کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2487359 | 1114413 | 2008 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Polymorph Transitions of Bicalutamide: A Remarkable Example of Mechanical Activation
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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
Bicalutamide, an active pharmaceutical ingredient possessing antiandrogenic activity, is known to exhibit polymorphism. The higher melting Form I relates monotropically to the lower melting Form II. The amorphous form can be easily produced by quench cooling the melt, but it is known to crystallize spontaneously to Form II at room temperature within days. Our results show that crystallization of amorphous bicalutamide is greatly influenced by experimental conditions and sample treatment. The effect of mechanical activation on the polymorph transitions is investigated in detail. Seeds of Form I can be formed in the amorphous phase even due to gentle mechanical treatment, which results in crystallization to the more stable structure at elevated temperature. The crystalline Form II may as well be transformed to the stable modification through mechanical activation at elevated temperature. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97: 3222-3232, 2008
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 97, Issue 8, August 2008, Pages 3222-3232
Journal: Journal of Pharmaceutical Sciences - Volume 97, Issue 8, August 2008, Pages 3222-3232
نویسندگان
Zoltán Német, Janisz Sztatisz, Ádám Demeter,