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对日本人群中司巴丁氧化情况的进一步分析以及与不同种族人群中观察到的数据进行比较。

Further analysis of sparteine oxidation in a Japanese population and comparison with data observed in different ethnic populations.

作者信息

Horai Y, Ishizaki T, Eichelbaum M, Hashimoto K, Chiba K, Dengler H J

机构信息

Division of Clinical Pharmacology, National Medical Center, Tokyo, Japan.

出版信息

Xenobiotica. 1988 Sep;18(9):1077-84. doi: 10.3109/00498258809042230.

Abstract
  1. Data on the oxidation polymorphism of sparteine (SP) studied in 84 unrelated Japanese subjects of whom two (2.4%) were classified as poor metabolizers (PMs) were re-evaluated. The data were obtained from 6-hour urinary excretion ratios of SP to 2- and 5-dehydrosparteines (DHS), after an oral dose of 100 mg of SP sulphate. 2. Urinary excretion of both SP and DHS correlated with the SP/DHS ratio (rs = 0.862 and -0.756, respectively, P less than 0.001). In addition, urinary excretion of 2-DHS, 5-DHS or total DHS discriminated between PMs and extensive metabolizers (EMs). There was also a highly significant correlation (rs = 0.669, P less than 0.001) between the urinary excretion of 2- and 5-DHS. 3. These re-evaluated results on the oxidation polymorphism of SP indicate that 2- and 5-DHS formation from SP shares a common metabolic pathway (presumably via the same P-450 isozyme), and that the SP/DHS ratio, conventionally used as a discriminating index between PMs and EMs, quantitatively reflects the capacity of 2- and 5-DHS formation. 4. The benefit of using a shorter (6 h) collection period for assessing the individual oxidation phenotype of SP and inter-ethnic comparison of SP oxidation is also discussed.
摘要
  1. 对84名无亲缘关系的日本受试者进行了鹰爪豆碱(SP)氧化多态性研究的数据进行了重新评估,其中两名(2.4%)被归类为慢代谢者(PMs)。数据是在口服100毫克硫酸SP后,通过SP与2-和5-脱氢鹰爪豆碱(DHS)的6小时尿排泄率获得的。2. SP和DHS的尿排泄均与SP/DHS比值相关(rs分别为0.862和-0.756,P<0.001)。此外,2-DHS、5-DHS或总DHS的尿排泄可区分PMs和快代谢者(EMs)。2-和5-DHS的尿排泄之间也存在高度显著的相关性(rs = 0.669,P<0.001)。3. 这些对SP氧化多态性的重新评估结果表明,SP形成2-和5-DHS共享一条共同的代谢途径(可能通过相同的P-450同工酶),并且传统上用作区分PMs和EMs的指标的SP/DHS比值定量反映了2-和5-DHS形成的能力。4. 还讨论了使用较短(6小时)收集期来评估SP的个体氧化表型和SP氧化的种族间比较的益处。

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