LeGrange S N, Boothe D M, Herndon S, Willard M D
Department of Small Animal Medicine, College of Veterinary Medicine, Texas A&M University, College Station 77843, USA.
J Am Anim Hosp Assoc. 1997 Nov-Dec;33(6):517-23. doi: 10.5326/15473317-33-6-517.
The disposition of cisapride in seven healthy cats was determined following administration of either a single oral (2 mg/kg body weight) or intravenous (i.v.) (1 mg/kg body weight) dose. Cats were studied using a random crossover design. After administration of the oral capsule, maximum plasma drug concentration (Cmax) +/- standard deviation (SD) was 73.32 +/- 16.59 ng/ml, and bioavailability +/- SD was 29.0 +/- 22.6%. Following i.v. administration, extrapolated peak cisapride concentration (C0) +/- SD was 421.30 +/- 155.37 ng/ml, and clearance +/- SD was 15 +/- 0.67 ml/kg per minute. Elimination half-life (T1/2) was similar for both routes of administration (T1/2(oral) +/- SD was 5.27 +/- 3.16 hr, T1/2(i.v.) +/- SD was 5.19 +/- 3.77 hr). Adverse effects were not observed. Based on these results, a dose of 1 mg/kg body weight per os (PO) every eight hours or 1.5 mg/kg body weight every 12 hours is expected to result in plasma drug concentrations within the therapeutic ranges established for humans.
在七只健康猫中，分别给予单次口服（2毫克/千克体重）或静脉注射（1毫克/千克体重）剂量后，测定了西沙必利的处置情况。采用随机交叉设计对猫进行研究。口服胶囊给药后，最大血浆药物浓度（Cmax）±标准差（SD）为73.32±16.59纳克/毫升，生物利用度±SD为29.0±22.6%。静脉注射给药后，推算的西沙必利峰值浓度（C0）±SD为421.30±155.37纳克/毫升，清除率±SD为15±0.67毫升/千克每分钟。两种给药途径的消除半衰期（T1/2）相似（口服T1/2±SD为5.27±3.16小时，静脉注射T1/2±SD为5.19±3.77小时）。未观察到不良反应。基于这些结果，预计每八小时口服（PO）1毫克/千克体重或每12小时1.5毫克/千克体重的剂量可使血浆药物浓度处于为人类确定的治疗范围内。
