中国临床药理学杂志2025，Vol.41Issue(5)：706-711,6.DOI:10.13699/j.cnki.1001-6821.2025.05.021
磷酸奥司他韦干糖浆在中国健康受试者中的生物等效性研究
Bioequivalence study of oseltamivir phosphate dry syrup in Chinese healthy subjects
摘要
Abstract
Objective To study the pharmacokinetic profile of oseltamivir phosphate dry syrup in Chinese healthy subjects and to evaluate the bioequivalence and safety of the test formulation(T)and the reference formulation(R)under fasting and fed conditions.Methods In a randomized,open,two-agent,two-sequence,two-cycle,double-crossover trial design,36 healthy subjects were enrolled in the fasting and fed groups,respectively,who received a single oral dose of 2.5 g of oseltamivir phosphate dry syrup of either the T or R.The blood concentrations of oseltamivir were determined by liquid chromatography-tandem mass spectrometry(LC-MS/MS),and the pharmacokinetic parameters were calculated by using the WinNonlin(8.2)software and evaluated for bioequivalence and safety.Results Under fasting conditions,the Cmax of oseltamivir of the T and R were(64.40±17.50)and(64.10±20.90)ng·mL-1,AUC0-t were(142.76±43.64)and(151.60±35.10)h·ng·mL-1,AUC0-∞ were(147.67±37.60)and(153.05±35.30)h·ng·mL-1,respectively.Under fed conditions,the Cmax of oseltamivir of the T and R were(47.70±18.30)and(46.90±17.20)ng·mL-1,AUC0-twere(170.52±26.28)and(168.70±24.51)h·ng·mL-1,AUC0-∞ were(173.08±26.50)and(171.30±24.59)h·ng·mL-1,respectively.The 90％confidence intervals for the geometric mean ratios of Cmax,AUC0-t and AUC0-∞ for the T and R fell in the range of 80.00％to 125.00％for both the fasting and fed groups.Adverse drug reaction rates were 27.78％and 44.44％in the fasting and fed groups,respectively.Conclusion Two kinds of oseltamivir phosphate dry syrups were bioequivalent and had favorable safety profiles in Chinese healthy subjects in both fasted and fed states.关键词
磷酸奥司他韦干糖浆/生物等效性/药代动力学/安全性/液相色谱-质谱法Key words
oseltamivir phosphate dry syrup/bioequivalence/pharmacokinetics/safety/liquid chromatography-tandem mass spectrometry分类
医药卫生引用本文复制引用
刘娴,秦如斋,成玘,陈学义,易德平,黄和意,谢志红,叶丽卡,段炼..磷酸奥司他韦干糖浆在中国健康受试者中的生物等效性研究[J].中国临床药理学杂志,2025,41(5):706-711,6.基金项目
广州市科技计划重点研发计划基金资助项目(202103000024) （202103000024）
广东省医学科学技术研究基金资助项目(B2023146) （B2023146）
