白藜芦醇苷固体分散体的制备及体内外评价

Wei-ye CHENG, Yi CHEN,Cai-yun ZHANG, Meng MA, Hao-zhi WANG, Shan-shan XU,Hui-ling YUAN

Chinese Traditional and Herbal Drugs(2017)

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Abstract
目的 制备白藜芦醇苷(PD)固体分散体(SD),以期提高PD的生物利用度.方法 以溶出度为指标,采用溶剂蒸发法制备PD-SD,利用傅里叶变换红外光谱(FT-IR)、差示扫描量热分析(DSC)、粉末X衍射(XRD)和扫描电子显微镜(SEM)对PD-SD进行表征.采用HPLC法测定大鼠ig给药后的血药浓度.结果 PD-SD的体外溶出度较PD明显提高,FT-IR显示药物与载体间没有形成新的化学键,DSC和XRD结果显示PD在载体中以无定型的形式存在,SEM结果表明制备成的PD-SD外观形态为不规则球形.ig给药后,PD-SD和PD的药时曲线下面积(AUC0-∞)分别为328.79、139.70 μg.min/mL.结论 溶剂蒸发法制备PD-SD工艺简单可行,PD-SD能显著提高PD的生物利用度.
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Key words
polydatin,solid dispersion,in vitro dissolution,pharmacokinetics,bioavailability,dissolution,solvent evaporation,HPLC,Fourier transform infrared spectroscopy,differential scanning calorimetry,X-ray power diffraction
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