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作 者:谭朝丹[1] 马越鸣[1] 石荣[1] 陈莹蓉[1]
机构地区:[1]上海中医药大学中药药代动力学实验室,上海201203
出 处:《中成药》2011年第7期1153-1158,共6页Chinese Traditional Patent Medicine
基 金:上海高校创新团队建设项目(2009)
摘 要:目的研究黄芩对甲苯磺丁脲药动学的影响。方法大鼠12只,雌雄各半,随机分为两组,生理盐水组(NS组)和黄芩组(HQ组)。分别灌服生理盐水和等体积的黄芩水提物,0.5 h后灌胃给予甲苯磺丁脲50 mg/kg。采用HPLC-UV法检测甲苯磺丁脲及其代谢产物4-羟基甲苯磺丁脲的血浆浓度,计算药代动力学参数。结果在雌性大鼠体内,NS组中甲苯磺丁脲及其代谢产物4-羟基甲苯磺丁脲的AUC0-t分别为(1 760±82)μg/(mL.h)和(18±2)μg/(mL.h),HQ组中分别为(2 360±298)μg/(mL.h)和(25±4)μg/(mL.h),即给予黄芩后,甲苯磺丁脲的AUC0-t升高约34.1%(P<0.05);而甲苯磺丁脲的t1/2以及AUC0-t(甲苯磺丁脲)/AUC0-t(4-羟基甲苯磺丁脲)比值,无论雌雄,NS组和HQ组间的差异无统计学意义。结论黄芩可提高雌性大鼠体内甲苯磺丁脲的总体暴露水平。AIM To investigate the influence of Scutellaria baicalensis on the pharmacokinetics of tolbutamide in rats.METHODS Twelve rats of either sex were randomly divided into two groups,NS group(pretreated with 0.9% saline solution) and HQ group(pretreated with the aqueous extracts of Scutellaria baicalensis).After the pretreatment,each group was treated with a single oral administration of tolbutamide 50 mg/kg.The plasma concentrations of tolbutamide and 4-hydroxytolbutamide were measured by HPLC-UV,and then pharmacokinetic parameters were determined from the plasma concentration-time data.RESULTS In the female rats,AUC0-t of tolbutamide and 4-hydroxytolbutamide were(1 760±82) and(18±2) μg/(mL·h) in NS group and(2 360±298) and(25±4) μg/(mL·h) in HQ group,respectively.Compared with NS group,Scutellaria baicalensis increased AUC0-t of tolbutamide by nearly 34.1%(P〈0.05).However,in male and female rats there was no significant difference in the t1/2 of tolbutamide and AUC0-t ratio of tolbutamide to 4-hydroxytolbutamide between NS group and HQ group.CONCLUSION Scutellaria baicalensis may increase the overall exposure of tolbutamide in female rats.
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