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枳壳对丁螺环酮在健康大鼠体内药物动力学的影响
作者姓名:姚佳梅  邱新建  黄惠勇  赵琳琳  王文波  周露  王胜  陈琼  胡随瑜
作者单位:中南大学湘雅医院老年病科, 湖南 长沙 410008;湖南中医药大学中医诊断研究所, 湖南 长沙 410208;中南大学湘雅医院中西医结合研究所, 湖南 长沙 410008;湖南中医药大学中医诊断研究所, 湖南 长沙 410208;中南大学湘雅医院中西医结合研究所, 湖南 长沙 410008;中南大学湘雅医院中西医结合研究所, 湖南 长沙 410008;中南大学湘雅医院中西医结合研究所, 湖南 长沙 410008;中南大学湘雅医院中西医结合研究所, 湖南 长沙 410008;中南大学湘雅医院老年病科, 湖南 长沙 410008;中南大学湘雅医院中西医结合研究所, 湖南 长沙 410008
基金项目:国家中医药管理局全国名老中医药专家胡随瑜传承工作室建设项目(国中医药人教发[2014]20号);国家自然科学基金青年基金资助项目(81202807);中国博士后科学基金第57批面上资助项目(2015M572254)
摘    要:目的 研究枳壳对丁螺环酮在健康大鼠体内药物动力学的影响。方法 将SD大鼠随机分为丁螺环酮组,丁螺环酮加枳壳低剂量组(15 g/kg),丁螺环酮加枳壳高剂量组(30 g/kg),测定给药后5、10、20、30、45、60、90、120、240、360、480、600 min丁螺环酮的血药浓度,计算并比较其药动学参数。结果 与丁螺环酮组比较,丁螺环酮加枳壳低剂量组和高剂量组中丁螺环酮AUC(0-t)分别增加2.49和4.18倍,Cmax分别增加1.63和2.57倍,Tmax从0.28 h分别延长至0.52和1.06 h,t1/2从0.96 h分别延长至2.18和4.87 h,差异具有统计学意义(P<0.05)。结论 枳壳可增加同服药物丁螺环酮的AUC(0-t)和Cmax,提高丁螺环酮生物利用度,并有剂量依赖性趋势,枳壳与丁螺环酮发生显著的药动学相互作用。

关 键 词:枳壳  丁螺环酮  药物动力学  药动学相互作用
收稿时间:2016/6/29 0:00:00

Effects of Fructus aurantii on Pharmacokinetics of Buspirone in Healthy Rats
Authors:YAO Jiamei  QIU Xinjian  HUANG Huiyong  ZHAO Linlin  WANG Wenbo  ZHOU Lu  WANG Sheng  CHEN Qiong and HU Suiyu
Institution:Department of Gerontology, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China;Institute of TCM Diagnostics, Hunan University of Chinese medicine, Changsha, Hunan 410007, China;Institute of Integrated Traditional Chinese and Western Medicine, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China;Institute of TCM Diagnostics, Hunan University of Chinese medicine, Changsha, Hunan 410007, China;Institute of Integrated Traditional Chinese and Western Medicine, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China;Institute of Integrated Traditional Chinese and Western Medicine, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China;Institute of Integrated Traditional Chinese and Western Medicine, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China;Institute of Integrated Traditional Chinese and Western Medicine, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China;Department of Gerontology, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China;Institute of Integrated Traditional Chinese and Western Medicine, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China
Abstract:Objective To investigate the effect of Fructus aurantii on the pharmacokinetics of buspirone in healthy rats.Methods SD rats were randomly divided into buspirone group,the low dose group of Fructus aurantii (15 g/kg) plus buspirone,and the high dose group of Fructus aurantii (30 g/kg) plus buspirone,respectively.The blood concentrations of buspirone were determined after 5,10,20,30,45,60,90,120,240,360,480,600 min and their pharmacokinetic parameters were calculated.Results Compared with the buspirone group,the AUC(0-t) of the low dose group and high dose group were increased by 2.49 and 4.18 time and the Cmax were increased by 1.63 and 2.57 time,respectively.The Tmax of the low dose group and high dose group were extended from 0.28 h to 0.52 h and 1.06 h and the t1/2 were extended from 0.96 h to 2.18 h and 4.87 h,respectively.The differences were statistically significant (P<0.05).Conclusion Fructus aurantii can increase the AUC(0-t) and Cmax of buspirone,improve the bioavailability of buspirone,and the changs of parameters show the dependence trendency.Fructus aurantii and buspirone have significant pharmacokinetic interactions.
Keywords:Fructus aurantii  buspirone  pharmacokinetics  pharmacokinetic interactions
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