葛根素对家兔体内格列吡嗪药代动力学的影响  

Effect of Puerarin on the pharmacokinetics of glipizide in rabbits

作　　者：周鹏 厉世笑[2] 陈芳芳[3] 孙渊 夏爱晓 杜有功 

机构地区：[1]台州医院药剂科,浙江临海317000 [2]台州医院检验科,浙江临海317000 [3]台州市第二人民医院药剂科,浙江天台317200

出　　处：《中国临床药理学杂志》2014年第7期623-625,共3页The Chinese Journal of Clinical Pharmacology

基　　金：浙江省台州市科技计划基金资助项目(100KY15)

摘　　要：目的研究葛根素在健康和糖尿病家兔体内对格列吡嗪胶囊代谢的影响。方法健康新西兰家兔随机分组:健康组和糖尿病组(各5只),每只家兔口服格列吡嗪5 mg。经2周清洗期后,于家兔耳缘静脉注射葛根素(18 mg·kg-1),每天1次,持续3 d,第4天口服相同剂量格列吡嗪。在给药前与给药后,经耳缘静脉采血,用HPLC法测定各时间点格列吡嗪的血药浓度,用DAS2.0进行曲线拟合。结果格列吡嗪在家兔体内的药代动力学符合单室模型,健康组给予葛根素前后药代动力学参数,t1/2分别为(4.2±0.5),(3.58±0.7)h,ρmax分别为(15.5±0.8),(8.4±0.6)mg·L-1,AUC0-35分别为(134.8±0.7),(77.2±1.4)mg·h·L-1;糖尿病组给予葛根素前后药代动力学参数,t1/2分别为(7.6±0.9),(5.6±0.9)h,ρmax分别为(13.4±0.8),(10.6±0.9)mg·L-1,AUC0-35分别为(10.5±0.8),(7.7±1.6)mg·h·L-1。给予葛根素前后,格列吡嗪的t1/2、ρmax、AUC差异均有统计学意义(P<0.05)。结论葛根素对家兔体内格列吡嗪的药代动力学有明显的影响。Objective To study the influence on the metabolism of Pu-erarin on the pharmacokinetics of glipizide capsule in healthy and diabetic rabbits.Methods Healthy New Zealand rabbits randomly assigned , one group was modeled , each group had 5 rabbits.Glipizide （5 mg） was taken orally once to every rabbit.After 2 weeks of clearing stage, Puerarin （18 mg· kg -1） was administered daily by auricular vein injection qd for 3 d, then glipizide was taken orally at the same dosage on the 4 d.The blood was drawn from ear vein before and after administe-ring glipizide in every rabbit.Then the blood concentration of glipizide was measured by HPLC.The pharmacokinetic parameter was calculated with pharmacokinetic software DAS 2.0.The pharmacokinetics of glipiz-ide in rabbits administered with or without Puerarin were analyzed by auto-control.Results The concentration time -curves were fit to the one-compartment model.In healthy group , administered with Puerarin , the t1/2 were （4.2 ±0.5）,（3.58±0.7） h,ρmax were （15.5±0.8）, （8.4±0.6 ） mg· L-1 , AUC0-35 were （ 134.8 ±0.7 ） , （ 77.2 ±1.4 ） mg· h· L -1; respectively before and after.In diabetic group , t1/2 were （7.6 ±;0.9）,（5.6±0.9） h,ρmax were （13.4 ±0.8）,（10.6 ±0.9） mg· L-1,AUC0-35 were （10.5 ±0.8）,（7.7 ±1.6） mg· h· L-1 respectively before and after.There were notable differences on t1/2 ,ρmax , AUC values of glipizide in rabbits administered with or without Puerarin （ P〈0.05 ）.Conclusion Puerarin shows significant impact on the pharmacokinetics of glipizide.

关 键 词：葛根素 格列吡嗪 相互作用 糖尿病家兔 代谢 

分 类 号：R977.1[医药卫生—药品]