酒石酸阿福特罗大鼠肺内药动学研究  

Pharmacokinetic Study of Arformoterol Tartrate in Rat Lungs

作　　者：平丽[1] 洪雅雯 朱狄峰[1] PING Li;HONG Ya-wen;ZHU Di-feng(Center for Drug Safety Evaluation and Research,Zhejiang University,Hangzhou 310058,China)

机构地区：[1]浙江大学药物安全评价研究中心,杭州310058

出　　处：《中国药学杂志》2020年第17期1456-1459,共4页Chinese Pharmaceutical Journal

基　　金：浙江省科技厅项目资助(2017C33139)。

摘　　要：目的建立测定大鼠肺脏中酒石酸阿福特罗含量的LC-MS/MS方法,研究酒石酸阿福特罗在大鼠肺脏内的药动学特征。方法SD大鼠雾化给予酒石酸阿福特罗吸入溶液,不同时间点取大鼠肺脏组织并以LC-MS/MS测定肺脏内药物含量,采用DAS3.0软件处理,计算药动学参数并进行统计学分析。结果大鼠肺脏中酒石酸阿福特罗的主要药动学参数t1/2为15.55 h,cmax为16.48 ng·g-1,AUC0-t为48.41 ng·h·g-1,MRT0-t为5.45 h。结论大鼠雾化给予酒石酸阿福特罗吸入溶液后,在肺脏内分布快,半衰期较长,并能维持一段时间,提示酒石酸阿福特罗雾化给药能有效用于治疗慢性阻塞性肺疾病。OBJECTIVE To establish an LC-MS/MS method for the determination of arformoterol tartrate in rat lungs and study the pharmacokinetics of arformoterol tartrate in rat lungs.METHODS Lung samples were collected at different time points after SD rats were given nebulized infusion solution of arformoterol tartrate.An LC-MS/MS method was established and validated to analyze the drug concentrations,and pharmacokinetic parameters were calculated by professional software named DAS3.0 pharmacokinetic program.RESULTS The main pharmacokinetic parameters of arformoterol tartrate in the lungs of rats were as follows:t1/2 was 15.55 h,cmax was 16.48 ng·g-1,AUC0-t was 48.41 ng·h·g-1,and MRT0-t was 5.45 h.CONCLUSION After aerosolization of arformoterol tartrate inhalation solution,the drugis rapidly distributed in the lung,has a long half-life and can be maintained for a certain period of time,suggesting that atomized administration of arformoterol tartrate can be used for the treatment of chronic obstructive pulmonary disease.

关 键 词：酒石酸阿福特罗 肺脏组织 药动学 

分 类 号：R965.3[医药卫生—药理学]