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Pharmacokinetics and ex vivo pharmacodynamics of Minocycline against Salmonella abortus equi in donkey plasma and tissue cage fluid
Research in Veterinary Science ( IF 2.4 ) Pub Date : 2020-10-09 , DOI: 10.1016/j.rvsc.2020.10.003
Zaijian Li , Wenqiang Liu , Jianqing Su , Xiuling Chu , Changfa Wang

Tissue Cage (TC) model was used to evaluate the pharmacokinetics and ex vivo pharmacodynamics of Minocycline (MINO) after intramuscular (IM) administration to donkeys at 4 mg/kg body-weight. The Cmax of MINO with 1.79 and 2.63 μg mL−1 was obtained at 2.96 and 1.41 h in TCF (tissue cage fluid) and plasma respectively. The absorption half-lives (t1/2ka) of MINO were calculated to be 0.71 h in TCF and 0.32 h in plasma, whereas the elimination half-lives (t1/2ke) were 10.46 h in TCF and 5.95 h in plasma. The distribution volume (Vd/F) of MINO was estimated to be 1.84 L kg−1 in TCF and 1.28 L kg−1 in plasma. The total clearance (CLb/F) of MINO was computed as 0.12 and 0.15 L/ (h·kg) in TCF and plasma respectively. The area under the concentration-time curve (AUC) of MINO was 32.77 μg mL−1h in TCF and 25.27 μg mL−1h in plasma, respectively.The ex vivo time-kill curves were established for plasma and TCF samples using Salmonella abortus equi. The MIC and MBC of MINO against salmonella were 0.08 and 0.16 μg mL−1 for plasma, 0.04 and 0.08 μg mL−1 for TCF. The plasma Cmax/MIC and AUC/MIC values after IM administration were 32.88 ± 9.87 and 315.88 ± 42.65 h, respectively. The TCF Cmax/MIC and AUC/MIC values after IM administration were 44.75 ± 9.32 and 819.25 ± 65.23 h, respectively. The values of T > MIC were approximately >36 h in plasma and > 65 h in TCF. These findings from this study suggest that MINO may be therapeutically effective in diseases of donkeys caused by salmonella when used at a dose of 4 mg/kg IM administration.



中文翻译:

米诺环素对驴血浆和组织笼液中马尾沙门氏菌的药代动力学和离体药效

使用组织笼(TC)模型评估以4 mg / kg体重对驴进行肌肉(IM)施用后米诺环素(MINO)的药代动力学和离体药效学。在2.96和1.41 h分别在TCF(组织笼液)和血浆中分别获得1.79和2.63μgmL -1的MINO的C max。MINO的吸收半衰期(t 1 / 2ka)在TCF中为0.71 h,在血浆中为0.32 h,而消除半衰期(t 1 / 2ke)在TCF中为10.46 h,在血浆中为5.95 h。MINO的分布体积(V d / F)在TCF中估计为1.84 L kg -1,在血浆中为1.28 L kg -1。总间隙(CL b在TCF和血浆中,MINO的/ F)分别计算为0.12和0.15 L /(h·kg)。的浓度-时间曲线的MINO(AUC)下面积为32.77微克毫升-1在TCF和h 25.27微克毫升-1血浆小时,respectively.The建立用于使用等离子体和TCF样品体外时间-杀菌曲线沙门氏菌马匹流产。MINO的针对沙门氏菌的MIC和MBC分别为0.08和0.16微克毫升-1为等离子体,0.04和0.08微克毫升-1为TCF。IM给药后的血浆C max / MIC和AUC / MIC值分别为32.88±9.87和315.88±42.65 h。TCF C最大值IM给药后的/ MIC和AUC / MIC值分别为44.75±9.32和819.25±65.23h。T> MIC的值在血浆中约为> 36 h,在TCF中为> 65 h。这项研究的这些发现表明,当以4 mg / kg的剂量IM施用时,MINO在沙门氏菌引起的驴病中可能具有治疗效果。

更新日期:2020-10-11
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