磷酸哌喹分散片的处方前研究  

Preformulation Study on Piperaquine Phosphate Dispersible Tablets

作　　者：唐嘉曦 许小红[1] Tang Jiaxi;Xu Xiaohong(School of Pharmacy,Chengdu Medical College,Chengdu 610500,China)

机构地区：[1]成都医学院药学院,成都610500

出　　处：《成都医学院学报》2019年第2期178-181,共4页Journal of Chengdu Medical College

摘　　要：目的阐明磷酸哌喹原料药的基本理化性质,为设计分散片优良的处方提供依据。方法采用HPLC测定磷酸哌喹含量,分别进行磷酸哌喹的平衡溶解度、油水分配系数、吸湿性考察、破坏性试验和稳定性试验等处方前研究。结果磷酸哌喹原料药的溶解度随pH值增大呈减小趋势;磷酸哌喹在pH(1.0～4.5)中的油水分配系数<0,在pH(5.8～8.0)中的油水分配系数>0;在25℃,RH80%条件下吸湿性较小;磷酸哌喹在酸、碱、氧化溶液中相对稳定,高温、高湿条件下也相对稳定,光照易变色。结论本研究结果可为磷酸哌喹分散片处方设计及工艺研究提供实验依据。Objective To elucideat the basic physiochemical properties of piperaquine phosphate and provide evidence for designing dispersible tablets. Methods The content of piperaquine phosphate was determined by high performance liquid chromatography (HPLC). The preformulation studies on the equilibrium solubility, oil-water partition coefficient, hygroscopicity, destructive test and stability test of piperaquine phosphate were carried out respectively. Piperaquine phosphate is relatively stable in acid, alkali and oxidation solutions, and is relatively stable under high temperature and humidity conditions, and the light is easily discolored. Results The solubility of piperaquine phosphate active pharmaceutical ingredient (API) decreased with the increase of pH value. The oil-water partition coefficient of piperaquine phosphate was less than zero when the pH value was between 1.0 and 4.5 and greater than zero when the pH value was between 5.8 and 8.0. Its hygroscopicity is small under the condition of RH80% at the temperature of 25 °C. Piperaquine phosphate was relatively stable in the acid, alkali, and oxidation solutions and it was also relatively stable under the condition of high temperature and high humidity. The color of piperaquine phosphate was easily changed under light. Conclusion The results of this study can provide experimental evidence for the formulation design and process research of piperaquine phosphate dispersible tablets.

关 键 词：磷酸哌喹 处方前研究 HPLC 

分 类 号：R943[医药卫生—药剂学]