کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
8513596 1556497 2018 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Development of a Novel Amorphous Agomelatine Formulation With Improved Storage Stability and Enhanced Bioavailability
ترجمه فارسی عنوان
توسعه فرمول آمونیاک آمورف رمان با بهبود پایداری ذخیره سازی و افزایش قابلیت دسترسی به آن
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
چکیده انگلیسی
The present work describes the development of a novel formulation of amorphous agomelatine (AGM) that exhibits enhanced in vitro dissolution rate and bioavailability, as well as improved storage stability. AGM was loaded on a mixture of microcrystalline cellulose with a high specific surface area excipient, namely colloidal silicon dioxide, employing a wet granulation method, and the resultant AGM granules were subsequently formulated into immediate release film-coated tablets. Modulated temperature differential scanning calorimetry, hot-state light microscopy, powder X-ray diffraction, attenuated total reflectance FTIR, and micro-Raman spectroscopy revealed that the active pharmaceutical ingredient existed primarily in the amorphous state within the prepared formulations, with some crystals of polymorph I also present. Accelerated stability studies for up to 6 months in alu-alu blisters showed good physicochemical stability during storage. Finally, in vitro dissolution studies and clinical trials in healthy human volunteers showed a remarkable increase in the in vitro dissolution rate and a ∼1.5-fold increase in bioavailability, respectively, compared to the marketed product.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 107, Issue 1, January 2018, Pages 257-266
نویسندگان
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