Development of Oral Controlled Release Tablet Formulations Based on Diltiazem-Carrageenan Complex

Diltiazem HCl and lambda carrageenan react in distilled water to give a slightly soluble interaction product. The aim of this work was to verify the possible employment of lambda carrageenan-diltiazem (DTZ) complex in controlled-release formulations. The influence of complex particle size, compressi...

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Bibliographic Details
Published in:Pharmaceutical development and technology 2004, Vol.9 (2), p.155-162
Main Authors: Bonferoni, M. C., Rossi, S., Ferrari, F., Caramella, C.
Format: Article
Language:English
Subjects:
Administration, Oral
Biological and medical sciences
Carrageenan - chemistry
Compressive Strength
Controlled release
Delayed-Action Preparations
Diltiazem - administration & dosage
Diltiazem - chemistry
Diltiazem HCl
Drug Compounding - methods
Drug-polymer complex
Excipients - chemistry
General pharmacology
Hydrogen-Ion Concentration
Lambda carrageenan
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Solubility
Tablets
Time Factors
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Summary:Diltiazem HCl and lambda carrageenan react in distilled water to give a slightly soluble interaction product. The aim of this work was to verify the possible employment of lambda carrageenan-diltiazem (DTZ) complex in controlled-release formulations. The influence of complex particle size, compression force, pH of the dissolution medium, and tablet dimensions on drug release has been evaluated. The results confirm the suitability of the DTZ-carrageenan interaction product for controlled-release formulations. Good compaction properties allow tablets to slowly erode, with only the addition of the amount of hydroxypropyl methylcellulose (HPMC) necessary as a binding agent. The use of the finest sieve fraction results in the highest crushing strength values and in the slowest release rate, both in pH 1.2 and in pH 6.8. The force of compression does not affect the drug release for values over 16 kN. The release rate increases when the geometry of the tablet is varied so the surface volume ratio of the tablet is increased, suggesting a release mechanism involving surface dissolution erosion.
ISSN:1083-7450
1097-9867
DOI:10.1081/PDT-120027428