Sisodia C S, Kramer L L, Gupta V S, Lerner D J, Taksas L
Can J Comp Med. 1975 Apr;39(2):216-23.
Pharmacological disposition of chloramphenicol was studied in horses. Minimum levels of the antibiotic (greater than or equal to 5 mu g/ml) in blood or plasma recommended to combat infections could not be achieved by 4.4 and 8.8 mg/kg I.V. or 30 and 50 mg/kg I.M. or 30 mg/kg oral (as palmitate salt) doses of chloramphenicol. Increasing the dose to 19.8 and 26.4 mg/kg I.V. provided such levels for about two and three hours respectively. A combination of 20 mg/kg I.V. and 30 mg/kg I.M. administered simultaneously did not provide more prolonged levels than 26.4 mg/kg I.V. alone. Chloramphenicol succinate produced higher but not more prolonged levels in blood and plasma than those produced by pure chloramphenicol. Succinate salt is very little, if at all, bound to red blood corpuscles. Plasma half life and the apparent volume of distribution of chloramphenicol in horses were determined as 0.98 hours and 0.92 L/kg, respectively. At 5-10 mu g/ml concentrations in equine plasma approximately 30 percent of the chloramphenicol is bound to plasma proteins. From these studies it is concluded that the biological half life of chloramphenicol may be too short for therapeutic application against systemic infections in horses.
对马匹体内氯霉素的药理分布进行了研究。静脉注射4.4和8.8毫克/千克、肌肉注射30和50毫克/千克或口服30毫克/千克(棕榈酸盐形式)的氯霉素剂量,均无法达到血液或血浆中推荐用于对抗感染的最低抗生素水平(大于或等于5微克/毫升)。将静脉注射剂量增加到19.8和26.4毫克/千克,分别可维持该水平约两小时和三小时。同时静脉注射20毫克/千克和肌肉注射30毫克/千克的联合用药,其血药浓度维持时间并不比单独静脉注射26.4毫克/千克更长。琥珀氯霉素在血液和血浆中产生的水平高于纯氯霉素,但维持时间并不更长。琥珀酸盐与红细胞的结合极少,甚至可以忽略不计。马匹体内氯霉素的血浆半衰期和表观分布容积分别确定为0.98小时和0.92升/千克。在马血浆浓度为5 - 10微克/毫升时,约30%的氯霉素与血浆蛋白结合。从这些研究得出结论,氯霉素的生物半衰期可能过短,不足以用于治疗马匹的全身感染。