Comparison of the Pharmacokinetics of Generic Versus Branded Obeticholic Acid in a Chinese Population: Effects of Food and Sex
| Autor: | Yue Hu, Min Wu, Wenbo zheng, Li Liu, Yanhua Ding, Hong Zhang, Dandan Huo, Meng Wang, Deming Yang, Zhongnan Xu, Xiaojiao Li, Cuiyun Li |
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| Rok vydání: | 2021 |
| Předmět: |
Adult
Male Adolescent Cmax Pharmaceutical Science Physiology Bioequivalence Chenodeoxycholic Acid 030226 pharmacology & pharmacy Food-Drug Interactions Young Adult 03 medical and health sciences chemistry.chemical_compound Sex Factors 0302 clinical medicine Asian People Pharmacokinetics Tandem Mass Spectrometry Drugs Generic Humans Medicine Pharmacology (medical) Active metabolite Chinese population Cross-Over Studies business.industry Obeticholic acid Middle Aged eye diseases Therapeutic Equivalency Plasma exposure chemistry Area Under Curve 030220 oncology & carcinogenesis Plasma concentration Female business Chromatography Liquid |
| Zdroj: | Clinical Pharmacology in Drug Development. |
| ISSN: | 2160-7648 2160-763X |
| Popis: | The present study assessed the pharmacokinetics and bioequivalence of a single 10-mg dose of a generic and the branded formulation (Ocaliva) of obeticholic acid (OCA) in healthy Chinese subjects under fasting and fed conditions. The possible effects of food and sex on the pharmacokinetics of OCA and its 2 active metabolites (glyco-OCA and tauro-OCA) were evaluated. Plasma concentrations of OCA and its 2 active metabolites were measured by liquid chromatography-tandem mass spectrometry. The 90%CIs of the ratios of the test and reference formulations for Cmax , AUC0-t , and AUC0-∞ of OCA, glyco-OCA, and tauro-OCA were contained entirely within the 80% to 125% range required for bioequivalence under fasting and fed conditions. Plasma exposure of OCA was 30% to 36% higher under fed compared with fasting conditions. Plasma exposure of OCA, glyco-OCA, and tauro-OCA was 39% to 66%, 22% to 58%, and 37% to 84% higher, respectively, in women compared with men under fasting and fed conditions. In conclusion, OCA was well tolerated in healthy Chinese subjects under fasting and fed conditions. The single 10-mg dose of a generic OCA formulation was bioequivalent to Ocaliva. Food and sex impacted the pharmacokinetics of OCA and/or its 2 active metabolites. Further studies are required to determine if these effects are clinically relevant. |
| Databáze: | OpenAIRE |
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