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常规和长效土霉素制剂在基利斯山羊体内的药代动力学

Pharmacokinetics of Conventional and Long-Acting Oxytetracycline Preparations in Kilis Goat.

作者信息

Aktas İbrahim, Yarsan Ender

机构信息

Faculty of Veterinary Medicine, Department of Pharmacology and Toxicology, Ankara University, Ankara, Turkey.

出版信息

Front Vet Sci. 2017 Dec 22;4:229. doi: 10.3389/fvets.2017.00229. eCollection 2017.

Abstract

The pharmacokinetics of conventional and long-acting (LA) oxytetracycline (OTC), widely used broad-spectrum antibacterial drugs in veterinary medicine, were evaluated in Kilis goats at single dosage of 20 mg/kg body weight (bw). A total of 21 goats were divided into three groups: intravenous (Group I) and intramuscular (IM) (Group II) administration of the conventional formulation and IM administration of the LA formulation (Group III). Blood samples were taken at 0.25, 0.5, 1, 2, 4, 8, 12, 24, 36, 48, 60, 72, and 96 h; and OTC analysis was performed by HPLC. For Group III and Group II, time to reach maximal plasma drug concentration () was 0.6 ± 0.28 and 0.46 ± 0.09 h and maximal plasma drug concentrations () were 8.72 ± 2.47 μg/ml and 13.57 ± 5.83 μg/ml, respectively. In Group I, concentration was found to be 63.51 ± 11.59 μg/ml. The elimination times () were 10.84 ± 3.20, 27.96 ± 11.66, and 10.47 ± 1.30 h; and AUC were 115 ± 29.12, 96.44 ± 9.49, and 80.86 ± 12.76 μg/ml/h for Group I; Group II, and Group III, respectively. Bioavailability by IM administration were 69.71% for the conventional OTC and 83.15% for the LA OTC.

摘要

土霉素(OTC)是兽医学中广泛使用的广谱抗菌药物,本研究以单剂量20毫克/千克体重对基利斯山羊的常规土霉素和长效土霉素的药代动力学进行了评估。总共21只山羊被分为三组:静脉注射(第一组)和肌肉注射(第二组)常规制剂,以及肌肉注射长效制剂(第三组)。在0.25、0.5、1、2、4、8、12、24、36、48、60、72和96小时采集血样;并通过高效液相色谱法进行土霉素分析。对于第三组和第二组,达到最大血浆药物浓度()的时间分别为0.6±0.28小时和0.46±0.09小时,最大血浆药物浓度()分别为8.72±2.47微克/毫升和13.57±5.83微克/毫升。在第一组中,浓度为63.51±11.59微克/毫升。消除时间()分别为10.84±3.20、27.96±11.66和10.47±1.30小时;第一组、第二组和第三组的曲线下面积(AUC)分别为115±29.12、96.44±9.49和80.86±12.76微克/毫升/小时。常规土霉素肌肉注射的生物利用度为69.71%,长效土霉素为83.15%。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/181d/5743916/d91d2eeb986e/fvets-04-00229-g001.jpg

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