Luders R C, Chao D
J Pharm Sci. 1981 Dec;70(12):1370-1. doi: 10.1002/jps.2600701221.
The extent of warfarin and tolbutamide binding to plasma proteins was determined with and without pirprofen by an ultrafiltration procedure employing 14C-labeled drugs. Results from in vitro studies at 37 degrees showed that the degree of binding amounted to 97.8% for warfarin and 95.6% for tolbutamide. The binding characteristics of these drugs were not altered when plasma containing either warfarin or tolbutamide at concentrations equivalent to those expected normally after therapeutic dosing were concomitantly spiked with therapeutic amounts of pirprofen. Consequently, potentiation resulting from drug displacement would not be anticipated in humans when pirprofen is administered along with warfarin or tolbutamide.
采用14C标记药物的超滤法，测定了有或无吡洛芬存在时华法林和甲苯磺丁脲与血浆蛋白的结合程度。37℃体外研究结果表明，华法林的结合程度为97.8%，甲苯磺丁脲的结合程度为95.6%。当含有与治疗给药后正常预期浓度相当的华法林或甲苯磺丁脲的血浆同时加入治疗量的吡洛芬时，这些药物的结合特性未发生改变。因此，当吡洛芬与华法林或甲苯磺丁脲一起给药时，预计在人体内不会出现因药物置换导致的增效作用。
