Abstract：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.
平丽, 洪雅雯, 朱狄峰. 酒石酸阿福特罗大鼠肺内药动学研究[J]. 中国药学杂志, 2020, 55(17): 1456-1459.
PING Li, HONG Ya-wen, ZHU Di-feng. Pharmacokinetic Study of Arformoterol Tartrate in Rat Lungs. Chinese Pharmaceutical Journal, 2020, 55(17): 1456-1459.
CHEN L F, GONG J, GU M H, et al. Antibiotic use among chronic obstructive pulmonary disease inpatients with acute exacerbation in Pudong New Area:a pharmacoepidemiologic study[J]. Chin J Public Health(中国公共卫生), 2018, 34(5):771-773.
[2]
DONG H, ZHANG H B, LYU Z J, et al. Effects of long-term oral low-dose of azithromycin on pulmonary function and clinical signs of patientswith stable COPD: a systematic review[J]. J China Pharm(中国药房), 2017, 28(21):2951-2954.
[3]
YAO L J, LIU Y. Protective effects of salidroside on chronic obstructive pulmonary disease in mice[J]. Chin Pharm J (中国药学杂志), 2017, 52 (17):1515-1518.
[4]
KHARIDIA J, FOGARTY C M, LAFORCE C F, et al. A pharmacokinetic/pharmacodynamic study comparing arformoterol tartrate inhalation solution and racemic formoterol dry powder inhaler in subjects with chronic obstructive pulmonarydisease[J]. Pulm Pharmacol Ther, 2008, 21(4):657-662.
[5]
HANANIA N A, DONOHUE J F, NELSON H, et al. The safety and efficacy of arformoterol and formoterol in COPD[J]. J Chronic Obstruct Pulmon Dis, 2010, 7(1):17-31.
[6]
PAHWA R, SONI V, SHARMA P C, et al. Arformoterol tartrate:areview of pharmacologyanalysis and clinical studies[J]. Trop J Pharm Res, 2010, 9(6):595-603.
[7]
MIAO X,DU P Y,ZHANG Z Z,et al. Determination of arformoterol in arformoterol dry powder inhalation by HPLC[J]. West China J Pharm Sci(华西药学杂志), 2011, 26(3):284-285.
[8]
ZHUYY,PING L,TIAN W F.Pharmacokinetic profile of cefoselis sulfate in mice brain[J]. Chin Pharm J (中国药学杂志), 2014, 49 (1):61-63.
[9]
DENG Y, CAI H L, HE G X, et al. LC-MS/MS method for the simultaneous quantitative analysis of dihydromyricetin and myricetin in mice plasma and its application to a tissue distribution study[J]. Chin Pharm J (中国药学杂志), 2016, 51 (23):2053-2058.
[10]
SUN C L, HE J M, WU H B, et al. A rapid and sensitive UPLC-MS/MS method for quantitative determination of arformoterol in rat plasma, lung and tracheatissues[J]. Chin Chem Lett(中国化学快报英文版), 2018, 29(8):1284-1286.
2020, Vol. 55 
