Conformational polymorphs of isotretinoin and their impact on physicochemical and biological properties
文献类型：期刊论文
| 作者 | Cheng, Yinxiang1,2; Rong, Xiaoyi1; Xia, Mengyuan1,2; Zhang, Zaiyong1; Wang, Jian-Rong1 ; Mei, Xuefeng1,2
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| 刊名 | INTERNATIONAL JOURNAL OF PHARMACEUTICS
 |
| 出版日期 | 2021-12-15 |
| 卷号 | 610页码:10 |
| 关键词 | Polymorph Isotretinoin Stability Solubility Bioavailability |
| ISSN号 | 0378-5173 |
| DOI | 10.1016/j.ijpharm.2021.121222 |
| 通讯作者 | Wang, Jian-Rong(jrwang@simm.ac.cn) ; Mei, Xuefeng(xuefengmei@simm.ac.cn) |
| 英文摘要 | Isotretinoin is the first-line drug for treatment of severe acne. Only one polymorph was reported even though it has been launched for nearly 40 years, and its clinic application was however limited by its stability and solubility challenges. In our study, two new polymorphs of isotretinoin were discovered and fully characterized. The transformation relationships between these solid forms were fully discussed, and a visible color change during single-crystal-to-single-crystal phase transition with the conformational change was investigated. Form II is determined to be thermodynamic stable form at room temperature, but metastable form at body temperature. The results show that form II is an ideal solid state possessing both superior thermal stability (60celcius, open air) and higher absorption once delivered into body. The thermal stability can be associated with the crystal structure such as torsion angle. The relative bioavailability of form II is higher than form I as expected, and the bioavailability of form II formulation is about 2 times as that of the marketed form I capsule. Therefore, form II formulation could provide an alternative for better performing isotretinoin. |
| WOS关键词 | RETINOIC ACID ; CRYSTAL-STRUCTURE ; CIS-STILBENE ; PHOTOISOMERIZATION ; ISOMERIZATION ; CHEMISTRY ; TRETINOIN ; ACNE |
| 资助项目 | Shanghai Science and Technology Innovation Action Plan[20142201800] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000718950500008 |
| 出版者 | ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/299030]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Wang, Jian-Rong; Mei, Xuefeng |
| 作者单位 | 1.Chinese Acad Sci, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai Inst Mat Med, 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 | Cheng, Yinxiang,Rong, Xiaoyi,Xia, Mengyuan,et al. Conformational polymorphs of isotretinoin and their impact on physicochemical and biological properties[J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS,2021,610:10. |
| APA | Cheng, Yinxiang,Rong, Xiaoyi,Xia, Mengyuan,Zhang, Zaiyong,Wang, Jian-Rong,&Mei, Xuefeng.(2021).Conformational polymorphs of isotretinoin and their impact on physicochemical and biological properties.INTERNATIONAL JOURNAL OF PHARMACEUTICS,610,10. |
| MLA | Cheng, Yinxiang,et al."Conformational polymorphs of isotretinoin and their impact on physicochemical and biological properties".INTERNATIONAL JOURNAL OF PHARMACEUTICS 610(2021):10. |
入库方式： OAI收割
来源：上海药物研究所
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