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目的:动态观察了乙醇摄入对口服磺胺嘧啶在小鼠体内过程及生物利用度的影响。方法:灌胃(ig)给予2.5g·kg-1乙醇,一天一次,分别于2,4,6,8周静脉注射磺胺嘧啶400mg·kg-1,2d后灌胃给于同等剂量磺胺嘧啶,比色法测定血浓,3P87药物动力学软件计算AUCiv、T1/2βiv、AUCig、T1/2βig、Tmax、Cmax。结果:2至4周,磺胺嘧啶在小鼠体内的AUCig、T1/2βig、Tmax、Cmax明显减少,6周后,AUCig、T1/2βig、Tmax、Cmax及生物利用度均明显增加,8周后与乙醇摄入6周相比,AUCig、T1/2βig明显增加,Tmax明显延长,Cmax及生物利用度则下降。结论:乙醇摄入可明显影响磺胺嘧啶的体内过程及生物利用度,其影响程度和方法取决于乙醇摄入时间和量
OBJECTIVE: To dynamically observe the effects of ethanol intake on the course and bioavailability of oral sulfadiazine in mice. Methods: Intravenous (ig) was given 2.5g · kg-1 ethanol once a day, respectively, at 2,4,6,8 weeks after intravenous injection of sulfadiazine 400mg · kg-1d after oral administration of the same dose of sulfadiazine , Blood concentration was measured by colorimetric method, and AUCiv, T1 / 2βiv, AUCig, T1 / 2βig, Tmax, Cmax were calculated by 3P87 pharmacokinetic software. Results: The AUCig, T1 / 2βig, Tmax and Cmax of sulfadiazine in mice were significantly decreased from 2 to 4 weeks. After 6 weeks, the AUCig, T1 / 2βig, Tmax, Cmax and bioavailability increased significantly. Compared with 6 weeks of ethanol ingestion, AUCig, T1 / 2βig significantly increased, Tmax significantly prolonged, Cmax and bioavailability decreased. Conclusions: Ethanol ingestion can significantly affect the in vivo process and bioavailability of sulfadiazine, and its extent and effect depend on the time and amount of ethanol intake