阿莫西林克拉维酸钾片的人体相对生物利用度

Study on Relative Bioavailability of Amoxillin & Clavulanate potassium Tablets in Healthy Volunteers

目的 :研究两种阿莫西林克拉维酸钾 (AMO&CLV)片的药物动力学及生物等效性。方法 :采用反相高效液相色谱法测定 10名志愿受试者单剂量口服 75 0mg两种AMO&CLV片 (内含AMO 5 0 0mg ,CLV 2 5 0mg)后 ,AMO和CLV血药浓度的变化情况 ,数据经 3p87药物动力学程序处理。结果 :AMO药时曲线下面积分别是 :(2 4.6± 2 .6 ) μg·ml-1·h-1与 (2 5 .0± 2 .5 )μg·ml-1·h-1;达峰时间分别为 :(1.4± 0 .2 )h与 (1.4± 0 .2 )h ;峰浓度分别是 :(6 .2± 0 .7) μg·ml-1与 (6 .4± 0 .6 ) μg·ml-1。CLV药时曲线下面积分别是 :(13.5± 1.0 ) μg·ml-1·h-1与 (14.0± 1.1) μg·ml-1·h-1;达峰时间分别为 :(1.3± 0 .2 )h与 (1.3± 0 .2 )h ;峰浓度分别是 :(3.6± 0 .4) μg·ml-1;与 (3.7± 0 .4) μg·ml-1。结论 :配对t检验与双单侧t检验结果表明 :二者药时曲线下面积、峰浓度及达峰时间差异无显著性 (P >0 .0 5 ) ,两种AMO&CLV片为生物等效制剂。供试品的相对生物利用度分别为 :(98.5± 4.9) % (AMO) ,,(96 .9± 6 .8) % (CLV)。

OBJECTIVE:The pharmacokinetics and relative bioavailability of two amoxillin & clavulanate potassium tablets were studied.METHODS:amoxillin and clavulanate potassium concentration in serum was determined by RP HPLC after a single oral dose 750 mg of two amoxillin & clavulanate potassium tablets given respectively to 10 volunteers in an open randomized cross over test.RESULTS:The AUC 0→∞ of amoxillin of the two formulations were ( 24.6 ± 2.6 )μg·ml -1 ·h -1 and ( 25.0 ± 2.5 )μg·ml -1 ·h -1 ; T max were ( 1.4 ± 0.2 )h and ( 1.4 ± 0.2 )h; C max were ( 6.2 ± 0.7 )μg·ml -1 and ( 6.4 ± 0.6 )μg·ml -1 respectively the AUC 0→∞ of clavulanate potassium of the two formulations were ( 13.5 ± 1.0 )μg·ml -1 ·h -1 and ( 14.0 ± 1.1 )μg·ml -1 ·h -1 ; T max were ( 1.3 ± 0.2 )h and ( 1.3 ± 0.2 )h; C max were ( 3.6 ± 0.4 )μg·ml -1 and ( 3.7 ± 0.4 )μg·ml -1 respectively.CONCLUSIONS:The result of statistical analysis showed that there were no significant differences of the AUC 0→∞ 、 T max and C max of amoxillin and clavulanate potasssium between the two formulations ( P > 0.05 ) and two amoxillin & clavulanate potassium tablets were bioequivalent. [