中国临床药理学杂志
中國臨床藥理學雜誌
중국림상약이학잡지
THE CHINESE JOURNAL OF CLINICAL PHARMACOLOGY
2014年
7期
623-625
,共3页
周鹏%厉世笑%陈芳芳%孙渊%夏爱晓%杜有功
週鵬%厲世笑%陳芳芳%孫淵%夏愛曉%杜有功
주붕%려세소%진방방%손연%하애효%두유공
葛根素%格列吡嗪%相互作用%糖尿病家兔%代谢
葛根素%格列吡嗪%相互作用%糖尿病傢兔%代謝
갈근소%격렬필진%상호작용%당뇨병가토%대사
Puerarin%glipizide%inteaction%diabetes mellitas rabbit%metabolism
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。
目的:研究葛根素在健康和糖尿病傢兔體內對格列吡嗪膠囊代謝的影響。方法健康新西蘭傢兔隨機分組:健康組和糖尿病組(各5隻),每隻傢兔口服格列吡嗪5 mg。經2週清洗期後,于傢兔耳緣靜脈註射葛根素(18 mg· kg-1),每天1次,持續3 d,第4天口服相同劑量格列吡嗪。在給藥前與給藥後,經耳緣靜脈採血,用HPLC法測定各時間點格列吡嗪的血藥濃度,用DAS2.0進行麯線擬閤。結果格列吡嗪在傢兔體內的藥代動力學符閤單室模型,健康組給予葛根素前後藥代動力學參數,t1/2分彆為(4.2±0.5),(3.58±0.7) h,ρmax分彆為(15.5±0.8),(8.4±0.6) mg· L-1,AUC0-35分彆為(134.8±0.7),(77.2±1.4) mg· h· L-1;糖尿病組給予葛根素前後藥代動力學參數,t1/2分彆為(7.6±0.9),(5.6±0.9) h,ρmax分彆為(13.4±0.8),(10.6±0.9) mg· L-1,AUC0-35分彆為(10.5±0.8),(7.7±1.6) mg· h· L-1。給予葛根素前後,格列吡嗪的t1/2、ρmax、AUC差異均有統計學意義(P<0.05)。結論葛根素對傢兔體內格列吡嗪的藥代動力學有明顯的影響。
목적:연구갈근소재건강화당뇨병가토체내대격렬필진효낭대사적영향。방법건강신서란가토수궤분조:건강조화당뇨병조(각5지),매지가토구복격렬필진5 mg。경2주청세기후,우가토이연정맥주사갈근소(18 mg· kg-1),매천1차,지속3 d,제4천구복상동제량격렬필진。재급약전여급약후,경이연정맥채혈,용HPLC법측정각시간점격렬필진적혈약농도,용DAS2.0진행곡선의합。결과격렬필진재가토체내적약대동역학부합단실모형,건강조급여갈근소전후약대동역학삼수,t1/2분별위(4.2±0.5),(3.58±0.7) h,ρmax분별위(15.5±0.8),(8.4±0.6) mg· L-1,AUC0-35분별위(134.8±0.7),(77.2±1.4) mg· h· L-1;당뇨병조급여갈근소전후약대동역학삼수,t1/2분별위(7.6±0.9),(5.6±0.9) h,ρmax분별위(13.4±0.8),(10.6±0.9) mg· L-1,AUC0-35분별위(10.5±0.8),(7.7±1.6) mg· h· L-1。급여갈근소전후,격렬필진적t1/2、ρmax、AUC차이균유통계학의의(P<0.05)。결론갈근소대가토체내격렬필진적약대동역학유명현적영향。
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.