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所有非甾体抗炎药(NSAIDs)都有血浆蛋白结合率高及分布容积低的特点,其半衰期的不同是由清除率的大小所致。NSAIDs以不同的途径经由肝脏代谢,可以几种机理发生药物相互作用:如药物蛋白结合的置换,诱导或抑制肝脏药物代谢,与其他有机酸竞争肾小管主动分泌。近年来的大量研究表明,应特别注意NSAIDs动力学的一些特点:(1)仅以药物总浓度来计算药物体内过程会出现失误,而应以有药理活性的游离药物浓度来分析;(2)丙酸类NSAIDs仅一个对映体有活性,研究这类药物的药动学应着眼于活性立体异构体的分析;(3)丙酸类NSAIDs能被肝脏代谢为不稳定的酰基葡萄糖醛酸结合物,
All non-steroidal anti-inflammatory drugs (NSAIDs) have the characteristics of high plasma protein binding and low volume of distribution, the difference in half-life is due to the size of the clearance rate. NSAIDs are metabolized via the liver in different ways and may interact with several mechanisms such as drug protein binding, inducing or inhibiting hepatic drug metabolism, and competing with other organic acids for the active secretion of the renal tubules. In recent years, a large number of studies have shown that special attention should be paid to some of the characteristics of NSAIDs kinetics: (1) only the total drug concentration to calculate the process of the drug will be mistakes, but should be pharmacologically active free drug concentration to analyze; (2) Propionic acid NSAIDs only one enantiomer activity, the study of pharmacokinetics of these drugs should focus on the analysis of active stereoisomers; (3) propionic acid NSAIDs can be metabolized by the liver into unstable acyl glucuronic acid Combination,