Gutiérrez María Laura, Di Federico Guillermo, Dale Jorge A, Minoia Juan M, Corrales Carlos D, Schaiquevich Paula, Wikinski Silvia
CONICET, Argentina; Instituto de Farmacología, Facultad de Medicina, Universidad de Buenos Aires, Paraguay 2155, C1121ABF Ciudad Autónoma de Buenos Aires, Argentina; Plataforma Tecnológica EBAL, Paraguay 2155, C1121ABF Ciudad Autónoma de Buenos Aires, Argentina.
Servicio de Cirugía, Hospital Escuela, Facultad de Ciencias Veterinarias, Universidad Nacional de La Plata, Calle 60 y 118, 1900 La Plata, Provincia de Buenos Aires, Argentina.
Vet Parasitol. 2017 May 30;239:46-49. doi: 10.1016/j.vetpar.2017.04.022. Epub 2017 Apr 17.
Praziquantel (PZQ) is an anthelmintic drug used both in humans and animals that can be administered through various routes. There are transdermal formulations for cats, but only oral or subcutaneous dosage forms for dogs. Given the fact that the cat's skin and the dog's skin have different characteristics, which in turn affect bioavailability, we developed a PZQ spot-on formulation for dogs. This study was aimed at determining the plasmatic behavior of topically administered PZQ (Labyes) in adult dogs. Dogs were administered PZQ (14.5mg/kg PZQ, from a solution of 100mg/ml). Blood samples were drawn before treatment onset and at the following time points after PZQ administration: 1, 2, 4, 6, 12, 24 and 48h. PZQ plasma concentration was determined by ultra-high performance liquid chromatography (UPLC) coupled to tandem mass spectrometry (MS/MS). Observed maximum concentration (C), area under the concentration-time curve from the time of drug administration to infinity (AUC) and time to maximum concentration (T) were calculated for each animal, and mean±SD for each parameter was obtained. Results were as follows: C=56.0±15ng/ml; AUC=910.2±220ng*h/ml, T=5.0±1.1h. This is the first study to provide pharmacokinetic data of a praziquantel spot-on formulation for dogs.
吡喹酮（PZQ）是一种用于人和动物的驱虫药，可通过多种途径给药。有针对猫的透皮制剂，但针对狗只有口服或皮下剂型。鉴于猫和狗的皮肤具有不同特性，这反过来又会影响生物利用度，我们开发了一种针对狗的吡喹酮滴剂制剂。本研究旨在确定局部给药的吡喹酮（Labyes）在成年犬体内的血浆行为。给犬只施用吡喹酮（14.5mg/kg吡喹酮，来自100mg/ml的溶液）。在治疗开始前以及吡喹酮给药后的以下时间点采集血样：1、2、4、6、12、24和48小时。通过超高效液相色谱（UPLC）与串联质谱（MS/MS）联用测定吡喹酮血浆浓度。计算每只动物的观察到的最大浓度（C）、从给药时间到无穷大的浓度-时间曲线下面积（AUC）以及达到最大浓度的时间（T），并获得每个参数的平均值±标准差。结果如下：C = 56.0±15ng/ml；AUC = 910.2±220ng*h/ml，T = 5.0±1.1小时。这是第一项提供犬用吡喹酮滴剂制剂药代动力学数据的研究。
