丁酸氯维地平脂肪乳注射液在健康人体中的生物等效性评价  

Bioequivalence Evaluation of Clevidipine Butyrate Fat Emulsion Injection in Healthy Volunteers

作　　者：罗艳菲 LUO Yanfei(Shandong Weigao Pharmaceutical Co.,Ltd.,Weihai 264210,China)

机构地区：[1]山东威高药业股份有限公司,山东威海264210

出　　处：《生物化工》2024年第5期8-11,15,共5页Biological Chemical Engineering

摘　　要：目的:评价丁酸氯维地平脂肪乳注射液在健康人体中的生物等效性。方法:采用随机、开放、单次给药、双周期、交叉的试验设计,共入组32例健康受试者,连续静脉泵注丁酸氯维地平脂肪乳注射液60 min±1 min,给药速率为6 mg/h(约12 mL/h)。采用高效液相色谱-串联质谱法测定注射前后26个时间点全血中氯维地平与其代谢物H152/81的浓度,采用Phoenix^(TM)WinNonlin^(®)8.1计算药动学参数。结果:氯维地平及其代谢物H152/81的C_(max)的几何均值比值为103.39%、106.49%,90%置信区间(I_(C))为99.07%~107.90%、104.79%~108.22%;AUC_(0-t)的几何均值比值为104.16%、103.56%,90%I_(C)为100.64%~107.81%,101.44%~105.73%;AUC_(0-∞)的几何均值比值为104.16%、103.65%,90%I_(C)为100.62%~107.82%,101.40%~105.96%。结论:丁酸氯维地平脂肪乳注射液受试制剂与参比制剂在健康人体中具有生物等效性。Objective:To evaluate the bioequivalence of generic formulation of clevidipine butyrate fat emulsion in healthy subjects.Methods:A total of 32 healthy subjects are enrolled in a randomized,open-lable,single-dose,two period,two-sequence and self-crossover study.Clevidipine butyrate fat emulsion injection is injected by continuous intravenous pump 60 min±1 min,and the administration rate is 6 mg/h(about 12 mL/h).The concentrations of clevidipine and its metabolite H152/81 in whole blood at 26 time points before and after injection are determined by high performance liquid chromatography tandem mass spectrometry.Pharmacokinetic parameters are calculated by Phoenix^(TM)WinNonlin^(®)8.1.Results:The geometric mean ratio of C_(max) of clevidipine and its metabolite H152/81 is 103.39%and 106.49%,the 90%Confidence interval(I_(C))is 99.07%to 107.90%and 99.07%to 107.90%.The geometric mean ratio of AUC_(0-t) is 104.16%and 103.56%,the 90%I_(C) is 100.64%to 107.81%and 101.44%to 105.73%.The geometric mean ratio of AUC_(0-∞)is 104.16%and 103.65%,the 90%I_(C) is 100.62%to 107.82%and 101.40%to 105.96%.Conclusion:The generic formulation of clevidipine is bioequivalent to the reference marketed brand in healthy subjects.

关 键 词：丁酸氯维地平 脂肪乳注射液 药动学 生物等效 安全性 

分 类 号：R969[医药卫生—药理学]