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以灰黄霉素(GRIS)-聚乙烯吡咯烷酮(PVP)体系为例,研究了电喷雾法制备药物-高分子固体分散体,并采用偏光显微镜(POM)、X射线衍射仪(XRD)和差示扫描量热仪(DSC)等方法对体系进行表征。电喷雾法制备得到的微米级固体分散体样品中,体系玻璃化转变温度,很好地符合半经验公式Fox方程,说明GRIS在体系中分散均匀。POM和XRD结果表明,GRIS在样品中的质量分数达50%时,才有少量的GRIS以结晶形式存在于体系中,DSC结果进一步半定量地说明GRIS在制备得到的固体分散体中结晶明显受到抑制。电喷雾法样品用量少,装置和操作简便,是一种制备固体分散体的理想方法。

Griseofulvin(GRIS)-poly(vinyl pyrrolidone) solid dispersion systems were prepared by electro-spraying methods,and characterized by polarized optical microscope(POM),X-ray diffraction(XRD) and differential scanning calorimeter(DSC).The results demonstrate that electro-spraying can produce micron-sized particle samples with homogeneous structures,as Tg values of the systems with different drug loading are consistent with predictions from the Fox equation.The electro-spraying also can significantly inhibit GRIS crystallization,since no crystal is observed in freshly prepared solid dispersion until GRIS content up to 50%,and the measured fusion enthalpy of the systems is dramatically lower than the theoretical ones.Compared with the conventionally-used rotary evaporation and spray drying methods,electro-spraying needs very little amount of drugs and is a convenient method for solid dispersion preparation.

参考文献

[1] Vasconcelos T;Sarmento B;Costa P .Solid dispersions as strategy to improve oral bioavailability of poor water soluble drugs.[J].Drug discovery today,2007(23/24):1068-1075.
[2] Feng T;Pinal R;Carvajal MT .Process induced disorder in crystalline materials: differentiating defective crystals from the amorphous form of griseofulvin.[J].Journal of Pharmaceutical Sciences,2008(8):3207-3221.
[3] Zhou D;Zhang GG;Law D;Grant DJ;Schmitt EA .Thermodynamics, molecular mobility and crystallization kinetics of amorphous griseofulvin.[J].Molecular pharmaceutics,2008(6):927-936.
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