2种多潘立酮片的人体生物等效性研究

Bioequivalence of Domperidone Tablets in Healthy Volunteers

目的:研究2种多潘立酮片在健康人体内的生物等效性。方法:健康志愿者22名,采用随机交叉试验设计,单剂量口服多潘立酮片受试制剂或参比制剂10mg,应用高效液相色谱串联质谱电喷雾(LC-MS/MS)法测定各受试者给药后不同时间点的血药浓度,计算药动学参数,应用BAPP2.0软件进行生物等效性评价。结果:受试制剂与参比制剂的药动学参数分别为:tma(x0.55±0.15)、(0.57±0.11)h,t1/(210.22±1.29)、(10.90±1.44)h,cma(x12.721±5.567)、(13.265±5.787)μg·L-1,AUC0～36(h42.550±11.724)、(44.259±8.813)mg·h·L-1,AUC0～∞(45.539±12.327)、(47.900±9.446)mg·h·L-1。多潘立酮片受试制剂相对于参比制剂的生物利用度为(96.5±19.2)%,主要药动学参数经统计学分析无显著性差异。结论:受试制剂与参比制剂具有生物等效性。

OBJECTIVE： To study the bioequivalence of Domperidone tablets in healthy volunteers. METHODS： In randomized cross-over design, 22 healthy volunteers were given single oral dose of test preparations 10 mg and reference preparation 10 mg. The plasma concentration of domperidone was determined by LC-MS/MS. The pharmacokinetic parameters were calculated and the bioequivalence was evaluated using BAPP2.0 software. RESULTS： The main pharmacokinetic parameters of test preparations and reference preparations were as follows：tmax（0.55±0.15）h and （0.57±0.11）h; t1/2（10.22±1.29） h and （10.90±1.44）h;cmax（12.721±5.567）μg·L-1 and （13.265±5.787）μg·L-1;AUC0～36 h（42.550±11.724）mg·h·L^-1 and（44.259±8.813）mg·h·L^-1;AUC0～∞（45.539±12.327）mg·h·L^-1 and （47.900±9.446）mg·h·L^-1. The relative bioavailability was （96.5±19.2）%. The main pharmacokinetic parameters showed no statistically significant difference between two preparations. CONCLUSION： Test preparations and reference preparations are bioequivalent.