目的 測定氫溴酸沃替西汀油水分配系數(shù)并對其片劑進(jìn)行一致性評價。方法 模擬體內(nèi)環(huán)境配制不同pH的緩沖液(或水溶液),以正辛醇-緩沖液(或水溶液)為分散系統(tǒng),搖瓶法作為測定方法,采用高效液相色譜法進(jìn)行測定。通過氫溴酸沃替西汀分配平衡后在油相(正辛醇)和水相的濃度比,計(jì)算氫溴酸沃替西汀的油水分配系數(shù),并對比測定氫溴酸沃替西汀片劑(自制片、原研片)中氫溴酸沃替西汀的油水分配系數(shù)。結(jié)果 在正辛醇-緩沖液(或水溶液)體系中,pH=1.0時氫溴酸沃替西汀的油水分配系數(shù)為2.20;pH=4.5時為2.18;pH=6.8時為0.823;在水中時為0.657。結(jié)論 采用搖瓶-高效液相色譜法能夠準(zhǔn)確測定氫溴酸沃替西汀的油水分配系數(shù),為預(yù)測體內(nèi)吸收過程提供依據(jù)。并且氫溴酸沃替西汀自制片和原研片中氫溴酸沃替西汀油水分配系數(shù)結(jié)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.