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目的:测定盐酸文拉法辛(Ven)的表观油水分配系数(P)及其水溶液的化学稳定性,为今后研制Ven的黏膜吸收给药液体制剂奠定基础。方法:采用HPLC法测定Ven的浓度;测定Ven在正辛醇-水/p H 2~10磷酸缓冲液系统中的P值;测定Ven在p H 2~12磷酸缓冲液以及不同离子强度条件下的降解百分率。结果:Ven在正辛醇-水系统中的P值为0.16;在正辛醇-p H 2~10缓冲液系统中,当p H≤6.0时,Ven的P值接近于1,当p H>6.0时,随着p H的增加,药物的P值显著增大。Ven溶液在p H≤8.0时,其化学稳定性良好,在碱性p H下,化学稳定性较差;离子强度对Ven溶液的化学稳定性无影响。结论:Ven的油水分配系数及溶液的化学稳定性与p H密切相关。在p H约为7.0时,Ven具有较高油水分配系数及化学稳定性。
OBJECTIVE: To determine the apparent oil-water partition coefficient (P) and the chemical stability of aqueous solution of venlafaxine hydrochloride, and to lay the foundation for the preparation of venous liquid for absorption by Ven in the future. Methods: The concentration of Ven was determined by HPLC. The value of Ven in n-octanol-water / p H 2 ~ 10 phosphate buffer system was determined. The effect of Ven on p H 2 ~ 12 phosphate buffer and different ionic strength The percentage of degradation. Results: The P value of Ven in n-octanol-water system was 0.16. In the system of n-octanol-p H 2 ~ 10 buffer solution, when p H ≤ 6.0, the P value of Ven was close to 1, > 6.0, the P value of the drug increases significantly with increasing p H. The chemical stability of Ven solution is good when p H is less than or equal to 8.0, the chemical stability is poor under basic pH, and the ionic strength has no effect on the chemical stability of Ven solution. Conclusion: The partition coefficient of oil and water of Ven and the chemical stability of solution are closely related to p H. With a p H of about 7.0, Ven has a high oil-water partition coefficient and chemical stability.