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碘醚柳胺脂质体定向剂在绵羊体内的药代动力学及组织残留量 被引量:9

Pharmacokinetics and Tissue Residues of Rafoxanide liposomes in the Sheep
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摘要 应用碘醚柳胺脂质体定向剂(包封率58%)给绵羊单剂量皮下注射(0.3mg/kg),用 反相高效液相色谱法(RP-HPLC)测定了该药在绵羊体内不同时间的血浆药物浓度以及组织中的药物残留量。利用3p87实用药作动力学软件分析,结果表明,该药的药代动力学符合一室模型,动力学方程为:C=3.1164(e^-0.0192t-e^-1. 5155t)。药代动力学参数为:达矣时间(Tmax)为(2.8112±0.7492) The concentrations of rafoxanide in plasma and tissues of sheep injected with rafoxanide liposomes subcutaneously at a dose of 0.3 mg/kg were determined by reserve phase high performance liquid chromatography (RP HPLC). Analyzed by 3p87 practical pharmacokinetics software, the results showed that the pharmacokinetics of rafoxanide liposomes in sheep fitted one compartment model with an equation of C=3.116 4(e -0.019 2t -e -1.515 5t ). The average peak time (T max ) was (2.811 2±0.749 2) d; the average elimination half time (t 1/2β ), (36.381 6±3.038 5) d and the average area under curve (AUC) (143.553 0±47.235 4) μg·mL -1 ·d -1 . In contrast with the result of subcutaneous injection of rafoxanide at a dose of 0.3 mg/kg, the T max of rafoxanide liposomes was 1.464 7 days earlier, and the T 1/2β of rafoxanide liposomes prolonged 16.209 7 days. The tissue residues of rafoxanide in liver was (23.033 1±3.204 8) μg/g after 28 days of administration. No residue was detectable in kidney, bile and muscle all the time .In contrast with the results of subcutaneous injection of rafoxanide at a dose of 3 mg/kg, the residues of sheep treated with rafoxanide liposomes was higher in liver and lower in kidney and muscle. The above results indicated that the rafoxanide liposomes would be more effective than rafoxanide injection for the treatment of fascioliasis.
出处 《中国兽医杂志》 CAS 北大核心 2000年第1期62-65,共4页 Chinese Journal of Veterinary Medicine
基金 吉林省科委基金!(960 4 0 8)
关键词 脂质体定向剂 药代动力学 组织残留量 绵羊 RAF rafoxanide liposome pharmacokinetics tissue residue sheep RP HPLC
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  • 1刘汉清.提高难溶性药物生物利用度的技术措施[J].药学通报,1983,18:14-14. 被引量:1
  • 2胡昌良.难溶性药物增溶的某些方法(药学讲座)[M].中国药学会江苏分会科学技术普及委员会,1981(2).24. 被引量:1
  • 3(英)布拉德(Blood,D.C.)著,萧佩蘅等.家畜传染病学和寄生虫病学[M]农业出版社,1986. 被引量:1

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