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巴喹普明在矮山羊中的口服生物利用度和药代动力学

Oral bioavailability and pharmacokinetics of baquiloprim in dwarf goats.

作者信息

Lewicki J, Maas R F, Witkamp R F, Van-Miert A S

机构信息

Department of Veterinary Basic Sciences, Utrecht University, The Netherlands.

出版信息

Res Vet Sci. 1995 May;58(3):268-71. doi: 10.1016/0034-5288(95)90115-9.

Abstract

The pharmacokinetics of baquiloprim at a dose of 8 mg kg-1 bodyweight were determined after its intravenous and intra-ruminal administration to seven healthy female dwarf goats. After intravenous injection, the plasma elimination curve showed a rapid distribution phase (mean [SD] t1/2 alpha 0.89 [0.4] hours). The mean volume of distribution at steady-state (Vdss) was 14.1 (2.7) litres kg-1 bodyweight. The mean elimination half-life (t1/2 beta) was 14.0 (2.3) hours. After intra-ruminal administration its maximum concentration in plasma (Cmax) was 0.09 (0.01 microgram ml-1 and this maximum was not reached until approximately 35 hours after administration. The systemic oral bioavailability, calculated up to 48 hours after dosing, was 33.7 (7.1) per cent. Owing to a prolonged absorption phase, the data from only four of the goats fitted reasonably to a compartmental model.

摘要

对7只健康的雌性矮山羊静脉注射和瘤胃内注射8 mg kg-1体重的巴喹普明后,测定了其药代动力学。静脉注射后,血浆消除曲线显示出快速分布相(平均[标准差]t1/2α为0.89[0.4]小时)。稳态分布容积(Vdss)平均为14.1(2.7)升 kg-1体重。平均消除半衰期(t1/2β)为14.0(2.3)小时。瘤胃内给药后,其血浆最大浓度(Cmax)为0.09(0.01)微克 ml-1,且直到给药后约35小时才达到此最大值。给药后48小时内计算得出的全身口服生物利用度为33.7(7.1)%。由于吸收期延长,只有4只山羊的数据能合理地拟合房室模型。

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