兽用退热栓剂在家兔体内的药物动力学研究

Study on Pharmacokinetics of Defervescence Suppository for Animals in Rabbits

为了解自制的双氯灭痛退热栓剂在家兔体内的药物动力学过程,将6只健康家兔每次经肛门单剂量给予双氯灭痛栓剂50mg,定时收集血样,采用紫外分光光度法测定血中药物浓度后,以3p97软件包计算基本的药物动力学参数。结果显示,消除半衰期t1/2k为(5.1±1.2)h,峰浓度Cmax为(126.3±2.4)μg/mL,达峰时间tmax为(1.8±0.5)h,血药浓度—时间曲线下面积(AUC)为(20.4±1.3)mg/(L.h);双氯灭痛退热栓剂在家兔体内的药物运转过程符合一级吸收的一室模型。以上参数表明,双氯灭痛也可研制成动物直肠给药的新剂型。

To study the plasma pharmacokinetics of diclofenac sodium suppositories which was made by ourself in rabbit,diclofenac sodium suppositories for 6 healthy rabbits(as a single rectal formulation) was used at a dose of 50 mg per rabbit.The plasma concentration of diclofenac sodium were determined using UV spectrophotometry,and pharmacokinetic analysis was carried out by using software 3p97.The results showed that the main pharmacokinetic parameters were as follows:elimination half-life(t1/2k) was(5.1±1.2) h,the peak plasma concentration(Cmax) was(126.3±2.4) μg/mL,the time to Cmax(Tmax) was(1.8±0.5) h,the area under the curve(AUC) was(20.4±1.3) mg/(L·h),and the concentrations-time data were best described by a one-compartment open model with first order absorption.The data could be used for the application of diclofenac sodium to be made of suppository rectally.