注射用富马酸伊布利特的制备及质量研究

Preparation and quality control of ibutilide fumarate for injection

目的：制备注射用富马酸伊布利特并建立其质量控制方法。方法：考察预冻溶液pH值，筛选赋形剂的种类和用量，得出最佳处方。建立了高效液相色谱法测定其含量及有关物质，并通过长期试验考察其稳定性。结果：预冻溶液最佳pH值为4．0—5．0；所采用的4种赋形剂中，甘露醇效果最优，其最佳用量为10．0％；含量测定中回收率为99．3％～100．1％（RSD〈1．0％）。注射用富马酸伊布利特的各项检测指标均达到质量标准的要求，经长期留样12个月质量稳定。结论：处方合理，制备工艺可行，产品质量可控。

Objective：To study preparation and quality control of ibutilide fumarate for injection. Methods： The formulation of ibutilide fumarate for injection was optimized by investigating the pH environment and the types and quantity of vehicles. A HPLC procedure was established to determine the content of ibutilide fumarate and its related substances. The stability test was performed in a long-term setting. Results： The optimal pH value was 4.0 - 5.0. 10% mannitol was used as the optimal excipient. The mean recovery of ibutilide fumarate was 99.3%- 100. 1% （ RSD 〈 1.0% ）. The optimal formulation was stable for 12 months at room temperature. Conclusion：The optimal formulation and quality control of ibutilide fumarate were achievable.