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丙硫苯咪唑及其代谢物在黄牛体内的药物动力学研究

STUDY ON PHARMACOKINETICS OF ALBENDAZOLE AND ITS METABOLITE IN CATTLE
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摘要 给装置了皱胃瘘管的四头健康成年黄牛(体重217.50±42.91公斤)口服丙硫苯味唑(Albendazole),剂量:10mg/kg,给药后定时从颈静脉采血和从皱胃瘘管中收集皱胃液。用乙醚萃取法从血浆和皱胃上清液中提取药物。用高效液相色谱法测定血浆和皱胃液中的药物浓度。结果在胃液中的原药未能测出,而具有活性的代谢产物亚砜和砜于给药72小时后仍可测出。亚砜和砜的出现峰浓度时间(T_(max))分別为15.50±6.20h和22.80±6.70h:峰浓度(C_(max))分别为3.07±0.81μg/ml和4.91±1.45μg/ml;给药后血浆中原药亦未能测出,而具有活性的代谢物亚砜和砜在血浆中的药物动力学参数是:亚砜T_(1/2)Kel 20.46±5.43h,T_(max)15.50±5.75h,C_(max)0.50±0.21μg/ml:砜T_(1/2)Ke1 11.58±4.29h,T_(max)14.50±6.40h,C_(max)0.99±0.79μg/ml。上述结果,说明该药是长效的。. Four healthy adult cattle(217.5 ± 42.91 kg ) installed with abomasal fistula were given albendazole orally. Blood and abomasai juice samples were collected from jugular vein and the fistula at different Intervals after administration respectively. The drugs was extracted from the plasma of blood and the supernatant of abomasal juice by ether extraction technique. Its concentration in the plasma and the supernatant was measured by high-perf ormance liquid chromatography. The results were as follows. Albendazole was not detected in abomasal juice, but its active metabolites, sulfoxide and sulfone, were measured even after 72 hours of administration. The appearance of peak concentration times of sulfoxide and sulfone were 15.50±6.20 and 22.80±6.70 hr,respectively, and peak concentrationa of them were 3.07±0.81 μg/ml and 4.91±1.45 μg/ml respectively. Albendazole was not measured in the plasma either. However, the sulfoxide and sulfone could remainer loger time. The parameters calculated by microcomputer for sulfoxide were T _(1/2) Kel 20.64 ±5.43 hr, Tmax 15.5±5.75 hr, Cmax 0.50±0.21 μg/ml, and those for Sulfone were T(1/2) Kel. 11.58±4.29 hr, Tmax 14.5 ±6.40 hr, Cmax 0.99±0.79 μg/ml. The results indicate that albendazole has a long-time effect.
出处 《华中农业大学学报》 CAS CSCD 北大核心 1989年第2期155-159,共5页 Journal of Huazhong Agricultural University
关键词 丙硫苯咪唑 黄牛 药物动力学 亚砜 albendazole sulfoxide sulfone cattle pharmacokinetics
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