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Abstract

FORMULATION DESIGN AND EVALUATION OF NOVEL SUSTAINED RELEASE GASTRO-RETENTIVE TABLET OF VENLAFAXINE HYDROCHLORIDE

Sanap S A, ChaudhariA.V, Mahale N.B, Chaudhari. S.R.

ABSTRACT

Venlafaxine (Effexor) is an antidepressant of the serotoninnorepinephrine reuptake inhibitor (SNRI) class first introduced by Wyeth in 1993. It is prescribed for the treatment of clinical depression and anxiety disorders. Due to the pronounced side effects and suspicions that venlafaxine may significantly increase the risk of suicide it is not recommended as a first line treatment of depression. Venlafaxine is having a short biological half-life of 5 hours. To overcome the multiple doses at short intervals of time due to short biological half-life and poor bioavailability of venlafaxine , it was formulated into gastroretentive floating tablets, employing a new floating polymer tamarind kernel gum and known polymers HPMCK4M . Even though there are several floating polymers, there is a continuous need to develop new floating polymer for better buoyancy and controlled release of drug. Isolated tamarind kernel gum is off white, free flowing and amorphous in nature which is supported by micromeritic studies. The tablets were evaluated for thickness, weight variation, hardness, friability, drug content; in vitro buoyancy test, in vitro drug release and Fourier transform infrared (FT-IR) spectroscopy,DSC. Formulation F7 can be considered as an optimized formulation for gastroretentive floating tablet of venlafaxine HCl. The results of in vitro release studies showed that optimized formulation F7 could sustain drug release (99.11%) for 24 hours and remain buoyant for more than 24 hours.The formulation employing tamarind kernel gum showed slow release i.e spread over 24 hrs and followed Zero order kinetics & Higuchi model with non fickian diffusion of drug release. Isolated tamarind gum is comparable to HPMC K-4M in floating and a drug release characteristics and it was found to be better than HPMC K4M. So it was concluded that tamarind kernel gum could be used as floating and controlled release polymer in the formulation of gastroretentive formulations.

Keywords: Gastroretentive drug delivery systems, Floating tablet, effervescent, non effervescent. Tamarind gum, HPMC K4M.


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