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利福平吸入干粉制剂突出了实验性肺结核气溶胶治疗制剂开发的潜力和缺陷。

Inhalable dry powders of rifampicin highlighting potential and drawbacks in formulation development for experimental tuberculosis aerosol therapy.

机构信息

Department of Pharmaceutics, Institute of Pharmacy, Rheinische Friedrich-Wilhelms-Universität, Bonn, Germany.

Department of Pharmaceutical Sciences, College of Pharmacy, University of New Mexico, Albuquerque, NM, USA.

出版信息

Expert Opin Drug Deliv. 2020 Mar;17(3):305-322. doi: 10.1080/17425247.2020.1720644. Epub 2020 Feb 4.

DOI:10.1080/17425247.2020.1720644
PMID:32017637
Abstract

: Recently, tuberculosis was reported as the leading cause of death from a single infectious agent. Standard therapy includes administration of four first-line antibiotics, i.e. rifampicin, isoniazid, ethambutol, and pyrazinamide over a period of at least 26 weeks, which in case of rifampicin oftentimes is accompanied by unwanted side effects and variable bioavailability that compromise a positive therapeutic outcome. As the main site of infection is the lungs, it is desirable to develop a therapeutic formulation to be administered via the pulmonary route.: This work presents a literature review on studies investigating inhalable dry powder formulations including rifampicin in the context of an experimental tuberculosis therapy, with a special focus on aerosol performance.: It was found that formulation approaches involving different strategies and functional excipients are under investigation but as of now, no formulation has managed to leap into commercial clinical testing. Reasons for this might not primarily be associated with a lack of suitable candidates, but amongst others a lack of suitable models to assess the efficacy, therapeutic benefit, and cost-effectiveness of the candidate formulations.

摘要

: 最近,结核病被报道为单一传染病原体导致死亡的主要原因。标准治疗包括在至少 26 周的时间内使用四种一线抗生素,即利福平、异烟肼、乙胺丁醇和吡嗪酰胺,而利福平常常伴有不良副作用和可变的生物利用度,从而影响治疗效果。由于感染的主要部位是肺部,因此理想的治疗方法是开发一种通过肺部给药的治疗制剂。: 本工作对研究可吸入干粉制剂的文献进行了综述,这些制剂包括利福平在实验性结核病治疗中的应用,特别关注了气溶胶性能。: 结果发现,涉及不同策略和功能赋形剂的制剂方法正在研究中,但到目前为止,还没有一种制剂能够进入商业临床测试。其原因可能主要不是缺乏合适的候选药物,而是缺乏合适的模型来评估候选制剂的疗效、治疗效果和成本效益。

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