| 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2.0~2.2 kg)单剂量(64 mg/只)阴道给药NP-9栓剂;取血浆经预处理后采用DiamonsilTM ODS柱(200 mm×4.6 mm,5 μm),以甲醇-水(955)作为流动相,流速 1.0 ml/min,荧光检测的激发波长226 nm,发射波长300 nm,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0.05～5.00 μg/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、2.00 μg/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。 |
| 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 |
| DOI：10.3724/SP.J.1008.2009.0549 |
| 投稿时间：2008-10-17修订日期：2009-02-24 |
| 基金项目: |
|
| RP-HPLC in determination of plasma nonoxynol-9 level in New Zealand rabbit and its application in pharmacokinetic study |
| CUI Li-jun,WEN Jun,ZHOU Ting-ting,WANG Shuo-wen,FAN Guo-rong* |
| (Department of Pharmaceutical Analysis,Shanghai Key Laboratory for Pharmaceutical Metabolite Research,School of Pharmacy,Second Military Medical University,Shanghai 200433,China) |
| Abstract: |
| 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 (955) 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 0.05-5.00 μg/ml; both the intra- and inter-day precisions were lower than 10%. The recovery rates at three concentrations (0.10,0.50,and 2.00 μg/ml) were (101.67±8.12)%,(100.84±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,AUC0-12 (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. |
| Key words: nonoxynol-9 plasma concentration pharmacokinetics RP-HPLC |
