Silybin Cocrystals with Improved Solubility and Bioavailability
文献类型：期刊论文
| 作者 | Zhu, Bingqing; Ding, Zhenfeng; Rong, Xiaoyi; Li, Shengqiang; Mei, Xuefeng
|
| 刊名 | PHARMACEUTICALS
 |
| 出版日期 | 2025 |
| 卷号 | 18期号:1页码:11 |
| 关键词 | silybin cocrystal solubility bioavailability L-proline |
| DOI | 10.3390/ph18010090 |
| 通讯作者 | Mei, Xuefeng(xuefengmei@simm.ac.cn) |
| 英文摘要 | Backgroud/Objectives: Silymarin, an extract from milk thistle, is widely recognized for its therapeutic potential in treating liver disorders. However, its clinical utility is limited by the poor solubility and low bioavailability of its key active ingredient, Silybin. In this study, we sought to address this issue through the development of a novel cocrystal of Silyin. Methods: Silybin-L-proline cocrystal was synthesized and the physicochemical properties of the cocrystal were characterized by PXRD, TGA, DSC, and FTIR. Dissolution tests were conducted in various pH solutions, and the impact of precipitation inhibitors was evaluated. Furthermore, pharmacokinetic study in rats were performed to assess the bioavailability. Results: The dissolution studies demonstrated that the cocrystal has a significant improvement in dissolution performance, particularly in acidic environments. Furthermore, the use of precipitation inhibitors, such as PVP, prolonged the supersaturation period for adequate absorption. Pharmacokinetic studies in rats revealed that the cocrystal exhibited a 16-fold increase in bioavailability compared to the raw Silybin extract, outperforming the commercial Silybin-phosphatidylcholine complex. Conclusions: The Silybin-L-proline cocrystal significantly enhances dissolution and bioavailability, indicating its potential to improve the therapeutic efficacy of Silybin in clinical applications. |
| WOS关键词 | SILYMARIN ; SILIBININ ; DRUG |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:001403846600001 |
| 出版者 | MDPI |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/315935]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Mei, Xuefeng |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhu, Bingqing,Ding, Zhenfeng,Rong, Xiaoyi,et al. Silybin Cocrystals with Improved Solubility and Bioavailability[J]. PHARMACEUTICALS,2025,18(1):11. |
| APA | Zhu, Bingqing,Ding, Zhenfeng,Rong, Xiaoyi,Li, Shengqiang,&Mei, Xuefeng.(2025).Silybin Cocrystals with Improved Solubility and Bioavailability.PHARMACEUTICALS,18(1),11. |
| MLA | Zhu, Bingqing,et al."Silybin Cocrystals with Improved Solubility and Bioavailability".PHARMACEUTICALS 18.1(2025):11. |
入库方式： OAI收割
来源：上海药物研究所
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