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柠檬酸:一种多功能药用辅料。

Citric Acid: A Multifunctional Pharmaceutical Excipient.

作者信息

Lambros Maria, Tran Thac Henry, Fei Qinqin, Nicolaou Mike

机构信息

Department of Pharmaceutical Sciences, College of Pharmacy, Western University of Health Sciences, 309 E Second Street, Pomona, CA 91766, USA.

Doric Pharma LLC, 5270 California Ave, Suite 300, Irvine, CA 92617, USA.

出版信息

Pharmaceutics. 2022 Apr 30;14(5):972. doi: 10.3390/pharmaceutics14050972.

Abstract

Citric acid, a tricarboxylic acid, has found wide application in the chemical and pharmaceutical industry due to its biocompatibility, versatility, and green, environmentally friendly chemistry. This review emphasizes the pharmaceutical uses of citric acid as a strategic ingredient in drug formulation while focusing on the impact of its physicochemical properties. The functionality of citric acid is due to its three carboxylic groups and one hydroxyl group. These allow it to be used in many ways, including its ability to be used as a crosslinker to form biodegradable polymers and as a co-former in co-amorphous and co-crystal applications. This paper also analyzes the effect of citric acid in physiological processes and how this effect can be used to enhance the attributes of pharmaceutical preparations, as well as providing a critical discussion on the issues that may arise out of the presence of citric acid in formulations.

摘要

柠檬酸作为一种三羧酸,因其生物相容性、多功能性以及绿色环保的化学性质,在化学和制药行业有着广泛的应用。本综述着重阐述了柠檬酸作为药物制剂中的一种关键成分的药用价值,同时关注其物理化学性质所产生的影响。柠檬酸的功能归因于其三个羧基和一个羟基。这些基团使其能够以多种方式被使用,包括用作交联剂以形成可生物降解的聚合物,以及在共无定形和共晶体应用中作为共形成剂。本文还分析了柠檬酸在生理过程中的作用,以及如何利用这种作用来增强药物制剂的特性,并对制剂中存在柠檬酸可能引发的问题进行了批判性讨论。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8215/9148065/01cd547b142d/pharmaceutics-14-00972-g001.jpg

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