Comparative Bioavailability of Diltiazem in Prolonged-Release Oral Preparations

This study was conducted to compare the bioavailability of two prolonged-release pharmaceutical forms containing 300 mg of diltiazem. The test formulation is a new design of tablets with a hydrophilic matrix, and the reference formulation is capsules containing prolonged liberation microgranules, in...

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Bibliographic Details
Published in:Drug development and industrial pharmacy 2001-01, Vol.27 (10), p.1099-1106
Main Authors: Quiroga, Pablo A. M., Yuln, Graciela V., Palummo, Mariela, Cingolani, Andrea, Dall, Luis L., Volonté, María G.
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Antiarythmic agents
Antihypertensive agents
Bioavailability
Bioequivalence
Biological and medical sciences
Biological Availability
Calcium Channel Blockers - blood
Calcium Channel Blockers - pharmacokinetics
Capsules
Cardiovascular system
Chromatography, High Pressure Liquid
Cross-Over Studies
Diltiazem
Diltiazem - blood
Diltiazem - pharmacokinetics
Female
General pharmacology
Humans
Male
Matrix hydrophilic
Medical sciences
Middle Aged
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Solubility
Tablets, Enteric-Coated
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Summary:This study was conducted to compare the bioavailability of two prolonged-release pharmaceutical forms containing 300 mg of diltiazem. The test formulation is a new design of tablets with a hydrophilic matrix, and the reference formulation is capsules containing prolonged liberation microgranules, in the same dose, that are commercially available in the pharmaceutical market. Diltiazem plasma concentrations were analyzed by high-performance liquid chromatography (HPLC), which involves solid-phase extraction for plasma sample preparation. Twelve healthy volunteers participated in the study, which had a single-dose, two-treatment, two-sequence-crossover, randomized design. The preparations were compared using pharmacokinetic parameters such as the area under the plasma concentration-time curve AUC(0-36), peak plasma concentration Cmax, and Cmax AUC(0-36) ratio as a measure for the absorption rate. No statistically significant difference was observed for any of the parameters, and the 90% confidence intervals calculated for the ratio of the logarithmically transformed AUC(0-36) and Cmax AUC(0-36) values of both formulations were within the bioequivalence limit of 0.80-1.25. Moreover, an in vitro study of dissolution according to USP 23 was conducted, and the in vitro parameters were calculated.
ISSN:0363-9045
1520-5762
DOI:10.1081/DDC-100108372