کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10162117 | 1114317 | 2015 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Isostructurality Among Solvates of Cabazitaxel: X-ray Structures and New Solvates Preparation
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Cabazitaxel is an anticancer drug and its marketed product (form A) is acetone solvate (1:1) (Didier E, Perrin MA. 2005. Patent WO2005/028462 A1). This work describes three crystal structures of cabazitaxel 1:1 solvates with isopropyl alcohol (B), 2-butanol (C), and dioxane (D). These solvates are isostructural with cabazitaxel forming a host framework through hydrogen bonds and the guest solvent molecules located in channels from which they can escape. The host is hydrogen bonded to each other through hydroxyl O1 and sec-amide N3â², whereas the hydroxyl O2â² plays an important role in connecting the host to the guest. Moreover, because of the existence of channels in the crystal structure, the solvent-replacement method was established to prepare four new solvates of cabazitaxel with dimethyl formamide (E), cyclohexane (F), n-hexane (G), and ethyl ether (H). All the seven solvates involved in this work were proven to be isostructural by methods of X-ray crystallography and contain the same amount of solvents by thermogravimetric analysis. The single-crystal structures of solvate C-E and the solvates prepared by solvent-replacement method have been reported for the first time.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 104, Issue 4, April 2015, Pages 1256-1262
Journal: Journal of Pharmaceutical Sciences - Volume 104, Issue 4, April 2015, Pages 1256-1262
نویسندگان
Wei Xu, Ningbo Gong, Shiying Yang, Na Zhang, Lan He, Guanhua Du, Yang Lu,