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J Microencapsul ; 23(2): 135-52, 2006 Mar.
Article in English | MEDLINE | ID: mdl-16754371

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, Cellactose80, Flow-Lac100 and excipients Compritol888 ATO, KollidonSR. 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 Compritol888 ATO or KollidonSR were designed successfully and maintained drug release for 24 h with zero order and Higuchi kinetics, respectively.


Subject(s)
Calcium Channel Blockers/pharmacokinetics , Cellulose/analogs & derivatives , Diltiazem/pharmacokinetics , Sclerosing Solutions/pharmacokinetics , Buffers , Calcium Channel Blockers/chemistry , Cellulose/chemistry , Cellulose/pharmacokinetics , Cellulose/ultrastructure , Delayed-Action Preparations , Diltiazem/chemistry , Drug Compounding/methods , Evaluation Studies as Topic , Excipients , Hydrogen-Ion Concentration , In Vitro Techniques , Microspheres , Particle Size , Sclerosing Solutions/chemistry , Solubility , Tablets , Water/chemistry
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