丙磺舒对阿莫西林在家兔体内的药动学影响

The effect of probenecid on the pharmacokinetics of amoxicillin in rabbits

目的：观察丙磺舒对阿莫西林在健康家兔体内药动学的影响。方法：采用微生物杯碟法测定兔血清中阿莫西林的浓度。结果：阿莫西林单剂量肌内注射后，吸收迅速，Tmax=(0．78±0．09)h，Cmax=(0．87±0．30)μg·mL-1，其代谢模型为一级速率一房室模型。当阿莫西林和丙磺舒等剂量伍用时丙磺舒对阿莫西林药动学参数的影响达到最大值：阿莫西林的t1／2由(2．06±0．09)h延长至(5．50±0．52)h，AUC由(4．07±0．05)μg·mL-1·h增加至(13．75±3．09)μg·mL-1·h，Cmax由(0．87±0．30)μg·mL-1增加至(6.30±1．46)μg·mL-1，且三者统计学差异极显薯(P<0 01)。结论：丙磺舒对阿莫西林的药动学参数的影响呈S型。当两者等剂量（？）用时影响最大。

Objective:To study the effect of probenecid on the pharmacokinetics of amoxicillin in rabbits.Methods:The serum amoxicillin concentration of rabbits was measured by microbial plate assay technique. Results:After intramuscular injection of a single dose of amoxicillin, it was quickly absorbed and a Tmax of (0.78±0.09)h and a Cmax of (0.87±0.30) μg·mi-1 were obtained. The maximum effect of probenecid was reached when the dosage ratio of probenecid and amoxicillin was 1:1 and at the same time, t1/2 of amoxicillin prolonged from (2. 06±0. 09)h to (5. 50±0. 52)h, AUC and Cmax of amoxicillin was increased from (4.07±0.05) /μg·mL-1·h to (13.75±3.09)μg·mL-1·h and from (0.87±0.30)μg·mL-1 to (6.30±1.46) μg·mL-1 respectively and there was significant difference among the 3 parameters (P<0.01). Conclusion:The effect of probenecid on the pharmacokinetic parameter of amoxicillin is in a shape of S and the maximum effect of probenecid is reached when the dosage ratio of probenecid and amoxicillin is 1:1.