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引用本文:沈旭,郑运亮,申屠建中.酸浆苦素L在大鼠体内的药动学研究[J].中国现代应用药学,2017,34(12):1663-1667.
SHEN Xu,ZHENG Yunliang,SHENTU Jianzhong.Pharmacokinetic of Physalin L in Rat Plasma[J].Chin J Mod Appl Pharm(中国现代应用药学),2017,34(12):1663-1667.
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酸浆苦素L在大鼠体内的药动学研究
沈旭1, 郑运亮2, 申屠建中2
1.浙江工业大学, 杭州 310014;2.浙江大学医学院附属第一医院, 杭州 310003
摘要:
目的 建立一种特异、灵敏、快速地检测酸浆苦素L在大鼠体内的药动学特征的LC-MS/MS方法。方法 采用Waters XBridgetm-C18色谱柱(4.6 mm×150 mm,3.5 μm),含有0.1%甲酸的水溶液-乙腈(45:55)为流动相,等度洗脱,流速为0.6 mL·min-1。采用负离子模式、MRM模式进行检测。结果 酸浆苦素L浓度在0.492~493 ng·mL-1与峰面积呈良好线性关系,最低定量限为0.492 ng·mL-1;批间、批内RSD均<7.86%,平均回收率为99.23%~106.73%,方法重复性良好。药动学结果表示,每只SD雄性大鼠灌胃2.0 mg酸浆苦素L后,酸浆苦素L在大鼠体内平均达峰时间tmax为0.69 h,平均药峰浓度Cmax为77.48 ng·mL-1,药时曲线下面积AUC0→t为280.78 ng·h·mL-1,平均半衰期t1/2为2.89 h。结论 本研究探明了酸浆苦素L在大鼠体内的药动学特征,为锦灯笼在动物体内的血药监测提供了一个新的指标,利于研究人员对锦灯笼(尤其是酸浆苦素类化合物)药理活性与药动学的深入研究。
关键词:  酸浆苦素L  液质联用  定量分析  药动学
DOI:10.13748/j.cnki.issn1007-7693.2017.12.004
分类号:R969.1
基金项目:国家自然科学基金资助项目(81402807);高等学校博士学科点专项科研基金(新教师类)(20130101120136)
Pharmacokinetic of Physalin L in Rat Plasma
SHEN Xu1, ZHENG Yunliang2, SHENTU Jianzhong2
1.Zhejiang University of Technology, Hangzhou 310014, China;2.First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou 310003, China
Abstract:
OBJECTIVE To establish a specific, sensitive, efficient method for the quantitative determination of physalin L in rats plasma using LC-MS/MS system, and provide a detection means for its pharmacokinetic characteristic. METHODS The separation of physalin L was performed on a Waters XBridgetm-C18 column (4.6 mm×150 mm, 3.5 μm) with a mobile phase consisted of 0.1% formic acid aqueous solution and acetonitrile (45:50). The assay was based on a negative MRM scan. RESULTS The linear range of the calibration curve (0.492-493 ng·mL-1) was obtained with a good correlation coefficient. The lower limit of quantification was 0.492 ng·mL-1. The average recovery was 99.23%-106.73% and the RSD of intra-and inter-day precision were <7.86%. The repeatability of the method was good. After intragastric administration of 2.0 mg physalin L to each rat, the mean peak time (tmax) was 0.69 h and the mean maximum concentration (Cmax) was 77.48 ng·mL-1. The area under the curve (AUC0→t) was 280.78 ng·h·mL-1, its t1/2 was 2.89 h. CONCLUSION This study provides the physalin L characteristics of pharmacokinetics in rats, whitch is good for researchers on Physalis Calyx Seu Fructus (especially physalin compounds) in-depth study of pharmacological activity and pharmacokinetics.
Key words:  physalin L  LC-MS/MS  quantitative analysis  pharmacokinetic
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