摘要
萘丁美酮（Ｎａｂｕｍｅｔｏｎｅ，ＮＡＢ）为一新型非甾体抗炎前体药物，本文通过整体实验，采用高效液相色谱法，测定犬服药后门静脉和股静脉中ＮＡＢ和其主要活性代谢物６－甲氧基－２－萘乙酸（６－ＭＮＡ），来评价ＮＡＢ的肝首过代谢，结果表明：萘丁美酮几乎全部从肝脏代谢，在外周血液（股静脉中不能测出ＮＡＢ原形药物。同时采用平衡透析法，测定了６－ＮＭＡ蛋白结合率，６－ＭＮＡ的浓度在５～４０μｇ／ｍｌ范围内，血浆蛋白结合率为９２．７９ｇ～９８．１１％。
Nabumetone(NAb)is a novel non-steroidal anti-inflammatory
prodrug.To evaluate its first-pass hepatic metabolism,We have determined nabumetone and its
major active metabiolite(6-MNA)in portal and femoral vein of dogs after oral admin-istration (80
mg/kg).The results indicated that unchanged nabumetone was not detectable in femoral vein and
undergone ex-itensive first-pass metabiolism. The protein binding rate of 6-MNA was 92. 79%～98.
11%when 6-MNA level was in 5～4oμg/mg.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
1995年第4期149-151,共3页
Chinese Journal of Hospital Pharmacy
