کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2485038 | 1114343 | 2013 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Small Molecule, Big Difference: The Role of Water in the Crystallization of Paclitaxel
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
Paclitaxel is an important antineoplastic drug, which is used widely in the treatment of many forms of cancer. The crystal structures of the anhydrous form and the hemihydrate were determined from laboratory X-ray powder diffraction data, whereas the dihydrate was solved from single-crystal synchrotron diffraction data. Intermolecular spaces allow for the inclusion of loosely bound water molecules, which are then lost easily upon heating. All three forms were found to crystallize in the orthorhombic spacegroup P212121, with Zâ² = 2. The unit cell parameters were found to be a = 9.6530(3) Ã
, b = 28.1196(8) Ã
, c = 33.5378(14) Ã
, and V = 9103.5(5) Ã
for the anhydrous form (363 K); a = 9.6890(2) Ã
, b = 28.0760(4) Ã
, c = 33.6166(8) Ã
, and V = 9144.7(3) Ã
3 for the hemihydrate (333 K); and a = 9.512(6) Ã
, b = 28.064(16) Ã
, c = 33.08(2) Ã
, and V = 8829.0(9) Ã
3 for the dihydrate (120 K). Water loss occurs in two steps between 120 K ⤠t ⤠363 K. The thermal stability of the hydrates and accompanying unit cell changes were observed in situ via temperature-resolved X-ray powder diffraction and thermogravimetric analysis.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 2, February 2013, Pages 674-683
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 2, February 2013, Pages 674-683
نویسندگان
Liana Vella-zarb, Ulrich Baisch, Robert E. Dinnebier,