注射用亚锡替曲膦的制备及处方设计

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。

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

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.