HPLC测定盐酸美金刚胺及其前药的脂水分配系数  

Determination of partition coefficients of memantine hydrochloride and its prodrug PMH

作　　者：曹俊涵[1] 毛惠英[1] 张丹[1] 粟立[1] 李文莉[1] 

机构地区：[1]四川大学华西药学院,四川成都610041

出　　处：《华西药学杂志》2009年第5期536-537,共2页West China Journal of Pharmaceutical Sciences

摘　　要：目的测定盐酸美金刚胺(MH)及其前药(PMH)的脂水分配系数。方法用HPLC法测定脂水两相药物的浓度,采用恒温摇瓶法测定脂水分配系数;色谱柱为Luna C18,流动相为甲醇-水-三乙胺(70:30:0.5,磷酸调pH7),检测波长为225nm,流速1.0 ml.min-1。结果MH及PMH脂水分配系数分别为2.09、227.05。结论PMH的脂水分配系数显著大于MH,证明PMH比MH具有更高的脂溶性,推测其具有良好的血脑屏障通透性。OBJECTIVE To determine the partition coefficients of memantine hydrochloride （MH） and its prodrug （PMH）. METHODS The partition coefficient in trichlormethane/water system was measured using shaking flask method by determining the drug concentrations in two phases. Luna C 18 column（ phenomenex 150 mm× 4.6 mm,5 μm） was used with detection wawelength at 225 nm, and the mobile phase consisted of methane - water - triethylamine （70 ： 30 ： 0.5, adjust to pH7.0 with phosphoric acid）. The flow rate was 1.0 ml·min^ -1. RESULTS The partition coefficients of MH and PMH were 2.09 and 227.05, respectively. CONCLUSION The partition coefficient of PMH is higger than that of MH which proves PMH shows higher liposolubility than MH, and implies that the infiltration ability of MH across BBB is increased in the form of PMH.

关 键 词：盐酸美金刚胺 PMH 脂水分配系数 高效液相色谱法 

分 类 号：R917[医药卫生—药物分析学]