Abstract

FORMULATION AND EVALUATION OF GASTRORETENTIVE DRUG DELIVERY SYSTEM OF CAREVEDILOL PHOSPHATE BY SINTERING TECHNOLOGY

Satish Polshettiwar*, Vasudha Arve, Ajinkya Battuwar and Rahul Hajare

ABSTRACT

The objective of the present work is to design gastro retentive matrix tablets of Carvedilol phosphate. Carvedilol phosphate is a nonselective beta + selective alpha 1 blocker. Beta blockers antagonize the effects of sympathetic nerve stimulation or circulating catecholamine at beta adrenoreceptors which are widely distributed throughout body systems. They also decrease plasma markers of activation of sympathetic and thus beta blockers are set to possess intrinsic sympathomimetic activity. The polymers like HPMC K4M, Eudragit L 100, Guar gum, Sodium bicarbonate, Citric acid were utilized in the formulation of matrix tablets containing Carvedilol phosphate by wet granulation techniques and evaluated for its in-vitro drug release. Granules were prepared and evaluated for bulk density, tapped density, compressibility index and angle of repose shows characteristic results. Formulation was optimized on the basis of acceptable tablet parameters such as hardness, friability, drug content, weight variation, in-vitro drug release and stability studies. The present work also deals with the application of sintering technique to matrix tablets of Carvedilol phosphate to achieve sustained release. The results revealed that sintering caused decrease in drug release as compared to unsintered tablets. On sintering these formulations for thermal was found that F6, L2, I2 and H4 gave better results compared to other formulations. The release data was fitted to various mathematical models such as Hixon Crowell, Korsmeyer peppas, First order, Zero order to evaluate the kinetics and the mechanism of drug release. The stability studies were carried out according to ICH guideline which indicates that the selected formulations were stable. Thus it could be useful to retain Carvedilol phosphate. in stomach, minimize the mucosal irritation by drug releasing slowly at controlled rate, reduces drug waste and better patient compliance.

Keywords: Sintering, Matrix tablets, Eudragit L-100, Guar gum, Sodium bicarbonate.