含氯法辛的吸入式微粒在治疗实验性小鼠结核病方面是有效的。
Inhaled microparticles containing clofazimine are efficacious in treatment of experimental tuberculosis in mice.
机构信息
Pharmaceutics Division, CSIR-Central Drug Research Institute, Lucknow, India.
出版信息
Antimicrob Agents Chemother. 2013 Feb;57(2):1050-2. doi: 10.1128/AAC.01897-12. Epub 2012 Nov 26.
Abstract
Inhalable clofazimine-containing dry powder microparticles (CFM-DPI) and native clofazimine (CFM) were evaluated for activity against Mycobacterium tuberculosis in human monocyte-derived macrophage cultures and in mice infected with a low-dose aerosol. Both formulations resulted in 99% killing at 2.5 μg/ml in vitro. In mice, 480 μg and 720 μg CFM-DPI inhaled twice per week over 4 weeks reduced numbers of CFU in the lung by as much as log(10) 2.6; 500 μg oral CFM achieved a log(10) 0.7 reduction.
摘要
可吸入氯法齐明载药干粉微球（CFM-DPI）和天然氯法齐明（CFM）在人单核细胞来源的巨噬细胞培养物中和感染低剂量气溶胶的小鼠中均被评估了对结核分枝杆菌的活性。这两种制剂在体外均以 2.5μg/ml 的浓度达到了 99%的杀灭率。在小鼠中，每周两次吸入 480μg 和 720μg 的 CFM-DPI 持续 4 周，可使肺部 CFU 数量减少多达 2.6 个对数；500μg 口服 CFM 可使对数减少 0.7。
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