| 泰拉霉素注射液在猪体内的药物动力学及生物利用度研究 |
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| 引用本文： | 赵永达,刘帅帅,焦晓军,倪姮佳,于慧敏,贺湘仁,王斯帆,曾振灵,黄显会.泰拉霉素注射液在猪体内的药物动力学及生物利用度研究[J].中国农业科学,2011,44(4):823-828. |
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| 作者姓名： | 赵永达 刘帅帅 焦晓军 倪姮佳 于慧敏 贺湘仁 王斯帆 曾振灵 黄显会 |
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| 作者单位： | (华南农业大学兽医学院/国家残留基准实验室); |
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| 基金项目： | 国家十一五科技支撑计划(2006BAD31B06) |
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| 摘 要： | 【目的】 研究并比较新型大环内酯类抗生素泰拉霉素注射液和瑞可新注射液在猪体内的药物代谢动力学特征及生物利用度。【方法】 30头健康猪,随机分为3组,进行单次给药剂量(2.5mg?kg-1)静注、肌注泰拉霉素注射液和肌注瑞可新注射液,前腔静脉采血,HPLC-ESI-MS/MS法检测猪血浆中泰拉霉素的浓度,罗红霉素做内标。采用药动学软件 WinnonlinTM 的非房室模型分析方法,计算出有关药物动力学参数。【结果】 猪静注给药的药时数据符合非房室模型,静脉注射给药后,血浆清除率为158.3mL?kg-1?h-1,稳态表观分布容积为14.9L?kg-1,消除半衰期为65.8h。肌注泰拉霉素注射液(河南惠中)和肌注瑞可新注射液(美国辉瑞)后,吸收迅速,注射给药后15min,血药浓度达峰值,Cmax 分别为839.22ng?mL-1、746.31ng?mL-1。血浆中平均消除半衰期分别为70.3h和65.1h;采用统计分析软件Excel 2003和SPSS 16.0分析各项药动学参数,均没有显著性差异(P＞0.05),表明两者药动学特征相似。与瑞可新注射液(美国辉瑞)相比,国产的泰拉霉素注射液,相对生物利用度为117%,绝对生物利用度为112%,说明肌注给药吸收较完全,消除缓慢,生物利用度高。【结论】泰拉霉素肌注后在猪体内具有吸收迅速,体内分布广,达峰迅速,消除较慢,与肌注瑞可新注射液(辉瑞)药动学特征相似。
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| 关 键 词： | 泰拉霉素 药物代谢动力学 生物利用度 生物等效性 猪 |
| 收稿时间： | 2010-07-31; |
Pharmacokinetic and Bioavailability Study of Tulathromycin in Swine |
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| ZHAO Yong-da,LIU Shuai-shuai,JIAO Xiao-jun,NI Heng-jia,YU Hui-min,HE Xiang-ren,WANG Si-fan,ZENG Zhen-ling,HUANG Xian-hui.Pharmacokinetic and Bioavailability Study of Tulathromycin in Swine[J].Scientia Agricultura Sinica,2011,44(4):823-828. |
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| Authors: | ZHAO Yong-da LIU Shuai-shuai JIAO Xiao-jun NI Heng-jia YU Hui-min HE Xiang-ren WANG Si-fan ZENG Zhen-ling HUANG Xian-hui |
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| Affiliation: | ZHAO Yong-da1,LIU Shuai-shuai1,JIAO Xiao-jun1,NI Heng-jia1,YU Hui-min1,HE Xiang-ren2,WANG Si-fan2,ZENG Zhen-ling1,HUANG Xian-hui1(1College of Veterinary Medicine/National Reference Laboratory of Veterinary Drug Residues,South China Agricultural University,Guangzhou 510642,2Swine-Breeding of Guangdong,Guangzhou 510642) |
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| Abstract: | 【Objective】The pharmacokinetics and bioavailability of the triamilide antimicrobial, tulathromycin, were investigated in swine. 【Method】Thirty pigs received 2.5 mg?kg-1 of tulathromycin injection by either intravenous (i.v.) or intramuscular (i.m.) route in three studies: study A (0 pigs, i.v.) ,study B (0 pigs, i.m, Huizhong, China.) and study C (0 pigs, i.m, Pfizer,USA.). Blood samples were collected and analysed by high-performance liquid chromatography (HPLC) with tandem mass pectrometry detection (LC-MS/MS) using ESI. Pharmacokinetic parameters were estimated using the WinNonlinTM software package and SPSS 16.0 analysis of the time and concentration data. 【Result】The tulathromycin concentration time data were fitted to noncompartment model. After i.v. injection plasma clearance (Cl) was 182.7 mL?h-1?kg-1, the volume of distribution at steady-state (Vss) was 17.2 L?kg-1 and the elimination t1/2 was 64.8 h. Statistical analysis on plasma showed that there were no signi?cant differences between pharmacokinetic parameters (P＞0.05).Compared with tulathromycin (Pfizer,USA.), the relative bioavailability (Huizhong, China) following i.m. administration was 117%,the absolute bioavailability (Huizhong, China) following i.v. administration was 112%. It appeared that tulathromycin was rapidly absorbed , eliminated slowly and highly bioavailable . 【Conclusion】The results indicate that the two formulations are bioequivalent in both the rate and extent of absorption. |
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| Keywords: | Tulathromycin pharmacokinetic bioavailability bioequivalence swine |
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