氟康唑片在中国健康受试者的生物等效性研究  

Bioequivalence of fluconazole tablets in healthy Chinese volunteers

作　　者：张丽英[1] 郭彩会[1] 宋浩静[1] 刘亚丽 ZHANG Li-ying;GUO Cai-hui;SONG Hao-jing;LIU Ya-li(Department of Pharmacy,Hebei General Hospital,Shijiazhuang 050051;Shijiazhuang Siyao Co.,Ltd.,Shijiazhuang 050011)

机构地区：[1]河北省人民医院药学部,石家庄050051 [2]石家庄四药有限公司,石家庄050011

出　　处：《中南药学》2022年第6期1251-1255,共5页Central South Pharmacy

摘　　要：目的评价健康受试者空腹和餐后条件下单剂量服用氟康唑片的生物等效性。方法采用单中心、单剂量、随机、开放、两周期、自身交叉对照试验设计,液相色谱串联质谱法测定健康受试者空腹或餐后给药后血浆中氟康唑的药物浓度,使用WinNonlin 7.0软件计算药动学参数,使用SAS 9.4软件进行生物等效性评价。结果空腹生物等效性试验:24例健康受试者分别单次空腹服用氟康唑受试制剂和参比制剂150 mg后,C_(max)、AUC_(0~t)及AUC_(0~∞)的几何均值的比值分别为104.64%、98.01%和97.64%,90%CI分别为97.04%~112.85%、96.57%~99.48%和96.18%~99.12%,均落在等效区间80.00%~125.00%;餐后生物等效性试验:21例健康受试者高脂餐后服用受试制剂和参比制剂150 mg后,C_(max)、AUC_(0~t)及AUC_(0~∞)的几何均值的比值分别为97.42%、98.65%和98.88%,90%CI分别为94.28%~100.67%、95.90%~101.48%和95.69%~102.17%,均落在等效区间80.00%~125.00%。结论在空腹和餐后条件下,两制剂均具有生物等效性。Objective To evaluate the bioequivalent of single dose fluconazole tablets test formulation and reference formulation in fasting and postprandial conditions in healthy Chinese subjects.Methods A single center,single dose,randomized,open label,two cycle,self crossover controlled trial design was used to determine the concentrations of fluconazole in the plasma after fasting or postprandial administration in healthy subjects by liquid chromatography tandem mass spectrometry.The pharmacokinetic parameters were calculated with WinNonlin 7.0 software,and the bioequivalence was evaluated with SAS 9.4 software.Results Fasting bioequivalent test:after the administration of a single,fasting dose of fluconazole test formulation and reference formulation 150 mg in 24 healthy subjects,the odds ratios for the geometric means of C_(max),AUC_(0~t),and AUC_(0~∞) were 104.64%,98.01%,and 97.64%,respectively;the 90%CI was 97.04%-112.85%,96.57%-99.48%,and 96.18%-99.12%,respectively,which fell within the equivalence interval of 80.00%-125.00%.bioequivalent test after meal:the ratios of the geometric means of C_(max),AUC_(0~t),and AUC_(0~∞) after a high-fat meal were 97.42%,98.65%,and 98.88%,respectively,with 90%CI of 94.28%-100.67%,95.90%-101.48%,and 95.69%-102.17%in 21 healthy subjects,which fell within the equivalence interval of 80.00%-125.00%.Conclusion Both formulations are bioequivalent in healthy Chinese subjects under fasting and postprandial conditions.

关 键 词：氟康唑 生物等效性研究 药动学 健康受试者 

分 类 号：R96[医药卫生—药理学]