کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2486742 1114392 2010 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Improved Pharmacokinetics of AMG 517 Through Co-Crystallization Part 1: Comparison of Two Acids With Corresponding Amide Co-crystals
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
پیش نمایش صفحه اول مقاله
Improved Pharmacokinetics of AMG 517 Through Co-Crystallization Part 1: Comparison of Two Acids With Corresponding Amide Co-crystals
چکیده انگلیسی

ABSTRACTThe dissolution and pharmacokinetics (PK) of two carboxylic acid co-crystals (cinnamic acid and benzoic acid) with the corresponding amide co-crystals (cinnamamide and benzamide) of AMG 517 were investigated. Powder and intrinsic dissolution studies were performed in fasted simulated intestinal fluid (FaSIF). Suspension formulations in 1% polyvinylpyrrolidone K25 in water were administered orally at 100 mg/kg to rats. The four cocrystals were found to have faster intrinsic and powder dissolution rates in FaSIF than the free base. This correlated with a 2.4- to 7.1-fold increase in the area under the concentration-time curve in rat PK investigations. When contrasting the acid to its corresponding amide co-crystal, cinnamamide shows improvement over cinnamic acid, while benzamide and benzoic acid perform similarly. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:3769–3778, 2010

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 99, Issue 9, September 2010, Pages 3769–3778
نویسندگان
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