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多次给药后葡甲胺锑酸盐在实验感染婴儿利什曼原虫的犬体内的药代动力学。

Pharmacokinetics of meglumine antimoniate after administration of a multiple dose in dogs experimentally infected with Leishmania infantum.

作者信息

Valladares J E, Riera C, Alberola J, Gállego M, Portús M, Cristòfol C, Franquelo C, Arboix M

机构信息

Departament de Farmacologia i Terapèutica, Facultat de Veterinària, Universitat Autònoma de Barcelona, Bellaterra, Spain.

出版信息

Vet Parasitol. 1998 Feb 15;75(1):33-40. doi: 10.1016/s0304-4017(97)00193-3.

Abstract

Pharmacokinetics of meglumine antimoniate in dogs with experimentally induced leishmaniosis has been investigated. After infection, dogs received a dose of 75 mg kg-1 of meglumine antimoniate twice daily by subcutaneous injection for 10 days. Blood samples were collected throughout the treatment. No statistical differences were found in the kinetic behaviour of the drug administered as a single dose to healthy dogs and that administered as a multiple dose to infected animals. However, peak plasma concentrations (Cmax) of 30.8 +/- 12.8 micrograms ml-1 found after this dosage regimen were higher than those observed after the single dose administration of 100 mg kg-1 24 h-1. Furthermore, sustained antimony concentrations of 1.14 +/- 0.52 micrograms Sb ml-1 were detected throughout the treatment. No signs of toxicity were found in the animals treated indicating that this regimen would be very appropriate to treat canine leishmaniosis.

摘要

已对实验性诱导利什曼病的犬体内葡甲胺锑酸盐的药代动力学进行了研究。感染后,犬每天皮下注射2次,剂量为75 mg kg-1的葡甲胺锑酸盐,持续10天。在整个治疗过程中采集血样。对健康犬单剂量给药和对感染动物多剂量给药时,药物的动力学行为未发现统计学差异。然而,该给药方案后测得的血浆峰值浓度(Cmax)为30.8 +/- 12.8微克/毫升,高于24小时内单剂量给药100 mg kg-1后观察到的浓度。此外,在整个治疗过程中检测到锑的持续浓度为1.14 +/- 0.52微克锑/毫升。在接受治疗的动物中未发现毒性迹象,表明该方案非常适合治疗犬利什曼病。

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