联合载体用于改善白藜芦醇固体分散体性能

doi:10.11944/j.issn.1000-0518.2016.12.160363

摘要/Abstract

摘要：

通过载体聚乙烯吡咯烷酮(PVPk29/32)和羟丙基甲基纤维素(HPMC),采用溶剂法制备白藜芦醇(Res)二元及三元固体分散体。用傅里叶变换红外光谱(FTIR)、调制式差示扫描量热(MDSC)和X射线粉末衍射(XRD)等技术手段来表征Res二元和三元固体分散体并考察其溶出度。 FTIR结果显示,Res与PVPk29/32及HPMC均存在氢键相互作用;溶出结果表明,二元和三元固体分散体均能提高药物的溶出度。而XRD和MDSC结果表明,三元固体分散体的相容性优于二元固体分散体;3个月的加速实验(40 ℃,75%RH(relative humidity))中,XRD、MDSC及体外溶出结果表明,Res三元固体分散体的稳定性优于Res二元固体分散体。 HPMC的加入可以改善Res三元固体分散体的溶出及稳定性。

关键词: 白藜芦醇, 无定形固体分散体, 氢键, 溶出, 稳定性

Abstract:

Resveratrol(Res) binary and ternary solid dispersions solid dispersions with poly(vinylpyrrolidone)(PVP) and hydroxypropylmethylcellulose(HPMC) were prepared by the solvent evaporation. Solid dispersions were characterized by Fourier transform infrared spectroscopy(FTIR), X-ray powder diffraction(XRD) and modulated differential scanning calorimetry(MDSC), and the release profiles were also invested. FTIR results reveal hydrogen bonding formed between Res and polymers. The release profiles of both Res solid dispersions are enhanced. However, XRD and MDSC results show that the miscibility of ternary solid dispersions is better than that of its binary solid dispersions. Under accelerated testing condition(40 ℃, 75%RH(relative humity)) for 3 months, XRD, MDSC and the release profiles indicate that Res ternary solid dispersions are more stable than that of its binary solid dispersions. The release profiles and stability of Res ternary solid dispersions are improved with the addition of HPMC.

Key words: resveratrol, amorphous solid dispersion, hydrogen bonding, dissolution, stability

王冰, 黄晓斌, 赵姗, 张建斌, 吕岩, 吕国军, 马小军. 联合载体用于改善白藜芦醇固体分散体性能[J]. 应用化学, 2016, 33(12): 1383-1388.

WANG Bing, HUANG Xiaobin, ZHAO Shan, ZHANG Jianbin, LYU Yan, LYU Guojun, MA Xiaojun. Improve the Properties of Resveratrol Solid Dispersions by Combined Polymers[J]. Chinese Journal of Applied Chemistry, 2016, 33(12): 1383-1388.

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