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华西医学  2015 

洛伐他汀烟酸缓释片人体药物代谢动力学研究

DOI: 10.7507/1002-0179.20150540, PP. 1881-1886

Keywords: 洛伐他汀烟酸缓释片,高效液相色谱-串联质谱法,药物代谢动力学

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Abstract:

目的?研究洛伐他汀烟酸缓释片在中国健康受试者体内的药物代谢动力学特征。方法?单次给药每周期分别口服洛伐他汀烟酸缓释片20/500、20/750、20/1000mg;连续给药每次口服洛伐他汀烟酸缓释片20/1000mg,1次/d,连续5d。每周期给药前及给药后10、20、30、45min,1、1.5、2、2.5、3、3.5、4、5、7、9、12、15h采集血样。采用高效液相色谱-串联质谱法检测血浆中洛伐他汀、烟酸及其代谢产物烟酰胺和烟脲酸的浓度。结果?烟酸在500~1000mg剂量范围内,烟脲酸峰浓度和药-时曲线下面积(0-t)与剂量呈线性关系;连续给药情况下,烟脲酸和洛伐他汀在体内没有蓄积;不同配比的烟酸组分对洛伐他汀的体内代谢无影响;男女受试者药物代谢动力学参数差异无统计学意义(P>0.05)。结论?洛伐他汀烟酸缓释片具备线性动力学特征,连续给药无蓄积,代谢不受性别影响。

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