European Journal of Biomedical and Pharmaceutical Sciences

FORMULATION AND EVALUATION OF GASTRO INTESTINAL RESISTANT MICROPOROUS MEMBRANE PERMEATED DRUG DELIVERY SYSTEM OF VILDAGLIPTIN

Srilakshmi N*, P Srinivasa Babu, M Bhagavan Raju, G Kishore Babu, T Praveen Kumar

ABSTRACT

The purpose of the present study is to obtain an oral controlled release formulation for highly water soluble drugs which have shorter half-life. In this study Vildagliptin has been used. Vildagliptin belongs to a class of orally active anti-diabetic drug which inhibits dipeptidyl peptidase-4(DPP-4) and potentiates the secretion of insulin in the β-cells, thereby decreasing blood glucose level. The desired effect is obtained by preparing matrix tablets and applying a coat of gasto-intestinal resistant micro-porous membrane on the core tablet. Core tablet is obtained by wet granulation and compression method. Core tablets are tested for dissolution studies and the best formulation has been chosen for further studies. Optimized core tablet has been coated with ethyl cellulose in which sodium lauryl sulphate was dispersed. Effect of formula compositions of core tablets and coating suspensions on the pharmaceutical characteristics, such as drug release kinetics and membrane stability of the coated tablets was investigated in vitro. Vildagliptin released from the coated tablets at a zero-order rate in a pH-independent manner. This independency of Vildagliptin release to pH change from 1.2 to 7.2 is favorable for the controlled oral drug delivery, since it will produce a constant drug release in the stomach to intestine regardless of the pH change in the GI tract. Drug release could be extended upto 10 h according to the coating condition. The release rate could be controlled by changing the formula compositions of the core tablets and coating suspensions, coat weight per each tablet, and especially ethyl cellulose/sodium lauryl sulphate ratio in the coating suspension. Among the prepared formulations, formulation C12 (optimized formula with ethyl cellulose 5% and sodium lauryl sulphate 2%) was the optimized one and it showed non-fickian transport and korsmeyer peppas mode and is concluded as the best formulation.

Keywords: Vildagliptin, Anti-diabetic drug, Wet granulation, Ethyl cellulose, Sodium lauryl sulphate.