and repulsion 9

Fig 4

Calibration curve for Valsartan

59

Fig 5

FT-IR spectra of Valsartan with Kyron T-314

60

Fig 6

FT-IR spectra of Valsartan with Crospovidone

60

Fig 7

FT-IR spectra of Valsartan with Emcosoy

60

Fig 8

FT-IR spectra of physical mixture of VL, KY,EM and CP

61

Fig 9

In vitro disintegration time profile of standard formulations

64

Fig 10

Comparison of wetting time of Valsartan FDTs

66

Fig 11

Comparison of water absorption ratio of Valsartan FDTs

66

Fig 12

Comparison of disintegration time of Valsartan FDTs

66

Fig 13

Dissolution profile of VL FDTs with KYRON T-314

67

Fig 14

Dissolution profile of VL FDTs with CROSPOVIDONE

68

Fig 15

Dissolution profile of VL FDTs with EMCOSOY

69

ABBREVATIONS
max

Absorbance maxima

CDR

Cumulative drug release

Cm

Centimeter

CP

Crospovidone

Degree centigrade

FDTs

Fast dissolving tablets

FT-IR

Fourier transform infrared spectr

GI

Gastro intestine

Gm

Grams

IP

Indian Pharmacopoeia

VL

Valsartan

Ky

Kyron t 314

Mg

Milligram

Ml

Millilitre

Min

Minutes

Mm

Millimeter

MCC

Micro crystalline cellulose

Micro gram

Nm

Nanometer

Percentage

Rpm

Rotation per minute

UV

Ultraviolet

USP

United states pharmacopoeia

w/w

Weight by weight

w/v

Weight by volume