注射用亚锡替曲膦的制备及处方设计

Optimized Formulation of Tetrofosmin and Stannous Chloride for Injection Using Orthogonal Design

目的探讨注射用亚锡替曲膦的处方。方法以放射化学纯度为指标,选取替曲膦用量、氯化亚锡用量、制剂pH值和氮气保护时间四个因素,每个因素选取三个水平,选用L9(34)表进行正交实验,对注射用亚锡替曲膦的处方进行筛选。结果四个因素中对评估指数的影响大小依次为制剂pH值>氮气保护时间>氯化亚锡用量>替曲膦用量。按照优化处方进行复核实验表明,注射用亚锡替曲膦的放射化学纯度为96.1%,且制剂性质稳定,符合2005年版药典要求。结论本处方工艺稳定,具有良好的应用前景。

OBJECTIVE To study the new preparation of tetrofosmin（TF） and stannous chloride for injection.METHODS The formulation of tetrofosmin and stannous chloride for injection was optimized using orthogonal design with radiochemical purity（RCP%）.Four factors,including TF,SnCl2,pH and the time of N2 protect,and three levels for each factor that may affect the formulation of kit were selected and arranged in a L9（34）orthogonal experimental table. RESULTS The four factor affected the evaluating indicator（EI%） differently.PH behaved as the maximum,followed N2 protect time and SnCl2,TF behaved as the minimum.The orthogonal experiment was checked up,and the result indicated chat RCP% were 96.1%.The quality of the kit stability was complied with the Ch.P.2005.CONCLUSION The preparation procedure is good and reproducible.