阿莫西林可溶性粉在猪体内的药代动力学和绝对生物利用度研究

Pharmacokinetics and Absolute Bioavailability of Amoxicillin Soluble Powder in Pigs

研究阿莫西林可溶性粉在猪体内的药代动力学特征,并评价其与市售注射用阿莫西林钠的生物等效性。采用高效液相色谱法(HPLC)测定血浆中阿莫西林浓度,通过Data Analysis System(DAS 3.0)计算药动学参数,采用非房室模型分析方法对药代动力学参数进行评价,猪经内服给药后,药物平均滞留时间MRT(0-t)为3.12±0.41 h,平均达峰时间T max为1.63±0.35 h,平均达峰浓度C max为4101.35±631.55μg/L,平均药-时曲线下面积AUC(0-t)为13540.33±3445.51μg/L×h,消除速率常数λz为0.36±0.14/h,半衰期t 1/2z为2.48±1.73 h。猪经静脉注射给药后,平均滞留时间MRT(0-t)为1.54±0.35 h,平均药-时曲线下面积AUC(0-t)为8522.56±1430.51μg/L×h,消除速率常数λz为0.23±0.12/h,半衰期t 1/2z为3.84±2.03 h。结果表明:受试制剂阿莫西林可溶性粉经内服给药后,具有较快的吸收速度,吸收进血液后在体内的停留时间较短,代谢较快,平均达峰时间短,药物消除速度较快,平均绝对生物利用度为79.44%,为临床制定合理用药方案提供科学依据。

To study the pharmacokinetic characteristics of amoxicillin soluble powder in pigs and evaluate its bioequivalence with amoxicillin sodium for injection,the concentration of amoxicillin in plasma was determined by high performance liquid chromatography(HPLC),the pharmacokinetic parameters were calculated by Data Analysis System(DAS 3.0),and the pharmacokinetic parameters were evaluated by non-compartment model analysis.After oral administration,the average retention time of the drug in pigs was 3.12±0.41 h,and the average time to peak was 1.63±0.35 h.The average peak concentration C max is 4101.35±631.55μg/L,the average area AUC(0-t)under the drug-time curve is 13540.33±3445.51μg/L×h,the elimination rate constantλz is 0.36±0.14/h,and the half-life t 1/2z is 2.48±1.73 h.After intravenous administration,the average retention time MRT(0-t)was 1.54±0.35 h,the average area under the drug-time curve AUC(0-t)was 8522.56±1430.51μg/L×h,the elimination rate constantλz was 0.23±0.12/h,and the half-life t 1/2z was 3.84±2.03 h.The results showed that amoxicillin soluble powder,a test preparation,had a fast absorption rate after oral administration,a shorter retention time in the body,a faster metabolism,a shorter average peak time,a faster drug elimination rate,and an average absolute bioavailability of 79.44%,which provided a scientific basis for making a rational drug use plan in clinic.