Desiderio C, Fanali S
Istituto di Cromatografia, C.N.R., Roma, Italia.
Boll Chim Farm. 1995 Nov;134(10):541-6.
Biological fluids drugs analysis are important to investigate the pharmacokinetic and pharmacodynamic of the subministered compounds for the comprehension of their behaviour and bioavailability. Many pharmaceutical preparations contain a chiral molecule as active compound often as racemic mixture of the two enantiomers of which only one exhibits pharmacological effect, the other enantiomer being inactive or responsible of toxicological effects. In fact two enantiomers with almost identical physical and chemical properties can exhibit a different behaviour in an highly stereoselective environment as the human body. With respect to the analytical methods in use for chiral separation Capillary Electrophoresis shows high efficiency and resolution together with feasibility, low costs and very short analysis time. CE and MEKC have been used for enantiomers resolution of antihypertensive and anticoagulant drugs in body fluids. By cyclodextrin modified MECK the separation of mephenytoin and 4-hydroxymephenytoin metabolite in urine samples has been performed in order to identify different phenotypes in the oxidative metabolising ability in man.
生物流体药物分析对于研究给药化合物的药代动力学和药效学非常重要,有助于理解其行为和生物利用度。许多药物制剂含有手性分子作为活性化合物,通常是两种对映体的外消旋混合物,其中只有一种表现出药理作用,另一种对映体无活性或具有毒理学作用。事实上,两种物理和化学性质几乎相同的对映体在人体这种高度立体选择性的环境中可能表现出不同的行为。关于用于手性分离的分析方法,毛细管电泳具有高效率、高分辨率,同时具有可行性、低成本和极短的分析时间。毛细管电泳(CE)和胶束电动毛细管色谱(MEKC)已用于体液中抗高血压和抗凝药物对映体的拆分。通过环糊精修饰的MEKC,已对尿液样本中的美芬妥英及其代谢物4-羟基美芬妥英进行了分离,以确定人类氧化代谢能力的不同表型。