扎莱普隆胶囊的相对生物利用度研究

Relative Bioavailability of Zaleplon Capsule in Healthy Volunteers

目的:比较扎莱普隆胶囊和片剂在健康人体内的药代动力学过程,并对两制剂的生物等效性做出评价。方法:20名健康男性志愿者采用交叉给药方案,分别单剂量口服10mg扎莱普隆胶囊和片剂,用高效液相色谱荧光检测法测定血浆中扎莱普隆浓度,进行生物等效性评价。结果:实验表明扎莱普隆胶囊和片剂的tmax分别是1.04±0.35h和1.10±0.45h,Cmax分别是26.06±9.14μg·L-1和27.39±7.51μg·L-1,t(1/2)ke分别是1.33±0.26h和1.34±0.22h,AUC0-∞分别是83.39±37.35μg·h·L-1和 87.44±35.25μg·h·L-1。相对生物利用度为94.40%±11.06%。结论:结果显示两种制剂具有生物等效性。

OBJECTIVE:The pharmacokinetics and bioavailability of test capsulewere compared with reference tablet.METHODS:A single oral dose l0mg zaleplonof reference (tablet) or test (capsule) drugs was given to healthy male volunteersaccording to an open randomized crossover study.The concentrations in plasmawere determined by HPLC method.RESULTS:The main pharmacokinetics parametersof zaleplon were:tmaxl.04±0.35h and l.l0±0.45h,Cmax 26.06±9.l4μg.L-1 and27.39±7.5lμg.L-1,t(1/2ke)l.33±0.26h and l.34±0.22h,AUC0-8 83.39±37.35μg.h.L-1and 87.44±35.25μg.h.L-1for capsule and tablet respectively.The bioavailability ofeffervescent capsule to tablet was 94.40%±ll.06%. CONCLUSION:The resultsof statistical analysis showed that two formulations were bioequivalent.