Design and Development of Controlled Release Gastroretentive Dosage Forms by various Approaches

Abstract

Gastroretentive drug delivery system is the fast growing drug delivery system. Gastroretentive dosage forms are base on different mechanism like effervescent system, swelling system, bioadhesive system, and high density system. But, according to the literature survey we cannot say that which system or which mechanism is more efficient for the gastroretention. So, the chief objective of the present work is to develop controlled release gastroretentive dosage forms by various approaches and to find out the optimize approach. Propafenone HCl undergoes degradation in the colon, due to this reason it was selected as the candidate drug for gastroretentive drug delivery system. It is expected that gastroretentive drug delivery system will bring the drug in the vicinity of absorption window and the rate and extent of poorly absorbed drug will be expected to be increased. It is also expected that the increased plasma concentration (rate and extent) will be in the therapeutic window. This will reduce the dose of drug and treatment will be cost effective. newlineThe present study directed to formulate, optimize and evaluate a gastroretentive dosage forms in three parts. Part I deals with floating system containing sodium bicarbonate as a gas forming agent. Part II deals with mucoadhesive system containing sodium CMC as a mucoadhesive polymer and part III deals with high density system containing zinc oxide as a density increasing agent. Preformulation study for propafenone HCl was conducted to investigate drug-excipients interaction and physiochemical property, which showed that excipients used in formulation have no interaction or change in physical nature. The melting point of propafenone HCl complies with the reported value. The calibration curves of propafenone HCl were measured and showed good linearity with the high regression coefficient (R2). Thus, the designed formulations can be considered as one of the promising formulation technique of gastroretentive drug delivery system of propafenone HCl in management of cardiac arrhythmias.