高脂饮食对环丝氨酸在中国健康受试者体内药动学中的影响  

Effect of high-fat food intake on pharmacokinetics of cycloserine in healthy subjects

作　　者：毛征生 赵娜[1] 王鑫[1] 刘有平[1] 邸欣[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2014年第2期143-146,共4页Journal of Shenyang Pharmaceutical University

摘　　要：目的研究高脂饮食对环丝氨酸在健康中国人体内药动学中的影响。方法 10名健康受试者(男女各半)双周期交叉设计,分别于空腹或进食高脂餐后经口给予环丝氨酸胶囊1粒(含环丝氨酸250 mg),采用液相色谱-串联质谱(LC-MS/MS)法测定血浆中环丝氨酸的质量浓度,用Phoenix WinNonlin 6.0软件计算主要药动学参数,用SPSS 16.0软件对主要药动学参数进行统计学分析。结果受试者于空腹和进食高脂餐后的主要药动学参数分别为:ρmax:(9.56±3.15)和(7.21±2.90)mg·L-1;t1/2:(11.4±3.2)和(12.5±4.4)h;t max:(1.8±1.4)和(2.8±1.1)h;AUC0-48 h:(125.73±34.36)和(111.83±43.49)mg·h·L-1;AUC0-∞:(134.97±36.84)和(125.23±46.75)mg·h·L-1。对空腹与进食高脂餐后给药的主要药动学参数采用配对t检验进行统计分析:ρmax具有显著性差异(P<0.05)。结论进食高脂餐可对环丝氨酸的吸收速度有显著影响,使t max延迟、ρmax显著降低,但并不影响环丝氨酸的吸收程度。Objective To study the effect of high-fat food intake on pharmacokinetics of cycloserine in healthy Chinese subjects. Methods Ten healthy volunteers were orally administrated with cycloserine capsule （250 mg per capsule） by a random doubly periodic cross-resident study design. The concentration of cy- closerine in plasma was determined by LC-MS/MS. The main pharmacokinetic parameters were calculated with Phoenix WinNonlin 6.0 software, and completed the data analysis with SPSS16.0. Results The main pharmacokinetic parameters of cycloserine following single oral administration of the cycloserine capsule to volunteers under high-fat meal and fasting conditions were as follows ： ρmax ： （ 9. 56 ± 3. 15 ） and （7.21 ± 2.90） mg.L-1 ; t1/2 ：（11.4 ±3.2） and （12. 5 ±4.4） h; tmax ：（1.8±1.4） and （2. 8 ±1.1） h; AUC0-48h ：（125. 73 ± 34.36） and （111.83 ±43.49） mg.h.L-1; AUC0-∞ ：（134.97 ±36.84） and （125.23±46.75） mg.h.L-1 ,respectively. Paired-samples t-test was used in those parameters statistical analysis. The results demonstrated ρmax was sig- nificantly difference between high-fat meal and fasting conditions （P 〈 0. 05 ）. Conclusions Eating high-fat meal can significantly affect the absorption rate of cycloserine, which makes tin,x delay and ρmax reduce signif- icantly, but does not affect the extent of absorption of cycloserine.

关 键 词：环丝氨酸 药动学 饮食 液相色谱串联质谱 

分 类 号：R971[医药卫生—药品]