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Inhalable dry powders of rifampicin highlighting potential and drawbacks in formulation development for experimental tuberculosis aerosol therapy.
Expert Opinion on Drug Delivery ( IF 6.6 ) Pub Date : 2020-02-04 , DOI: 10.1080/17425247.2020.1720644
Kai Berkenfeld 1 , Jason T McConville 1, 2 , Alf Lamprecht 1, 2
Affiliation  

Introduction: 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.Areas covered: 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.Expert opinion: 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 in vitro models to assess the efficacy, therapeutic benefit, and cost-effectiveness of the candidate formulations.

中文翻译:

利福平的可吸入干粉突出了实验性肺气雾剂治疗制剂开发的潜力和弊端。

简介:最近,有报道称结核病是单一传染病致死的主要原因。标准疗法包括在至少26周内施用四种一线抗生素,即利福平,异烟肼,乙胺丁醇和吡嗪酰胺,在利福平的情况下,通常会伴有不良副作用和可变的生物利用度,从而损害积极的治疗结果。由于感染的主要部位是肺部,因此需要开发一种通过肺部途径给药的治疗性制剂。研究范围:这项工作为研究可吸入性干粉制剂(包括利福平)的研究提供了文献综述结核病治疗,特别关注气溶胶性能。专家意见:已经发现涉及不同策略和功能性赋形剂的制剂方法正在研究中,但是到目前为止,还没有制剂能够成功进入商业临床测试。造成这种情况的原因可能主要与缺乏合适的候选物有关,而在其他方面则缺乏评估候选物制剂的功效,治疗益处和成本效益的合适的体外模型。
更新日期:2020-03-22
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