Lebkowska-Wieruszewska B, De Vito V, Owen H, Poapholatep A, Giorgi M
Department of Pharmacology, University of Life Sciences, Lublin, Poland.
Department of Veterinary Medicine, University of Sassari, Sassari, Italy.
J Vet Pharmacol Ther. 2017 Dec;40(6):e11-e15. doi: 10.1111/jvp.12414. Epub 2017 Apr 29.
Drugs that provide effective analgesia in cats are limited. The aim of the study was to assess the pharmacokinetics of grapiprant after 2 mg/kg administration via p.o. and i.v. routes in cats. Six healthy adult cats were used according to an open, single-dose, two-treatment, two-period, randomized cross-over design. Cats were assigned to two treatment groups and administered with 2 mg/kg of grapiprant (pure powder) through p.o. and i.v. administration. Blood samples were collected at preassigned times and analysed by a validated HPLC method. After both administrations, grapiprant concentrations were detectable in plasma for up to 24 hr in five of six animals. The critical parameters including clearance (173.2 ml hr kg , range 120-326 ml hr kg ) and volume of distribution (918 ml/kg, range 611-1608 ml/kg) were calculated from the i.v. group. The mean oral F% was low (39.6% range 31.5%-45.2%). If the assumption that the minimal effective concentration in dogs (164 ng/ml) applies in cats too, grapiprant orally administered at 2 mg/kg might be effective for 10 hr. Further studies are necessary to establish the minimal effective concentration in this animal species.
对猫有效的镇痛药种类有限。本研究的目的是评估猫经口服和静脉途径给予2mg/kg格拉普兰特后的药代动力学。根据开放、单剂量、双治疗、双周期随机交叉设计，使用了6只健康成年猫。将猫分为两个治疗组，通过口服和静脉给药给予2mg/kg的格拉普兰特（纯粉末）。在预定时间采集血样，并通过经过验证的高效液相色谱法进行分析。两次给药后，六只动物中有五只在长达24小时的时间内血浆中均可检测到格拉普兰特浓度。根据静脉给药组计算出包括清除率（173.2ml·hr⁻¹·kg⁻¹，范围120 - 326ml·hr⁻¹·kg⁻¹）和分布容积（918ml/kg，范围611 - 1608ml/kg）在内的关键参数。平均口服F%较低（39.6%，范围31.5% - 45.2%）。如果犬的最低有效浓度（164ng/ml）在猫中也适用这一假设成立，那么口服2mg/kg的格拉普兰特可能在猫体内有效10小时。有必要进行进一步研究以确定该动物物种的最低有效浓度。
