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丙硫咪唑在囊虫患者体内药代动力学的研究
引用本文:关天颖,宫相义,孙伟之,刘淑珍,郑连舫,李明珪,李阿丽.丙硫咪唑在囊虫患者体内药代动力学的研究[J].吉林农业大学学报,1988(3).
作者姓名:关天颖  宫相义  孙伟之  刘淑珍  郑连舫  李明珪  李阿丽
作者单位:吉林农业大学 (关天颖,宫相义,孙伟之,刘淑珍,郑连舫,李明珪),吉林农业大学(李阿丽)
摘    要:用反相高效液相色谱法测定丙硫咪唑的中间代谢体丙硫咪唑亚砜和丙硫咪唑砜,在7名囊虫患者体内的血药含量及药代动力学研究,以含0.40%乙酸的光谱纯甲醇为流动相,以色谱柱MicrQ Bondpak CN 0.39×15cm 10μ为固定相,紫外检测器波长290nm,以甲苯咪唑为内标物亚砜收率为95.23±6.74%;砜收率为90.04%±5.32%。不同浓度水平测定结果,日内和日间变动系数均小于10%;以亚砜加砜为实测值的药代动力学符合有吸收因素二室模型。患者单剂量口服丙硫咪唑25mg/kg体重时,平均血药10h达峰,亚砜加砜之和为558.14±208.34ng/ml血;生物半衰期t_(1/2)β为13.54±3.11h;血浆清除率CLB为132.79±45.58L/kg·h。

关 键 词:高效液相色谱  丙硫咪唑  丙硫咪唑亚砜  丙硫咪唑砜  药代动力学

STUDY ON PHARMACOKINETICS OF ALBENDAZOLE AND ITS INTERMEDIATES (SULFONE AND SULFOXIDE) IN HUMAN BODY OF PATIENT SUFFERING FROM CYSTICERCOSIS
Guan Tianying.STUDY ON PHARMACOKINETICS OF ALBENDAZOLE AND ITS INTERMEDIATES (SULFONE AND SULFOXIDE) IN HUMAN BODY OF PATIENT SUFFERING FROM CYSTICERCOSIS[J].Journal of Jilin Agricultural University,1988(3).
Authors:Guan Tianying
Institution:Guan Tianying
Abstract:A RP-HPLC method for assay of albendazole and its intermediates, e.g. sulfoxide and sulfone in blood has been established. The blood levels and pharmacokinetics of sulfoxide and sulfone are studied in 7 volunteers with neurocysticercosis and muscle-skin type of cysticercosis and in 3 healthy volunteers.Methanol (purity of spectrum) containing acetic acid is employed as mobile phase, and Micro Bondpak CN 0.39x 15cm 10u. as stationary phase column. UV detector at 290nm and mebendazole as internal standard are used. Lowermost contents of sulfoxide and sulfone in blood are 3.054ng/ml and 1.024ng/ml respectively. Phatmacokinetics of intermediates of albendazole conforms to two-compartments model presenting factor of absorption.After a single oral dose of 25mg/kg to neurocysticercosis patients and healthy person vrith albendazole, the pharmacokinetic parameters are as follows- for the patients, tmax (tp) = 10 (hr) ; Cmax = 558.1494+208.3397(ng/ml), t1/2B= 13.5419+3. 1133 (hr); Vd = 23075. 1013 +7668.5696 (100ml/kg), C1b = 1327.981+455.8059 (100ml/kg-hr)
Keywords:HPLC  albendazole  sulfoxide  sulfone  pharmacokinetics    
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