Holland P S, Brumbaugh G W, Ruoff W W, Brown S A
Department of Large Animal Medicine and Surgery, College of Veterinary Medicine, Texas A&M University College Station 77843-4475, USA.
J Vet Pharmacol Ther. 1997 Dec;20(6):447-52. doi: 10.1046/j.1365-2885.1997.00093.x.
Plasma pharmacokinetics of ranitidine HCl were investigated after intravenous (i.v.) and oral (p.o.) administration of drug to six healthy foals. Twelve- to sixteen-week-old foals received 2.2 mg ranitidine/kg i.v. and 4.4 mg ranitidine/kg p.o. Concentrations of ranitidine were determined using normal phase high performance liquid chromatography. Plasma concentrations of ranitidine HCl declined from a mean of 3266 ng/mL at 5 min to 11 ng/mL at 720 min after administration. The profile of the plot of concentrations of ranitidine HCl vs. time was best described by a two-exponent equation for two foals; data for the remaining four foals were best described by a three-exponent equation. Mean values for model-independent values were: apparent volume of distribution (Vdss) = 1.46 L/kg; area under the curve (AUC) = 167,442 ng.min/mL; area under the moment curve (AUMC) = 18,068,221 ng.min2/mL; mean residence time (MRT) = 108.9 min; and clearance (Cl) = 13.3 mL/min.kg. Following p.o. administration, a two-exponent equation best described data for five foals; data for the remaining foal were best described by a three-exponent equation. Mean values of the pharmacokinetic values from the p.o. study include: AUC = 126,413 ng.min/mL; AUMC = 18,039,825 ng.min2/mL; mean absorption time (MAT) = 32.0 min; observed time to maximum plasma concentration (Tmax) = 57.2 min; maximum observed plasma concentration (Cmax) = 635.7 ng/mL; and bioavailability (F) = 38%.
对6匹健康马驹静脉注射(i.v.)和口服(p.o.)雷尼替丁盐酸盐后,研究了其血浆药代动力学。12至16周龄的马驹静脉注射2.2 mg雷尼替丁/千克,口服4.4 mg雷尼替丁/千克。使用正相高效液相色谱法测定雷尼替丁的浓度。给药后,雷尼替丁盐酸盐的血浆浓度从5分钟时的平均3266 ng/mL下降到720分钟时的11 ng/mL。对于两匹马驹,雷尼替丁盐酸盐浓度与时间的关系曲线最适合用双指数方程描述;其余四匹马驹的数据最适合用三指数方程描述。非模型依赖值的平均值为:分布容积(Vdss)=1.46 L/千克;曲线下面积(AUC)=167442 ng·min/mL;矩量曲线下面积(AUMC)=18068221 ng·min²/mL;平均驻留时间(MRT)=108.9分钟;清除率(Cl)=13.3 mL/分钟·千克。口服给药后,双指数方程最适合描述五匹马驹的数据;其余一匹马驹的数据最适合用三指数方程描述。口服研究的药代动力学值的平均值包括:AUC = 126413 ng·min/mL;AUMC = 18039825 ng·min²/mL;平均吸收时间(MAT)= 32.0分钟;观察到的最大血浆浓度时间(Tmax)= 57.2分钟;观察到的最大血浆浓度(Cmax)= 635.7 ng/mL;生物利用度(F)= 38%。