کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8513555 | 1556497 | 2018 | 39 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Monitoring the Phase Behavior of Supersaturated Solutions of Poorly Water-Soluble Drugs Using Fluorescence Techniques
ترجمه فارسی عنوان
نظارت بر رفتار فاز از محلول های بیش از حد مواد مخدر حاوی آب آشامیدنی با استفاده از تکنیک های فلورسانس
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
چکیده انگلیسی
Phase transformations of poorly water-soluble drugs, in low concentration, supersaturated aqueous solutions are of considerable interest. Herein, fluorescence lifetime and steady-state fluorescence spectroscopy were employed to investigate the fluorescence properties of the autofluorescent compound, felodipine (a 1,4-dihydropyridine calcium channel blocker), when present as free drug in solution, drug-rich aggregates, and crystals. Measurements were also performed in the absence and presence of liver microsomes. To study nonfluorescent drugs, an environment-sensitive fluoroprobe, 6-propionyl-2-dimethylaminonaphthalene, was employed. The lifetime of free felodipine in solution in simple media was found to be â¼0.4Â ns, whereas felodipine present in drug-rich aggregates and crystals was characterized by a longer lifetime of â¼2 and â¼9Â ns, respectively. In the presence of structures containing lipids, the local environment of felodipine was found to change based on fluorescence characteristics and the concentration where felodipine aggregates formed was greatly increased. The lifetime of 6-propionyl-2-dimethylaminonaphthalene in solutions containing clotrimazole (an imidazole derivative with antimycotic activity) or efavirenz (a non-nucleoside reverse transcriptase inhibitor with antiviral activity) increased on aggregate formation as a result of the change in polarity of the probe local environment. Fluorescence lifetime coupled with steady-state fluorescence spectroscopy was demonstrated to be effective in identifying the concentration where drug aggregates formed, contributing to improved understanding of the phase behavior of poorly water-soluble drugs in biologically relevant media.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 107, Issue 1, January 2018, Pages 94-102
Journal: Journal of Pharmaceutical Sciences - Volume 107, Issue 1, January 2018, Pages 94-102
نویسندگان
Francesco Tres, Stephen D. Hall, Michael A. Mohutsky, Lynne S. Taylor,