Effects of Humidity on the Dissolution Profiles of Controlled Release Theophylline Matrix Tablets Containing Release Enhancers Prepared By Melt Granulation and Coacervation Techniques

Abstract

The quantity of moisture present in tablets plays a major role in influencing the physical/chemical properties of tablets especially dissolution profiles. The purpose of the present study is to investigate the effects of relative humidity on the dissolution profiles of controlled release  theophylline matrix tablets containing release enhancer prepared by melt granulation and simple coacervation techniques. Sucrose and  microcrystalline cellulose at concentration of 3% w/w, 5% w/w, 7.5% w/w, and 10% w/w were included in the blends as release enhancers before compression into nondisintegrating matrix tablets. Resulting tablets were exposed to 0% and 75% relative humidity. Sample were withdrawn at 0, 15 days, 1 month, 2 months and 3 months and evaluated for cumulative drug release. Interactions were investigated using modern technology: Differential scanning calorimetry (DSC). Initial and maximum release were increased after exposure to 75% relative humidity. There was no drug – excipients interaction. Thus moisture increased theophylline release from both sets of tablets prepared by melt granulation and simple coacervation techniques.

Keywords: Theophylline, Matrix tablets, Dissolution profiles, Release enhancers, Relative humidity