Salt Cocrystallization-A Method to Improve Solubility and Bioavailability of Dihydromyricetin.

IF 5.5 3区医学 Q1 PHARMACOLOGY & PHARMACY

Pharmaceutics Pub Date : 2025-09-17 DOI:10.3390/pharmaceutics17091209

Jingping Li, Xinke Chen, Yanan Liu, Caiwu Jiang

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引用次数: 0

Abstract

Objectives: This study aimed to find salts with similar pharmacological effects designed as cocrystals to improve the aqueous solubility and bioavailability of dihydromyricetin (DMY). Methods: A salt-cocrystal solvate (DMY-CIP·C₂H₆O) of dihydromyricetin and ciprofloxacin hydrochloride (CIP) was successfully prepared via solvent evaporation method, and further characterized using powder X-ray diffraction, thermal analysis, and infrared spectroscopy. The solubility, stability, bioavailability, and in vitro antimicrobial efficacy of the cocrystal were also studied. Results: The cocrystal could increase the solubility of DMY in water and greatly improve the absorption of DMY in vivo (8-fold enhancement in relative bioavailability). In addition, the in vitro antimicrobial efficacy of the cocrystal was comparable to that of CIP, which is a great improvement for DMY. However, due to the formation of cocrystals with salts, the humidity stability of DMY is reduced and it should not be stored in high-humidity environments. Conclusions: These findings demonstrate that cocrystallization with water-soluble salts represents an effective strategy for optimizing the pharmaceutical properties of poorly soluble compounds.

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盐共结晶——提高二氢杨梅素溶解度和生物利用度的方法。

目的：寻找具有相似药理作用的盐类共晶设计，以提高二氢杨梅素（DMY）的水溶性和生物利用度。方法：采用溶剂蒸发法制备了二氢杨梅素和盐酸环丙沙星（CIP）的盐-共晶溶剂化物（DMY-CIP·c2h60），并用粉末x射线衍射、热分析和红外光谱对其进行了表征。研究了该共晶的溶解度、稳定性、生物利用度和体外抗菌效果。结果：该共晶提高了DMY在水中的溶解度，大大提高了DMY在体内的吸收（相对生物利用度提高8倍）。此外，共晶的体外抗菌效果与CIP相当，这对DMY来说是一个很大的改进。但由于与盐形成共晶，降低了DMY的湿度稳定性，不宜存放在高湿环境中。结论：这些发现表明，与水溶性盐共结晶是优化难溶性化合物的有效策略。

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来源期刊

Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

CiteScore

7.90

自引率

11.10%

发文量

2379

审稿时长

16.41 days

期刊介绍： Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications, and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.