微柱离心-高效液相色谱法在测定注射用紫杉醇(白蛋白结合型)包封率中的应用

Application of micro-column gel centrifugation-HPLC method in determining the encapsulation efficiency of Paclitaxel for Injection(Albumin Bound)

目的:采用微柱凝胶离心法(Micro-Column gel centrifugation,MCGE)-RPHPLC联用技术测定注射用紫杉醇(白蛋白结合型)(Paclitaxelfor Injection(Albumin Bound))的包封率。方法:采用Sephadex G-50微柱离心对样品进行前处理,分离结合型药物与游离药物。色谱条件:Pro C18色谱柱(250 mm×4.6 mm,5μm),乙腈-水(50∶50)为流动相,柱温30℃,流速1.0 mL·min^-1,检测波长228 nm。结果:紫杉醇在浓度范围0.0001~0.0601 mg·mL^-1与峰面积呈线性关系,r=0.9999,平均回收率为98.6%,RSD为1.1%(n=9)。微柱离心法能将结合型药物与游离药物完全分离,测得注射用紫杉醇(白蛋白结合型)的平均包封率为93.6%(n=3)。结论:该方法简便快速、重复性良好,可用于测定注射用紫杉醇(白蛋白结合型)的包封率。

OBJECTIVE To determine the entrapment efficiency of Paclitaxelfor Injection(Albumin Bound)by microcolumn gel centrifugation(MCGE)-RPHPLC.METHODS Sephadex G-50 Micro-Column Centrifugation-RPHPLC was performed to separate bound and free drugs.Chromatographic conditions:Pro C18 column(250 mm×4.6 mm,5μm),acetonitrile-water(50∶50)as mobilephase.The column temperature was 30℃,the flow rate was 1.0 mL·min^-1,and the detection wave length was 228 nm.RESULTS The method showed a good linearity in the range of 0.0001-0.0601 mg·mL^-1(r=0.9999).The average recovery was 98.6%,the RSD was 1.1%(n=9).MCGE can completely separate the bound drug from the free drug,and the average encapsulation efficiency of Paclitaxel for Injection(Albumin Bound)is 93.6%(n=3).CONCLUSION The method is simple,rapid and reproducible,and can be used to determine the entrapment efficiency of paclitaxel for injection(albumin-bound).