中国临床药理学与治疗学2025，Vol.30Issue(9)：1193-1199,7.DOI:10.12092/j.issn.1009-2501.2025.09.005
利托那韦片在中国健康受试者中的生物等效性试验
Bioequivalence of ritonavir tablets in healthy Chinese volunteers
摘要
Abstract
AIM:To appraise the bioequivalence and safety of the test preparation of ritonavir tab-lets and the reference preparation(trade name:Norvir®)in healthy adult subjects under fasting and postprandial conditions.METHODS:This study was a randomized,open-label,single-dose,four-period,fully repeated crossover design bioequivalence study protocol.Thirty-six healthy male and female volunteers were enrolled in the fasting and post-prandial conditions,and a single dose of the test preparation and reference preparation was orally administered.We used liquid chromatography-tan-dem mass spectrometry(LC-MS/MS)to finish the bioassay of the drug concentration of ritonavir in plasma.Pharmacokinetic parameters were statisti-cally analyzed using PhoenixWinNonlin8.1 software(Pharsight,USA)and a non-compartmental model.RESULTS:Under fasting conditions,the pharmacoki-netic parameters of the test and reference prepara-tions:Cmax(792.010±369.282)ng/mL and(856.939±394.427)ng/mL,AUC0-t(6 463.043±2 876.849)ng·mL-1·h and(6 907.690±3 046.132)ng·mL-1·h,AUC0-∞(6 603.617±2 916.352)ng·mL-1·h and(7 051.614±3 093.047)ng·mL-1·h.Here are the pharmacokinetic parameters for both the test prep-aration and the reference preparation in the post-prandial condition:Cmax(574.380±289.566)ng/mL and(615.796±297.382)ng/mL,AUC0-t(5 084.796±2 435.557)ng·mL-1·h and(5 414.167±2 416.952)ng·mL-1·h,AUC0-∞(5 219.144±2 487.793)ng·mL-1·h and(5 551.060±2 490.604)ng·mL-1·h.The 90%confidence interval of the geometric mean ratio of AUC0-t,AUC0-∞,and Cmax for the test preparation and reference preparation lied in the equivalent range of statistics.CONCLUSION:The tested preparation was bioequivalent to the reference preparation un-der fasting and postprandial conditions.关键词
利托那韦片/生物等效性/药代动力学/HIV蛋白酶Key words
ritonavir tablets/bioequivalence/pharmacokinetics/HIV-1 PR分类
医药卫生引用本文复制引用
王琰,夏玉明,朱仁弟,欧阳紫微,程远志,周仁鹏,胡伟..利托那韦片在中国健康受试者中的生物等效性试验[J].中国临床药理学与治疗学,2025,30(9):1193-1199,7.基金项目
重大新药创制科技重大专项(2020ZX09201014) （2020ZX09201014）
