Adams S S, McCullough K F, Nicholson J S
Arzneimittelforschung. 1975 Nov;25(11):1786-91.
2-(2-Fluoro-4-biphenyl)propionic acid (flurbiprofen) possesses peripheral analgesic, anti-inflammatory and antipyretic properties. It does not possess glucocorticoid or adrenocortical-stimulating properties. It is a highly potent agent which in acute pharmacological test systems produced a significant pharmacological effect in single oral doses varying from 0.04 to 0.47 mg/kg. The peak plasma concentrations attained after these doses were generally of the order of 1 to 3 mug/ml. Doses of 0.33 mg/kg/day, which gave peak plasma concentrations of 0.6 mug/ml, produced a significant inhibition of rat adjuvant arthritis, both developing and established. The very shallow dose-response curves for flurbiprofen compared with acetylsalicylic acid, especially in the mouse and the rat test systems, are not due to an unreliable or abnormal absorption, which suggests that in these species the mode of action of flurbiprofen is not identical with that of acetylsalicylic acid.
2-(2-氟-4-联苯)丙酸(氟比洛芬)具有外周镇痛、抗炎和解热特性。它不具有糖皮质激素或肾上腺皮质刺激特性。它是一种高效药物,在急性药理试验系统中,单次口服剂量为0.04至0.47mg/kg时能产生显著药理作用。这些剂量后达到的血浆峰值浓度一般在1至3μg/ml左右。每日剂量0.33mg/kg可使血浆峰值浓度达到0.6μg/ml,对大鼠佐剂性关节炎的发展期和已形成期均产生显著抑制作用。与阿司匹林相比,氟比洛芬的剂量-反应曲线非常平缓,尤其是在小鼠和大鼠试验系统中,这并非由于吸收不可靠或异常,这表明在这些物种中氟比洛芬的作用方式与阿司匹林不同。