Development and in-vitro evaluation of modified release tablets including ethylcellulose microspheres loaded with diltiazem hydrochloride

Abstract

In this study, development of modified release tablet formulations containing diltiazem hydrochloride-loaded microspheres to be taken once rather than two or three times a day was attempted. For this purpose, ethylcellulose microspheres were prepared by emulsion-solvent evaporation technique. The influence of emulsifier type and drug/polymer ratio on production yield, encapsulation efficiency, particle size, surface morphology and in-vitro release characteristics of the microspheres was evaluated. Suitable microspheres were selected and tabletted using different tabletting agents, Ludipress®, Cellactose®80, Flow-Lac®100 and excipients Compritol®888 ATO, Kollidon®SR. Tablets were evaluated from the perspective of physical and in-vitro drug release characteristics. It was seen that type and ratio of the excipients played an important role in the tabletting of the microspheres. As a result, two tablet formulations containing 180 mg diltiazem hydrochloride and using either Compritol®888 ATO or Kollidon®SR were designed successfully and maintained drug release for 24 h with zero order and Higuchi kinetics, respectively.

Key Words: :

• Diltiazem hydrochloride
• Kollidon®SR
• Compritol ®888 ATO
• ethylcellulose microspheres
• tablets