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目的:研究低氧条件下阿苯达唑在小鼠体内药代动力学的特点。方法:在低压氧舱中给予小鼠阿苯达唑灌胃,分别于不同时间点摘眼球取血。常氧实验组按相同方法灌胃和取血,行高效液相色谱法测定血清药物浓度,并采用DAS2.0软件计算各组阿苯达唑及其代谢产物阿苯达唑亚砜的药代动力学参数。结果:低氧组阿苯达唑和阿苯达唑亚砜的最高血药浓度分别为:(0.73±0.05)mg/L、(4.40±0.55)mg/L,药时曲线下面积分别为(54.35±9.77)mg/(h·L)、(734.40±26.55)mg/(h·L);常氧组分别为:(0.23±0.09)mg/L、(8.55±0.53)mg/L以及(28.35±6.37)mg/(h·L)、(922.36±31.38)mg/(h·L)(n=10,P<0.01)。结论:低氧条件下阿苯达唑代谢速率较常氧时缓慢进行,有效成分阿苯达唑亚砜的产量低于常氧组,而原药残留量高于常氧组。
Objective: To study the pharmacokinetics of albendazole in mice under hypoxic conditions. Methods: The mice were given albendazole intragastrically in the hypobaric chamber, and the eyeballs were taken blood at different time points respectively. The experimental group of normoxia was fed by the same method with blood and the serum concentration of drugs was determined by HPLC. The data of albendazole and its metabolite albendazole sulfoxide in each group were calculated by DAS2.0 software Kinetic parameters. Results: The maximum plasma concentrations of albendazole and albendazole sulfoxide in hypoxia group were (0.73 ± 0.05) mg / L and (4.40 ± 0.55) mg / L, respectively. The areas under the curve were 54.35 ± 9.77 mg / (h · L) and (734.40 ± 26.55) mg / (h · L), respectively; normoxia group was (0.23 ± 0.09) mg / L and 28.35 ± 6.37) mg / (h · L), (922.36 ± 31.38) mg / (h · L) (n = 10, P <0.01). CONCLUSION: The rate of albendazole metabolism in hypoxia is slower than that in normoxia. The yield of albendazole sulfoxide is lower than that in normoxia group, while the residual content of albendazole is higher than normoxia group.