کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5820374 | 1557396 | 2012 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Modification of concomitant drug release from oil vehicles using drug-prodrug combinations to achieve sustained balanced analgesia after joint installation
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کلمات کلیدی
PDIPBSNSAIDMCTIntra-articular administrationIn vitro release - آزمایشی in vitroDrug delivery - تحویل(رهایش) داروMedium-chain triglyceride - تری گلیسرید متوسط زنجیره ایNon-steroidal anti-inflammatory drug - غیر استروئیدی دارو ضد التهابیsynovial fluid - مایع زلالهای، مایع مفصلی، مایع سینوویالIntra-articular - مفصلی داخلmultimodal analgesia - مقاربت چندگانهProdrug - پروتئین
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
علوم دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Modification of concomitant drug release from oil vehicles using drug-prodrug combinations to achieve sustained balanced analgesia after joint installation Modification of concomitant drug release from oil vehicles using drug-prodrug combinations to achieve sustained balanced analgesia after joint installation](/preview/png/5820374.png)
چکیده انگلیسی
Intra-articular injection of two drugs in a sustained drug delivery system combining the use of lipophilic solution with the prodrug approach may provide efficient and prolonged postoperative pain treatment after arthroscopic procedures. In the present study, the concomitant release of N,N-diethyl glycolamide ester of naproxen and ropivacaine from an oil vehicle consisting of medium-chain triglycerides were investigated in vitro. The release into both phosphate buffer and 80% (v/v) synovial fluid at pH 7.4 was examined in two dialysis membrane-based release models. The ester prodrug exhibited high solubility in medium-chain triglyceride, a high partition coefficient and was rapidly converted to naproxen in synovial fluid. Compared to naproxen, the release of the prodrug from the oil was sustained. In synovial fluid, the reconversion to naproxen resulted in faster release compared to that observed using buffer. In both release models, the use of ropivacaine-prodrug combination provided concomitant release from the oil into synovial fluid with ropivacaine being released faster than naproxen. The use of lipophilic prodrugs that are converted fast to the parent drug in synovial fluid seems to be a feasible approach to obtain prolonged joint residence time.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 439, Issues 1â2, 15 December 2012, Pages 246-253
Journal: International Journal of Pharmaceutics - Volume 439, Issues 1â2, 15 December 2012, Pages 246-253
نویسندگان
Mette Thing, Sabrine Smedegaard Jensen, Claus Larsen, Jesper Ãstergaard, Susan Weng Larsen,