کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2498401 1556740 2016 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Development of amorphous dispersions of artemether with hydrophilic polymers via spray drying: Physicochemical and in silico studies
ترجمه فارسی عنوان
توسعه پراکندگی های آمورف آرتمتر با پلیمرهای هیدروفیلی از طریق اسپری خشک کردن: فیزیکوشیمیایی و در مطالعات سیلیکا
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
چکیده انگلیسی

Artemether (ARM) is a poorly water soluble and poorly permeable drug effective against acute and severe falciparum malaria, hence there is a strong need to improve its solubility. The objective of the study was to enhance the solubility and dissolution rate of ARM by preparation of solid dispersions using spray-drying technique. Solid dispersions of ARM were prepared with Soluplus, Kollidon VA 64, HPMC and Eudragit EPO at weight ratios of 1:1, 1:2, 1:3 using spray drying technology, and characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry (DSC), and X-ray powder diffraction (XRD) to identify the physicochemical interaction between drug and carrier, as well as effect on dissolution. The prepared solid dispersion of ARM with polymers showed reduced crystallinity as compared to neat ARM, which was confirmed by DSC and XRD. Drug/polymer interactions were studied in-silico by docking and molecular dynamics which indicated formation of van der Waals type of interactions of ARM with the polymers. Based on solubility studies, the optimum drug/Soluplus ratio was found to be 1:3. The dissolution studies of formulation SD3 showed highest drug release up to 82% compared to neat ARM giving only 20% at 60 minutes. The spray-dried products were free of crystalline ARM; possessed higher dissolution rates, and were stable over a period according to ICH guidelines. These findings suggest that an amorphous solid dispersion of ARM could be a viable option for enhancing the dissolution rate of ARM.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Asian Journal of Pharmaceutical Sciences - Volume 11, Issue 3, June 2016, Pages 385–395
نویسندگان
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