Pharmacokinetic difference between S-(+)- and R-(-)-etodolac in rats

来源 :Acta Pharmacologica Sinica | 被引量 : 0次 | 上传用户:abczvw
下载到本地 , 更方便阅读
声明 : 本文档内容版权归属内容提供方 , 如果您对本文有版权争议 , 可与客服联系进行内容授权或下架
论文部分内容阅读
AIM: To study whether etodolac enantiomers have pharmacokinetic difference after oral administration. METHODS: Fourteen rats, divided into two groups randomly, were orally given S-(+)- or R-(-)-etodolac at a single dose of 20 mg/kg, respectively. Blood samples were collected before and at 5, 10, 20, 30 min and 1, 3, 6, 12, 24, 48, 72 h after treatment. The plasma samples were analyzed with a high-performance liquid chromatographic method. RESULTS: The calibration curves were linear in the range of 0.5-50.0 mg/L (r=0.9999) to S-(+)-etodolac and 2.0-200.0 mg/L (r=0.9999) to R-(-)-etodolac, respectively. The main pharmacokinetic parameters of S-(+)- and R-(-)-etodolac were as follows: t1/2(λz)18±4 h vs 19.4±2.2 h, tmax 3.3±2.6 h vs 4±4 h; Cmax 29±6 mg/L vs97±14 mg/L, AUC0-t 706±100 h·mg·L-1 vs 2940±400 h·mg·L-1, CL(s) 0.030±0.006 L·kg-1·h-1 vs 0.0065±0.0010 L·kg-1·h-1 and V/F 0.25±0.22 L·kg-1 vs 0.03±0.05 L·kg-1. There was no significant difference in t1/2(λz) and tmax between S-(+)- AIM: To study whether etodolac enantiomers have pharmacokinetic difference after oral administration. METHODS: Fourteen rats divided into two groups randomly, were orally given S - (+) - or R - (-) - etodolac at a single dose of 20 mg / kg, respectively. Blood samples were collected before and at 5, 10, 20, 30 min and 1, 3, 6, 12, 24, 48, 72 h after treatment. The plasma samples were analyzed with a high-performance liquid chromatographic method . RESULTS: The calibration curves were linear in the range of 0.5-50.0 mg / L (r = 0.9999) to S - (+) - etodolac and 2.0-200.0 mg / The main pharmacokinetic parameters of S - (+) - and R - (-) - etodolac were as follows: t1 / 2 (λz) 18 ± 4 h vs 19.4 ± 2.2 h, tmax 3.3 ± 2.6 h vs 4 ± 4 h; Cmax 29 ± 6 mg / L vs 97 ± 14 mg / L, AUC0-t 706 ± 100 h · mg · L-1 vs 2940 ± 400 h · mg · L-1, CL L · kg -1 · h -1 vs 0.0065 ± 0.0010 L · kg -1 · h -1 and V / F 0.25 ± 0.22 L · kg -1 vs 0.03 ± 0.05 L · kg -1 There was no significant difference in t1 / 2 (λz) and tmax between S - (+) -
其他文献
病历摘要患者男,53岁。1984年5月入院。患者于3年前曾因受凉而发热、心悸,经服中药无效,故在某医院按风湿性心脏病治疗40天好转出院。出院后多次出现心悸、咳嗽,尤在受凉或
肿瘤免疫方面的最新进展表明,有效的抗肿瘤免疫需要天然免疫和获得性免疫的协同作用。我们在前期工作中成功制备了小鼠β-防御素2(MBD2)和IL-18基因修饰的白血病疫苗,并证实
采用引入外电场微扰的量子化学方法,对具有A型和B型碳链结构聚乙炔电子的极化率进行了推算。其中,A型为碳─-碳单双键交替结构,B型为碳-碳键长均一型结构。结果表明,B型聚乙炔电子的极化
全国规模庞大、历史悠久的摩托车及配件展示交易会——第22届(2002春季)全国摩托车及配件展示交易会于2002年4月8~10日在美丽的奥运水上城市青岛市国际会展中心召开。这是摩
用频谱分析磨床砂轮主轴振动故障北京轴承研究所果占平,崔程久,刘尔膺SpectrumAnalysisforVibrationTroubleofWheelSpindle¥GuoZhanping,etalAbstract:Determinationofpr... Spectrum analysis grinding wheel spindle vibration fault Beijing Institute of Bearing fruit a
随着电力和电子技术的飞速发展,相应的元器件向高频化、小型化、高效率和节能的方向发展,从而对元器件用材料也提出了更高要求。为此,本文概述了冶金部钢铁研究总院近年来所研究
2016年高考,广东采用全国卷,本届高三师生面临着很大的压力,特别是物理,总体难度比广东卷要大;虽更利于分层学生,但对大多数高三学生来说,则充满挑战。选好题,是提高高三复习
用不同方法制备了淀粉-丙烯腈接枝共聚物水解产物,测定了其X衍射曲线。用5种非晶态表征函数进行了理论计算,由Hindeleh多项式得到最好结果。确定了Hindeleh多项式的结构参数,并用此多项式进行了曲线
前不久,著名女中音歌唱家关牧村参加了文化部主办的艺术歌曲演唱会。“我深深地爱着你,这片多情的土地……”那浑厚、凝重、激越的歌声,带着浓烈的东方神韵和民族自豪感。有些老
刘少奇同志是伟大的马克思主义者和无产阶级革命家,是中国共产党和中华人民共和国的主要领导人之一。1921年,他就加入了刚刚创立的中国共产党,是我党最早的党员之一。解放前,