Delivery of theophylline as dry powder for inhalation  

作　　者：Bing Zhu Mehra Haghi Anphy Nguyen Mary Goud Stewart Yeung Paul MYoung Daniela Traini 

机构地区：[1]Respiratory Technology,TheWoolcock Institute for Medical Research and Discipline of Pharmacology,Sydney Medical School,University of Sydney,NSW 2006,Australia [2]Faculty of Pharmacy,University of Technology Sydney,NSW 2007,Australia [3]Avans University of Applied Science,Breda,The Netherlands

出　　处：《Asian Journal of Pharmaceutical Sciences》2015年第6期520-527,共8页亚洲药物制剂科学（英文）

基　　金：Professor Young is the recipient of an Australian Research Council Future Fellowship(project number FT110100996);Associate Professor Traini is the recipient of an Australian Research Council Future Fellowship(project number FT12010063).

摘　　要：Theophylline(TP)is a very well established orally or intravenously delivered antiasthma drug with many beneficial effects.This study aims to improve asthma treatment by creating a dry powder inhalable(DPI)formulation of TP to be delivered directly to the lung,avoiding the side effects associated with conventional oral delivery.The DPI TP formulation was investigated for its physico-chemical characteristics using scanning electron microscopy,laser diffraction,thermal analysis and dynamic vapour sorption.Furthermore,aerosol performance was assessed using the Multi Stage Liquid Impinger(MSLI).In addition,a Calu-3 cell transport assay was conducted in vitro using a modified ACI to study the impact of the DPI formulation on lung epithelial cells.Results showed DPI TP to be physico-chemically stable and of an aerodynamic size suitable for lung delivery.The aerosolisation performance analysis showed the TP DPI formulation to have a fine particle fraction of 29.70±2.59%(P<0.05)for the TP formulation containing 1.0%(w/w)sodium stearate,the most efficient for aerosolisation.Regarding the deposition of TP DPI on Calu-3 cells using the modified ACI,results demonstrated that 56.14±7.62%of the total TP deposited(13.07±1.69μg)was transported across the Calu-3 monolayer over 180 min following deposition,while 37.05±12.62%of the deposited TP was retained in the cells.This could be due to the presence of sodium stearate in the current formulation that increased its lipophilicity.A DPI formulation of TP was developed that was shown to be suitable for inhalation.

关 键 词：THEOPHYLLINE Powder formulation Aerosol performance Physiochemical characteristics 

分 类 号：R74[医药卫生—神经病学与精神病学]