Microsphere-based once-daily modified release matrix tablets for oral administration in angina pectoris

Abstract

The objective of this research was to develop microsphere-based once-daily modified release tablet formulations of diltiazem hydrochloride (DH), a potent calcium channel blocker used in angina pectoris. For this purpose, DH-loaded microspheres were prepared by the solvent evaporation technique using Eudragit®RS 100. The effect of variation in the drug/polymer ratio on the physical and release characteristics of the microspheres was investigated. After the selection of the suitable microspheres, tablets were compressed using Compritol®888 ATO, Ludipress® and Cellactose®80 as different direct tableting agents and excipients. As a result, modified release tablet formulations of DH-loaded microspheres were designed successfully for oral administration once rather than two or three times a day in angina pectoris.

Key Words: :

• Diltiazem hydrochloride
• Compritol®888 ATO
• Ludipress®
• Cellactose®80
• Eudragit®RS 100 microspheres
• tablets