@article{oai:fukuyama-u.repo.nii.ac.jp:00008776,
 author = {五郎丸, 毅 and 柿原, 良枝 and 本屋敷, 敏雄},
 issue = {31},
 journal = {福山大学薬学部研究年報, Annual report of the Faculty of Pharmacy & Pharmaceutical Sciences, Fukuyama University},
 month = {Dec},
 note = {<sup>13</sup>C標識テオフィリン(TP)経口投与後のヒト尿中代謝物の<sup>13</sup>C-NMRによる定量を検討した。腎及び肝機能正常な5人の男性被験者に<sup>13</sup>C標識テオフィリン(1，7-ジメチル-<sup>13</sup>C<sub>2</sub>-キサンチン)50mgを投与し，Sep-Pac Vac RCカラムにより固相抽出した。抽出試料より未変化TP及び1，3-ジメチル尿酸(13U)，3-メチルキサンチン(3X)，1-メチル尿酸(1U)をNMRにより特異的に検出できた。<sup>13</sup>C標識代謝物標品と内部標準として［3-メチル-<sup>13</sup>C］カフェイン(3-<sup>13</sup>C-CF)のシグナル積算値の比はそれらのモル比に比例した。他の代謝物についても同様の関係が成立するものと推定される。<sup>13</sup>C標識TPの尿中代謝物の定量結果より，喫煙者と非喫煙者の間には肝臓のCYP1A2活性を反映した著しい個人差が認められた。薬物代謝研究において，<sup>13</sup>C-NMR法は代謝物の検索及び定量に有用であることが認められた。, Determination of human urinary metabolites after oral administration of <sup>13</sup>C-labeled theophylline (TP) was examined by <sup>13</sup>C-NMR spectroscopy. <sup>13</sup>C-labeled TP(1,7-dimethyl-<sup>13</sup>C<sub>2</sub>-xanthine)was administered at a dose of 50mg to 5male volunteers who have normal hepatic and renal functions. Urinary samples were prepared by solid phase extraction with Sep-Pac Vac RC columns. NMR spectra of the urinary extracts indicated the specific resonances signals of unchanged TP and its main metabolites, 1, 3-dimethyluric acid(13U), 3-methylxanthine(3X) and 1-methyluric acid(1U). The integral signal intensity ratio of authentic <sup>13</sup>C-labeled metabolites to [3-methyl-<sup>13</sup>C] caffeine(3-<sup>13</sup>C-CF) as an internal standard was directly proportional to the molar ratio of the compounds. Similar relationship was expected to other metabolites. From the results of quantification of urinary metabolites of <sup>13</sup>C-labeled TP, remarkable individual difference was observed in the urinary excretion of metabolites between smoker and nonsmoker due to influence of hepatic CYP1A2 activity. In drug metabolism study, <sup>13</sup>C-NMR spectroscopy with <sup>13</sup>C-tracer was useful technique for detection and quantification of the metabolites.},
 pages = {43--43},
 title = {^<13>C標識テオフィリン服用後のヒト尿中代謝物のNMRによる定量(発表論文抄録(2012))},
 year = {2013}
}