头孢地尼胶囊在中国健康人群空腹/高脂餐后给药的生物等效性研究  

Bioequivalence of cefdinir capsules in Chinese healthy population under fasting/high-fat fed condition

作　　者：张泽宇 张行飞 杨双[1] 阳晓燕[1] 叶玲 崔畅 阳国平[1] 黄洁[1] ZHANG Zeyu;ZHANG Xingfei;YANG Shuang;YANG Xiaoyan;YE Ling;CUI Chang;YANG Guoping;HUANG Jie(Center of Clinical Pharmacology,the Third Xiangya Hospital,Central South University,Changsha 410013,Hunan,China;Postdoctoral Research Station of Clinical Medicine,the Third Xiangya Hospital,Central South University,Changsha 410013,Hunan,China)

机构地区：[1]中南大学湘雅三医院临床药理中心,湖南长沙410013 [2]中南大学湘雅三医院博士后科研流动站,湖南长沙410013

出　　处：《中国临床药理学与治疗学》2020年第7期740-745,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：中南大学湘雅三医院博士后科研启动资金。

摘　　要：目的:评价健康人空腹/餐后服用两种头孢地尼胶囊的生物等效性及安全性。方法:26例健康志愿者空腹随机交叉单剂量口服头孢地尼胶囊受试制剂或参比制剂,36例健康志愿者餐后随机交叉单剂量口服头孢地尼胶囊受试制剂或参比制剂,头孢地尼体内血药浓度采用液相色谱-质谱串联(LC-MS/MS)法测定,药动学参数及等效性采用WinNonlin 6.4和SAS 9.4软件计算和评价。结果:25例健康志愿者空腹服用头孢地尼胶囊受试制剂和参比制剂的Cmax、AUC0-t和AUC0-∞的几何均值比的90%置信区间分别为93.01%~109.22%、96.16%~110.06%和96.38%~110.16%,均在80.00%~125.00%的生物等效性范围内。36例健康志愿者餐后服用头孢地尼胶囊受试制剂和参比制剂的Cmax、AUC0-t和AUC0-∞的几何均值比的90%置信区间分别为93.91%~103.28%、92.93%~100.72%和92.97%~101.26%,均在80.00%~125.00%的生物等效性范围内。健康志愿者空腹服用头孢地尼胶囊受试制剂和参比制剂的不良事件发生率分别是12.0%和11.5%。健康志愿者餐后服用头孢地尼胶囊受试制剂和参比制剂的不良事件发生率分别是25.0%和27.8%。结论:头孢地尼胶囊受试制剂与参比制剂具有生物等效性,志愿者在本试验给药剂量下安全性和耐受性良好。AIM:To evaluate the bioequivalence and safety of two cefdinir capsules under a fasting/high-fat fed condition in healthy people.METHODS:Twenty-six healthy volunteers were randomized to cross-test single-dose oral cefdinir capsules or reference preparations for fasting.Thirty-six healthy volunteers were randomized to crossed single-dose oral cefdinir capsule test preparations or reference preparations after high-fat meals.The blood concentration of cefdinir was determined by liquid chromatographymass spectrometry(LC-MS/MS).Pharmacokinetic parameters and equivalence were calculated and evaluated using Win Nonlin 6.4 and SAS 9.4 software.RESULTS:The 90%confidence intervals of the geometric mean ratios of the Cmax,AUC0-t,and AUC0-∞for the test and reference preparations of cefdinir capsules taken by twenty-five healthy volunteers for fasting were 93.01%-109.22%,96.16%-110.06%,and96.38%-110.16%,all at 80.00%-125.00%within the range of bioequivalence.The 90%confidence intervals of the geometric mean ratios of the Cmax,AUC0-t,and AUC0-∞for the test and reference preparations of cefdinir capsules taken by thirty-six healthy volunteers for a high-fat fed were 93.91%-103.28%,92.93%-100.72%and 92.97%-101.26%,all at 80.00%-125.00%within the range of bioequivalence.The incidences of adverse reactions in healthy volunteers taking cefdinir capsules for the fasting test and reference preparations were 12.0%and 11.5%,respectively.The incidence of adverse reactions in healthy volunteers taking cefdinir capsules after the meal was25.0%and 27.8%,respectively.CONCLUSION:The test preparation of cefdinir capsules and the reference preparation are bioequivalent,and the volunteers show good safety and tolerability under the test dose.

关 键 词：头孢地尼胶囊 空腹/高脂餐后给药 生物等效性 药动学 

分 类 号：R969.1[医药卫生—药理学]