Song Yonggui, Su Dan, Lu Tulin, Mao Chunqin, Ji De, Liu Yali, Wei Binbin, Fan Ronghua
The National Pharmaceutical Engineering Center for Solid Preparation in Chinese Herbal Medicine, Jiangxi University of Traditional Chinese Medicine, Nanchang, China; College of Chemistry and Chemical Engineering, Jiangxi Normal University, Nanchang, China.
J Sep Sci. 2014 Feb;37(4):352-9. doi: 10.1002/jssc.201300886. Epub 2014 Jan 6.
Opioid and ephedra alkaloids known as the active ingredients for Keke capsule, which is used to treat coughs and bronchial asthma, could have potential adverse effects on the central nervous system. Therefore, an efficient, sensitive rapid-resolution LC-MS/MS method for the simultaneous determination of morphine, ephedrine, and pseudoephedrine in rat plasma and brain tissue homogenate has been developed. The method was validated in the plasma and brain tissue samples, showed good linearity over a wide concentration range (r(2) > 0.99). The intra- and interday assay variability was less than 15% for all analytes, and the accuracy was between -8.8 and 5.7%. The study provided the pharmacokinetics profiles and the brain regional distribution of the three active alkaloids after oral administration of Keke capsule. The results also indicated that significant difference in pharmacokinetics parameters of the epimers was observed between ephedrine and pseudoephedrine.
可待因胶囊用于治疗咳嗽和支气管哮喘，其活性成分阿片类药物和麻黄生物碱可能对中枢神经系统产生潜在不利影响。因此，已开发出一种高效、灵敏的快速液相色谱-串联质谱法，用于同时测定大鼠血浆和脑组织匀浆中的吗啡、麻黄碱和伪麻黄碱。该方法在血浆和脑组织样本中得到验证，在较宽浓度范围内显示出良好的线性关系（r(2)>0.99）。所有分析物的日内和日间测定变异系数均小于15%，准确度在-8.8%至5.7%之间。该研究提供了口服可待因胶囊后三种活性生物碱的药代动力学特征和脑区分布。结果还表明，麻黄碱和伪麻黄碱的差向异构体在药代动力学参数上存在显著差异。
