摘要
目的:建立大鼠血浆中瑞格列奈浓度的HPIC测定方法,并研究瑞格列奈在大鼠体内药物动力学行为。方法:血浆样品经酸化后,加入内标物,用醋酸乙酯提取,色谱柱为Kromasil C_(18)(150mm×4.6 mm,5 μm),流动相为0.1mol·L^(-1)柠檬酸-醋酸钠缓冲液(pH 4.0)-甲醇(27:73),流速为1.0mL·min^(-1),紫外检测波长243 nm,进样量20μL。测定了12只受试大鼠单剂量灌服瑞格列奈4 mg后血药浓度-时间过程。结果:最低检测为2.5 ng·mL^(-1),相对回收率平均为97.85%,日间和日内的变异系数小于5,线性范围为2.5～100 ng·mL^(-1),符合生物样品分析的要求。受试大鼠灌服瑞格列奈片4 mg后,估算的末端相半衰期(0.83±0.16)h,t_(max)(0.75±0.41)h,C_(max)(48.6±15.7)ng·mL^(-1)。结论:建立的HPLC方法适合于血浆中瑞格列奈浓度的测定及药动学研究。
OBJECTIVE To establish a reversed phase HPLC method for determination of repaglinide and to study pharmacokinetics of repaglinide in rats. METHODS The drug was acidfied and then cxtracted from plasma with acetate ether. The chromatography analysis was performed on an Kromasil C18 column（Ф150mm×4.6mm,5μm）was used. Mobile phase consisted of 27% 0. 10 mol.L i citrate acid-sodium acetate buffer （pH 4. 0） and 73% methanol ,with a flow rate of 1.0 mL-min-1. The UV detection wavelength was 243 nm and the injection volume was 20 μL. RESULTS The recoveries of repaglinide from plasma were 97. 8% and RSD of intra-day and inter-day were less than 5%. Calibration curves were linear in the range of 2. 5- 100 ng.mL-1 （r = 0. 998 6）and the minimum detection concentration was 2. 5 ng-mL 1. The pharmacokinetics of repaglinide in 12 rats was studied. After oral admin/stration of 4 mg repa g,linide tablet, the pha rmacokinetics parameters were estimated as follows：t1/2 （0. 83 ± 0. 16）h,tmax （0. 75 ± 0. 41）h,Cmax （48. 6± 15.7）ng.mL-1. CONCLUSION A reliable and rugged simultaneous HPLC assay for repaglinide was developed. The assay method was convenient for clinical laboratory.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2011年第19期1583-1585,共3页
Chinese Journal of Hospital Pharmacy
