枸橼酸莫沙必利分散片的药物动力学研究  

Pharmacokinetics study on Mosapride Citrate dispersible tablets

作　　者：谭培[1] 徐小平[1] 尹华熙[1] 严绍华[1] 廖丽云[1] 任霞[1] 黄荣川[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2004年第4期283-285,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的　研究枸橼酸莫沙必利分散片 (MCDT)在家犬体内的药物动力学特征并与 3种枸橼酸莫沙必利片 (MCT)进行比较。方法　 2 0只健康家犬 4× 4交叉设计分成 4组 ,分别口服MCT 10mg ,采用HPLC法测定给药后不同时间点血浆中莫沙必利的浓度 ,用 3p97程序拟合房室模型并计算其药动学参数 ,评价不同莫沙必利片在动物体内的药物动力学特征和生物等效性。结果　MCDT和 3种MCT的血药浓度—时间曲线符合口服二室开放模型 ,主要药动学参数分别为Cmax:135 .4 2 5± 3.72 8、12 5 .75 9± 7.5 12、12 1.334± 4 .6 5 6、12 1.6 79± 6 .910ng·ml-1;Tmax:0 .6 4 8± 0 .16 5、0 .710± 0 .194、0 .814± 0 .2 0 7、0 .731± 0 .176h ;AUC(0～t) :344 .4 32± 37.173、32 9.6 2 5± 36 .4 5 5、30 2 .931± 36 .0 4 4、30 3.86 0± 30 .4 19ng·h·ml-1;AUC(0～inf) :396 .733± 4 6 .6 16、374 .787± 4 3.0 6 8、337.173± 4 9.0 5 7、348.4 80± 2 0 .0 88ng·h·ml-1;MCDT相对加斯清片的生物利用度F0～t为 :10 5 .5 %± 15 .5 %。结论　统计结果表明MCDT与其他 3种MCT具有生物等效性 (P >0 .0 5 ) ,而Cmax和Tmax明显优于MCT。OBJECTIVE To study the pharmacokinetics characteristics of Mosapride Citrate dispersible tablets(MCDT) in dogs, which was compared with three kinds of Mosapride Citrate tablets(MCT).METHODS 20 healthy dogs were divided into 4 groups by 4×4 cross-over design.Each group orally took one kind of MCT.Mosapride concentrations of various time point in dogs′ plasma were determined by HPLC.3p97 program was used to fit the compartment model,calculate the pharmacokinetics parameters and assess the characteristics of pharmacokinetics of various MCT and bioequivalence.RESULTS The concentration-time curves of four kinds of MCT were conformed to a two-compartment open model.The main pharmacokinetics parameters of MCDT and three kinds of MCT were as follow:C max :135.425±3.728,125.759±7.512,121.334±4.656,121.679±6.910 ng·ml -1 ;T max :0.648±0.165,0.710±0.194,0.814±0.207,0.731±0.176h;AUC (0～t) : 344.432 ±37.173,329.625±36.455,302.931±36.044,303.860±30.419 ng·h·ml -1 ;AUC (0～inf) :396.733±46.616,374.787± 43.068, 337.173±49.057,348.480±20.088 ng·h·ml -1 .The relative bioavailability F (0～t) % of MCDT relate to Gasmotin tablets was 105.5%±15.5%. CONCLUSION The statistic results show that MCDT and the other MCT are bioequivalent(P>0.05).C max and T max of MCDT are apparently better than the others.

关 键 词：枸橼酸莫沙必利分散片 药物动力学 高效液相色谱法 MCDT 血药浓度 

分 类 号：R975[医药卫生—药品] R969.1[医药卫生—药学]