| 人体中氧氟沙星的立体选择性代谢 |
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| 引用本文： | 曾苏,章立.人体中氧氟沙星的立体选择性代谢[J].中国药理学与毒理学杂志,1995,9(2):87-90. |
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| 作者姓名： | 曾苏 章立 |
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| 作者单位： | 浙江医科大学药物分析教研室 |
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| 摘 要： | ５名健康志愿者日服单剂３００ｍｇ氧氟沙星［（±）－Ｏｆ１］后，采用立体选择性的ＲＰ－ＨＰＬＣ手性流动相添加剂法测定尿中Ｓ－（－）－Ｏｆ１和Ｒ－（＋）－Ｏｆ１浓度结果显示Ｏｆ１在人体内呈现立体选择性代谢。尿中排泄的Ｓ－（－）－Ｏｆ１／Ｒ－（＋）－Ｏｆ１之比随时间变化。服药后２ｈＳ／Ｒ是０．８７５，２４ｈ增加到１．１５０．Ｓ－（－）－Ｏｆ１的消除半衰期（ｔ１／２）是４．５７ｈ；消除速率常数（ｋ）是０．１５４ｈ；药时曲线下的面积（ＡＵＣ）为１．１７ｍｇ·ｈ－１．ｍＬ－１；Ｒ－（＋）－Ｏｆ１的ｔ１／２为４．１８ｈ，ｋ为０．１６８ｈ－１，ＡＵＣ是１．７８ｍｇ·ｈ－１·ｍＬ－１；经配对ｔ检验这三对参数间有显著性差异，Ｐ值分别小于０．０１，０．００１和０．００５．因此两对映体在人体内呈现立体选择性处置
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| 关 键 词： | 氧氟沙星 药物代谢 高效液相色谱 对映体 |
Stereoselective metabolism of ofloxacin in human |
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| ZENG Su,ZHANG Li,SHEN Xiang-Zhong,WANG Si-Jiu,LIU Zhi-Qiang.Stereoselective metabolism of ofloxacin in human[J].Chinese Journal of Pharmacology and Toxicology,1995,9(2):87-90. |
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| Authors: | ZENG Su ZHANG Li SHEN Xiang-Zhong WANG Si-Jiu LIU Zhi-Qiang |
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| Abstract: | The stereoselective metabolism of ofloxacin(Of1) was studied in healthy subjects after oral administrationof (±)-Of1 at a dose of 300 mg S-(-)-Of1 and R-(+)-Of1concentrations in urine were determined by RP-HPLC withchiral mobile phase additive. The ratio of SO to R-(+)enantiomer excretions increased with time. with S/ R ratioof 0.88 at 2 h and l. 15 at 24 h. The elimination half-life ofS form was 4.57 h, that was significantly greater (p<0.01)than that of R form (4.18 h). The elimination rate constant(k) of S-(-)-Of1 was lowcr than R(+)Of1. It was foundthat the disposition of Sand ROfl in human beingswas enantioselective although the difference in theirpharmacokinetic parameters was small. |
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| Keywords: | ofloxacin pharmacokinetics high pres-sure liquid chromatography enantiomer |
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