کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9918594 | 1557550 | 2005 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Evasion of P-gp mediated cellular efflux and permeability enhancement of HIV-protease inhibitor saquinavir by prodrug modification
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موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
علوم دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Uptake of [3H]erythromycin by MDCKII-MDR1 cells exhibited a four-fold increase in the presence of 75 μM SQV. However, equimolar concentrations of Val-Val-SQV and Gly-Val-SQV showed only 2.5-fold increase in [3H]erythromycin uptake. Concentration dependent inhibition of [3H]glycylsarcosine (Gly-Sar), a model peptide transporter substrate, was observed in the presence of SQV prodrugs. Transepithelial transport studies of Val-Val-SQV and Gly-Val-SQV exhibited an enhanced absorptive flux and reduced secretory flux relative to studies employing SQV. These results are very likely due to decreased efflux of SQV dipeptide prodrugs by P-gp. Peptide prodrug derivatization constitutes an exciting strategy to improve intestinal absorption and oral bioavailability of SQV.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 303, Issues 1â2, 13 October 2005, Pages 8-19
Journal: International Journal of Pharmaceutics - Volume 303, Issues 1â2, 13 October 2005, Pages 8-19
نویسندگان
Ritesh Jain, Sheetal Agarwal, Soumyajit Majumdar, Xiaodong Zhu, Dhananjay Pal, Ashim K. Mitra,