通过与柠檬酸形成盐共晶来改善盐酸小檗碱的固态性质。
Improving solid-state properties of berberine chloride through forming a salt cocrystal with citric acid.
机构信息
School of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai 201620, China.
Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, University of Minnesota, Minneapolis, MN 55455, United States.
出版信息
Int J Pharm. 2019 Jan 10;554:14-20. doi: 10.1016/j.ijpharm.2018.10.062. Epub 2018 Oct 29.
Berberine 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.
盐酸小檗碱（BCl）可以无水物、一水物、二水物和四水物的形式存在。因此，当盐酸小檗碱片在制造和储存过程中环境湿度发生变化时，它会面临着依赖湿度的固相反 应问题。我们发现了盐酸小檗碱和柠檬酸（BCl-CA）之间形成的新的 1:1 共晶物，其在保持相似的热稳定性、溶解度、溶解速率和可压性的同时，对湿度变化表现出更好的稳定性。因此，BCl-CA 是一种替代晶体形式，可用于制造盐酸小檗碱片的配方。
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