壬苯醇醚-9胶囊在比格犬体内的药代动力学研究  

A Pharmacokinetic Study of a Nonoxynol-9 Capsule in Female Beagle Dogs

作　　者：崔俐俊[1] 范国荣[2] 廖跃华[1] 闻俊[2] 

机构地区：[1]上海医疗器械高等专科学校精密医疗器械系,上海200093 [2]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：《解放军药学学报》2011年第5期404-407,共4页Pharmaceutical Journal of Chinese People's Liberation Army

摘　　要：目的建立一种快速、专属的反相高效液相色谱法测定比格犬血浆中壬苯醇醚-9的浓度,研究壬苯醇醚-9在比格犬体内的药代动力学。方法 6只健康♀比格犬,体质量9.5～10.0 kg,单剂量(192 mg/只)口服给药壬苯醇醚-9自制胶囊,采用DiamonsilTM(钻石)ODS柱(200 mm×4.6 mm,5μm,ID),以甲醇-水(95∶5)作为流动相,流速:1.0 ml/min,聚乙二醇辛基苯基醚为定量内标物,荧光检测的激发波长:226 nm,发射波长:300 nm,柱温:30℃,测定壬苯醇醚-9经时血药浓度,计算药代动力学参数。结果壬苯醇醚-9在0.1～10.0μg/ml范围内线性关系良好,日内、日间精密度均小于10%,低、中、高(0.2、1.0、5.0μg/ml)3种浓度的方法回收率分别为(96.7±7.0)%、(103.4±6.8)%、(101.6±5.3)%。主要药代动力学参数为:t 1/2(11.81±2.94)h,t max(1.75±0.76)h,C max(8.58±1.11)μg/ml,AUC0-24(50.77±14.67)μg.h/ml,AUC0-∞(66.58±25.00)μg.h/ml,MRT(14.84±4.31)h。结论本法简便、灵敏度高、专属性好,可以满足壬苯醇醚-9在比格犬体内的药代动力学研究。Objective To establish a reversed-phase high performance liquid chromatography method for the determination of the plasma concentration of nonoxynol-9 and for the pharmacokinetic study of nonoxynol-9 in healthy female dogs.Methods A single dose of nonoxynol-9 was given to 6 healthy female dogs.Their plasma was collected and the concentration of nonoxynol-9 was determined by reversed-phase high performance liquid chromatography method using DiamonsilTM（diamond） ODS column（200 mm×4.6 mm,5 μm,ID） and a mobile phase of methanol-water（95：5） at a flow rate of 1.0 ml/min.TritonX-100 was used as the internal standard.The excitation and emission wavelengths were 226 nm and 300 nm,respectively.The column temperature was 30℃.Results The calibration curve of nonoxynol-9 showed good linearity over the range of 0.1-10.0 μg/ml.The intra-and inter-day precision was below 10%.The recovery at three concentrations（0.2,1.0,5.0 μg/ml） was（96.7±7.0）%,（103.4±6.8）%,（101.6±5.3）%,respectively.The main pharmacokinetic parameters of nonoxynol-9 were as follows：t1/2（11.81±2.94） h,tmax（1.75± 0.76） h,Cmax（8.58±1.11） μg/ml,AUC0-24（50.77±14.67） μg · h/ml,AUC0-∞（66.58±25.00） μg · h/ml.Conclusion The established method is simple,sensitive and specific,and can be used for the determination of the plasma concentration nonoxynol-9 and for pharmacokinetic studies.

关 键 词：壬苯醇醚-9 药代动力学 反相高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学]