HPLC法测定乳酸氟罗沙星分散片的血药浓度及药动学研究

Determination of lactic acid fleroxacin disket's concentration in blood by HPLC and pharmacokinetics analysis

目的建立乳酸氟罗沙星分散片人体血药浓度的HPLC测定法,研究其药动学。方法血浆样品加入内标,用二氯甲烷提取,HPLC进行分析。色谱柱为HypersiLODS2,流动相为甲醇-10mmol/L的磷酸二氢钠-5mmol/L四丁基溴化铵溶液(磷酸调PH3.0,1:1)(35:65),内标为加替沙星。结果在51.31～3284.00ng/ml内氟罗沙星与内标峰面积的比值与浓度的线性关系良好。批内RSD<6.7%,批间RSD<4.5%;提取回收率为96.29%～98.98%。乳酸氟罗沙星分散片(以氟罗沙星计)的消除半衰期为(14.241.26)h;峰质量浓度为(2307.80419.83)ng/mL;达峰时间为(0.70.1)h。结论本试验所建立的HPLC方法简便、快速、灵敏,可用于乳酸氟罗沙星分散片的人体动力学研究。

Objective To develop a method for determining of Fleroxacin Lactate Dispersible Tablets in plasma. Methods After being mixed with the internal standard fleroxacin, plasma samples were extracted with Dichlormethane and separated by HPLC on HypersiLODS2 with a mobile phase of methanol-10 mmoL/ LNaH2PO4-tetrabutylammoniu bromide（ phosphoric acid PH3.0,1 ： 1 ） ） （ 35 ： 65 ）. In the clinical trial, a single dose of 200 mg was administered orally to 19 healthy volunteers, and the pharmacokinetic parameters of fleroxatin were calculated. Results Calibration curve for fleroxacin was linear over the range of 51.31-3284. 00 ng/ ml. The RSDs of intra- and inter-run were less than 6. 7% and 4. 5% ,respectively. The extraction recovery of fleroxacin in plasma was 96. 29%-98. 98%. The main pharmaeokinetie parameters tl/2 ,tmax and pmax of fleroxaein in human were （ 14. 24 1.26）h, （0. 7 0. 1 ） h and （2307.80 419.83） ng/ml,respectively. Conclusion The assay is proved to be sensitive, accurate and convenient. It can be applied to study the pharmacokinetics of fleroxacin lactate dispersible tablets formulation in human.