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[摘要]
目的 探讨金芪降糖片中黄连、黄芪和金银花配伍对主要活性成分小檗碱体内药动学的影响。方法 雄性SD大鼠分别单次ig金芪降糖片(0.42 g/kg,相当于5 mg/kg盐酸小檗碱)、盐酸小檗碱(5 mg/kg)+绿原酸(3 mg/kg)及盐酸小檗碱(5 mg/kg),采用LC-MS/MS法检测不同时间点血浆中盐酸小檗碱的血药浓度,并采用非房室模型、统计矩法计算盐酸小檗碱在大鼠体内的药动学参数。结果 各组MRT0~∞、tmax及t1/2无显著变化;盐酸小檗碱组AUC0~∞及Cmax最大,绿原酸与盐酸小檗碱合用组AUC0-∞及Cmax最小,但其CLz和Vz显著高于其他2组(其他2组无显著变化)。结论 绿原酸与小檗碱合用可以降低小檗碱的体内吸收、促进小檗碱的血浆清除及体内分布。黄芪、金银花与黄连配伍可能对小檗碱的血浆消除与体内分布存在相反的影响。
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[Abstract]
Objective To study the effects of Jinqi Jiangtang Tablet (JQJT) in compatibility on the pharmacokinetics of berberine hydrochloride (BH) in rats.Methods Male SD rats were ig administered with JQJT (0.42 g/kg,equivalently 5 mg/kg BH),BH (5 mg/kg)+chlorogenic acid (CA,3 mg/kg),and BH (5 mg/kg),respectively.The plasma concentration at indicated time points were determined by LC-MS/MS method after the drug administrations.The pharmacokinetic parameters of BH were calculated with DAS 3.0 software using non-compartmental model.Results After the drug administration,no significant change was found for the MRT0~∞,tmax,and t1/2 values of BH,whereas the AUC0~∞ and Cmax values of BH were in the order of BH group >JQJT group >BH+CA group,and the CLz and Vz values of BH were in the order of BH+CA group >JQJT group≈BH group.Conclusion The pharmacokinetic results indicate that the co-administration of BH+CA decreases the absorpation,while increases the plasma clearance and distribution of BH in rats.Additionally,the results also suggest that the compatibility of astragalus root or honeysuckle with Coptidis Rhizoma is likely to produce the opposite effect on the plasma elimination and distribution of BH in vivo in rats.
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