[利用高场核磁共振波谱法分析大鼠尿液中布洛芬（R）-对映体的立体选择性代谢产物]
[Use of high-field nulear magnetic resonance spectroscopy for the analysis of stereoselective metabolites of ibuprofen (R)-enantiomer in rat urine].
作者信息
Yang C, He W Y, Kong M, Xu R M, Zhang S R, Si Y K
机构信息
Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
出版信息
Yao Xue Xue Bao. 2000 Nov;35(11):843-6.
AIM
To study the metabolic chiral inversion and chiral metabolites of R-(-)-ibuprofen.
METHODS
Following administration of R-(-)-ibuprofen (250 mg.kg-1), analysis was performed on rat urine purified extracts obtained by solid phase extraction onto C-18 bonded silica gel, then the metabolites of ibuprofen were detected and identified by 1HNMR spectroscopy.
RESULTS
Except for a little ibuprofen, there were 2'-hydroxy-ibuprofen and its glucuronide, 1'-carboxy-ibuprofen glucuronide and ibuprofen glucuronide in rat urine. 2'-hydroxy-ibuprofen is the main metabolite. 1'-carboxy-ibuprofen glucuronide and ibuprofen glucuronide were diastereoisomers.
CONCLUSION
There was the phenomenon of metabolic chiral inversion, whereby the R-enantiomer is transformed in vivo to its active S-antipode via an unusual process.
目的
研究R-(-)-布洛芬的代谢手性转化及手性代谢产物。
方法
给予大鼠R-(-)-布洛芬（250 mg·kg-1）后，对通过C-18键合硅胶固相萃取得到的大鼠尿液纯化提取物进行分析，然后用1HNMR光谱法检测并鉴定布洛芬的代谢产物。
结果
大鼠尿液中除少量布洛芬外，还有2'-羟基布洛芬及其葡萄糖醛酸苷、1'-羧基布洛芬葡萄糖醛酸苷和布洛芬葡萄糖醛酸苷。2'-羟基布洛芬是主要代谢产物。1'-羧基布洛芬葡萄糖醛酸苷和布洛芬葡萄糖醛酸苷为非对映异构体。
结论
存在代谢手性转化现象，即R-对映体通过一个不寻常的过程在体内转化为其活性S-对映体。
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