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乙醇对含盐酸环丙沙星的干粉吸入制剂的习性和空气动力学结果的影响。

The effect of ethanol on the habit and aerodynamic results of dry powder inhalation formulations containing ciprofloxacin hydrochloride.

作者信息

Benke Edit, Winter Christina, Szabó-Révész Piroska, Roblegg Eva, Ambrus Rita

机构信息

Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Szeged H-6720, Hungary.

Institute of Pharmaceutical Sciences, Pharmaceutical Technology and Biopharmacy, University of Graz, Universitätsplatz 1, Graz A-8010, Austria.

出版信息

Asian J Pharm Sci. 2021 Jul;16(4):471-482. doi: 10.1016/j.ajps.2021.04.003. Epub 2021 May 28.

Abstract

In the case of dry powder inhalation systems (DPIs), the development of carrier-free formulations has gained increased attention. Thereby, spray-drying is a promising technology and is widely used to produce carrier-free DPIs. Numerous works have been published about the co-spray-drying of active ingredients with various solid excipients and their effect on the physicochemical characteristics and aerodynamic properties of the formulations. However, only a few studies have been reported about the role of the solvents used in the stock solutions of spray-dried formulations. In the present work, DPI microcomposites containing ciprofloxacin hydrochloride were prepared by spray-drying in the presence of different ethanol concentrations. The work expresses the roughness, depth and width of the dimples for particle size as a novel calculation possibility, and as a correlation between the MMAD/D ratio and correlating it with cohesion work, these new terms and correlations have not been published - to the best of our knowledge - which has resulted in gap-filling findings. As a result, different proportions of solvent mixtures could be interpreted and placed in a new perspective, in which the influence of different concentrations of ethanol on the habit of the DPI formulations, and thus on aerodynamic results. Based on these, it became clear why we obtained the best aerodynamic results for DPI formulation containing 30% ethanol in the stock solution.

摘要

在干粉吸入系统(DPI)的情况下,无载体制剂的开发受到了越来越多的关注。因此,喷雾干燥是一项很有前景的技术,被广泛用于生产无载体DPI。关于活性成分与各种固体辅料的共喷雾干燥及其对制剂物理化学特性和空气动力学性质的影响,已经发表了大量的研究成果。然而,关于喷雾干燥制剂储备溶液中所用溶剂的作用,仅有少数研究报道。在本研究中,通过在不同乙醇浓度存在下进行喷雾干燥,制备了含盐酸环丙沙星的DPI微复合材料。这项工作提出了将粒径凹坑的粗糙度、深度和宽度作为一种新的计算可能性,并将MMAD/D比值与内聚功相关联,据我们所知,这些新术语和相关性尚未发表,从而填补了空白。结果,不同比例的溶剂混合物可以得到解释,并从一个新的角度进行分析,其中不同浓度乙醇对DPI制剂习性的影响,进而对空气动力学结果的影响。基于这些,就清楚了为什么我们在储备溶液中含30%乙醇的DPI制剂获得了最佳的空气动力学结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f74e/8520052/8a716c7549d5/fx1.jpg

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