阿莫西林注射用混悬液及其在猪体内的药物动力学研究

Studies on Amoxicillin for Injectable Suspension and its Pharmacokinetics in Swine

以阿莫西林为原料,注射用大豆油为溶媒,成功研究出阿莫西林注射用混悬液,并对制剂进行了稳定性研究。所有参试样品的相对含量、外观性状、粒度、分解产物等指标均无明显变化,表明该制剂对光、热稳定。选用5头健康猪进行了药物动力学研究,按15mg/kgB.W的阿莫西林剂量肌内注射,药时曲线符合一级吸收二室模型,主要动力学参数为:Tmax=0 53±0 17h,Cmax=12 33±0 47μg/ml,AUC=79 62±4 32(μg/ml)h,T1/2β=33 62±4 06h。结果表明,阿莫西林注射用混悬液在猪体内吸收缓慢,持效时间长。临床应用48h给药1次仍能维持对常见病原菌的有效血药浓度。

Amoxicillin(AMO) for injectable suspension had been developed successfully by suspending the AMO in soybean oil in this dissertation.The AMO concentrations of preparation samples were determined by HPLC/UV.The preparation had been carried on a stability experiment.At the end of the test,all programs such as color,particulate,decomposed product and so on had not significant changes.The experimental results indicated that the injectable suspension was stable to light and heat.The pharmacokinetics of the preparation administrated intramuscularly at a dose of AMO 15 mg/kg b.w.to 5 swine was studied.The standard curves for AMO were linar in a range of 05～20 μg/ml,r=09998(n=5).The limit of detection was 035 μg/ml.The plasma drug concentrations determined were calculated by software 3P97.The results suggested that the kinetics of the injecton had been fit to two compartment model with first order absorption.The main parameters were as follows:Tmax=053±017h,Cmax=1233±047μg/ml,AUC=7962±432(μg/ml)h,T1/2β=3362±406h.The dosage of the recommendation for AMO for injectable suspension is 15 mg/kg b.w.given once in every two days.