低氧条件下阿苯达唑在小鼠体内的药代动力学研究  

Research on Pharmacokinetics of Albendazole in Vivo under Hypoxic Environment in Mice

作　　者：王晴晴[1] 万陈飞 朱彪 李梅 

机构地区：[1]青海大学附属医院乳腺甲状腺外科,810001 [2]青海省人民医院普外科,810007 [3]青海电力集体产业管理公司医务室,810008

出　　处：《高原医学杂志》2016年第3期3-7,共5页Journal of High Altitude Medicine

摘　　要：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 explore the pharmacokinetics of albendazole under hypoxic conditions for providing some references on clinical pharmaceutical research at plateau region. Methods： Albendazole orally administered to mice in the hypobaric chamber,eyeball blood were got at different time points. Mice in normoxic group were given the same manner and taking blood. Drug concentrations in serum were detected by high performance liquid chromatography. Pharmacokinetics parameters of albendazole and its metabolites were calculated by DAS 2. 0 software in each group. Results： Maximum serum concentrations of albendazole and albendazole sulfoxide in hypoxia group were（ 0. 73 ± 0. 05） mg /Land（ 4. 40 ± 0. 55） mg /L,respectively,the area under the curve were（ 54. 35 ± 9. 77）mg /（ h·L） and（ 734. 40 ± 26. 55） mg /（ h·L）. Normoxia group were（ 0. 23 ± 0. 09） mg / L,（ 8. 55 ± 0. 53）mg / L and（ 28. 48 ± 6. 37） mg /（ h·L）,（ 922. 36 ± 31. 38） mg /（ h·L）,respectively,（ n = 10,P 0. 01）.Conclusion： Metabolic rate of albendazole was slower under hypoxic conditions,and the yield of albendazole sulfoxide as active ingredient was less than normoxic gloup. However,the original drug residue was with a high concentration under normoxic conditions.

关 键 词：低氧 阿苯达唑 药代动力学 

分 类 号：R965[医药卫生—药理学]