کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10162433 | 1114329 | 2014 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A Prodrug Approach Involving In Situ Depot Formation to Achieve Localized and Sustained Action of Diclofenac After Joint Injection
ترجمه فارسی عنوان
یک روش پیشگیرانه درگیر در تشکیل سازند انبار برای دستیابی به فعالیت موضعی و پایدار دیکلوفناک پس از تزریق مفصلی
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کلمات کلیدی
سیستم های تحویل دارو، تزریق مشترک تزریق انسولین داروهای ضد التهابی غیر استروئید، بارش، پیش داروها، سیستم های تعلیق، خواص فیزیکوشیمیایی،
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
چکیده انگلیسی
Long-acting nonsteroidal anti-inflammatory drug formulations for intra-articular injection might be effective in the management of joint pain and inflammation associated sports injuries and osteoarthritis. In this study, a prodrug-based delivery system was evaluated. The synthesized diclofenac ester prodrug, a weak base (pKa 7.52), has relatively high solubility at low pH (6.5 mg mLâ1 at pH 4) and much lower solubility at physiological pH (4.5 μg mLâ1 at pH 7.4) at 37°C. In biological media including 80% (v/v) human synovial fluid (SF), the prodrug was cleaved to diclofenac mediated by esterases. In situ precipitation of the prodrug was observed upon addition of a concentrated slightly acidic prodrug solution to phosphate buffer or SF at pH 7.4. The degree of supersaturation accompanying the precipitation process was more pronounced in SF than in phosphate buffer. In the rotating dialysis cell model, a slightly acidic prodrug solution was added to the donor cell containing 80% SF resulting in a continuous appearance of diclofenac in the acceptor phase for more than 43 h after an initial lag period of 8 h. Detectable amounts of prodrug were found in the rat joint up to 8 days after knee injection of the acidic prodrug solution. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 103, Issue 12, December 2014, Pages 4021-4029
Journal: Journal of Pharmaceutical Sciences - Volume 103, Issue 12, December 2014, Pages 4021-4029
نویسندگان
Mette Thing, Li Ã
gÃ¥rdh, Susan Larsen, Rune Rasmussen, Jakob Pallesen, Nina Mertz, Jesper Kristensen, Martin Hansen, Jesper Ãstergaard, Claus Selch Larsen,