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犬使用不同制剂治疗后阿苯达唑亚砜的动力学处置

Albendazole sulphoxide kinetic disposition after treatment with different formulations in dogs.

作者信息

Dib A, Palma S, Suárez G, Farías C, Cabrera P, Castro S, Allemandi D, Moreno L, Lanusse C, Sánchez Bruni S

机构信息

Laboratory of Pharmacology, Faculty of Veterinary Medicine- Universidad de la República, Uruguay Laboratory of Pharmaceutical Technology, Department of Pharmacy, Faculty of Chemical Sciences, Universidad Nacional de Córdoba, Argentina.

出版信息

J Vet Pharmacol Ther. 2011 Apr;34(2):136-41. doi: 10.1111/j.1365-2885.2010.01203.x.

Abstract

New therapeutic strategies based on the search of alternative formulations of albendazole (ABZ) and albendazole sulphoxide (ABZSO) are under current development to optimize posology and antiparasite efficacy in dogs. In an incomplete block design, nine dogs were randomly divided into three groups (n = 6). Treatments were carried out in two phases as follows. Phase I: Group I (treatment A), animals received ABZ at 25 mg/kg of conventional formulation. Group II (treatment B), dogs received 25 mg/kg of a modified poloxamer-ABZ formulation. Group III (treatment C), animals were treated with ABZSO in equimolar amount to ABZ doses. After 21 days of wash-out period the experiment was repeated (Phase II). Blood samples were collected over 24 h and subsequently analysed by high performance liquid chromatography. ABZSO and ABZSO(2) were the analytes recovered in plasma. Significant higher (P < 0.001) ABZSO area under the concentration-time curve (+500%) and C(max) (+487%) values were obtained for the treatment C in comparison with treatments A and B. However, no statistical differences on pharmacokinetic parameters were found between formulations A and B. In conclusion, the enhanced plasma concentration profile obtained for the ABZSO formulation used in treatment C may contribute to optimize the anthelmintic control in dogs.

摘要

目前正在研发基于寻找阿苯达唑(ABZ)和阿苯达唑亚砜(ABZSO)替代制剂的新治疗策略,以优化犬类的用药剂量和抗寄生虫效果。在不完全区组设计中,将9只犬随机分为三组(n = 6)。治疗分两个阶段进行,具体如下。第一阶段:第一组(治疗A),动物接受25 mg/kg常规制剂的ABZ。第二组(治疗B),犬接受25 mg/kg的改良泊洛沙姆-ABZ制剂。第三组(治疗C),动物接受与ABZ剂量等摩尔量的ABZSO治疗。经过21天的洗脱期后,重复该实验(第二阶段)。在24小时内采集血样,随后通过高效液相色谱法进行分析。ABZSO和ABZSO(2)是血浆中回收的分析物。与治疗A和B相比,治疗C的ABZSO浓度-时间曲线下面积(+500%)和C(max)(+487%)值显著更高(P < 0.001)。然而,制剂A和B之间在药代动力学参数上未发现统计学差异。总之,治疗C中使用的ABZSO制剂所获得的增强的血浆浓度曲线可能有助于优化犬类的驱虫控制。

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