中国临床药理学杂志2016，Vol.32Issue(1)：36-38,3.DOI:10.13699/j.cnki.1001-6821.2016.01.012
噻托溴铵吸入粉雾剂在大鼠体内的药代动力学研究
Pharmacokinetic study of dry powder inhalation of tiotropium bromide in rats
高文超 1李军袖 1张晴 1徐佳秋 1邢晗 1李宁 1陈西敬 1赵娣1
作者信息
- 1. 中国药科大学 药物代谢动力学研究中心,南京 210009
- 折叠
摘要
Abstract
Objective To demonstrate the better process for the prepa-ration of dry powder inhalation via investigation of the influence of formu-lation composition and preparing technique on the disposition of tiotro-pium bromide (TIO) in rats.Methods Lung samples and broncho -alveolar lavage ( BAL ) of pre -anesthetized rats were collected at different time points after intratracheal inhalation of two dry powder inha-lation formulation at single dose ( active parmaceutical ingredient content , 6 mg· kg -1 ) and the drug concentration was determined by LC -MS/MS. The pharmacokinetic parameters were calculated based on the special two-compartmental model established by WinNonlin ? 6.1 pharmacoki-netic program and compared by One -way ANOVA and t-test.Results Jet milling ( JF ) and spray dry ( SF ) formulation indicated respectively that Cmax was (4551.69 ±1731) ng· g -1 and (2403.09 ±1096) ng· g -1 , which exhibited significant difference between the two group ( P<0.05 );MRT was ( 2.45 ±23.1 ) h-1 and ( 1.97 ±17.2 ) h-1; AUC0-8h was (9778.55 ±869) ng· h· g-1 and (4769.40 ±995) ng· h· g-1, which exhibited significant difference ( P<0.05).Conclusion The JF exhibited a more prolonged retention time , which may appropriate to be industria-lized in the manufacture of clinically used products .关键词
噻托溴铵/吸入粉雾剂/肺组织/药代动力学Key words
tiotropium bromide/dry powder inhalation/lung tissue/pharmacokinetics分类
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高文超,李军袖,张晴,徐佳秋,邢晗,李宁,陈西敬,赵娣..噻托溴铵吸入粉雾剂在大鼠体内的药代动力学研究[J].中国临床药理学杂志,2016,32(1):36-38,3.
