乙酰天麻素平衡溶解度、油水分配系数及稳定性的测定  

Determination of equilibrium solubility,apparent oil/water partition coefficient and stability of acetagastrodin

作　　者：张琪[1] 黄娟[1] 薛鸿娇 鲍辉[1] 杨兆祥 普俊学 蔡铮[1] 

机构地区：[1]南方医科大学药学院,广东省新药筛选重点实验室,广东广州510515 [2]昆药集团股份有限公司药物研究院,云南昆明650100

出　　处：《中国医院药学杂志》2017年第9期819-821,共3页Chinese Journal of Hospital Pharmacy

基　　金：广东省自然科学基金(编号:2016A030313562)

摘　　要：目的:测定乙酰天麻素平衡溶解度、油水分配系数及水解速率常数,为其制剂设计与吸收机制的研究提供依据。方法:建立乙酰天麻素UPLC分析方法,采用摇瓶法测定乙酰天麻素在不同pH值缓冲液中的平衡溶解度,以及在正辛醇-磷酸盐缓冲溶液中的油水分配系数,并考察其在60℃下不同pH值的水中的稳定性。结果:乙酰天麻素在水中的平衡溶解度约为300μg·mL-1,油水分配系数lgP值约为1.1,pH值的影响较小。乙酰天麻素在强酸性与碱性条件下易水解,在pH值5.0附近较为稳定。结论:乙酰天麻素在水中极微溶解,脂溶性较强,酸碱均可催化其发生水解反应。OBJECTIVE To determine the equilibrium solubility,apparent oil/water partition coefficient（lgP）and the hydrolysis constants of acetagastrodin.METHODS An UPLC method was established to determine the solubility and lgPof acetagastrodin at 37 ℃ at different pH values.The stability of acetagastrodin was tested at 60 ℃in various pH buffers,and then the hydrolysis constants were calculated.RESULTS The solubility of acetagastrodin was about 300 g·mL^-1,and lgP was around 1.1.Both the solubility and lgPof acetagastrodin were slightly affected by pH values.Acetagastrodin was easy to hydrolyze in strong acidic or alkalic solutions and became to stable around pH5.0.CONCLUSION Acetagastrodin is very slightly soluble in water and shows a proper lipophilic character.Both acid and alkali can promote catalytic hydrolytic reaction of acetagastrodin.

关 键 词：乙酰天麻素 平衡溶解度 油水分配系数 稳定性 

分 类 号：R943[医药卫生—药剂学]