Nouws J F, Vree T B
Vet Q. 1983 Oct;5(4):165-70. doi: 10.1080/01652176.1983.9693891.
The oxytetracycline (OTC) disposition was studied in a group of six calves following the administration of an oxytetracycline-10 per cent formulation (i) intravenously (i.v.), (ii) subcutaneously (s.c.) in the lateral neck, and intramuscularly (i.m.) in (iii) the lateral neck, (iv) the shoulder (M. triceps brachii), and (v) the buttock (M. semitendineus). The dose levels used for the intravenous route and other routes were respectively 17.0 +/- 2.3 and 18.3 +/- 1.25 mg OTC/kg. The peak OTC concentrations (Cmax) were achieved with the s.c. and i.m. routes between 4 and 8 hours after injection, the highest being found after application in the shoulder (Cmax:6.9 +/- 0.82 microgram/ml plasma). The Cmax for the s.c. and other i.m. routes in application was similar to each other, ranging from 5.0 to 5.5 micrograms/ml plasma. For different points in time after injection the partial bioavailability was calculated. At 52 h post injection (p.i.) maximal bioavailability was observed for the i.m. shoulder route, viz. 98.1 +/- 7.0 per cent of the administered dose, while at 76 h p.i. similar bioavailabilities were achieved for the i.m. neck and shoulder route, namely 93.3 +/- 8.9 and 99.4 +/- 4.2 per cent, respectively. The lowest bioavailability (83.1 +/- 13.4 per cent) was obtained following the i.m. buttock route at 76 p.i. An obvious irritating effect was observed after s.c. application in the neck an di.m. injection in the buttock, which had disappeared at 5 days p.i. It is assumed that the longer persistence of OTC in plasma resulting with the latter two routes of administration was due to this irritation effect.
在一组六头犊牛中研究了土霉素(OTC)的处置情况,分别通过以下方式给予10%土霉素制剂:(i)静脉注射(i.v.);(ii)颈部外侧皮下注射(s.c.);(iii)颈部外侧肌肉注射(i.m.);(iv)肩部(肱三头肌)肌肉注射;(v)臀部(半腱肌)肌肉注射。静脉注射途径和其他途径使用的剂量水平分别为17.0±2.3和18.3±1.25毫克OTC/千克。皮下注射和肌肉注射途径在注射后4至8小时达到土霉素峰值浓度(Cmax),在肩部注射后最高(Cmax:6.9±0.82微克/毫升血浆)。皮下注射和其他肌肉注射途径的Cmax彼此相似,范围为5.0至5.5微克/毫升血浆。计算了注射后不同时间点的部分生物利用度。注射后52小时(p.i.),肌肉注射肩部途径观察到最大生物利用度,即给药剂量的98.1±7.0%,而注射后76小时,肌肉注射颈部和肩部途径获得相似的生物利用度,分别为93.3±8.9%和99.4±4.2%。注射后76小时,肌肉注射臀部途径的生物利用度最低(83.1±13.4%)。颈部皮下注射和臀部肌肉注射后观察到明显的刺激作用,在注射后5天消失。推测后两种给药途径导致土霉素在血浆中持续时间较长是由于这种刺激作用。