2种阿莫西林分散片人体药动学及生物等效性研究

Pharmacokinetics and Bioequivalence of 2 Kinds of Amoxicillin Dispersible Tablets in Healthy Volunteers

目的:研究2种阿莫西林分散片在人体内的药动学及生物等效性。方法:采用随机自身交叉对照试验设计,20名健康男性志愿者分别单剂量口服500mg阿莫西林受试制剂与参比制剂后,采用高效液相色谱法测定血浆阿莫西林的浓度,用DAS药动学软件计算二者药动学参数及生物利用度。结果:阿莫西林受试制剂与参比制剂的药动学参数分别为:Cma(x11.11±3.63)、(9.93±3.39)μg.mL-1,tma(x1.14±0.42)、(1.34±0.47)h,t1/(21.08±0.52)、(1.07±0.66)h,AUC0～(624.49±6.22)、(22.44±5.98)μg.h.mL-1,AUC0～∞(25.21±6.44)、(23.40±6.25)μg.h.mL-1。以AUC0～6估算,受试制剂相对于参比制剂的生物利用度为110.3%。结论:2种阿莫西林分散片生物等效,可以替换使用。

OBJECTIVE：To study the pharmacokinetics and bioequivalence of 2 kinds of Amoxicillin dispersible tablets in healthy volunteers. METHODS： In randomized cross-over controlled study, 20 healthy male volunteers received a single oral dose of test amoxicillin tablets 500 mg and reference amoxicillin tablets 500 mg. Plasma concentration of amoxicillin was detected by HPLC and pharmacokinetic parameters and bioavailability of 2 kinds of amoxicillin dispersible tablets were calculated by DAS software. RESULTS： The main pharmacokinetic parameters of test tablets vs. reference tablets were as follows：Cmax（11.11±3.63） μg·mL-1 vs. （9.93±3.39）μg·mL-1;tmax（1.14±0.42） h vs. （1.34±0.47） h; t1/2（1.08±0.52） h vs. （1.07±0.66） h; AUC0～6（24.49±6.22）μg·h·mL-1 vs. （22.44±5.98）μg·h·mL-1; AUC0～∞（25.21±6.44）μg·h·mL-1 vs. （23.40±6.25）μg·h·mL-1 respectively. According to AUC0～6, the relative bioavailability of test tablets was 110.3%. CONCLUSION： Two kinds of amoxicillin tablets are bioequivalent and interchangeable.