论文部分内容阅读
美沙酮(MET)是一个对μ-阿片受体具有高度亲和力的中枢镇痛药。MET含二个对映体,人肌注或口服该药,R异构体的止痛作用比S异构体强约25倍。由于目前尚无高灵敏的立体选择性分析方法,人们还不清楚这种效价上的差别究竟仅是药效学上不同,还是也涉及到立体选择性的药动学因素。本文提供了一种简便、快速和准确的分析方法。用HPLC手性柱和内标法立体选择性测定人和小猎兔犬(beagle)血浆中MET对映体的含量。
Methadone (MET) is a central analgesic that has a high affinity for μ-opioid receptors. MET contains two enantiomers, human intramuscular injection or oral administration, R isomer analgesic effect than S isomer about 25 times stronger. Because of the lack of highly sensitive stereoselective methods, it is unclear whether this difference in potency is only pharmacodynamically different or involves stereoselective pharmacokinetic factors. This article provides a simple, fast and accurate method of analysis. The stereoselectivity of the MET enantiomer in human and beagle blood plasma was determined by HPLC chiral column and internal standard method.