Abstract

STUDIES ON MUCOADHESIVE BUCCAL FILMS OF ISOSORBIDE DINITRATE

V. Sri Venkateswara Rao*, M. Bala Krishnaiah, S. M. Shanta Kumar, N. Venkata Rao and S. Anil Kumar

ABSTRACT

Isosorbide dinitrate is used to prevent chest pain (angina) in patients with a certain heart condition (coronary artery disease). This medication belongs to a class of drugs known as nitrates. It works by relaxing and widening blood vessels so blood can flow more easily to the heart. This medication will not relieve chest pain once it occurs. It is also not intended to be taken just before physical activities (such as exercise, sexual activity) to prevent chest pain. Absorption of isosorbide dinitrate after oral dosing is nearly complete, but bioavailability is highly variable (10% to 90%), with extensive first-pass metabolism in the liver. Serum levels reach their maxima about an hour after ingestion. Hence the present work was aimed to formulate mucoadhesive buccal films of Isosorbide dinitrate with an objective to improve its therapeutic efficacy, bioavailability and patient compliance. A total eight formulations of mucoadhesive drug delivery system of Isosorbide dinitrate were prepared as buccal films, by solvent casting technique. Hydroxylpropylmethylcellulose (HPMC-15), EudragitRL-100, Polyvinyl pyrrolidone, Carbopol-934 were used as mucoadhesive polymers in various proportions. Prepared films were evaluated for their weight, thickness, surface pH, swelling index, drug content uniformity, folding endurance in vitro release, permeation studies and stability studies. Films exhibited controlled release over more than 6 h in permeation studies were selected for further studies. It was concluded that the formulation F1 contained Isosorbide dinitrate and HPMC E-15 in proportion of 1:5 showed somewhat promising results. Hence it can be selected for the development of buccal film for effective therapeutic purposes.

Keywords: Buccal film, Isosorbide dinitrate, in vitro and in situ studies, mucoadhesive.