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利用双螺杆制粒机实现含西甲硅油和盐酸洛哌丁胺的液固分散体片的连续生产

Towards the Continuous Manufacturing of Liquisolid Tablets Containing Simethicone and Loperamide Hydrochloride with the Use of a Twin-Screw Granulator.

作者信息

Zakowiecki Daniel, Richter Margarethe, Yuece Ceren, Voelp Annika, Ries Maximilian, Papaioannou Markos, Edinger Peter, Hess Tobias, Mojsiewicz-Pieńkowska Krystyna, Cal Krzysztof

机构信息

Chemische Fabrik Budenheim KG, Rheinstrasse 27, 55257 Budenheim, Germany.

Thermo Electron (Karlsruhe) GmbH, Pfannkuchstrasse 10-12, 76185 Karlsruhe, Germany.

出版信息

Pharmaceutics. 2023 Apr 18;15(4):1265. doi: 10.3390/pharmaceutics15041265.

Abstract

Continuous manufacturing is becoming the new technological standard in the pharmaceutical industry. In this work, a twin-screw processor was employed for the continuous production of liquisolid tablets containing either simethicone or a combination of simethicone with loperamide hydrochloride. Both active ingredients present major technological challenges, as simethicone is a liquid, oily substance, and loperamide hydrochloride was used in a very small amount (0.27% /). Despite these difficulties, the use of porous tribasic calcium phosphate as a carrier and the adjustment of the settings of the twin-screw processor enabled the optimization of the characteristics of the liquid-loaded powders and made it possible to efficiently produce liquisolid tablets with advantages in physical and functional properties. The application of chemical imaging by means of Raman spectroscopy allowed for the visualization of differences in the distribution of individual components of the formulations. This proved to be a very effective tool for identifying the optimum technology to produce a drug product.

摘要

连续制造正成为制药行业的新技术标准。在这项工作中,采用双螺杆处理器连续生产含有西甲硅油或西甲硅油与盐酸洛哌丁胺组合的液固分散体片。两种活性成分都带来了重大的技术挑战,因为西甲硅油是一种液体油性物质,且盐酸洛哌丁胺的用量非常少(0.27%)。尽管存在这些困难,但使用多孔磷酸三钙作为载体并调整双螺杆处理器的设置,能够优化载液粉末的特性,并使得高效生产在物理和功能性质方面具有优势的液固分散体片成为可能。通过拉曼光谱进行化学成像的应用能够可视化制剂中各个成分分布的差异。这被证明是确定生产药品的最佳工艺的非常有效的工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f48e/10142538/09bf5c7c5cd3/pharmaceutics-15-01265-g001.jpg

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