Casalini C, Mascellani G, Tamagnone G, Cesarano G, Giumanini A
J Pharm Sci. 1980 Feb;69(2):164-7. doi: 10.1002/jps.2600690212.
The in vivo metabolism of 2-ethyl-2,3-dihydro-5-benzofuranacetic acid (furofenac), a new drug, was studied in rats, dogs, and humans. The drug has antiplatelet-aggregation activity and anti-inflammatory activity combined with low ulcerogenic power. Hydroxylated derivatives and analogous compounds were prepared, and their syntheses and chemical characteristics are described. TLC. GLC, high-pressure liquid chromatography, and GLC--mass spectrometry were applied to urine extracts, and authentic synthetic specimens were used for comparison. The products identified in human and dog urine were mainly conjugation compounds of the drug, while the products in rat urine were hydroxylated derivatives. Some pharmacological characteristics of the metabolites are discussed.
对一种新药2-乙基-2,3-二氢-5-苯并呋喃乙酸（呋罗芬酸）在大鼠、狗和人体内的体内代谢进行了研究。该药物具有抗血小板聚集活性和抗炎活性，且致溃疡作用较弱。制备了羟基化衍生物和类似化合物，并描述了它们的合成方法和化学特性。采用薄层色谱法（TLC）、气相色谱法（GLC）、高压液相色谱法以及气相色谱-质谱联用法（GLC-MS）对尿液提取物进行分析，并使用真实的合成样品进行比较。在人和狗尿液中鉴定出的产物主要是该药物的结合物，而在大鼠尿液中的产物是羟基化衍生物。还讨论了这些代谢产物的一些药理学特性。
