کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5550380 1557288 2017 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
An investigation into the ability of alendronate ion pairs to increase oral absorption
ترجمه فارسی عنوان
بررسی توانایی زوج یونهای آلندرونیت برای افزایش جذب دهان
کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
چکیده انگلیسی

The purpose of this study is to increase oral absorption of the highly charged drug alendronate using an ion pair strategy. Ion pairing is a formulation approach in drug delivery that is performed to improve the lipophilicity of ionized drugs. Cationic counter ions, such as arginine, phenazopyridine, hyoscine and pyridostigmine, were selected to enhance the lipophilicity and permeability of alendronate. Data obtained from quasi-equilibrium analysis were used to calculate the binding constant and intrinsic partition coefficient of ion pairs in an octanol/water system. The results of the partitioning study in an octanol/water system were confirmed using in vitro transport models with PAMPA and Caco-2 monolayer assays. Two counter ions, phenazopyridine and arginine, substantially increased the partition coefficient of alendronate by up to 1.15 and 0.73 units, respectively, in the octanol/water system. Binding constants of 117 M−1 for alendronate-arginine and 90 M−1 for alendronate-phenazopyridine ion pairs were obtained using quasi equilibrium analysis. Arginine and phenazopyridine enhanced the apparent permeability of alendronate by 14- and 26-fold in the PAMPA model and 6.5- and 4.4-fold across caco-2 cell monolayers, respectively. Based on this study, the lipophilicity and permeability of alendronate across lipophilic membranes was increased by suitable counter ions and could be used to establish a new formulation to increase the oral absorption of alendronate.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 527, Issues 1–2, 15 July 2017, Pages 184-190
نویسندگان
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