7-乙基-10-羟基喜树碱与大鼠血浆蛋白结合率的测定  

Determination of the Plasma Protein Binding Rate of 7-Ethyl-10-hydroxycamptothecin to Rats

作　　者：银晓晶 YIN Xiao-jing(Department of Pharmacy,Cancer Hospital of China Medical University,Liaoning Cancer Hospital and Institute,Shenyang Liaoning 110042,China)

机构地区：[1]中国医科大学肿瘤医院,辽宁省肿瘤医院药学部,辽宁沈阳110042

出　　处：《当代化工》2022年第2期366-369,共4页Contemporary Chemical Industry

摘　　要：为了建立7-乙基-10-羟基喜树碱(SN-38)血浆蛋白结合率的测定方法,采用平衡透析法模拟SN-38在人体内与血浆蛋白结合的过程,并以HPLC法测定SN-38在透析袋内血浆中的药物浓度与透析袋外缓冲液中的浓度;透析内液用含0.5%乙酸的乙腈沉淀蛋白,透析内液过滤后直接测定。结果表明:透析内液和透析外液在25~5000 ng·mL^(-1)范围内线性关系良好;提取回收率大于80%;SN-38与大鼠血浆蛋白结合率为49.9%~59.1%,平均为55.3%。SN-38与大鼠血浆蛋白结合率相对较高,建立的方法灵敏度高,重现性好,操作简单。In order to establish a method for determining the plasma protein binding rate of 7-ethyl-10-hydroxycamptothecin(SN-38),equilibrium dialysis was used to simulate the process of SN-38 binding to plasma protein in human body,and the drug mass concentration of SN-38 in plasma of dialysis bag and buffer fluid outside dialysis bag were determined by HPLC.Proteins of dialysis fluid inside were precipitated with acetonitrile containing 0.5%acetic acid.The results showed that there was a good linear relationship between the internal and external dialysis fluids in the range of 25~5000 ng·mL^(;).The extraction recovery was more than 80%.The binding rate of SN-38 to plasma protein was 49.9%~59.1%,with an average of 55.3%.So SN-38 has a relatively high binding rate with plasma protein of rats,and the established method has high sensitivity,good reproducibility and simple operation.

关 键 词：7-乙基-10-羟基喜树碱 平衡透析法 血浆蛋白结合率 高效液相色谱法 

分 类 号：R28[医药卫生—中药学]