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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p H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,p H=1.0时氢溴酸沃替西汀的油水分配系数为2.20;p H=4.5时为2.18;p H=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 partition coefficients of oil and water hydrobromide and its consistency. Methods The in vivo environment was formulated with buffers (or aqueous solutions) of different pH, and n-octanol-buffer (or aqueous solution) was used as the dispersion system. The shake flask method was used as the determination method and the high performance liquid chromatography was used for the determination. The partition coefficients of vortioxetine hydrobromide were calculated by the concentration ratio of oil phase (n-octanol) and water phase after the balance of vortioxetine hydrobromide was partitioned, and the ratio of vortioxetine hydrobromide Oil and water partition coefficients of vortioxetine hydrobromide in agents (self-made tablets, original tablets). Results The coefficient of distribution of oil and water of vortioxetine hydrobromide was 2.20 in n-octanol-buffer (or aqueous solution) system when p H = 1.0, 2.18 for p H = 4.5, 0.823 for p H = 6.8, 0.657 in water. Conclusion The oil-water partition coefficients of vortioxetine hydrobromide can be accurately determined by shake flask-high performance liquid chromatography in order to provide a basis for the prediction of the absorption process in vivo. And the results of Wortezin hydrobromide oil-water partition coefficient in the homemade tablets and the original tablets were the same.