Polymorphism of the 5R-5-hydroxytriptolide
文献类型：期刊论文
| 作者 | Liu Ruili; Yang Yaxi ; Chen Dongying
|
| 刊名 | Acta Pharmaceutica Sinica
 |
| 出版日期 | 2011 |
| 卷号 | 46期号:11页码:1357-1360 |
| 关键词 | 5R-5-hydroxytriptolide crystalline polymorph preparation crystalline polymorph characterization drug candidate stability |
| ISSN号 | 0513-4870 |
| 其他题名 | 5R-5-羟基雷公藤内酯醇的晶型制备与表征 |
| 文献子类 | Article |
| 英文摘要 | 5R-5-hydroxytriptolide(LLDT-8)is a new drug candidate which is in clinical trial treating rheumatoid arthritis.Polymorph screening of the compound was carried out in this study.Polymorph of LLDT-8 was prepared by evaporative crystallization and antisolvent crystallization methods and was characterized by powder X-ray diffraction(p-XRD), infrared spectrometry(IR), differential scanning calorimetry(DSC)and thermogravimetric analysis(TG).It was found that p-XRD patterns, DSC curves, TG curves and IR spectra of the LLDT-8 samples prepared by the above recrystallization methods were all consistent.The 2thetaof main peaks in the p-XRD patterns appeared at 7.58°, 8.14°, 8.66°, 15.46°, 16.46°, 29.54°, 31.16°and 38.26°, while the infrared absorption peaks appeared at 3471.3, 2962.2, 2887.0, 1762.6, 1677.8, 1432.9, 1365.4, 1247.7, 1080.0, 1031.7 and 877.5 cm~(-1).LLDT-8 was decomposed at 271.2℃based on the determination from DSC and TG.It was showed in single crystal X-ray diffraction study that LLDT-8 crystal was monoclinic with the space group being P2(1).The cell parameters were found to be: a=11.4601(11), b=6.3205(6), c=13.0281(12), alpha=90.00, beta=115.557(2)andgamma=90.00.The crystal was a hydrogen-bonded dimmer.The slurry experiments, which were further conducted in solvents with different polarities, confirmed the stability of solid state of LLDT-8 based on the p-XRD determination.The polymorph of LLDT-8 made assurance of its efficacy consistence during its clinical trials. |
| 资助项目 | 新药研究国家重点实验室资助项目[00000000] ; 国家科技重大专项重大新药创制课题综合性大平台资助项目[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:4347777 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/267909]  |
| 专题 | 药物质量控制与固体化学研究中心 |
| 通讯作者 | Chen Dongying |
| 作者单位 | Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. |
| 推荐引用方式 GB/T 7714 | Liu Ruili,Yang Yaxi,Chen Dongying. Polymorphism of the 5R-5-hydroxytriptolide[J]. Acta Pharmaceutica Sinica,2011,46(11):1357-1360. |
| APA | Liu Ruili,Yang Yaxi,&Chen Dongying.(2011).Polymorphism of the 5R-5-hydroxytriptolide.Acta Pharmaceutica Sinica,46(11),1357-1360. |
| MLA | Liu Ruili,et al."Polymorphism of the 5R-5-hydroxytriptolide".Acta Pharmaceutica Sinica 46.11(2011):1357-1360. |
入库方式： OAI收割
来源：上海药物研究所
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