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用于盐酸普萘洛尔控释的多糖微粒的制剂与评价

Formulation and Evaluation of Polysaccharide Microparticles for the Controlled Release of Propranolol Hydrochloride.

作者信息

Stojmenovski Aneta, Gatarić Biljana, Vučen Sonja, Railić Maja, Krstonošić Veljko, Kukobat Radovan, Mirjanić Maja, Škrbić Ranko, Račić Anđelka

机构信息

Centre for Biomedical Research, Faculty of Medicine, University of Banja Luka, Save Mrkalja 16, 78000 Banja Luka, Bosnia and Herzegovina.

Department of Pharmacy, Faculty of Medicine, University of Banja Luka, Save Mrkalja 14, 78000 Banja Luka, Bosnia and Herzegovina.

出版信息

Pharmaceutics. 2024 Jun 11;16(6):788. doi: 10.3390/pharmaceutics16060788.

DOI:10.3390/pharmaceutics16060788
PMID:38931909
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11207763/
Abstract

Propranolol hydrochloride, a non-cardio-selective beta blocker, is used to treat several conditions in children, including hypertension, arrhythmias, hyperthyroidism, hemangiomas, etc. Commercial liquid formulations are available in Europe and the US, but they have disadvantages, such as limited stability, bitter taste, and the need for multiple daily doses due to the drug's short half-life. Considering these limitations, controlled-release solid formulations, such as microparticles, may offer a better solution for pediatric administration. The main objective of this study was to formulate an encapsulation system for propranolol hydrochloride, based on sodium alginate and other polysaccharide polymers, to control and prolong its release. Microparticles were prepared using the ionotropic gelation method, which involves instilling a polymer solution into a solution of gelling ions via the extrusion technique. Physicochemical characterization was conducted by assessing the entrapment efficiency, drug loading, swelling index, microparticle size, rheological properties, and surface tension. In order to improve the characteristics of the tested microparticles, selected formulations were coated with chitosan. Further experimental work included differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) analysis, and SEM imaging. This in vitro release study showed that chitosan-coated microparticles demonstrate favorable properties, suggesting a novel approach to formulating pediatric dosage forms, although further optimization is necessary.

摘要

盐酸普萘洛尔是一种非心脏选择性β受体阻滞剂,用于治疗儿童的多种病症,包括高血压、心律失常、甲状腺功能亢进、血管瘤等。欧洲和美国有市售液体制剂,但它们存在缺点,如稳定性有限、味道苦涩,且由于药物半衰期短需要每日多次给药。考虑到这些局限性,控释固体制剂,如微粒,可能为儿科给药提供更好的解决方案。本研究的主要目的是基于海藻酸钠和其他多糖聚合物制备一种盐酸普萘洛尔的包封系统,以控制并延长其释放。微粒采用离子凝胶法制备,该方法通过挤压技术将聚合物溶液滴入胶凝离子溶液中。通过评估包封率、载药量、溶胀指数、微粒大小、流变学性质和表面张力进行理化表征。为了改善测试微粒的特性,对选定的制剂用壳聚糖进行包衣。进一步的实验工作包括差示扫描量热法(DSC)、傅里叶变换红外(FTIR)分析和扫描电子显微镜(SEM)成像。这项体外释放研究表明,壳聚糖包衣微粒表现出良好的性能,提示了一种新型的儿科剂型制备方法,不过仍需进一步优化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/db2bd097240d/pharmaceutics-16-00788-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/b8eede1b9ce6/pharmaceutics-16-00788-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/7e903fc6bc31/pharmaceutics-16-00788-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/1389a4c157d0/pharmaceutics-16-00788-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/c9208b074ccd/pharmaceutics-16-00788-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/6b892fb32c43/pharmaceutics-16-00788-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/fb14ee00a107/pharmaceutics-16-00788-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/db2bd097240d/pharmaceutics-16-00788-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/b8eede1b9ce6/pharmaceutics-16-00788-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/7e903fc6bc31/pharmaceutics-16-00788-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/1389a4c157d0/pharmaceutics-16-00788-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/c9208b074ccd/pharmaceutics-16-00788-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/6b892fb32c43/pharmaceutics-16-00788-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/fb14ee00a107/pharmaceutics-16-00788-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/35df/11207763/db2bd097240d/pharmaceutics-16-00788-g007.jpg

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