本文選題：丁酸氯維地平　切入點：氯維地平酸　出處：《中國藥科大學學報》2015年03期

【摘要】：研究丁酸氯維地平脂微球(CDB-LM)注射液在小鼠體內(nèi)的藥代動力學過程,探討丁酸氯維地平(CDB)在體內(nèi)的代謝規(guī)律。采用HPLC-FLD法同時測定CDB及其代謝物氯維地平酸(MI)在小鼠全血樣品中的濃度。色譜柱Waters C18(4.6 mm×150 mm,5μm);流動相:乙腈-甲醇-磷酸鹽緩沖液(2∶1∶2);FLD檢測波長:激發(fā)波長358 nm,發(fā)射波長440 nm。采用DAS 2.0軟件分析計算出CDB和MI的藥代動力學參數(shù),所得參數(shù)采用PASW Statistics 18軟件進行統(tǒng)計分析。結果表明,CDB和MI的半衰期分別在4 min和20 min左右。低劑量組和高劑量組的藥代動力學參數(shù)依次為:CDB的CL為4.21和2.72 L·min-1·kg-1,AUC0-t為3.86和6.43 mg/L·min,MRT0-t為7.09和6.17 min。MI的CL為0.34和0.22 L·min-1·kg-1,AUC0-t為52.23和74.90 mg/L·min,MRT0-t為201.24和217.33 min。采用乙腈沉淀蛋白法處理全血樣品,操作簡單快速,全血中內(nèi)源性雜質(zhì)無干擾,方法準確可靠。體內(nèi)研究結果表明,建立的HPLC-FLD法簡便、靈敏,可同時測定CDB和MI的血藥濃度。高、低兩劑量組的血藥濃度-時間曲線趨勢相同,CDB在體內(nèi)迅速代謝為MI。
[Abstract]:To study the pharmacokinetic process of clonvedipine butyrate (CDB-LM) injection in mice and to study the metabolism of clonvedipine butyrate (CDB) in vivo.The concentration of CDB and its metabolite chlorvedipine in whole blood samples of mice was determined by HPLC-FLD.The mobile phase consisted of acetonitrile-methanol-phosphate buffer (2: 1: 2), the detection wavelength was 358 nm and the emission wavelength was 440 nm.The pharmacokinetic parameters of CDB and MI were calculated by DAS 2.0 software, and the parameters were analyzed by PASW Statistics 18 software.The results showed that the half-life of CDB and MI were about 4 min and 20 min, respectively.浣庡墏閲忕粍鍜岄珮鍓傞噺緇勭殑鑽唬鍔ㄥ姏瀛﹀弬鏁頒緷嬈′負:CDB鐨凜L涓，

本文編號：1707354