Physicochemical characterization of felodipine-kollidon VA64 amorphous solid dispersions prepared by hot-melt extrusion
文献类型：期刊论文
| 作者 | Deng, ZW(邓宗武) ; Wang, LY(汪莲艳); Zhang, HL(张海禄)
|
| 刊名 | JOURNAL OF PHARMACEUTICAL SCIENCES
 |
| 出版日期 | 2013-06 |
| 卷号 | 102期号:6页码:1915-1923 |
| 关键词 | hot-melt extrusion amorphous solid dispersion molecular dispersion solid-state NMR physicochemical properties solubility stabilization |
| 通讯作者 | Yang, P |
| 英文摘要 | To improve the dissolution and hence the oral bioavailability, amorphous felodipine (FEL) solid dispersions (SDs) with Kollidon (R) 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 extrudates 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 degrees C/75% Relative Humidity for 2 months. (c) 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:19151923, 2013 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000319071200024 |
| 公开日期 | 2014-01-20 |
| 源URL | [http://ir.sinano.ac.cn/handle/332007/1522]  |
| 专题 | 苏州纳米技术与纳米仿生研究所_纳米仿生研究部_邓宗武团队 |
| 推荐引用方式 GB/T 7714 | Deng, ZW,Wang, LY,Zhang, HL. Physicochemical characterization of felodipine-kollidon VA64 amorphous solid dispersions prepared by hot-melt extrusion[J]. JOURNAL OF PHARMACEUTICAL SCIENCES,2013,102(6):1915-1923. |
| APA | Deng, ZW,Wang, LY,&Zhang, HL.(2013).Physicochemical characterization of felodipine-kollidon VA64 amorphous solid dispersions prepared by hot-melt extrusion.JOURNAL OF PHARMACEUTICAL SCIENCES,102(6),1915-1923. |
| MLA | Deng, ZW,et al."Physicochemical characterization of felodipine-kollidon VA64 amorphous solid dispersions prepared by hot-melt extrusion".JOURNAL OF PHARMACEUTICAL SCIENCES 102.6(2013):1915-1923. |
入库方式： OAI收割
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。