中国临床药理学杂志2024，Vol.40Issue(14)：2113-2117,5.DOI:10.13699/j.cnki.1001-6821.2024.14.023
富马酸丙酚替诺福韦片在中国健康受试者体内的生物等效性研究
Bioequivalence study of tenofovir alafenamide fumarate tablets in Chinese healthy subjects
摘要
Abstract
Objective To evaluate the pharmacokinetics(PK)of tenofovir alafenamide Fumarate tablets(25 mg)in healthy Chinese subjects after single oral administration to provide a basis for bioequivalence evaluation.Methods Using a single-dose,randomized,open-lable,two-period,two-way crossover design under fasting condition,while three-way crossover design under fed condition,42 healthy subjects respectively for fasting and fed study were enrolled,and randomized into two groups to receive a single dose of test product(T)or reference product(R)25 mg.Plasma concentration of tenofovir alafenamide and tenofovir were determined by liquid chromatography-tandem mass spectrometry(LC-MS/MS)method.The pharmacokinetic parameters were calculated by WinNonlin software(8.1 version)using non-compartmental model,and bioequivalence evaluation was performed for the two preparations.Relevant safety evaluations were performed during the trial.Results The test product and the reference product under fasting study,the main PK parameters of tenofovir alafenamide were as follows:Cmax were(215.17±94.24)and(199.30±71.11)ng?mL-1;AUC0-t were(135.44±71.60)and(123.91±53.82)h?ng?mL-1;the main PK parameters of tenofovir were as follows:Cmax were(7.30±2.27)and(7.12±1.74)ng?mL-1,AUC0-t of tenofovir were(186.78±60.22)and(179.44±47.44)h?ng?mL-1,respectively.The test product and the reference product under fed study,the main PK parameters of tenofovir were as follows:Cmax were(197.69±82.19)and(197.10±110.54)ng?mL-1;AUC0-t were(227.08±74.33)and(238.51±128.30)h?ng?mL-1;the main PK parameters of tenofovir were as follows:CMax were(7.51±1.63)and(7.23±1.65)ng?mL-1;AUC0-t were(237.16±47.09)and(230.06±43.41)h?ng?mL-1,respectively.The 90％confidence interval for geometric mean ratio of Cmax,AUC0-tof T and R under fed condition were between 80.00％-125.00％,respectively.The incidence of adverse events in fasting and fed tests was 21.43％and 30.95％,respectively,and no serious adverse event was reported.Conclusion The test formulation and reference formulation of tenofovir alafenamide fumarate tablets were equivalent and was safe.关键词
丙酚替诺福韦/替诺福韦/生物等效性/安全性Key words
tenofovir alafenamide fumarate tablets/bioequivalence/safety分类
医药卫生引用本文复制引用
李晓斌,汪楠,胡妮娜,王宁,董晨东,崔晓彤,谢荷,田妍,王文萍..富马酸丙酚替诺福韦片在中国健康受试者体内的生物等效性研究[J].中国临床药理学杂志,2024,40(14):2113-2117,5.基金项目
辽宁省教育厅课题基金资助项目(辽教办[2023]274号) （辽教办[2023]274号）
