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对家兔进行的关于抗锥虫药乙酰氨基阿苯胂(贝尼尔)的体内分布及杀锥虫活性的研究。

Studies in rabbits on the disposition and trypanocidal activity of the anti-trypanosomal drug, diminazene aceturate (Berenil).

作者信息

Gilbert R J

出版信息

Br J Pharmacol. 1983 Sep;80(1):133-9. doi: 10.1111/j.1476-5381.1983.tb11058.x.

DOI:10.1111/j.1476-5381.1983.tb11058.x
PMID:6652366
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2044970/
Abstract

After intramuscular injection of 3.5 mg kg-1 to rabbits, diminazene aceturate shows biphasic pharmacokinetics with maximum blood and interstitial fluid concentrations occurring after 15 min and 3 h respectively. Seven days after treatment, 40-50% of the dose had been excreted in the urine and 8-20% in faeces. Highest diminazene residues were determined in liver: 7 days after dosage, residues of 40.53 +/- 4.00 micrograms g-1 were present, corresponding to 35-50% of the dose. The recommended dose of 3.5 mg kg-1 was not curative for Trypanosoma congolense infections of rabbit but did cause the parasitaemia to become subpatent. A limited prophylactic effect was observed.

摘要

给兔子肌肉注射3.5毫克/千克乙酰氨基阿维菌素后,其呈现双相药代动力学,血药浓度和组织液浓度分别在15分钟和3小时后达到最大值。治疗7天后,40 - 50%的剂量经尿液排出,8 - 20%经粪便排出。肝脏中检测到最高的乙酰氨基阿维菌素残留:给药7天后,残留量为40.53±4.00微克/克,相当于剂量的35 - 50%。推荐剂量3.5毫克/千克对兔刚果锥虫感染没有治疗效果,但确实使寄生虫血症变为隐性。观察到有限的预防作用。

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1
Studies in rabbits on the disposition and trypanocidal activity of the anti-trypanosomal drug, diminazene aceturate (Berenil).对家兔进行的关于抗锥虫药乙酰氨基阿苯胂(贝尼尔)的体内分布及杀锥虫活性的研究。
Br J Pharmacol. 1983 Sep;80(1):133-9. doi: 10.1111/j.1476-5381.1983.tb11058.x.
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Trypanocidal activity of blood and tissue fluid from normal and infected rabbits treated with curative drugs.用治疗药物处理的正常和感染兔子的血液及组织液的杀锥虫活性。
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