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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 absolute bioavailability of Chuanhuning hollow suppository in rabbits. Methods: Thirty healthy rabbits were randomly divided into three groups. The first group was intravenous injection group; the second group was polyethylene glycol 300 Chuanhuning hollow suppository group; the third group was 1,2-propanediol Chuanhuning hollow suppository group, respectively, intravenous Chuanhuning 100mg or rectal administration Chuanhuning hollow plug. The plasma concentration was determined by HPLC. The pharmacokinetic parameters were calculated according to the statistical moment non-compartmental kinetics theory. RESULTS: The C max of polyethylene glycol 300 Chuanhuning hollow suppository and 1,2-propanediol Chuanhuning suppository were (37.4±5.3) and (20.2±4.6) μg·ml-1, respectively; AUC_(0-inf ) were (2885.92±214.578) and (1960.98±111.194) μg·min·ml~(-1) respectively; absolute bioavailability was 18.33% and 12.45%, respectively. Conclusion: There are significant differences in C max and AUC 0-inf between polyethylene glycol 300 Chuan Hu Ning hollow suppository and 1,2-propanediol Chuan Hu Ning hollow suppository.