Department of Large Animal Sciences, University of Copenhagen, 2630 Taastrup, Denmark.
Res Vet Sci. 2012 Feb;92(1):111-5. doi: 10.1016/j.rvsc.2010.11.001. Epub 2010 Dec 7.
Ampicillin concentrations in pulmonary epithelial lining fluid (PELF) and plasma was studied after single intravenous ampicillin administration (15mg/kg) or single intragastric administration of its prodrug, pivampicillin (19.9mg/kg) to horses and discussed in relation to minimum inhibitory concentrations (MIC) of common equine respiratory pathogens. After intravenous administration, elimination of ampicillin was fast and not detectable in plasma after 12h in three out of six horses. Pivampicillin was absorbed well in non-fasted horses with an oral bioavailability of 36%. The degree of penetration of ampicillin into PELF, as described by the AUC(PELF)/AUC(plasma) ratio from 0 to 12h was 0.40 after intravenous administration and 1.00 after pivampicillin administration. In horses, ampicillin administered either intravenously or orally, in the form of pivampicillin, can provide clinically relevant drug concentrations in PELF for at least 12h, when treating susceptible equine respiratory pathogens (e.g. streptococci). Treatment of other bacterial pathogens requires susceptibility testing and possibly more frequent dosing, depending of minimum inhibitory concentrations (MIC) values.
在单剂量静脉注射氨苄西林（15mg/kg）或其前药匹氨西林（19.9mg/kg）灌胃后，研究了肺部上皮衬液（PELF）和血浆中的氨苄西林浓度，并与常见马呼吸道病原体的最低抑菌浓度（MIC）进行了讨论。静脉给药后，6 匹马中有 3 匹马在 12 小时后血浆中氨苄西林无法检出，消除速度很快。非禁食马口服匹氨西林吸收良好，生物利用度为 36%。氨苄西林在 0 至 12 小时内透过 PELF 的程度，用 AUC（PELF）/AUC（血浆）比值表示，静脉给药后为 0.40，口服匹氨西林给药后为 1.00。在马中，静脉注射或口服给予的氨苄西林以匹氨西林的形式存在，至少在 12 小时内可在 PELF 中提供临床相关的药物浓度，用于治疗敏感的马呼吸道病原体（例如链球菌）。治疗其他细菌病原体需要进行药敏试验，可能需要根据最低抑菌浓度（MIC）值更频繁地给药。
