CAJ | 학술논문

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.
용용제법제비자삼순-PVP고체분산체,대기용해도급체외용출특성진행고찰병대물상진행감정.채용용제법제비자삼순-PVP고체분산체,대고체분산체중자삼순적용해도화용출솔진행측정,연구고체분산체적용출성질.동시,이용차열분석(Differential scanning calorimetry,DSC)、분말X연사(X-ray powder diffractometry,PXRD)、소묘전경(Scanning electron mi-croscopy, SEM)등방법대기진행물상감정.채용SRB법대자삼순-PVP고체분산체대SKOV-3세포약효진행측정.자삼순-PVP고체분산체중자삼순적용해도화용출속솔상대기원료약화물리혼합물균유료명현적제고;열차분석급분말X연사결과표명고체분산체중자삼순정비결정형식:소묘전경하고체분산체중무자삼순정체.세포약효결과표명자삼순PVP고체분산체적세포약효강우자삼순순약.채용용제법제비적자삼순-PVP고체분산체가현저제고자삼순적용해도화용출속도.
The objective of this study was to prepare and characterize paclitaxel-polyvinylpyrrolidone (PTX-PVP) solid disper- sions with the intention of improving its solubility and dissolution properties. The PTX-PVP solid dispersion systems were pre- pared by solvent method. The release rate of paclitaxel was determined from dissolution studies and the physicochemical proper- ties of solid dispersion were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scan- ning 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 analy- sis. 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.