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研究不同等级的磷酸钙基药用辅料的 pH 值依赖性溶解度。

Studies on the pH-Dependent Solubility of Various Grades of Calcium Phosphate-based Pharmaceutical Excipients.

机构信息

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

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

出版信息

J Pharm Sci. 2022 Jun;111(6):1749-1760. doi: 10.1016/j.xphs.2021.12.005. Epub 2021 Dec 7.

DOI:10.1016/j.xphs.2021.12.005
PMID:34890630
Abstract

Calcium phosphate-based pharmaceutical excipients, including calcium hydrogen phosphate anhydrous and dihydrate, calcium hydroxide phosphate have been well established in pharmaceutical technology for a very long time. Nowadays, they are of increasing interest to the pharmaceutical industry because, in addition to their advanced functional properties, they offer beneficial biocompatible and biodegradable properties. Yet, there is limited availability of embracing information regarding the solubility of these popular excipients, especially in variable pH conditions, reflecting those of the gastrointestinal tract (GIT). The study has shown that the solubility of calcium phosphates as well as their dissolution rate decreases significantly with increasing pH of dissolution fluids. The highest solubility was observed for dibasic calcium phosphate dihydrate, the lowest for tribasic calcium phosphate. This article provides also a comparison of various calcium phosphate types originating from different manufacturers, which may prove to be useful and help formulation scientists to design new medicinal products.

摘要

钙磷酸盐类药用辅料,包括无水和二水合磷酸氢钙、磷酸氢钙,在制药技术中已经有很长时间的应用历史。如今,它们越来越受到制药行业的关注,因为除了具有先进的功能特性外,它们还具有有益的生物相容性和可生物降解性。然而,关于这些流行辅料的溶解度信息,尤其是在可变 pH 值条件下(反映胃肠道(GIT)的 pH 值条件)的溶解度信息,可获取的信息有限。研究表明,钙磷酸盐的溶解度及其溶解速率随着溶解液 pH 值的增加而显著降低。二水合磷酸氢钙二水合物的溶解度最高,三磷酸钙的溶解度最低。本文还比较了来自不同制造商的各种钙磷酸盐类型,这可能证明是有用的,并帮助制剂科学家设计新的药物产品。

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