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用溶剂法制备紫杉醇-PVP固体分散体,对其溶解度及体外溶出特性进行考察并对物相进行鉴定。采用溶剂法制备紫杉醇-PVP固体分散体,对固体分散体中紫杉醇的溶解度和溶出率进行测定,研究固体分散体的溶出性质。同时,利用差热分析(Differential scanning calorimetry,DSC)、粉末X衍射(X-ray powder diffractometry,PXRD)、扫描电镜(Scanning electron mi- croscopy,SEM)等方法对其进行物相鉴定。采用SRB法对紫杉醇-PVP固体分散体对SKOV-3细胞药效进行测定。紫杉醇-PVP固体分散体中紫杉醇的溶解度和溶出速率相对其原料药和物理混合物均有了明显的提高;热差分析及粉末X衍射结果表明固体分散体中紫杉醇呈非结晶形式;扫描电镜下固体分散体中无紫杉醇晶体。细胞药效结果表明紫杉醇-PVP固体分散体的细胞药效强于紫杉醇纯药。采用溶剂法制备的紫杉醇-PVP固体分散体可显著提高紫杉醇的溶解度和溶出速度。
Paclitaxel-PVP solid dispersion was prepared by solvent method, its solubility and in vitro dissolution characteristics were investigated and the phase was identified. Paclitaxel-PVP solid dispersion was prepared by solvent method. The solubility and dissolution rate of paclitaxel in solid dispersion were determined to study the dissolution properties of solid dispersion. At the same time, the phases were identified by DSC, XRD and PXRD. The efficacy of paclitaxel-PVP solid dispersion on SKOV-3 cells was determined by SRB method. The solubilities and dissolution rates of paclitaxel in paclitaxel-PVP solid dispersions were significantly increased compared with that of the API and the physical mixtures. The results of thermal difference analysis and X-ray powder diffraction showed that the paclitaxel in the solid dispersions was amorphous. No paclitaxel crystals in dispersion. Cytotoxicity results showed that paclitaxel-PVP solid dispersion cell efficacy than paclitaxel pure drug. Paclitaxel-PVP solid dispersion prepared by solvent method can significantly improve the solubility and dissolution rate of paclitaxel.