黄连素单用及合用谷维素在家兔及健康志愿者体内的药代动力学研究  

Study on the pharmacokinetics of berberine in single dosage and coadministration with oryzanol in rabbits and healthy volunteers

作　　者：李宝馨[1] 杨宝峰[1] 郝晓敏[1] 周虹[1] 孙明智[2] 

机构地区：[1]哈尔滨医科大学药理教研室,哈尔滨150086 [2]哈尔滨医科大学生理教研室

出　　处：《中国药学杂志》2000年第1期33-35,共3页Chinese Pharmaceutical Journal

基　　金：黑龙江省自然科学基金!No .95 10

摘　　要：目的 :研究黄连素单用及与谷维素伍用在家兔和健康志愿者体内的药代动力学。方法 :反相高效液相色谱法 ,紫外检测。用 3P87程序软件处理数据 ,用t检验法进行显著性检验。结果 :在此色谱条件下 ,黄连素在 2 0～ 64 0 μg·L-1之间呈良好的线性关系 ,其最低检测极限为 2 0 μg·L-1,平均回收率为 (99 85± 3 2 0 ) %。黄连素单用制剂组 ,在家兔体内 :其最高血药浓度cmax为 92 7μg·L-1,tpeak为 0 63h ,AUC0 -∞ 为 4 91 7μg·L-1·h-1;在人体内 :其最高血药浓度cmax为 3 94 7μg·L-1,tpeak为2 3 7h ,AUC0 -∞ 为 3 0 2 8 3 μg·L-1·h-1。黄连素与谷维素合用制剂组 ,在家兔体内 :其最高血药浓度cmax为 2 10 8μg·L-1,tpeak为 0 65h ,AUC0 -∞ 为 110 5 4 g·L-1·h-1;在人体内 :其最高血药浓度cmax为 5 3 4 2 μg·L-1,tpeak为 2 4 5h ,AUC0 -∞ 为4 13 6 9g·L-1·h-1。两组体内的血药浓度 时间曲线无论在家兔及人体均符合一室开放模型。结论 :无论在家兔及人体 ,黄连素与谷维素合用比黄连素单用吸收好 ,说明谷维素可促进黄连素吸收 ,两组之间的AUC0 -∞ 值具有显著差别 (P <0 0 5 ) ,而其它的体内动力学行为基本一致。OBJECTIVE: To study the pharmacokinetics of berberine (Ber) in single dosage and coadministration with oryzanol in rabbits and healthy volunteers METHOD: Ber in serum was determined by RP HPLC with UV detector The concentration time data were fitted using 3P87 Pharmacokinetic Program and the pharmacokinetic parameters were compared by paried t test RESULTS: It was found that Ber in serum was linear over the range of 20 640 μg·L -1 The detection limit was 20 μg·L -1 The mean rate of recovery was (99 85±3 20)% After a single oral dosage of Ber, the pharmacokinetic parameters in rabbits were: c max 92 7 μg·L -1 , t peak 0 63 h, AUC 0-∞ 491 7 μg·L -1 ·h -1 respectively In healthy volunteers; its c max 394 7 μg·L -1 , t peak 2 37 h, AUC 0-∞ 3028 3 μg·L -1 ·h -1 respectively When it was coadministrated with oryzanol in rabbits, the c max 210 8 μg·L -1 , t peak 0 65 h, AUC 0-∞ 110?5 4 g·L -1 ·h -1 respectively; in healthy volunteers: the c max 534 21 μg·L -1 , t peak 2 45 h, AUC 0-∞ 413?6 9 g·L -1 ·h -1 respectively The concentration time curves of the two groups fitted one compartment model either in rabbits or in healthy volunteers CONCLUSION: Oryzanol could affect the absorption of Ber, the AUC value between single dosage and coadministration had significant difference ( P <0 05), but other pharmacokinetic parameters had not significant difference

关 键 词：黄连素 谷维素 药代动力学 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学]