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Int J Pharm. 2019 Jan 10;554:14-20. doi: 10.1016/j.ijpharm.2018.10.062. Epub 2018 Oct 29.

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

Author information

1
School of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai 201620, China.
2
Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, University of Minnesota, Minneapolis, MN 55455, United States.
3
School of Chemistry and Chemical Engineering, Tianjin University of Technology, Tianjin 300384, China.
4
School of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai 201620, China. Electronic address: liushuyu@sues.edu.cn.
5
Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, University of Minnesota, Minneapolis, MN 55455, United States. Electronic address: sunx0053@umn.edu.

Abstract

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.

KEYWORDS:

Berberine; Citric acid; Cocrystallization; Stability

PMID:
30385378
DOI:
10.1016/j.ijpharm.2018.10.062
[Indexed for MEDLINE]

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