Rucaparib cocrystal: Improved solubility and bioavailability over camsylate
文献类型：期刊论文
| 作者 | Xia, Mengyuan1,2; Jiang, Yihua1,2; Cheng, Yinxiang1,2; Dai, Wenjuan1; Rong, Xiaoyi1; Zhu, Bingqing1; Mei, Xuefeng1,2
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| 刊名 | INTERNATIONAL JOURNAL OF PHARMACEUTICS
 |
| 出版日期 | 2023-01-25 |
| 卷号 | 631页码:10 |
| 关键词 | Rucaparib Cocrystal Solubility Dissolution Bioavailability |
| ISSN号 | 0378-5173 |
| DOI | 10.1016/j.ijpharm.2022.122461 |
| 通讯作者 | Zhu, Bingqing(zhubingq@simm.ac.cn) ; Mei, Xuefeng(xuefengmei@simm.ac.cn) |
| 英文摘要 | Rucaparib (Ruc) is a drug used to treat advanced ovarian cancer associated with deleterious BRCA mutations. Its commercial form, the camsylate salt (Ruc-Cam), suffers from poor aqueous solubility and thus causes low and erratic oral bioavailability. In this work, we aimed to improve the oral exposure of Ruc through cocrystallization. Liquid-assisted grinding, slurry, and solvent evaporation methods were employed to prepare new solid forms of Ruc. Cocrystals of rucaparib-theophylline monohydrate (Ruc-Thp MH), rucaparib-maltol (Ruc-Mal), and rucaparib-ethyl maltol (Ruc-Emal) were obtained. Powder X-ray diffraction, Fourier transform infrared spec-troscopy, thermogravimetric analysis, differential scanning calorimetry, and dynamic vapor sorption were uti-lized to characterize these multi-component systems. All cocrystals dissolve faster than Ruc-Cam at pH 2.0 and 4.5, and Ruc-Thp MH displays the highest apparent solubility in pH 4.5 and 6.8 buffers. Pharmacokinetic studies in rats show that Ruc-Thp MH exhibits 2.4 times the Cmax and 1.4 times the AUC0-24h at a single dose compared with Ruc-Cam. The enhanced solubility and bioavailability of Ruc-Thp MH showcase the power of cocrystalli-zation in addressing absorption issues in drug development. |
| WOS关键词 | OVARIAN-CANCER ; PERMEABILITY ; SALT |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000903863800002 |
| 出版者 | ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/303543]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhu, Bingqing; Mei, Xuefeng |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xia, Mengyuan,Jiang, Yihua,Cheng, Yinxiang,et al. Rucaparib cocrystal: Improved solubility and bioavailability over camsylate[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2023,631:10. |
| APA | Xia, Mengyuan.,Jiang, Yihua.,Cheng, Yinxiang.,Dai, Wenjuan.,Rong, Xiaoyi.,...&Mei, Xuefeng.(2023).Rucaparib cocrystal: Improved solubility and bioavailability over camsylate.INTERNATIONAL JOURNAL OF PHARMACEUTICS,631,10. |
| MLA | Xia, Mengyuan,et al."Rucaparib cocrystal: Improved solubility and bioavailability over camsylate".INTERNATIONAL JOURNAL OF PHARMACEUTICS 631(2023):10. |
入库方式： OAI收割
来源：上海药物研究所
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