紫杉醇-PVP固体分散体的制备、物相鉴定及细胞药效

紫杉醇-PVP固体分散体的制备、物相鉴定及细胞药效

孙葭北, 刘祥瑞, 王坚成, 吕万良, 张烜*, 张强

北京大学药学院药剂学系, 北京 100083

收稿日期:2008-03-12 修回日期:2008-05-10 出版日期:2008-06-15 发布日期:2008-06-15
通讯作者: 张烜

Preparation, physicochemical characterization and cyctotoxicity of solid
dispersion of paclitaxel and polyvinylpyrrolidone

Jia-Bei Sun, Xiang-Rui Liu, Jian-Cheng Wang, Wan-Liang Lu, Xuan Zhang*,
Qiang Zhang

Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100083, China

Received:2008-03-12 Revised:2008-05-10 Online:2008-06-15 Published:2008-06-15
Contact: Xuan Zhang

摘要/Abstract

摘要：

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 microscopy, 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。

关键词: 紫杉醇, 紫杉醇, 紫杉醇, 聚乙烯吡咯烷酮, 聚乙烯吡咯烷酮, 聚乙烯吡咯烷酮, 固体分散体, 固体分散体, 固体分散体, 溶解度, 溶解度, 溶解度, 溶出度, 溶出度, 溶出度, 细胞药效, 细胞药效, 细胞药效, , ,

Abstract:

The objective of this study was to prepare and characterize paclitaxel-polyvinylpyrrolidone (PTX-PVP) solid dispersions with the intention of improving its solubility and dissolution properties. The PTX-PVP solid dispersion systems were prepared by solvent method. The release rate of paclitaxel was determined from dissolution studies and the physicochemical properties of solid dispersion were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM). The cytotoxicities of paclitaxel in solid dispersion to the SKOV-3 cells were assayed by a SRB staining method. The results showed that the solubility and dissolution rate of paclitaxel were significantly improved in solid dispersion system compared with that of the pure drug and physical mixture. The results of DSC and PXRD showed that the paclitaxel in solid dispersion was amorphous form. No paclitaxel crystals in the solid dispersions was found during SEM analysis. Cytotoxicity study suggested that the inhibitory rates of PTX-PVP solid dispersion to SKOV-3 cells were higher than that of pure paclitaxel. The solubility and dissolution of paclitaxel were improved by solid dispersion technique. In vitro cytotoxicity of paclitaxel in solid dispersion was higher than that of pure drug.

Key words: Paclitaxel, Paclitaxel, Polyvinylpyrrolidone, Polyvinylpyrrolidone, Solid dispersion, Solid dispersion, Solubility, Solubility, Dissolution rate, Dissolution rate, Cytotoxicity assay, Cytotoxicity assay, ,

中图分类号:

R943

Supporting:

孙葭北, 刘祥瑞, 王坚成, 吕万良, 张烜*, 张强.

紫杉醇-PVP固体分散体的制备、物相鉴定及细胞药效

[J]. .

Jia-Bei Sun, Xiang-Rui Liu, Jian-Cheng Wang, Wan-Liang Lu, Xuan Zhang*,
Qiang Zhang.

Preparation, physicochemical characterization and cyctotoxicity of solid
dispersion of paclitaxel and polyvinylpyrrolidone

[J]. .

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