کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2501741 1557347 2015 17 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
In situ perfusion in rodents to explore intestinal drug absorption: Challenges and opportunities
ترجمه فارسی عنوان
پرفیوژن موضعی در جوندگان برای کشف جذب داروهای روده: چالش ها و فرصت ها
کلمات کلیدی
متابولیسم حمل و نقل، جذب وابستگی به سایت، حیوانات نابود، نفوذپذیری حلقوی-نفوذپذیری، بیش از حد، پرفیوژن روده
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
چکیده انگلیسی

The in situ intestinal perfusion technique in rodents is a very important absorption model, not only because of its predictive value, but it is also very suitable to unravel the mechanisms underlying intestinal drug absorption. This literature overview covers a number of specific applications for which the in situ intestinal perfusion set-up can be applied in favor of established in vitro absorption tools, such as the Caco-2 cell model. Qualities including the expression of drug transporters and metabolizing enzymes relevant for human intestinal absorption and compatibility with complex solvent systems render the in situ technique the most designated absorption model to perform transporter-metabolism studies or to evaluate the intestinal absorption from biorelevant media.Over the years, the in situ intestinal perfusion model has exhibited an exceptional ability to adapt to the latest challenges in drug absorption profiling. For instance, the introduction of the mesenteric vein cannulation allows determining the appearance of compounds in the blood and is of great use, especially when evaluating the absorption of compounds undergoing intestinal metabolism. Moreover, the use of the closed loop intestinal perfusion set-up is interesting when compounds or perfusion media are scarce. Compatibility with emerging trends in pharmaceutical profiling, such as the use of knockout or transgenic animals, generates unparalleled possibilities to gain mechanistic insight into specific absorption processes.Notwithstanding the fact that the in situ experiments are technically challenging and relatively time-consuming, the model offers great opportunities to gain insight into the processes determining intestinal drug absorption.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 478, Issue 2, 30 January 2015, Pages 665–681
نویسندگان
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