| Title | Bioavailability of a controlled-release cyclobenzaprine tablet and influence of a high fat meal on bioavailability. | | Author(s) | Gai MN, Costa E, Arancibia A | | Institution | Center for Development in Pharmaceutical Technology, Department of Science and Pharmaceutical Technology, Faculty of Chemical and Pharmaceutical Sciences, University of Chile, Santiago de Chile. | | Source | Int J Clin Pharmacol Ther 2009 Apr; 47(4):269-74. | | MeSH | Adult
Amitriptyline
Area Under Curve
Biological Availability
Cross-Over Studies
Delayed-Action Preparations
Dietary Fats
Food-Drug Interactions
Humans
Male
Muscle Relaxants, Central
Tablets
Young Adult
| | Abstract | OBJECTIVE: To evaluate the systemic bioavailability of a new controlled release cyclobenzaprine tablet, and the influence of a high fat meal on its bioavailability. SUBJECTS,
MATERIALS AND METHODS: 24 and 12 healthy male subjects were recruited for the bioavailability and influence of diet studies, respectively. Experimental design for both studies was an open randomized, 2-period, single dose, crossover study. In the bioavailability study, each subject received in different occasions, a single oral dose of cyclobenzaprine of immediate (10 mg) or controlled release (20 mg) tablet, followed by a 2-week washout period. In the influence of diet study, the volunteers received the controlled-release tablet concomitantly with a high fat meal or in a state of fasting.
RESULTS: In the bioavailability study, plasma cyclobenzaprine profiles were in agreement with a controlled release system. This formulation presented a 92.8% of relative bioavailability (IC 85.5 - 105%) and a significant reduction in Cmax (IC 58 - 65.5%), when compared with equal dose of the immediate release tablet. The presence of food increased AUC (11.6%) and Cmax (48%). For both parameters the calculated 90% confidence interval was not in the bioequivalence interval, 97.4 - 125.8% for AUC and 111.7 - 184.2% for Cmax.
CONCLUSIONS: The controlled release tablet showed a relative bioavailability comparable with equal dose of the immediate release product and produced a significantly lower Cmax, as expected in a controlled release formulation. The concomitant administration of the tablet with a high fat meal produced an increase on its bioavailability, mainly in Cmax, with no evidence of dose-dumping. | | Language | eng | | Pub Type(s) | Comparative Study
Journal Article
Randomized Controlled Trial
| | PubMed ID | 19356393 |
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