高脂高热量饮食对中国健康受试者口服盐酸克林霉素胶囊药代动力学的影响  

Effect of high-fat diet intake on pharmacokinetics of clindamycin hydrochloride capsule in healthy Chinese volunteers

作　　者：赵娜[1] 孙雪 宋浩静[1] 万青华 史犇 贾彩云[1] 邱博[1] 胡义亭[1] 郭彩会[1] 董占军[1] ZHAO Na;SUN Xue;SONG Hao-jing;WAN Qing-hua;SHI Ben;JIA Cai-yun;QIU Bo;HU Yi-ting;GUO Cai-hui;DONG Zhan-jun(Department of Medicine,Hebei General Hospital,Shijiazhuang 050051,Hebei Province,China;China Shijiazhuang Pharmaceutical Company Zhongqi Pharmaceutical Technology(Shijiazhuang)Company Limited,Shijiazhuang 050035,Hebei Province,China;Suzhou Guochen Biotek Company Limited,Suzhou 215104,Jiangsu Province,Chirm)

机构地区：[1]河北省人民医院Ⅰ期临床研究室,河北石家庄050051 [2]石药集团中奇制药技术(石家庄)有限公司,河北石家庄050035 [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》2022年第6期570-574,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：目的探索空腹和高脂高热量饮食情况下盐酸克林霉素胶囊在中国健康受试者中的药代动力学特征。方法本方案按单中心、随机、开放、单剂量的试验设计。空腹和高脂饮食条件下各入组24例中国健康受试者,单次口服盐酸克林霉素胶囊0.15 g,给药前后按时间点采集静脉血样。用液相色谱-串联质谱法(LC-MS/MS)测定血浆中克林霉素的浓度并计算药代动力学参数。结果盐酸克林霉素胶囊空腹和高脂饮食后的主要药代动力学参数如下:C_(max)分别为(2008.13±595.75),(1733.29±407.77)ng·mL^(-1);t1/2分别为(3.17±0.80),(3.18±0.83)h;AUC_(0-t)分别为(6316.20±2521.19)和(8467.10±2428.23)ng·h·mL^(-1);AUC_(0-∞)分别为(6447.30±2569.29)和(8650.00±2488.65)ng·h·mL^(-1);T_(max)中位数(范围)分别为0.75(0.33,1.33)和2.50(0.50,4.00)h;高脂饮食后服药较空腹条件下服药,AUC_(0-t)及AUC_(0-∞)分别增加34.05%和34.16%,T_(max)延迟1.75 h,差异均有统计学意义(P<0.01),C_(max)降低13.68%,差异无统计学意义(P>0.05)。结论高脂饮食对盐酸克林霉素胶囊的药代动力学参数有显著影响,可使药物的吸收程度显著增加,达峰时间明显延迟。Objective To evaluate the effects of high-fat diet on the pharmacokinetics of clindamycin in Chinese healthy adult subjects.Methods This program is designed according to a single-center,randomized,open,single-dose trial.Forty-eight healthy subjects were assigned to receive single dose of clindamycin hydrochloride capsule 0.15g in either fasting and high-fat diet state,and blood samples were taken at different time points,repectively.The concentrations of clindamycin in plasma were determined by high-performance liquid chromatography-tandem mass spectrometry.Results The main pharmacokinetic parameters of clindamycin in fasting state and high-fat diet state were as follows:C_(max)were(2008.13±595.75)and(1733.29±407.77)ng·m L^(-1);t_(1/2) were(3.17±0.80)and(3.18±0.83)h;AUC_(0-t)were(6316.20±2521.19)and(8467.10±2428.23)ng·h·m L^(-1);AUC_(0-∞)were(6447.30±2569.29)and(8650.00±2488.65)ng·h·m L^(-1);median T_(max)(range)were0.75(0.33,1.33)h and 2.50(0.50,4.00)h,after high-fat diet,AUC_(0-t)and AUC_(0-∞)increased by 34.05%and 34.16%respectively,T_(max)delayed by 1.75 h,all with statistical significance(all P<0.01);C_(max) decreased by 13.68%(P>0.05).Conclusion High-fat diet has a significant impact on the pharmacokinetic parameters of clindamycin hydrochloride capsules,which can significantly increase the absorption of the drug and significantly delay the peak time.

关 键 词：克林霉素 高脂饮食 药代动力学 食物效应 

分 类 号：R969.1[医药卫生—药理学]