高脂高热量饮食对中国健康受试者口服莫西沙星片药代动力学的影响  

Effects of high-fat diet intake on pharmacokinetics of moxifloxacin tablets in healthy Chinese volunteers

作　　者：郭彩会[1] 赵娜[1] 孙文荣 丁琮洋 史犇 孙雪 宋浩静[1] 邱博[1] 白万军[1] GUO Cai-hui;ZHAO Na;SUN Wen-rong;DING Cong-yang;SHI Ben;SUN Xue;SONG Hao-jing;QIU Bo;BAI Wan-jun(Department of Pharmacy,Hebei General Hospital,Shijiazhuang 050051,Hebei Province,China;Shijiazhuang Siyao Co.,Ltd,Shijiazhuang 052100,Hebei Province,China;Suzhou Guochen Biotek Company Limited,Suzhou 215104,Jiangsu Province,China)

机构地区：[1]河北省人民医院药学部,河北石家庄050051 [2]石家庄四药有限公司,河北石家庄052100 [3]苏州国辰生物科技股份有限公司,江苏苏州215104

出　　处：《中国临床药理学杂志》2023年第23期3444-3448,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的观察中国健康受试者空腹和高脂高热量饮食情况下口服莫西沙星片的药代动力学特征。方法按单中心、随机、开放、单剂量的试验方法设计,其中空腹和餐后均为24例。健康受试者分别在空腹或高脂高热量饮食条件下单剂量口服莫西沙星片0.4 g,分别按方案规定的时间点采集静脉血样,用液相色谱-串联质谱法测定人血浆中莫西沙星的血药浓度,用Phoenix WinNonlin 8.2软件按非房室模型法计算主要药代动力学参数,并对其做描述性统计分析。结果莫西沙星片空腹和高脂高热量饮食后的主要药代动力学参数如下:C_(max)分别为(2286.09±802.64)和(1963.33±474.99)ng·mL^(-1),t1/2分别为(12.32±1.42)和(13.56±1.38)h,AUC_(0-t)分别为(2.70±0.51)×10^(4)和(2.60±0.55)×10^(4)ng·mL^(-1)·h,AUC_(0-∞)分别为(2.88±0.54)×10^(4)和(2.85±0.63)×10^(4)ng·mL^(-1)·h,t_(max)分别为1.50和2.00 h。高脂高热量饮食后服药与空腹条件下服药相比,AUC变化不明显,Cmax降低了14.12%,t_(max)推迟约0.5 h(均P>0.05)。结论食物对莫西沙星的吸收和代谢速度,吸收程度无影响。Objective To evaluate the effects of fasting and high-fat diet on the pharmacokinetics of moxifloxacin in Chinese healthy adult subjects.Methods A single-center,randomized,open,single-dose trial design was used in this study,healthy subjects were assigned to receive single dose of moxifloxacin tablets 0.4 g in either fasting or high-fat diet state,and blood samples were taken at different time points,respectively.The concentrations of moxifloxacin in plasma were determined by liquid chromatography-tandem mass spectrometry.Results The main pharmacokinetic parameters of moxifloxacin in fasting state and high-fat diet states were as follows:C_(max)were(2286.09±802.64)and(1963.33±474.99)ng·mL^(-1);t_(1/2)were(12.32±1.42)and(13.56±1.38)h;AUC_(0-t)were(2.70±0.51)×10^(4) and(2.60±0.55)×10^(4) ng·mL^(-1)·h;AUC_(0-∞)were(2.88±0.54)×10^(4) and(2.85±0.63)×10^(4) ng·mL^(-1)·h;t_(max)were 1.50 and 2.00 h.After high-fat diet,the AUC was not significantly changed,C_(max)was decreased by 14.12%,and t_(max)was indistinctively delayed(all P>0.05).Conclusion Food had no effects on the absorption rate and degree of moxifloxacin.

关 键 词：莫西沙星片 高脂高热量饮食 药代动力学 食物效应 液相色谱-串联质谱 

分 类 号：R978.1[医药卫生—药品]