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药物制剂中活性成分雷尼替丁与粘土矿物辅料之间的相互作用。

Interactions between Active Ingredient Ranitidine and Clay Mineral Excipients in Pharmaceutical Formulations.

作者信息

Wang Lijuan, Wang Xisen, Liao Libing, Wu Qingfeng, Yin Hui, Li Zhaohui

机构信息

Beijing Key Laboratory of Materials Utilization of Nonmetallic Minerals and Solid Wastes, National Laboratory of Mineral Materials, School of Materials Science and Technology, China University of Geosciences, 29 Xueyuan Road, Beijing 100083, China.

Chemistry Department, University of Wisconsin-Parkside, Kenosha, WI 53144, USA.

出版信息

Materials (Basel). 2020 Dec 6;13(23):5558. doi: 10.3390/ma13235558.

Abstract

Excipients play an important role in pharmaceutical formulations. Many clay minerals, because of their large specific surface area and inert behaviour in reactions with active ingredients, are commonly used as excipients. In this study, the uptake of ranitidine (RT), the active ingredient of Zantac, on and released from palygorskite (Pal), kaolinite (Kao), and talc was evaluated under different physicochemical conditions. The results showed that the uptake of RT on these minerals was limited to the external surface areas only. Cation exchange and electrostatic interactions were responsible for the RT uptake on Pal and Kao, resulting in a monolayer sorption. In contrast, multilayer RT uptake was found on the talc surfaces. Under different desorbing conditions, significant amounts of sorbed RT remained on the solid surface after 5 h of desorption. The results suggest that the sorptive interactions between the active ingredients and the excipients may not be neglected in pharmaceutical formulations, should these minerals be used as additives and/or excipients.

摘要

辅料在药物制剂中起着重要作用。许多粘土矿物由于其大的比表面积以及在与活性成分反应中的惰性,常被用作辅料。在本研究中,在不同的物理化学条件下,评估了雷尼替丁(RT,善胃得的活性成分)在坡缕石(Pal)、高岭土(Kao)和滑石上的吸附及从其上的释放情况。结果表明,RT在这些矿物上的吸附仅限于外表面区域。阳离子交换和静电相互作用导致RT在Pal和Kao上的吸附,形成单层吸附。相比之下,在滑石表面发现了多层RT吸附。在不同的解吸条件下,解吸5小时后,大量吸附的RT仍留在固体表面。结果表明,在药物制剂中,如果将这些矿物用作添加剂和/或辅料,活性成分与辅料之间的吸附相互作用可能不可忽视。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ad63/7730526/a83647680d76/materials-13-05558-g001.jpg

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