Improving solid-state properties of berberine chloride through forming a salt cocrystal with citric acid

Publication date: Available online 29 October 2018Source: International Journal of PharmaceuticsAuthor(s): Qi Lu, Jiangnan Dun, Jia-Mei Chen, Shuyu Liu, Changquan Calvin SunAbstractBerberine chloride (BCl) can exist as an anhydrate, monohydrate, dihydrate, and tetrahydrate. Therefore, it faces the problem of humidity dependent solid phase change when environmental humidity varies during manufacturing and storage of berberine tablets. We have discovered a new 1:1 cocrystal formed between berberine chloride and citric acid (BCl–CA) that exhibits better stability against variations in humidity while maintaining similar thermal stability, solubility, dissolution rate, and tabletability. Thus, BCl–CA is a good alternative crystal form for use in formulation to manufacture berberine tablets.Graphical abstract
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research