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

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 in...

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Bibliographic Details
Published in:Journal of microencapsulation 2006-03, Vol.23 (2), p.135-152
Main Authors: engel, Ceyda T., HasÇ Çek, Canan, Gönül, Nur n
Format: Article
Language:English
Subjects:
Biological and medical sciences
Buffers
Calcium Channel Blockers - chemistry
Calcium Channel Blockers - pharmacokinetics
Cellulose - analogs & derivatives
Cellulose - chemistry
Cellulose - pharmacokinetics
Cellulose - ultrastructure
Compritol ®888 ATO
Delayed-Action Preparations
Diltiazem - chemistry
Diltiazem - pharmacokinetics
Diltiazem hydrochloride
Drug Compounding - methods
ethylcellulose microspheres
Evaluation Studies as Topic
Excipients
General pharmacology
Hydrogen-Ion Concentration
In Vitro Techniques
Kollidon®SR
Medical sciences
Microspheres
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Sclerosing Solutions - chemistry
Sclerosing Solutions - pharmacokinetics
Solubility
Tablets
Water - chemistry
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Summary: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.
ISSN:0265-2048
1464-5246
DOI:10.1080/02652040500286474