کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5818351 1557328 2015 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Formulation of a modified-release pregabalin tablet using hot-melt coating with glyceryl behenate
ترجمه فارسی عنوان
فرمولاسیون یک قرص پرگابالین تجویز شده با استفاده از پوشش گرم ذوب با گلیسریل بنتات
کلمات کلیدی
پره گابالین، گلیسریل بینات، پوشش گرم داغ، انتشار مواد مخدر، فارماکوکینتیک، ثبات،
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
چکیده انگلیسی

A modified-release (MR) tablet of the anti-anxiety drug pregabalin (PRE) was prepared by hot-melt coating PRE with glyceryl behenate (GB) as a release retardant and compressing to form a matrix with microcrystalline cellulose (MCC) as a hydrophilic diluent. GB-coated PRE had a size in the range of 177-290 μm with good to acceptable flowability. Tablet hardness decreased slightly as GB content increased. PRE release from the tablet matrices was successfully modified by altering the ratio of MCC and GB, and it was found that dissolution- or diffusion-controlled release depended on the amount of GB used. Drug release was pH-independent. An accelerated stability test on the most promising MR tablet at 40 °C and 75% relative humidity for 6 months showed no significant changes in PRE content, and the occurrence of total impurities-including PRE-lactam-was within acceptable limits. After oral administration of the selected MR tablet or a commercial IR capsule (Lyrica) to healthy human volunteers, pharmacokinetic parameters including Tmax, Cmax, AUC0-24, and T1/2 were compared. The confidence interval of AUC0-24 was within the adequate range, but that of Cmax was inadequate. This study demonstrated the potential use of GB for PRE-containing MR formulations.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 495, Issue 1, 10 November 2015, Pages 1-8
نویسندگان
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