Smith P B, Caldwell J, Smith R L, Horner M W, Moss M S
Xenobiotica. 1987 Apr;17(4):435-43. doi: 10.3109/00498258709043950.
[phenyl-14C]-Phenylbutazone was administered to 2 horses p.o. and i.v. on separate occasions. Plasma levels and urinary and faecal elimination of 14C were monitored for up to 7 days after dosing. Phenylbutazone was rapidly and extensively absorbed after oral administration, and its bioavailability was 91% assessed by comparison of plasma AUCs of unchanged drug after p.o. and i.v. administration. The plasma elimination half-life of phenylbutazone was 9.7 h and this was independent of the route of administration. The pattern of elimination of phenylbutazone was independent of the route of administration, with 55% of the dose being found in the urine in 3 days and a further 39% in the faeces in 7 days. These data, which are the first reports of the absolute bioavailability and excretion pathways of phenylbutazone in the horse, are discussed in terms of their significance for the gastrointestinal toxicity of this drug.
将[苯-14C] - 保泰松分别经口服和静脉注射给予2匹马。给药后长达7天监测血浆水平以及14C的尿粪排泄情况。口服给药后,保泰松吸收迅速且广泛,通过比较口服和静脉注射后原形药物的血浆药时曲线下面积(AUC)评估,其生物利用度为91%。保泰松的血浆消除半衰期为9.7小时,且与给药途径无关。保泰松的消除模式与给药途径无关,给药后3天内55%的剂量经尿液排出,7天内另有39%经粪便排出。这些数据是关于保泰松在马体内绝对生物利用度和排泄途径的首次报道,并就其对该药物胃肠道毒性的意义进行了讨论。