Effect of Bile Salt on Permeation Characteristics of the Oral Mucosal Dosage Form of Diltiazem Hydrochloride

Abstract

An attempt was made to study the effect of bile salt [sodium glycocholate (SG)] as a permeation enhancer on mucoadhesive buccal patches of diltiazem hydrochloride (anti-anginal drug) using various polymers like hydroxypropyl methyl cellulosee (HPMC), Eudragit RL100, ethyl cellulose alone and in combination with PVP. The prepared mucoadhesive buccal patches were evaluated for their physical parameter such as thickness uniformity, weight variation, drug content and surface pH and were found to be uniform. Folding endurance, swelling index, bioadhesive strength and in vitro drug release studies were also performed. SEM study of the patch was also conducted. Films prepared with HPMC (3%) and ethyl cellulose (4%) showed fast and slow release, respectively, among all the nine formulations. SG was selected and incorporated as a permeation enhancers in both the formulations (0.5% and 1% w/w of drug, respectively). Among the formulations prepared, F10 and F13 showed significant drug release, so they were selected for a in situ diffusion studies using goat cheek pouch. About 93.04% and 91.83% of drug release were observed in in situ diffusion studies at the end of 9 h and 18 h, respectively. The stability studies were conducted at two different temperatures (37 °C and 45 °C) and no significant change was observed at 37 °C but slight change in drug content was observed at 45 °C. The FTIR and DSC studies showed that there was no interaction between drug and polymers. Keywords: mucoadhesive buccal patches, diltiazem hydrochloride, goat cheek pouch, bile salt, sodium glycocholate Ethiopian Pharmaceutical Journal Vol. 25 (1) 2007: pp. 29-34