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Pharmacokinetics and Bioequivalence Evaluation of Cyclobenzaprine Tablets

The purpose of this study was to investigate cyclobenzaprine pharmacokinetics and to evaluate bioequivalence between two different tablet formulations containing the drug. An open, randomized, crossover, single-dose, two-period, and two-sequence design was employed. Tablets were administered to 23 h...

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Detalles Bibliográficos
Autores principales: Brioschi, Tatiane Maria de Lima Souza, Schramm, Simone Grigoleto, Kano, Eunice Kazue, Koono, Eunice Emiko Mori, Ching, Ting Hui, Serra, Cristina Helena dos Reis, Porta, Valentina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi Publishing Corporation 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3787571/
https://www.ncbi.nlm.nih.gov/pubmed/24151591
http://dx.doi.org/10.1155/2013/281392
Descripción
Sumario:The purpose of this study was to investigate cyclobenzaprine pharmacokinetics and to evaluate bioequivalence between two different tablet formulations containing the drug. An open, randomized, crossover, single-dose, two-period, and two-sequence design was employed. Tablets were administered to 23 healthy subjects after an overnight fasting and blood samples were collected up to 240 hours after drug administration. Plasma cyclobenzaprine was quantified by means of an LC-MS/MS method. Pharmacokinetic parameters related to absorption, distribution, and elimination were calculated. Cyclobenzaprine plasma profiles for the reference and test products were similar, as well as absorption pharmacokinetic parameters AUC (reference: 199.4 ng∗h/mL; test: 201.6 ng∗h/mL), C(max) (reference: 7.0 ng/mL; test: 7.2 ng/mL), and T (max) (reference: 4.5 h; test: 4.6 h). Bioequivalence was evaluated by means of 90% confidence intervals for the ratio of AUC (93%–111%) and C (max) (93%–112%) values for test and reference products, which were within the 80%–125% interval proposed by FDA. Cyclobenzaprine pharmacokinetics can be described by a multicompartment open model with an average rapid elimination half-life (t ((1/2)β)) of 3.1 hours and an average terminal elimination half-life (t ((1/2)γ)) of 31.9 hours.