穿琥宁中空栓在兔体内的药物动力学及绝对生物利用度

Study on Pharmacokinetics and Bioavailability of Potassium Dehydroandrographolide Succinate Hollow Suppositories in Rabbits

目的:研究穿琥宁中空栓在兔体内的药物动力学及绝对生物利用度。方法:取健康家兔30只,随机分为3组。第1组为静脉注射组;第2组为聚乙二醇300穿琥宁中空栓组;第3组为1,2丙二醇穿琥宁中空栓组,分别静脉注射穿琥宁100 mg或直肠给予穿琥宁中空栓1枚。用HPLC法测定血药浓度。按统计矩的非隔室动力学理论计算药物动力学参数。结果:聚乙二醇300穿琥宁中空栓和1,2丙二醇穿琥宁中空栓的C_(max)分别为(37.4±5.3)和(20.2±4.6)μg·ml^(-1);AUC_(0-inf)分别为(2885.92±214.578)和(1960.98±111.194)μg·min·ml^(-1);绝对生物利用度分别为18.33%和12.45%。结论:聚乙二醇300穿琥宁中空栓组和1,2丙二醇穿琥宁中空栓组的C_(max)和AUC_(0-inf)有统计学差异。

Objective： To study the pharmacokinetics and the absolute bioavailability of Potassium dehydroandrographolide succinate（PDS） hollow suppositories in rabbits. Method： In an open randomized crossover test, 30 rabbits were divided into 3 group randomly, the first group were given PDS injection of 100mg ; PEG 300 PDS hollow suppositories were given to the second ones ; the third group were given 1,2 propylene glycol PDS hollow suppositories. HPLC method was developed to the drug serum concentration of rabbits. The pharmacokinetics parameters of PDS were analyzed by statistical moment non - compartment model. Result： The Cmax of PEG 300 PDS hollow suppository and 1,2 propylene glycol PDS hollow suppository were （ 37.4 ± 5.3 ） and （ 20.2 ± 4.6） μg·ml^-1, AUC（0-inf） were（2885.92 ±214.578） and （ 1960.98 ± 111. 194） μg· min·ml^-1 ; absolute bioavailability were 18.33% and 12.45%, respectively. Conclusion： The Cmax and AUC（0-inf） of two PDS hollow suppositories have significant difference.