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载体的固态和物理性质在肺部递药用黏附混合物中的作用。

The role of the solid state and physical properties of the carrier in adhesive mixtures for lung delivery.

机构信息

a Food and Drug Department , University of Parma , Parma , Italy.

出版信息

Expert Opin Drug Deliv. 2018 Jul;15(7):665-674. doi: 10.1080/17425247.2017.1371132. Epub 2017 Aug 28.

Abstract

Direct administration of drugs to the lung is commonly used for the treatment of local respiratory diseases, but it can also be employed to obtain a systemic effect. Besides the advantages offered in terms of higher therapeutic efficacy, this administration route raised specific drug delivery issues. In fact, to obtain a suitable bioavailability and therapeutic effect, the drug has to be efficiently deposited in the lower airways. Formulation is required to render the drug respirable. Area covered: The present paper deals with dry powders formulations, in particular it reviews the literature of the last two decades with respect to the role of the solid-state characteristics of the excipients used as carriers in adhesive mixture toward respirability of the active ingredient. Expert opinion: Many of the literature data on this topic are still not completely understood and sometimes they appear contradictory despite the intent to be complementary. More accurate and sensitive analytical methods for solid state characterization both for the drug and the carrier as well as a more systematic approach for the evaluation of the energetics of the carrier vs the drug surface is foreseen as a useful way to address some of the issues still opened in this field.

摘要

药物直接递送至肺部通常用于治疗局部呼吸道疾病,但也可用于获得全身疗效。除了在更高的治疗效果方面提供的优势外,这种给药途径还提出了特定的药物输送问题。事实上,为了获得合适的生物利用度和治疗效果,药物必须有效地沉积在下呼吸道中。需要制剂来使药物可吸入。涵盖范围:本文涉及干粉制剂,特别是它回顾了过去二十年关于用作载体的赋形剂的固体状态特性在活性成分的可吸入性方面对粘性混合物的作用的文献。专家意见:尽管意图是互补的,但关于这个主题的许多文献数据仍然没有被完全理解,有时它们看起来是矛盾的。对于药物和载体的固体状态特性,以及对于载体与药物表面的能量的更系统的评估方法的更准确和敏感的分析方法,预计将是解决该领域中仍然存在的一些问题的有用方法。

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