- 著者
- KAZUO IGARASHI FUMIYO KASUYA MIYOSHI FUKUI
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Journal of Pharmacobio-Dynamics (ISSN:0386846X)
- 巻号頁・発行日
- vol.6, no.8, pp.538-550, 1983 (Released:2008-02-19)
- 参考文献数
- 16
- 被引用文献数
- 3 4
The metabolism of dibucaine was studied in the rat, rabbit and man. A total of ten basic metabolites other than dibucaine were detected in the urine samples of three species by thin-layer chromatography (TLC) and gas chromatography (GC), and structures of these metabolites were identified by comparison of the properties given by TLC, GC and gas chromatography-mass spectrometry (GC-MS) with those of authentic compounds. Four of these metabolites were new metabolites which were found in the rabbit or human urine ; two were identified as the 2', 3'-dihydroxybutoxy product (M-6, diol) and its N-deethyl product (M-2), and others were identified as the 2'-hydroxyethoxy product (M-8, alcohol) and its N-deethyl product (M-3). One of the two hydroxyl groups on M-5 was at 6-position on the quinoline ring, while another was assumed to be at 3'-position on the O-alkyl side chain. There were apparent species differences with regard to the major metabolites found in each species ; i.e. M-10 and M-5 in rat, M-6 and M-4 in rabbit, and M-8 and M-4 in man. Small amounts of the conjugated basic metabolites were observed in the urine of all three species. The new metabolic pathways to the diols (M-2 and M-6) or the alcohols (M-3 and M-8) were also discussed.
- 著者
- KAZUO IGARASHI FUMIYO KASUYA MIYOSHI FUKUI HISASHI NANJYOU
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.35, no.7, pp.3033-3036, 1987-07-25 (Released:2009-10-19)
- 参考文献数
- 9
- 被引用文献数
- 4 5
A high-performance liquid chromatographic (HPLC) method using a fluorescence detector is described for the simultaneous determination of dibucaine and its metabolites (M-4, M-8 and M-10) in human urine. Urine samples from obstetric patients were chromatographed in a reversed-phase system. When a ultraviolet detector (320 nm) was used, some interfering peaks appeared on the chromatogram, but this interference could be overcome by employing a fluorescence detector (Ex 330 nm and Em 440 nm) instead. The calibration curves were linear in the range of 0.05-5.0 μg/ml for all compounds and the detection limits of dibucaine and its metabolites were about 5 ng/ml in urine. The urinary excretion of dibucaine and its metabolites by obstetric patients infused with Percamine S® in the spinal cord were determined. The mean cumulative amounts of dibucaine, M-4, M-8 and M-10 excreted during 10 h after administration were 1.1, 10.5, 3.5 and 1.1 % of the dose, respectively. The total urinary excretion was 16.2% of the dose. This method is sufficiently sensitive and specific to permit the determination of dibucaine and its metabolites in biological fluids.