雷帕霉素药物支架释放度测定

目的: 建立一种雷帕霉素冠脉药物支架体外释放度测定的方法。 方法 :根据美国药典释放度测定第7法的仪器装置, 改装了药物溶出度仪。释放介质为4%牛血清和0.1%叠氮化钠溶解在PBS(pH＝7.4, 0.01 M)的缓冲液;以ODS为固定相, 乙腈∶ 水(65∶ 35)为流动相, 柱温为60℃, 检测波长为280 nm。 结果 :雷帕霉素在0.5~100 μg·mL浓度范围内线性关系良好, 相关系数0.9999, 回收率99.7%, 最低检测限为0.025 μg;雷帕霉素在0~28 d的释放曲线与USP释放度测定第7法测定结果一致。 结论: 本法改装后的仪器简便, 适合国情, 符合USP7的要求, 检测结果较为满意。

Objective: To establish a method for the analysis of release of rapamycin in drug eluting stents(DES). Methods: Chp dissolution test method(modify USP7)was adopted and used 250 mL the mixture of 4% BSA and 0.1%NaN3 in PBS buffer(pH＝7.4,0.01 M)as the release media.Agilent Ecilpse C₁₈(150 mm×4.6 mm,5 μm)was adopted,The mobile phase consisted of acetonitrile and methanol solution(65∶ 35)at a flow rate of 1.0 mL·min^-1.Keep the detective wave length at 280 nm. Results: The linear correlation of rapamycin in acetonitrile is observed over the range of 1-100 μg· mL^-1(r=0.9999).The recoveries of rapamycin is 99.7%.The LOD is 0.025 μg.The release of rapamycin using improved method is identical to which using USP method Ⅶ. Conclusion: The method is fastness and convenience.