Brewster M E, Anderson W R, Estes K S, Bodor N S, Pop E, Panetta J A
Pharmos Corporation, Alachua, FL 32615, USA.
J Pharm Sci. 1995 Jul;84(7):791-3. doi: 10.1002/jps.2600840702.
The tissue distribution of a butylated phenol antioxidant, LY231617, which has been shown to exert potent neuroprotection action was examined. Preliminary pharmacokinetic examination suggests that LY231617 was eliminated in a biphasic fashion after iv administration to the rat with a distribution half-life of 5 min and an elimination half-life of close to 2.5 h. The volume of distribution of the compound was large (7.4 L), consistent with its lipophilic structure. Dosing paradigms that have historically resulted in pharmacologically relevant activity were examined and were found to generate brain tissue levels of LY231617 of approximately 45 micrograms/g.
已证明具有强效神经保护作用的丁基化苯酚抗氧化剂LY231617的组织分布情况得到了研究。初步药代动力学研究表明，给大鼠静脉注射LY231617后，它以双相方式消除，分布半衰期为5分钟，消除半衰期接近2.5小时。该化合物的分布容积很大（7.4升），与其亲脂性结构相符。对过去曾产生药理学相关活性的给药方案进行了研究，发现这些方案使脑组织中LY231617的水平达到约45微克/克。
