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目的:研究舒血宁注射液在健康兔和实验性糖尿病兔体内对格列吡嗪代谢的影响。方法:健康新西兰家兔和实验性糖尿病家兔各3只,每只分别口服格列吡嗪5 mg,经3 wk清洗期后,每只家兔均经耳缘静脉注射舒血宁注射液,每天1次,持续3天,第4天口服相同剂量格列吡嗪。取血时间均为给予格列吡嗪前0.5h及给药后0.5、1.5、3、5、7、9、11、24、35 h,经耳缘静脉采血1 mL,用HPLC法得到各时间点格列吡嗪的血药浓度,测得的结果用药动学软件DAS3.16进行曲线拟合,分析比较给予舒血宁前后格列吡嗪药动学参数的变化。结果:格列吡嗪在家兔体内的药动学符合单室模型,健康组家兔单用格列吡嗪时,其平均t1/2、Cmax、AUC分别为3.685±1.273,11453.1±697.1,66949.5±2393.3;加用舒血宁后其平均t1/2、Cmax、AUC分别为3.399±0.956,6055.2±458.4,41635.2±1767.2。糖尿病组家兔单用格列吡嗪,平均t1/2、Cmax、AUC分别为8.958±1.451,5829.1±371.5,58696.2±1899.1;加用舒血宁后其平均t1/2、Cmax、AUC分别为4.998(1.329,4917.3±287.7,20125.3±1238.7。给予舒血宁前后格列吡嗪的t1/2、Cmax、AUC差异均存有统计学意义(P<0.05)。结论:舒血宁对肝药酶450存在诱导作用,对家兔体内格列吡嗪的药动学行为有明显的影响。
Objective: To study Shuxuening injection in healthy rabbits and experimental diabetic rabbits glipizide metabolism. Methods: Three healthy New Zealand rabbits and experimental diabetic rabbits were treated with glipizide 5 mg orally respectively. After 3 weeks of cleaning, each rabbit was injected Shushuxing injection through the ear vein, 1 day, for 3 days, oral administration of the same amount of glipizide 4 days. Bleeding time were given before glipizide 0.5h and 0.5,1.5,3.5,7,9,11,24,35 h after administration, the blood collected through the ear vein 1 mL, obtained by HPLC at each time Point glipizide blood concentration, the measured results using pharmacokinetic software DAS3.16 curve fitting, compared Shuxuening given glipizide pharmacokinetic parameters. Results: The pharmacokinetics of glipizide in rabbits accorded with single-compartment model. The average t1 / 2, Cmax and AUC of healthy group were 3.685 ± 1.273, 11453.1 ± 697.1, 66949.5 ± 2393.3. The mean t1 / 2, Cmax and AUC of Shu-Ning-Ning were 3.399 ± 0.956, 6055.2 ± 458.4 and 41635.2 ± 1767.2, respectively. The mean t 1/2, C max and AUC of diabetic rabbits were 8.958 ± 1.451, 5829.1 ± 371.5 and 58696.2 ± 1899.1, respectively. The average t1 / 2, Cmax and AUC of the patients with diabetes were 4.998 (1.329,4917.3 ± 287.7 and 20125.3 ± 1238.7), the difference of t1 / 2, Cmax and AUC of glipizide before and after Shuxuening were statistically significant (P <0.05) .Conclusion: Enzyme 450 has an induction effect on the pharmacokinetics of glipizide in rabbits significantly.