Kaiser D G, Liggett W F, Forist A A
J Pharm Sci. 1976 Dec;65(12):1767-9. doi: 10.1002/jps.2600651218.
Interest in the 5-, 6-, and 7-trifluoromethyl-substituted 2,3-bis(4-methoxyphenyl)indoles as potent, orally active anti-inflammatory agents required a method for their determination in serum, urine, and feces to permit studies of their absorption, metabolism, and excretion. A simple, rapid, sensitive, and specific procedure was developed based on an ethyl acetate extraction of alkaline specimens and subsequent fluorometric analysis of ethanolic solutions of the extract residues. The method is sensitive to 0.1 microgram/ml, 0.5 microgram/ml, and 0.7 microgram/100 mg of these compounds in serum, urine, and feces, respectively. Overall mean recoveries and standard deviations of the 5-, 6-, and 7-trifluoromethyl-substituted compounds from biological samples were 102.2 +/- 3.0, 102.2 +/- 5.4, and 100.5 +/- 5.7%, respectively. The procedure was applied successfully to absorption studies with 2,3-bis(4-methoxyphenyl)-7-(trifluoromethyl)indole in the dog.
由于对5-、6-和7-三氟甲基取代的2,3-双(4-甲氧基苯基)吲哚这类强效口服活性抗炎药感兴趣,因此需要一种能在血清、尿液和粪便中测定它们的方法,以便研究其吸收、代谢和排泄情况。基于对碱性样本进行乙酸乙酯萃取,并对萃取残渣的乙醇溶液进行后续荧光分析,开发出了一种简单、快速、灵敏且特异的方法。该方法对血清、尿液和粪便中这些化合物的检测灵敏度分别为0.1微克/毫升、0.5微克/毫升和0.7微克/100毫克。生物样品中5-、6-和7-三氟甲基取代化合物的总体平均回收率和标准差分别为102.2±3.0%、102.2±5.4%和100.5±5.7%。该方法已成功应用于犬体内2,3-双(4-甲氧基苯基)-7-(三氟甲基)吲哚的吸收研究。