拉呋替丁胶囊的人体药动学研究

Pharmacokinetic Study of Lafutidine Capsule in Healthy Volunteers

目的:研究拉呋替丁胶囊在健康人体内的药动学。方法:12名健康志愿者分为男、女2组,分别交叉单剂量口服拉呋替丁胶囊10、20mg后,用高效液相色谱-荧光检测法测定血浆中拉呋替丁浓度,用DAS软件求算药动学参数。结果:口服拉呋替丁胶囊10、20mg后的主要药动学参数分别为:tma(x1.27±0.41)、(1.13±0.47)h,Cma(x165.98±43.01)、(344.22±70.70)μg·L-1,AUC0～16(673.96±196.84)、(1459.10±403.44)μg·h·L-1,AUC0～∞(752.82±196.84)、(1506.57±409.08)μg·h·L-1。结论:拉呋替丁胶囊口服后吸收迅速和完全,在健康受试者体内的药动学过程基本符合口服一级一室模型。

OBJECTIVE：To study the pharmacokinetics of Lafutidine capsule in healthy volunteers.METHODS：12 healthy volunteers were divided into male group and female group.They were given single crossover oral dose of Lafutidine capsule 10 mg or 20 mg respectively.The plasma concentration of lafutidine was determined by HPLC-fluorescence detection and pharmacokinetic parameters were calculated using DAS software.RESULTS：Main pharmacokinetic parameters of lafutidine in healthy volunteers after given oral dose of Lafutidine capsule 10 mg vs.20 mg were as follows：tmax（1.27±0.41）h vs.（1.13±0.47）h;Cmax（165.98±43.01） μg·L-1 vs.（344.22±70.70）μg·L-1;AUC0～16（673.96±196.84）μg·h·L-1 vs.（1 459.10±403.44）μg·h·L-1;AUC0～∞（752.82±196.84） μg·h·L-1 vs.（1 506.57±409.08） μg·h·L-1.CONCLUSION：Lafutidine can be absorbed rapidly and completely.The pharmacokinetics is fitted to one-order and one-compartment model in healthy volunteers after single dose of Lafutidine capsule.