琥珀酸索利那新片在健康人体内的生物等效性研究  

Bioequivalence of Solifenacin Succinate Tablets in Healthy Subjects

作　　者：李广辉 刘平[1] 徐国防 赖耀文 高盼 赵岳 朴永吉 齐华平 LI Guanghui;LIU Ping;XU Guofang;LAI Yaowen;GAO Pan;ZHAO Yue;PIAO Yongji;QI Huaping(The Fifth Clinical Medical College of Henan University of Chinese Medicine(Zhengzhou People’s Hospital),Zhengzhou 450003,China;Zhengzhou Orthopaedic Hospital,Zhengzhou 450003,China;Yangtze River Pharmaceutical Group Guangzhou Hairui Pharmaceutical Co.,Ltd.,Guangzhou 510000,China)

机构地区：[1]河南中医药大学第五临床医学院(郑州人民医院),河南郑州450003 [2]郑州市骨科医院,河南郑州450003 [3]扬子江药业集团广州海瑞药业有限公司,广东广州510000

出　　处：《河南医学研究》2024年第23期4234-4238,共5页Henan Medical Research

摘　　要：目的研究在中国健康受试者中,空腹条件下单次口服琥珀酸索利那新片后,受试制剂与参比制剂的生物等效性。方法采用单中心、随机、开放、两周期交叉设计,选取空腹组受试者30例,每周期口服受试制剂或参比制剂5 mg,采用高效液相色谱质谱联用法(LC-MS/MS)法测定索利那新血药浓度,采用WinNonlin 8.4软件计算药代动力学参数,并完成生物等效性分析。结果空腹组中,受试制剂和参比制剂的药代动力学参数分别为C_(max)(7.31±2.27)μg·L^(-1)和(7.40±2.35)μg·L^(-1),AUC 0-t(417.00±142.00)h·μg·L^(-1)和(429.00±156.00)h·μg·L^(-1),AUC 0-∞(502.00±201.00)h·μg·L^(-1)和(511.00±214.00)h·μg·L^(-1),T max 5.00 h和5.00 h,t 1/2(62.70±16.30)h和(60.70±16.60)h,相对生物利用度按AUC 0-t计算为97.85%,按AUC 0-∞计算为97.01%。在空腹条件下,两种制剂主要药代动力学参数C max、AUC 0-t及AUC 0-∞的几何均数比值的90%置信区间均为80.00%~125.00%。结论在空腹条件下,琥珀酸索利那新的受试制剂与参比制剂表现出生物等效性。Objective To assess the bioequivalence between the test and reference formulations of solifenacin succinate tablets following a single oral dose under fasting conditions in healthy Chinese volunteers.Methods The study was designed as single-center,randomized,open,self-crossover.Thirty healthy volunteers were recruited in fasting conditions.Subjects were assigned to receive a single oral dose of the test or reference formulation per period at a dose of 5 mg.The plasma concentration of solifenacin was analyzed by liquid chromatography-tandem mass spectrometry(LC-MS/MS).The major pharmacokinetic parameters were calculated by WinNonlin 8.4,and the bioequivalence was evaluated.Results The main pharmacokinetic parameters of single oral solifenacin succinate under fasting conditions for the test and reference preparations were as follows:C max(7.31±2.27)μg·L^(-1)and(7.40±2.35)μg·L^(-1),AUC 0-t(417.00±142.00)h·μg·L^(-1)and(429.00±156.00)h·μg·L^(-1),AUC 0-∞(502.00±201.00)h·μg·L^(-1)and(511.00±214.00)h·μg·L^(-1),T_(max) 5.00 hours and 5.00 hours,t 1/2(62.70±16.30)hours and(60.70±16.60)hours.The relative bioavailability was 97.85%for AUC 0-t,97.01%for AUC 0-∞.The 90%confidence intervals of the geometric mean ratios of the main pharmacokinetic parameters(C max,AUC 0-t,AUC 0-∞)of the two preparations under fasting conditions were all 80.00%-125.00%.Conclusion The test and reference preparations of solifenacin succinate tablets are bioequivalent under fasting conditions.

关 键 词：琥珀酸索利那新片 生物等效性 药代动力学 

分 类 号：R969[医药卫生—药理学]