摘要
Parkinson’s disease(PD) is a common degenerative disease of the central nervous system, and the pathologic features are mainly degeneration of substantianigra and dopamine neurons. Studies have shown that safflower flavonoid extract(SAFE) exhibits the neuroprotective effect. In this study, the safflower flavonoid extract drop pills(SAFE-DPs) for anti-PD were prepared by the heating and melting method using SAFE and matrix PEG6000. The performances of the pills were evaluated with powder X-ray diffraction(PXRD), differential scanning calorimetry(DSC), Fourier transform infrared spectroscopy(FT-IR), scanning electron microscopy(SEM) and dissolution testing. The analysis results demonstrated an amorphous state for SAFE dispersion in the matrix PEG6000 without any chemical reaction. The SAFE-DPs demonstrated acceptable chemical and physical stability irrespective of the manufacturing process and the storage period. Dissolution testing in three dissolution media(pH 1.0, pH 6.8 and pH 7.5) indicated that SAFE-DPs had excellent dissolution property. The transport of Kaempferol-3-rutinoside(K3 R) on the Caco-2 monolayer and the absorption of K3 R in situ intestinal perfusion revealed that the principal component of SAFE had a good transport and absorption capacity. Therefore, the drop pills had better release and absorption in the gastrointestinal tract, corresponding with the pharmacological and pharmacodynamic results for PD in vivo.
帕金森病(PD)是中枢神经系统常见的退行性疾病,其病理特征主要是黑质和多巴胺神经元的变性。研究表明,红花黄酮提取物(SAFE)具有神经保护作用。本研究采用SAFE和基质PEG6000通过加热熔融法制备抗帕金森病红花黄酮提取物滴丸(SAFE-DPs)。用粉末X射线衍射(PXRD),差示扫描量热法(DSC),傅立叶变换红外光谱(FT-IR),扫描电子显微镜(SEM)和溶出度测试评价药丸的性能。分析结果表明,在没有任何化学反应的情况下,基质PEG6000中的SAFE分散体具有无定形状态。在制造过程和储存期间,SAFE-DP都表现出可接受的化学和物理稳定性。在三种溶解介质(pH1.0,pH 6.8和pH7.5)中的溶解测试表明SAFE-DP具有优异的溶解性质。山奈酚-3-O-芸香糖苷(K3R)在Caco-2单层上的转运和在原位肠灌注的吸收揭示SAFE的主要成分具有良好的转运和吸收能力。因此,滴丸在胃肠道中具有好的释放和吸收,预计体内有较好的药理学和药效学结果。
基金
Science and Technology Major Projects:Significant New-Drugs Creation(Grant No.2012ZX09103201-042)
