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细胞色素P4501A2活性与奥氮平代谢的相关性研究 被引量:5

Study on correlation of cytochrome P4501A2 activity with olanzapine disposition in healthy volunteers
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摘要 目的研究奥氮平(抗精神病药)体内代谢与细胞色素P450酶亚型1A2(CYP1A2)活性的相关性。方法15例男性健康志愿者单次口服咖啡因150mg,第5 h末采血;2天后单次口服奥氮平10 mg,收集血样;用高效液相色谱电化学法测定奥氮平血浆浓度,紫外法测定咖啡因及其代谢产物次黄嘌呤的血浆浓度。结果次黄嘌呤与咖啡因的比值与奥氮平清除的奥氮平AUC0,96的倒数不相关(γ=0.057,P=0.84)。结论CYP1A2酶活性与奥氮平体内代谢不相关。 Objective To study the relationship between olanzapine disposition and CYP1A2 activities by a caffeine test. Methods Fifteen male normal volunteers took a single oral dose of 150 mg caffeine and plasma samples were collected at the 5th hours after administration of caffeine. With a washout interval of two days, the subjects received a single oral dose of olanzapine 10 mg. The plasma samples were collected. The concentration of olanzapine was detected by high - performance liquid chromatography with electrochemical detection (HPLC - ECD ). The concentration of paraxanthine (17X) and caffeine (137X) were measured by ultraviolet spectroscopy (UV). Results The indexes of CYP1 A2 activities, by the ratios of caffein's disposition (paraxanthine) and caffeine in plasma, were uncorrelated with reciprocals of olanzapine AUC0.96 (T = 0. 057, P = 0. 84 ). Conclusions It is concluded that CYP1 A2 may be not involved in olanzapine disposition in vivo.
出处 《中国临床药理学杂志》 CAS CSCD 北大核心 2009年第3期239-241,共3页 The Chinese Journal of Clinical Pharmacology
基金 北京卫生扶持学科基金资助项目 首都医学发展科研基金资助项目(ZD199816)
关键词 奥氮平 代谢 细胞色素P450 咖啡因 olanzapine disoosition cytochrome P450 caffeine
作者简介 于靖(1969-),女,副主任医师,主要从事精神科临床工作 通讯作者:王传跃,主任医师,博士生导师Tel:(010)58303195 E-mail:wang.cy@163.net
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