枸橼酸莫沙必利颗粒在健康人体的药动学和生物等效性评价研究

目的：研究枸橼酸莫沙必利颗粒的人体相对生物利用度和生物等效性.方法：健康志愿者24名,随机双交叉单剂量口服枸橼酸莫沙必利颗粒（受试制剂）和枸橼酸莫沙必利片（参比制剂）,剂量均为10mg,采用HPLC-MS/MS测定血浆中枸橼酸莫沙必利的浓度,用DAS2.1药动学程序计算药动学参数和生物利用度,并进行生物等效性评价.结果：单剂量口服枸橼酸莫沙必利受试和参比制剂后,血浆莫沙必利的Cmax分别为（48.26±22.67）ng·ml-1和（45.20±20.28）ng·ml-1,tmax分别为（0.62±0.89）h和（0.65±0.34）h,t1/2分别为（2.16±0.63）h和（2.62±1.42）h,AUC0→10分别为（86.87±39.21）ng·h·ml-1和（85.20±29.44）ng·h·ml-1,AUC0→∞ 分别为（90.55±41.50）ng·h·ml-1和（90.31 ±31.86）ng·h·ml-1.AUC0→10、AUC0→∞和Cmax的90%可信区间分别为87.3%～116.4%,86.7%～113.7%和85.7%～126.7%.受试制剂的相对生物利用度F0→10为（109.5±45.3）%.结论：两制剂具有生物等效性.

Pharmacokinetics and Bioequivalence of Mosapride Granules in Healthy Volunteers

Objective ： To study the relative bioavailability and bioequivalence of mosapride granules in healthy volunteers. Meth- ods ： A single oral dose （ 10mg of test or reference preparation） was given to 24 male healthy volunteers in a randomized crossover stud- y. The plasma concentration of mosapride was determined by HPLC-MS/MS. The pharmacokinetic parameters were calculated and the bioavailability and bioequivalence of the two formulations were evaluated by DAS program. Results ： After a single dose, the pharmaco- kinetic parameters of the test and reference mosapride were as follows ： Cmax （ 48.26 ± 22.67 ） ng · ml - 1 and （ 45.20 ±20.28 ） ng ·ml-1 ,tmax（0.62±0.89）h and（0.65 ±0.34）h,t1/2 （2.16 ±0.63）h and（2.62± 1.42）h,AUC0→10（86.87 ±39.21）ng · h · ml-1 and （85.20±29.44）ng· h· ml-1,AUC0→∞（90.55 ±41.50）ng· h · ml-1 and（90.31 ±31.86）ng · h · ml-1,respectively. The 90% confidential interval of AUC0→10, AUC0→∞ and Cmax was 87.3% - 116.4% ,86.7% - 113.7% and 85.7% - 126.7% , respectively. The relative bioavailability was （109.5± 45.3 ）%. Conclusion： The two formulations are bioequivalent.