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

 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20～640μg·L^-1之间呈良好的线性关系，其最低检测极限为20μg·L^-1，平均回收率为(99.85士3.20)%。黄连素单用制剂组，在家兔体内:其最高血药浓度c_max为92.7μg·L^-1，t_peak为0.63 h,AUCo-_∞为491.7μg·L^-1·h^-1在人体内:其最高血药浓度。c_max为394.7μg·L^-1，t_peak为2.37h，AUCo-_∞为3028.3μg·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c_peak为210.8μg·L^-1，t_peak为0.65 h，AUCo-_∞为1105.4g·L^-1·h^-1在人体内:其最高血药浓度。c_max为534.2μg·L^-1，t_peak为2.45 h，AUCo-_∞为4136.9g·L^-1·h。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AUCo-值具有显著差别(P<0.05)，而其它的体内动力学行为基本一致。

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

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_testRESULTS:It was found that Ber in serum was linear over the range of 20640 μg·L^-1The detection limit was 20 μg·L^-1 The mean rate of recovery was (9985±320)% After a single oral dosage of Ber,the pharmacokinetic parameters in rabbits were:c_max 927 μg·L^-1，t_peak 0.63h,AUC_0-∞ 4917 μg·L^-1·h^-1 respectively In healthy volunteers; its c_max 3947 μg·L^-1，t_peak 237 h,AUC_0-∞ 30283 μg·L^-1·h^-1respectively When it was coadministrated with oryzanol in rabbits,the c_max2108 μg·L^-1,t_peak0.65 h,AUC_0-∞110? 54 g·L^-1·h^-1respectively; in healthy volunteers:the c_max 53421 μg·L^-1，t_peak2.45 h,AUC_0-∞413?69 g·L^-1·h^-1respectively 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.