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 f...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.展开更多
基金Science and Technology Major Projects:Significant New-Drugs Creation(Grant No.2012ZX09103201-042)
文摘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.
