کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8994352 | 1114394 | 2005 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Biosensor Analysis of the Interaction between Drug Compounds and Liposomes of Different Properties; a Two-Dimensional Characterization Tool for Estimation of Membrane Absorption
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The interactions between 78 drug compounds and immobilised liposomes were investigated using an assay based on surface plasmon resonance technology. The drugs were screened at a single concentration and allowed to interact simultaneously with two different types of liposomes. When the drugâliposome responses are plotted against one another they generally fall into three distinct bands: low response-low percent fraction absorbed in humans (Fa), medium response-medium Fa, and high responseâhigh Fa. For drugs with medium to high Fa values, basic compounds could be resolved from acidic and neutral compounds to a large extent. This technique has the potential to be utilized as a screening tool for binning novel compounds into low, medium, or high Fa based on a simple experimental measurement. The assay was applied to 11 kinase inhibitors, 9 thrombin inhibitors, and 11 carbonic anhydrase inhibitors highlighting a subset that may have incomplete intestinal absorption (low to medium Fa). Assay conditions were optimized making the assay suitable for routine analysis and for compound characterization early in drug discovery where solubility may be an issue.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 94, Issue 1, January 2005, Pages 25-37
Journal: Journal of Pharmaceutical Sciences - Volume 94, Issue 1, January 2005, Pages 25-37
نویسندگان
Ã
sa FrostellâKarlsson, Helena Widegren, Caroline E. Green, Markku D. Hämäläinen, Lena Westerlund, Robert Karlsson, Katherine Fenner, H.a.n. van de Waterbeemd,