药物动力学的tildipirosin猪血浆、肺组织和支气管液和试验条件对体外活性的影响参考菌株和现场隔离的放线杆菌pleuropneumoniae。

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玫瑰M,门格M, Bohland C, Zschiesche E,威廉C, "年代,梅茨W,艾伦•米Ropke R, Nurnberger进行M

药物动力学的tildipirosin猪血浆、肺组织和支气管液和试验条件对体外活性的影响参考菌株和现场隔离的放线杆菌pleuropneumoniae。

J兽医杂志。2013年4月,36 (2):140 - 53。doi: 10.1111 / j.1365-2885.2012.01397.x。Epub 2012年4月15日。

PubMed ID

22500881 (在PubMed

]

文摘

tildipirosin的药物动力学(Zuprevo ((R)) 40毫克/毫升注射猪)解决方案,一种新型16-membered-ring大环内酯物对治疗猪呼吸道疾病(阶跃恢复二极管),调查研究收集血浆和尸检肺组织样本和支气管液(BF)从猪。针对影响因素的体外活性的大环内酯类,以及解释tildipirosin药物动力学与最低抑制浓度(MIC),额外的实验研究pH值的影响,碳dioxide-enriched氛围,缓冲区,和血清tildipirosin中等收入国家为各种参考菌株和放线杆菌(a) pleuropneumoniae隔离。单一肌内(坜)注射后4毫克/公斤体重,最大血浆浓度(Cmax) 0.9杯/毫升23分钟内观察(达峰时间)。平均停留时间从去年的时间计量的可测量的浓度(MRTlast)和终端半衰期(T1/2)都是大约4天。剂量反应关系无显著性效果观察血浆浓度时间曲线下的面积从0到最后采样时间可以计量的药物浓度(AUClast)的剂量范围6毫克/公斤。然而,线性剂量比例与统计方法无法得到证实。tildipirosin time-concentration概要的男朋友在血浆和肺远远超过。在肺,tildipirosin浓度达到3.1杯/ g (2 h,在第一天达到峰值4.3杯/ g,和慢慢地拒绝0.8杯/ g(17天。在高炉,tildipirosin水平是14.3,7.0,和6.5杯/ g在5天,10,14。T1/2肺大约是7天。 Tildipirosin is rapidly and extensively distributed to the respiratory tract followed by slow elimination. Culture media pH and carbon dioxide-enriched atmosphere (CO2 -EA) had a marked impact on in vitro activity of tildipirosin in reference strains of various rapidly growing aerobic and fastidious bacteria including Histophilus (H.) somni ATCC 700025 and A. pleuropneumoniae ATCC 27090. For A. pleuropneumoniae ATCC 27090 testing conditions without CO2 -EA resulted in reduced acidification of culture media pH and a reduction in the minimum inhibitory concentrations compared to standard in vitro test conditions by 2 log2 dilution steps (4-fold) from 8 to 2 mug/mL. Supplementary buffering of standard culture media resulted in a reduction in the A. pleuropneumoniae (n = 8) MIC range by 4 log2 dilution steps (16-fold) from 8-16 to 0.5-1 mug/mL. Incremental supplementation of culture media with 50% serum resulted in noticeable shifts to lower minimum or maximum MICs by at least 2 log2 dilution steps (>/=4-fold) in all aerobic and fastidious reference strains tested except for Pasteurella (P.) multocida. The MIC of A. pleuropneumoniae ATCC 27090 decreased by 2-4 log2 dilution steps (4 to 16-fold) from 8 to 0.5-2 mug/mL when 50% serum was added to the standard assay. Considering a higher presence of serum and the rather neutral pH conditions maintained in vivo, it is suggested to take the influence of these factors on in vitro activity into account when interpreting tildipirosin MICs for A. pleuropneumoniae in relation to pharmacokinetics.

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药物

Tildipirosin