目的 测定氢溴酸沃替西汀油水分配系数并对其片剂进行一致性评价。方法 模拟体内环境配制不同pH的缓冲液(或水溶液),以正辛醇-缓冲液(或水溶液)为分散系统,摇瓶法作为测定方法,采用高效液相色谱法进行测定。通过氢溴酸沃替西汀分配平衡后在油相(正辛醇)和水相的浓度比,计算氢溴酸沃替西汀的油水分配系数,并对比测定氢溴酸沃替西汀片剂(自制片、原研片)中氢溴酸沃替西汀的油水分配系数。结果 在正辛醇-缓冲液(或水溶液)体系中,pH=1.0时氢溴酸沃替西汀的油水分配系数为2.20;pH=4.5时为2.18;pH=6.8时为0.823;在水中时为0.657。结论 采用摇瓶-高效液相色谱法能够准确测定氢溴酸沃替西汀的油水分配系数,为预测体内吸收过程提供依据。并且氢溴酸沃替西汀自制片和原研片中氢溴酸沃替西汀油水分配系数结果一致。

Objective To determine the oil-water partition coefficient of Vortioxetine hydrobromide. Methods A shake flask-HPLC method was applied to determining the oil-water partition coefficient of Vortioxetine hydrobromide in n-octanol-buffer (aqueous solution) systems with different pH values. Results The LgP of Vortioxetine hydrobromide under pH 1.0 was 2.20, under pH 4.5 was 2.18, under pH 6.8 was 0.823, and under neutral water was 0.657. Conclusion The shake flask-HPLC method can be used to determine the oil-water partition coefficient of Vortioxetine hydrobromide, and help to predict the in vivo process. The LgP of Vortioxetine hydrobromide self-prepared tablets and Brintellix was consistency.