tailieunhanh - Báo cáo y học: " In vitro metabolism of beclomethasone dipropionate, budesonide, ciclesonide, and fluticasone propionate in human lung precision-cut tissue slices"

Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học 'Respiratory Research cung cấp cho các bạn kiến thức về ngành y đề tài: " In vitro metabolism of beclomethasone dipropionate, budesonide, ciclesonide, and fluticasone propionate in human lung precision-cut tissue slices. | Respiratory Research BioMed Central Open Access In vitro metabolism of beclomethasone dipropionate budesonide ciclesonide and fluticasone propionate in human lung precision-cut tissue slices Ruediger Nave 1 Robyn Fisher2 and Nigel McCracken1 Address 1DMPK Nycomed GmbH Konstanz Germany and 2Vitron Inc. Tucson Arizona USA Email Ruediger Nave - Robyn Fisher - robyn@ Nigel McCracken - Corresponding author Published 20 September 2007 Received 27 March 2007 Accepted 20 September 2007 Respiratory Research 2007 8 65 doi 1465-9921 -8-65 This article is available from http content 8 1 65 2007 Nave et al licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License http licenses by which permits unrestricted use distribution and reproduction in any medium provided the original work is properly cited. Abstract Background The therapeutic effect of inhaled corticosteroids ICS may be affected by the metabolism of the drug in the target organ. We investigated the in vitro metabolism of beclomethasone dipropionate BDP budesonide BUD ciclesonide CIC and fluticasone propionate FP in human lung precision-cut tissue slices. CIC a new generation ICS is hydrolyzed by esterases in the upper and lower airways to its pharmacologically active metabolite desisobutyryl-ciclesonide des-CIC . Methods Lung tissue slices were incubated with BDP BUD CIC and FP initial target concentration of 25 pM for 2 6 and 24 h. Cellular viability was assessed using adenosine 5 -triphosphate content and protein synthesis in lung slices. Metabolites and remaining parent compounds in the tissue samples were analyzed by HPLC with UV detection. Results BDP was hydrolyzed to the pharmacologically active metabolite beclomethasone-17-monopropionate BMP and predominantly to inactive beclomethasone BOH . CIC was hydrolyzed initially