کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2487732 | 1114429 | 2007 | 20 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Development of a high throughput equilibrium solubility assay using miniaturized shakeâflask method in early drug discovery
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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
Increasingly, pharmaceutical and biotech companies have begun to realize the importance of obtaining solubility information in early drug discovery as it is one of the critical parameters for lead selection and optimization. This report introduces a highâthroughput equilibrium solubility (HTâEq sol) assay using a novel miniaturized shakeâflask approach and streamlined HPLC analysis. The new HTâEq sol assay, validated and optimized via a test set of 85 marketed drugs and Novartis internal compounds, shows an excellent correlation to the conventional shakeâflask thermodynamic solubility data generated inâhouse and the equilibrium solubility results reported in literature. It therefore offers a fast, reliable and costâeffective screening tool for solubility assessment in early drug discovery, allowing for prioritization of drug candidates using aqueous solubility in conjunction with other profiling information and efficacy data. Our work demonstrates that presence of a small amount of DMSO (0.5-5%) will result in significant overstimation of equilibrium solubility (up to 6 folds). In addition, monitoring of drug dissolution process using the current approach as well as the interplay between equilibrium solubility data and those from kinetic solubility are discussed. © 2007 WileyâLiss, Inc. and the American Pharmacists Association J Pharm Sci 96: 3052-3071, 2007
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 96, Issue 11, November 2007, Pages 3052-3071
Journal: Journal of Pharmaceutical Sciences - Volume 96, Issue 11, November 2007, Pages 3052-3071
نویسندگان
Liping Zhou, Linhong Yang, Suzanne Tilton, Jianling Wang,