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Delivery of theophylline as dry powder for inhalation 被引量:1
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作者 Bing Zhu Mehra Haghi +4 位作者 Anphy Nguyen Mary Goud Stewart Yeung Paul MYoung Daniela Traini 《Asian Journal of Pharmaceutical Sciences》 SCIE CAS 2015年第6期520-527,共8页
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 ... 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. 展开更多
关键词 THEOPHYLLINE powder formulation Aerosol performance Physiochemical characteristics
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基于高凝集素亲和性载体的抗生素吸入粉雾剂用于高效治疗细菌生物膜相关肺部感染
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作者 周钥 黄嘉元 +9 位作者 王冠林 翟紫照 Maizbha Uddin Ahmed 夏晓 刘岑峰 金玉珍 潘昕 黄莹 吴传斌 张雪娟 《Science Bulletin》 SCIE EI CAS CSCD 2023年第24期3225-3239,M0006,共16页
多重耐药细菌引发的肺部感染对人类健康构成了严重威胁.细菌生物膜加剧了肺部感染的持续和复发,限制了抗生素的可及性和有效性.基于凝集素竞争策略和颗粒表面修饰策略,本研究设计了一种硫酸多粘菌素B(PMBS)的吸入粉雾剂(DPI)用于治疗肺... 多重耐药细菌引发的肺部感染对人类健康构成了严重威胁.细菌生物膜加剧了肺部感染的持续和复发,限制了抗生素的可及性和有效性.基于凝集素竞争策略和颗粒表面修饰策略,本研究设计了一种硫酸多粘菌素B(PMBS)的吸入粉雾剂(DPI)用于治疗肺部感染.该制剂的载体是具有高凝集素亲和性(HLA)的小分子糖(如棉子糖),可靶向细菌凝集素,限制生物膜的扩展.该制剂的粒径约为3μm,其表面褶皱程度和药物与载体的比例有关.处方F_(5)(PMBS:棉子糖=10:90)表现出最高的微细粒子分数(FPF=64.86%),表明其具备显著增强的肺部药物递送效率.通过添加棉子糖,制剂在抑制生物膜形成和清除成熟生物膜方面的效果显著提高.在急性和慢性肺部感染的大鼠模型中,相较于喷雾干燥的PMBS,处方F_(5)表现出更强的抗菌效果,并引起更低炎症反应.综上,基于HLA载体的抗生素DPI具有治疗细菌生物膜相关肺部感染的良好前景. 展开更多
关键词 Pulmonary infections Polymyxin B Dry powder formulation BIOFILM High-lectin-affinity sugar
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