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  

Pharmacokinetics and Bioequivalence of Mosapride Granules in Healthy Volunteers

作　　者：陈倩[1] 付伟[1] 任秀华[1] 张冬林[1] 雷永芳[1] 刘东[1] 

机构地区：[1]华中科技大学同济医学院附属同济医院药学部,武汉430030

出　　处：《中国药师》2014年第3期374-377,共4页China Pharmacist

基　　金："重大新药创制"科技重大专项(编号:2012ZX09303018001)

摘　　要：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C_(max)分别为(48.26±22.67)ng·ml^(-1)和(45.20±20.28)ng·ml^(-1),t_(max)分别为(0.62±0.89)h和(0.65±0.34)h,t_(1/2)分别为(2.16±0.63)h和(2.62±1.42)h,AUC_(0→10)分别为(86.87±39.21)ng·h·ml^(-1)和(85.20±29.44)ng·h·ml^(-1),AUC_(0→∞)分别为(90.55±41.50)ng·h·ml^(-1)和(90.31±31.86)ng·h·ml^(-1)。AUC_(0→10)、AUC_(0→∞)和C_(max)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F_(0→10)为(109.5±45.3)%。结论:两制剂具有生物等效性。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.

关 键 词：枸橼酸莫沙必利 药动学 生物等效性 HPLC-MS MS 

分 类 号：R969.1[医药卫生—药理学]