کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2484987 | 1114342 | 2013 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Physicochemical Characterization of Felodipine-Kollidon VA64 Amorphous Solid Dispersions Prepared by Hot-Melt Extrusion
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
To improve the dissolution and hence the oral bioavailability, amorphous felodipine (FEL) solid dispersions (SDs) with Kollidon® VA 64 (PVP/VA) were prepared. Hot-melt extrusion was employed with an extruding temperature below the melting point (Tm) of FEL. X-ray powder diffraction (XRPD) and 13C CP/MAS nuclear magnetic resonance (NMR) measurements show that the extrudates are amorphous. The intermolecular interaction between FEL and PVP/VA in SDs was investigated by Fourier transform infrared spectroscopy, 15N CP/MAS NMR, and 1H high-resolution MAS NMR. Furthermore, a single glass transition temperature (Tg) was detected by differential scanning calorimetry in addition to a single 1H T1 or T1rho relaxation time detected by 13C NMR signals. These results confirm that the extru-dates contain FEL dispersed into the polymer matrix at a molecular level with no detectable phase separation. This molecular-scale mixing results in a significantly faster dissolution rate compared with the pure crystalline FEL. Additionally, the molecular-scale mixing prevents the amorphous drug from recrystallizing even after being stored at 40°C/75% Relative Humidity for 2 months.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 6, June 2013, Pages 1915-1923
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 6, June 2013, Pages 1915-1923
نویسندگان
Yuejun Song, Lianyan Wang, Ping Yang, Robert M. Jr., Bo Tan, Hailu Zhang, Zongwu Deng,