反相高效液相色谱法测定新西兰兔血浆中壬苯醇醚-9的浓度及其药代动力学研究  

RP-HPLC in determination of plasma nonoxynol-9 level in New Zealand rabbit and its application in pharmacokinetic study

作　　者：崔俐俊[1] 闻俊[1] 周婷婷[1] 汪硕闻[1] 范国荣[1] 

机构地区：[1]第二军医大学药学院药物分析学教研室,上海市药物代谢产物研究重点实验室,上海200433

出　　处：《第二军医大学学报》2009年第5期549-552,共4页Academic Journal of Second Military Medical University

摘　　要：目的:建立兔血浆中壬苯醇醚-9(NP-9)的反相高效液相色谱(RP-HPLC)方法,研究NP-9栓剂在健康雌性新西兰兔体内的药代动力学。方法:6只健康雌性新西兰兔(体质量2.0～2.2kg)单剂量(64mg/只)阴道给药NP-9栓剂;取血浆经预处理后采用DiamonsilTM ODS柱(200mm×4.6mm,5μm),以甲醇-水(95:5)作为流动相,流速1.0ml/min,荧光检测的激发波长226nm,发射波长300nm,柱温30℃,测定NP-9经时血药浓度,计算药代动力学参数。结果:NP-9在0.05～5.00μg/ml范围内线性关系良好,日内、日间精密度均小于10%,低、中、高3种浓度(0.10、0.50、2.00μg/ml)的方法回收率分别为(101.67±8.12)%、(100.84±5.42)%、(100.29±3.81)%。主要药代动力学参数为:t1/2(3.75±0.87)h,tmax(3.2±0.4)h,Cmax(2.75±0.32)μg/ml,AUC0～12(12.72±2.14)μg.h.ml-1,AUC0～∞(15.05±2.84)μg.h.ml-1,平均滞留时间(6.85±1.13)h。结论:本方法简便、灵敏、专属性好,可用于NP-9栓剂在健康雌性新西兰兔体内的药代动力学研究。Objective： To establish a RP-HPLC method for determining the plasma concentration of nonoxynol-9 and to apply the method in studying the pharmacokinetics of nonoxynol-9 in healthy female rabbits. Methods： A single dose of nonoxynol-9 （64 mg to each animal） was given to 6 healthy female rabbits （weighing 2.0-2.2 kg） via vagina. The plasma samples were collected and the concentrations of nonoxynol 9 were determined by RP-HPLC method using DiamonsilTM ODS column （200 mm×4.6 mm,5 μm） and mobile phase of methanol water （95 ： 5） at a flow rate of 1.0 ml/min. The excitation and emission wavelengths were 226 nm and 300 nm, respectively. The column temperature was 30℃. The pharmacokinetic parameters were calculated. Results： The calibration curve of nonoxynol-9 showed good linearity over the range of 0.05-5.00μg/ml; both the intra- and inte-day precisions were lower than 10%. The recovery rates at three concentrations （0.10,0.50, and 2.00μg/ml） were （101.67± 8.12）%, （100.8±5.42）% ,and （100.29±3.81）%, respectively. The main pharmacokinetic parameters of nonoxynol-9 were as following： t1/2 （3. 75±0. 87） h, tmax（3. 2±0. 4） h, Cmax（2. 75±0. 32） μg/ml, AUC012 （12.72±2.14）μg·h·ml^-1,AUC0-∞（15.05±2.84）μg·h·ml^-1,and MRT （6. 85±1. 13） h. Conclusion： The established method is convenient,sensitive and specific,and can be used for determination of plasma nonoxynol-9 concentration and for its pharmacokinetic studies in rabbits.

关 键 词：壬苯醇醚-9 血药浓度 药代动力学 反相高效液相色谱法 

分 类 号：R969.11[医药卫生—药理学]