Winther L, Honoré Hansen S, Baptiste K E, Friis C
Department of Large Animal Sciences, Faculty of Life Sciences, University of Copenhagen, Taastrup, Denmark.
J Vet Pharmacol Ther. 2011 Jun;34(3):285-9. doi: 10.1111/j.1365-2885.2010.01229.x. Epub 2010 Aug 24.
Doxycycline concentrations, following two types of oral administration to horses, in pulmonary epithelial lining fluid (PELF) were examined and compared to plasma concentrations. The oral bioavailability was estimated from plasma concentrations achieved after an intravenous study in two horses. Doxycycline (10 mg/kg) was administered either intragastric or as topdressing to nonfasted horses. Blood samples were collected for drug analysis, before and 11 times after administration during 24 h. PELF samples were collected by a tampon device four times after drug administration and analysed for doxycycline concentrations. Another two horses received doxycycline intravenously at a dose of 3 mg/kg and plasma was taken 14 times during a 24- h period. The oral bioavailability of doxycycline was calculated to 17% after intragastric administration and 6% after topdressing administration in nonfasted horses. The degree of penetration of doxycycline into PELF, as described by AUC(PELF) /AUC(plasma) ratios, was 0.87 after intragastric administration. The results indicate that clinically relevant doxycycline concentrations are possible to maintain in PELF after intragastric administration. Furthermore, if bioavailability could be enhanced for per os administration, doxycycline might be a valuable drug for the treatment of lower airway infections in horses.
对马匹进行两种口服给药后,检测了肺上皮衬液(PELF)中的强力霉素浓度,并与血浆浓度进行比较。通过对两匹马进行静脉注射研究后获得的血浆浓度来估算口服生物利用度。将强力霉素(10毫克/千克)以胃内给药或撒布给药的方式给予未禁食的马匹。在给药前以及给药后24小时内的11个时间点采集血样进行药物分析。在给药后通过棉塞装置采集4次PELF样本,并分析其中强力霉素的浓度。另外两匹马静脉注射3毫克/千克剂量的强力霉素,并在24小时内采集14次血浆样本。计算得出,未禁食马匹胃内给药后强力霉素的口服生物利用度为17%,撒布给药后为6%。以AUC(PELF)/AUC(血浆)比值表示的强力霉素在PELF中的渗透程度,胃内给药后为0.87。结果表明,胃内给药后有可能在PELF中维持与临床相关的强力霉素浓度。此外,如果口服给药的生物利用度能够提高,强力霉素可能成为治疗马匹下呼吸道感染的一种有价值的药物。