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替米考星在猪口服给药后的药代动力学

Pharmacokinetics of tilmicosin after oral administration in swine.

作者信息

Shen Jianzhong, Li Cun, Jiang Haiyang, Zhang Suxia, Guo Ping, Ding Shuangyang, Li Xiaowei

机构信息

Department of Pharmacology and Toxicology, College of Veterinary Medicine, China Agriculture University, Beijing 100094, PR China.

出版信息

Am J Vet Res. 2005 Jun;66(6):1071-4. doi: 10.2460/ajvr.2005.66.1071.

DOI:10.2460/ajvr.2005.66.1071
PMID:16008233
Abstract

OBJECTIVE

To determine the pharmacokinetics of tilmicosin after oral administration of a single dose of tilmicosin base in swine.

ANIMALS

10 healthy swine.

PROCEDURE

Tilmicosin base was administered via stomach tube at a single dose of 20 mg/kg (n = 5) or 40 mg/kg (5). Blood samples were obtained from a jugular vein immediately before and at 10, 20, and 30 minutes and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 hours after administration of tilmicosin. Tilmicosin concentrations in serum were quantified by use of a high-performance liquid chromatography procedure with UV light. Data for tilmicosin concentrations versus time were analyzed by use of compartmental and noncompartmental methods.

RESULTS

Tilmicosin concentrations in serum decreased in a biexponential manner after oral administration. Mean +/- SD values for absorption half-lives were 1.49 +/- 0.23 hours and 1.64 +/- 0.40 hours, distribution half-lives were 2.96 +/- 0.58 hours and 3.20 +/- 0.76 hours, elimination half-lives were 25.26 +/- 8.25 and 20.69 +/- 5.07 hours, peak concentrations were 1.19 +/- 0.30 microg/mL and 2.03 +/- 0.28 microg/mL, and time to peak concentrations was 3.12 +/- 0.50 hours and 3.48 +/- 0.77 hours after oral administration of tilmicosin base at a single dose of 20 or 40 mg/kg, respectively.

CONCLUSIONS AND CLINICAL RELEVANCE

In swine, tilmicosin was rapidly absorbed and slowly eliminated after oral administration of a single dose of tilmicosin base powder.

摘要

目的

测定猪口服单剂量替米考星碱后替米考星的药代动力学。

动物

10头健康猪。

步骤

通过胃管给予替米考星碱,单剂量为20mg/kg(n = 5)或40mg/kg(n = 5)。在给予替米考星之前以及给药后10、20和30分钟,以及1、2、3、4、6、8、12、24、36、48、72、96和120小时,从颈静脉采集血样。血清中替米考星浓度通过高效液相色谱紫外检测法进行定量。采用房室和非房室方法分析替米考星浓度随时间变化的数据。

结果

口服给药后,血清中替米考星浓度呈双指数下降。单剂量给予20mg/kg或40mg/kg替米考星碱后,吸收半衰期的均值±标准差分别为1.49±0.23小时和1.64±0.40小时,分布半衰期分别为2.96±0.58小时和3.20±0.76小时,消除半衰期分别为25.26±8.25小时和20.69±5.07小时,峰浓度分别为1.19±0.30μg/mL和2.03±0.28μg/mL,达峰时间分别为3.12±0.50小时和3.48±0.77小时。

结论及临床意义

在猪中,口服单剂量替米考星碱粉末后,替米考星吸收迅速但消除缓慢。

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