Suppr超能文献

水载体的冻干粉化和热熔法制备蒿甲醚固体分散体的理化特性研究。

Physicochemical characterization of artemether solid dispersions with hydrophilic carriers by freeze dried and melt methods.

机构信息

Department of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan.

出版信息

Arch Pharm Res. 2010 Jun;33(6):901-10. doi: 10.1007/s12272-010-0613-7. Epub 2010 Jul 6.

Abstract

Solid dispersions of artemether (ARM), a poorly soluble drug, were prepared using polyvinylpyrrolidone (PVPK25, MW 25000) and polyethyleneglycol (PEG4000, MW 4000) as excipients. These dispersions were studied by physical mixture, freeze-drying, and melting methods. They were characterized by X-ray diffraction pattern, fourier transform infrared spectrophotometry, differential scanning calorimetery, and dissolution studies. X-ray diffraction pattern revealed the complete crystalline nature of artemether, whereas physical mixtures, melt mixtures (MM), and freeze-dried solid dispersions (FDSD) of ARM-PVP and ARM-PEG showed reduced peak intensities with increased PVP/PEG content. PEG showed lower decreases in intensity than PVP preparations. Differential scanning calorimetery also confirmed this finding by showing either a small or absent endotherm. Red shifts in O-H stretching vibrations of ARM were higher in the MM of ARM-PVP than its FDSD as exhibited by fourier transform infrared spectrophotometry. The carbonyl peak of PEG was blue shifted in MM and FDSD, whereas the C=O peak of PVP was red shifted in FDSD and MM, indicating different H-bonding by PEG and PVP with ARM. The rate of dissolution (phosphate buffer at pH 4.5) was improved up to 4-fold in MM and FDSD compared to artemether, and up to 50% compared to physical mixtures. The preparation of solid dispersions influenced the rate of dissolution at various drug-carrier ratios, i.e., the dissolution order of 1:1-1:4 ratio was MM > FDSD; FDSD > MM at 1:6-1:8 ratios of both ARM-PVP and ARM-PEG; and FDSD of ARM-PEG > FDSD of ARM-PVP > MM of ARM-PEG > MM of ARM-PVP at a 1:10 ratio.

摘要

固体分散体的青蒿素(ARM ),一种溶解度差的药物,是用聚乙烯吡咯烷酮(PVPK25 ,分子量为 25000 )和聚乙二醇(PEG4000 ,分子量为 4000 )作为赋形剂制备的。这些分散体通过物理混合物,冷冻干燥和熔融方法进行研究。它们的特征在于 X 射线衍射图,傅里叶变换红外分光光度法,差示扫描量热法和溶解研究。X 射线衍射图显示青蒿素完全具有结晶性质,而物理混合物,熔融混合物( MM )和冷冻干燥固体分散体( FDSD )的 ARM-PVP 和 ARM-PEG 的峰强度降低,随着 PVP/PEG 含量的增加而降低。PEG 显示出比 PVP 制剂更低的强度降低。差示扫描量热法也通过显示小的或不存在的吸热峰来证实这一发现。傅里叶变换红外分光光度法显示,ARM-PVP 的 MM 中 ARM 的 O-H 伸缩振动的红移高于其 FDSD 。MM 和 FDSD 中 PEG 的羰基峰发生蓝移,而 FDSD 和 MM 中 PVP 的 C=O 峰发生红移,表明 PEG 和 PVP 与 ARM 具有不同的氢键。与青蒿素相比,在 MM 和 FDSD 中,溶解速率( pH4.5 的磷酸盐缓冲液)提高了 4 倍,与物理混合物相比提高了 50 %。固体分散体的制备影响了在各种药物载体比下的溶解速率,即 1:1-1:4 比例的溶解顺序为 MM > FDSD ; 1:6-1:8 比例的 ARM-PVP 和 ARM-PEG 的 FDSD > MM ;而在 1:10 比例下,ARM-PEG 的 FDSD > ARM-PVP 的 FDSD > ARM-PEG 的 MM > ARM-PVP 的 MM 。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验