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体外模拟口服利福平降解试验

In vitro modeling of the degradation of rifampicin after oral administration
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摘要 目的:模拟研究酸碱度和异烟肼对利福平服药后降解的作用。方法:将利福平、利福平与不同比例的异烟肼混合,放入盛有pH 6.8缓冲溶液和pH 1盐酸溶液的溶出杯中,37℃,100 r.min-1的条件下,在0,1,2 h取样,用HPLC法测定利福平和三甲酰利福霉素的含量,观察利福平的降解情况。结果:利福平在碱性环境(pH 6.8)中很少降解,在酸性条件下降解增加,加入异烟肼后降解显著增加。结论:利福平在酸性条件下,与异烟肼同时存在时降解明显增加。 Objective: To investigate the influence of pH on degradationof rifampicin combined with isoniazid after oral administration.Methods: Rifampcin and isoniazid were mixed in different proportions.The mixture was added into cups containing dissolution buffer solutions at pH 6.8 or hydrochlric acid solution at pH1,at 37 ℃,and agitated at 100 r·min-1.Under the conditions,samples were taken at 0,1 and 2 h.An HPLC method was adopted to determine rifampcin and 3-formyl rifamycin contents.Results: The degradation of rifampcin increased in the acidic condition,and rarely occurred in the alkaline condition.However,the degradation significantly increased after adding isoniazid.Conclusion: In acidic conditions and in the presence of isoniazid,the degradation of rifampicin can be increased.
出处 《中国新药杂志》 CAS CSCD 北大核心 2012年第2期202-205,共4页 Chinese Journal of New Drugs
基金 河南省重点技术创新项目(2002232)
关键词 利福平 异烟肼 高效液相色谱 降解 rifampicin isoniazid high performance liquid chromatography degradation
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