Wiseman E H, McIlhenny H M, Bettis J W
J Pharm Sci. 1975 Sep;64(9):1469-75. doi: 10.1002/jps.2600640909.
Flumizole is a potent anti-inflammatory agent in animal models with an inhibitory activity severalfold that of indomethacin in rat foot edema and prostaglandin synthetase tests. The drug was well absorbed from the GI tract when administered in the solution used in pharmacological assays. However, markedly poorer absorption of the solid form of this poorly water-soluble agent led to the development of a flumizole dispersion with polyethylene glycol 6000. The solid dispersion exhibited an increased dissolution rate in simulated gastric fluid and improved absorption properties in dogs relative to unformulated flumizole. Studies with a capsule formulation of the solid dispersion in human volunteers were indicative of good drug absorption. Plasma levels of flumizole were rapidly achieved and declined with a short half-life (2-7 hr) in rats, dogs, and humans.
氟咪唑在动物模型中是一种强效抗炎剂，在大鼠足肿胀和前列腺素合成酶试验中的抑制活性是吲哚美辛的几倍。在药理试验中使用该药物溶液给药时，它能很好地从胃肠道吸收。然而，这种水溶性差的药物固体剂型的吸收明显较差，因此研发了一种含聚乙二醇6000的氟咪唑分散体。相对于未制剂化的氟咪唑，该固体分散体在模拟胃液中的溶解速率增加，在犬体内的吸收特性也得到改善。在人类志愿者中对该固体分散体胶囊制剂进行的研究表明药物吸收良好。在大鼠、犬和人类中，氟咪唑的血浆水平能迅速达到，并以较短的半衰期（2 - 7小时）下降。
