Delbeke F T, Landuyt J, Debackere M
Farmacie & Toxicologie, Falculteit Diergeneeskunde, Universiteit Gent, Merelbeke, Belgium.
J Pharm Biomed Anal. 1995 Jul;13(8):1041-7. doi: 10.1016/0731-7085(95)01512-j.
Plasma and urinary concentrations of the non-steroidal anti-inflammatory drug fenoprofen were determined by a high-performance liquid chromatographic procedure following oral administration of a dose of 3 g to fed and fasted horses. In plasma, fenoprofen was present in detectable concentrations for 6-12 h. Free access to hay significantly reduced the peak plasma concentration and bioavailability of fenoprofen, and large interindividual differences in absorption and elimination pattern occurred. In fasted horses, fenoprofen was rapidly absorbed with a mean half-life of 0.10 h. Maximum concentrations were found 0.63 +/- 0.21 h after dosing. The elimination half-life was 0.9 h. As early as 1 h after dosage, fenoprofen could be detected in hydrolysed and unhydrolysed urine, and remained detectable up to 48 h. The maximum excretion rate and peak concentration occurred 2 h after administration, irrespective of the feeding schedule. In fed horses, a second maximum occurred after 9 h. The percentage of the dose excreted as unchanged fenoprofen in 12 h was 13.0 +/- 6.8%. A recovery of 21.9 +/- 7.4% and 42.2 +/- 7.0% of the dose was obtained after enzymatic and alkaline hydrolysis, respectively. At least three hydroxylated metabolites were detected in hydrolysed urine.
给进食和禁食的马匹口服3克剂量的非甾体抗炎药非诺洛芬后，采用高效液相色谱法测定血浆和尿液中非诺洛芬的浓度。在血浆中，非诺洛芬在6 - 12小时内呈现可检测到的浓度。自由采食干草显著降低了非诺洛芬的血浆峰值浓度和生物利用度，并且在吸收和消除模式上存在较大的个体差异。在禁食的马匹中，非诺洛芬吸收迅速，平均半衰期为0.10小时。给药后0.63±0.21小时达到最大浓度。消除半衰期为0.9小时。给药后1小时，在水解和未水解的尿液中即可检测到非诺洛芬，并且在48小时内均可检测到。无论喂食时间表如何，最大排泄率和峰值浓度均在给药后2小时出现。在进食的马匹中，9小时后出现第二个峰值。12小时内以未改变的非诺洛芬形式排泄的剂量百分比为13.0±6.8%。酶解和碱解后分别获得了剂量的21.9±7.4%和42.2±7.0%的回收率。在水解尿液中至少检测到三种羟基化代谢物。
