کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2485199 | 1114348 | 2010 | 17 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Conformational polymorphism in aripiprazole: Preparation, stability and structure of five modifications
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کلمات کلیدی
Aripiprazole - آریپیپرازولThermal analysis - آنالیز حرارتیX-ray diffractometry - اشعه ماوراء بنفشThermodynamics - ترمودینامیکSingle crystal structure - ساختار کریستال تکHirshfeld surfaces - سطوح هیرشفلدRaman spectroscopy - طیف سنجی رامانIR spectroscopy - طیف فروسرخConformational polymorphism - پلی مورفیسم سازگاری
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Conformational polymorphism in aripiprazole: Preparation, stability and structure of five modifications Conformational polymorphism in aripiprazole: Preparation, stability and structure of five modifications](/preview/png/2485199.png)
چکیده انگلیسی
Five phase-pure modifications of the antipsychotic drug aripiprazole were prepared and characterized by thermal analysis, vibrational spectroscopy and X-ray diffractometry. All modifications can be produced from solvents, form I additionally by heating of form X° to â¼120°C (solid-solid transformation) and form III by crystallization from the melt. Thermodynamic relationships between the polymorphs were evaluated on the basis of thermochemical data and visualized in a semi-schematic energy/temperature diagram. At least six of the ten polymorphic pairs are enantiotropically and two monotropically related. Form X° is the thermodynamically stable modification at 20°C, form II is stable in a window from about 62-77°C, and form I above 80°C (high-temperature form). Forms III and IV are triclinic (), I and X° are monoclinic (P21) and form II orthorhombic (Pna21). Each polymorph exhibits a distinct molecular conformation, and there are two fundamental N-Hâ¯O hydrogen bond synthons (catemers and dimers). Hirshfeld surface analysis was employed to display differences in intermolecular short contacts. A high kinetic stability was observed for three metastable polymorphs which can be categorized as suitable candidates for the development of solid dosage forms. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:2010-2026, 2009
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 98, Issue 6, June 2009, Pages 2010-2026
Journal: Journal of Pharmaceutical Sciences - Volume 98, Issue 6, June 2009, Pages 2010-2026
نویسندگان
Doris E. Braun, Thomas Gelbrich, Volker Kahlenberg, Richard Tessadri, Josef Wieser, Ulrich J. Griesser,