Penicaut B, Maugein P, Maisonneuve H, Rossignol J F
Bull Soc Pathol Exot Filiales. 1983 Nov;76(5):698-708.
Albendazole, a new broad spectrum benzimidazole anthelmintic, has been administered in 10 male volunteers. Administration was randomized using 100 mg tablets, 200 mg tablets and a 2% suspension. Blood samples were obtained 0.5; 1; 1.5; 2; 2.5; 3; 3.5; 4; 5; 6; 8; 12; 24; 72 h after treatment. Albendazole sulfoxide, one of the mains albendazole blood metabolites, was assayed by HPLC and the blood half life was calculated as 8 1/2 h. The three different pharmaceutical formulations were considered bioequivalent. Urines were collected, and using T. L. C. Technics, main metabolites were identified and characterized. Hydrolysis of the carbamate function and oxidation of the sulfur atom, the alkyle chain and the aromatic ring were the main biotransformations observed.
阿苯达唑是一种新型广谱苯并咪唑驱虫药，已对10名男性志愿者进行了给药试验。使用100毫克片剂、200毫克片剂和2%混悬液进行随机给药。在治疗后0.5小时、1小时、1.5小时、2小时、2.5小时、3小时、3.5小时、4小时、5小时、6小时、8小时、12小时、24小时、72小时采集血样。阿苯达唑亚砜是阿苯达唑的主要血液代谢产物之一，采用高效液相色谱法进行测定，计算出血浆半衰期为8.5小时。三种不同的药物制剂被认为具有生物等效性。收集尿液，采用薄层色谱技术鉴定并表征主要代谢产物。观察到的主要生物转化包括氨基甲酸酯官能团的水解以及硫原子、烷基链和芳环的氧化。
