Celardo A, Dell'Elba G, Bonati M
Istituto Ricerche Farmacologiche Mario Negri, Consorzio Mario Negri Sud, S. Maria Imbaro, Italy.
Eur J Drug Metab Pharmacokinet. 1992 Jan-Mar;17(1):29-32. doi: 10.1007/BF03189984.
The bioavailability of isbufylline was assessed in male rabbits given 12 mg/kg i.v. (intravenous) or per os (oral) according to a randomized design. The concentrations of unbound (fu = 54.0) isbufylline were considered in plasma as a function of time, after i.v. and oral administration. After oral administration in saline solution, a mean absolute oral bioavailability of 59.6% was calculated. The drug is rapidly absorbed and the comparison of the kinetic profiles after i.v. and per os administration, revealed a rapid elimination: t1/2 27.3 and 28.8 min respectively, and a total body clearance of 67.06 ml/min/kg. Urinary recovery 0-48 h accounted for less than 1% of the dose.
按照随机设计，对雄性兔静脉注射（i.v.）或口服给予12mg/kg异布福林后，评估其生物利用度。静脉注射和口服给药后，将血浆中未结合（游离分数fu = 54.0）的异布福林浓度视为时间的函数。在盐溶液中口服给药后，计算出平均绝对口服生物利用度为59.6%。该药物吸收迅速，静脉注射和口服给药后的动力学曲线比较显示消除迅速：t1/2分别为27.3和28.8分钟，全身清除率为67.06ml/min/kg。0 - 48小时尿液回收率占给药剂量的不到1%。
