کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
8513786 | 1556500 | 2017 | 38 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Real-Time Analysis of Tenofovir Release Kinetics Using Quantitative Phosphorus (31P) Nuclear Magnetic Resonance Spectroscopy
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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
The dialysis method is classically used for drug separation before analysis, but does not provide direct and real-time drug quantification and has limitations affecting the dialysis rate. In this study, a phosphorus nuclear magnetic resonance (31P-qNMR) method is developed for the real-time quantification of therapeutic molecules in vitro. The release kinetics of model drug, tenofovir (anti-HIV microbicide), was analyzed in vaginal fluid simulant (VFS), seminal fluid simulant (SFS), and human plasma (HP) from chitosan nanofibers (size â¼100-200 nm) using the NMR (direct) method and compared with dialysis/UV-Vis (indirect) method. The assay was linear in VFS/SFS (0.20-5.0 mM), HP (0.30-5.0 mM of drug concentration range) and specific no drug 31P-qNMR chemical shift [â¼15 ppm] interference with formulation/media components. Limit of detection values were 0.075/0.10/0.20 mM, whereas limit of quantification values were 0.20/0.20/0.30 mM in VFS/SFS/HP, respectively. The method was robust, precise (%RSE <2%), and accurate (%mean recovery 90%-110%). After 12 h, â¼77%/72%/70% wt/wt of tenofovir release was observed with direct, compared to â¼47%/52%/52% wt/wt by indirect method in VFS/SFS/HP, respectively. Approximately 20% decrease in %drug release observed with dialysis method suggested an interference with drug transport process due to the dialysis membrane and the Gibbs-Donnan effect. Overall, 31P-qNMR provides more accurate, real-time, and direct drug quantification for effective in vitro-in vivo correlation.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 106, Issue 10, October 2017, Pages 3005-3015
Journal: Journal of Pharmaceutical Sciences - Volume 106, Issue 10, October 2017, Pages 3005-3015
نویسندگان
Vivek Agrahari, Jianing Meng, Sudhaunshu S. Purohit, Nathan A. Oyler, Bi-Botti C. Youan,