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| Solvent optimization and in vitro dissolution evaluation of baicalein-theophylline cocrystal |
| Hits 1448 Download times 842 Received:October 20, 2019 |
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| DOI
10.11656/j.issn.1672-1519.2020.01.20 |
| Key Words
baicalein;theophylline;cocrystal;ternary phase diagram;dissolution rate |
| Author Name | Affiliation | E-mail | | ZHANG Ying | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | PI Jiaxin | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | pijiaxin@tjutcm.edu.cn | | LI Wen | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | | | LIU Zhidong | Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-Established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China | lonerliuzd@163.com |
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| Abstract
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| [Objective] To optimize the solvent in the preparation of baicalein-theophylline cocrystal and investigate its dissolution behavior in vitro.[Methods] By determining the solubility of baicalein-theophylline cocrystal in theophylline-ethyl acetate,theophylline-methanol and theophylline-acetone solutions,the ternary phase diagram of the baicalein-theophylline-solvent system was drawn to screen the solvent in preparation process. The in vitro dissolution rate of the cocrystal was evaluated by using the simulated intestinal fluid (SIF) and the simulated gastric fluid (SGF) as the dissolution medium.[Results] The area of cocrystal conformation in acetone solution system was larger than that of ethyl acetate and methanol. Thus,baicalein-theophylline cocrystal was obtained by acetone co-solvent method. The dissolution rate of baicalein in SIF and SGF was 1.38 fold and 2.02 fold than that of raw material,and was 1.27 fold and 1.80 fold than that of physical mixture,respectively. The cocrystal in both media has a certain sustained release effect on theophylline.[Conclusion] The formation of cocrystal could promote the in vitro dissolution rate of the poorly soluble component baicalein,and also reduce the dissolution rate of theophylline,which provides evidences for further research and clinical application of baicalein-theophylline cocrystal. |
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