汉防己甲素的表观溶解度、油水分配系数和解离常数的测定  

Determination of apparent solubility,apparent partition coefficient and dissociation constant of tetrandrine

作　　者：张颖[1] 姜倩[2] 张焓[3] 宋爱查 蒋学华[2] 

机构地区：[1]中国医药集团总公司四川抗菌素工业研究所,四川成都610052 [2]四川大学华西药学院,四川成都610041 [3]成都军区总医院药剂科,四川成都610061

出　　处：《华西药学杂志》2013年第5期501-503,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的测定汉防己甲素的表观溶解度、油水分配系数和解离常数。方法分别采用平衡溶解度法、摇瓶法测定汉防己甲素在不同pH缓冲液中的表观溶解度和油水分配系数;采用分光光度指示剂法测定其在不同浓度乙醇中的解离常数,并外推至纯水中的解离常数。结果汉防己甲素的表观溶解度随pH的增加而降低;表观油水分配系数随pH的增加而增加;在纯水中的解离常数为8.08。结论汉防己甲素是一个亲脂性很强的碱性药物,其主要口服吸收部位可能在小肠。OBJECTIVE To determine the solubility, oil/water partition coefficient and dissociation constant of tetrandrine. METH- ODS An equilibrium solubility method and shake flask method were established to determine the apparent solubility and oil/water partition coefficients（P）of tetrandrine in phosphoric buffer solutions with different pH, respectively. The dissociation constant （pKa） of tetrandrine in ethanol solution with different concentrations was measured according to spectrophotometric indicator method. RESULTS With pH increased, apparent solubility of tetrandrine was decreased while its apparent P showed the increasing trend. The pKa of tetrandrine in water was 8.08. CONCLUSION Tetrandrine is a strong base with high lipophilia, it＇ s absorption position may be at small intestine.

关 键 词：汉防己甲素 表观溶解度 油水分配系数 解离常数 

分 类 号：R917[医药卫生—药物分析学]