代谢
口服400毫克愈创甘油醚后，该药物会经历快速水解（在七个小时内超过60%的剂量被水解），以β-(2-甲氧基苯氧基)-乳酸作为主要的尿液代谢物，但尿液中检测不到母药。此外，已经观察到愈创甘油醚还会经历氧化和解甲基化。特别是，该药物通过氧化迅速在肝脏代谢为β-(2-甲氧基苯氧基)-乳酸。此外，愈创甘油醚还通过肝脏微粒体中的O-脱甲基酶解甲基化，以至于大约40%的给药剂量在3小时内作为这种代谢物排出体外。事实上，O-脱甲基酶似乎是愈创甘油醚代谢的主要酶，该物质的主要代谢物是β-(2-甲氧基苯氧基)-乳酸和脱甲基的羟基愈创甘油醚，它们本身都是无活性的部分。
After the oral administration of 400 mg guaifenesin, the agent experiences rapid hydrolysis (more than 60% of the dose hydrolyzed over a range of seven hours) with β-(2-methoxyphenoxy)-lactic acid found as the major urinary metabolite but no parent drug detectable in the urine. Moreover, it has been observed that guaifenesin also experiences both oxidation and demethylation. In particular, the medication is quickly metabolized hepatically by way of oxidation to β-(2-methoxyphenoxy)-lactic acid. Furthermore, guaifenesin is also demethylated by O-demethylase in liver microsomes to the point where about 40% of an administered dose is excreted as this metabolite in the urine within 3 hours. In fact, O-demethylase appears to be the primary enzyme for the metabolism of guaifenesin and the primary metabolites of the substance are β-(2-methoxyphenoxy)-lactic acid and the demethylated hydroxyguaifenesin, both of which are themselves inactive moieties.
来源:DrugBank
