辛伐他汀片的人体生物等效性研究  

Bioequivalence of Simvastatin Tablets in Healthy Volunteers

作　　者：于洋[1] 杨汉煜[2] 侯艳宁[1] 张小丽[1] 张运好[1] 

机构地区：[1]解放军白求恩国际和平医院药剂科,石家庄050082 [2]石药集团中奇制药技术(石家庄)有限公司,石家庄050081

出　　处：《华北国防医药》2006年第6期385-387,共3页Medical Journal of Beijing Military Region

摘　　要：目的：研究两种辛伐他汀片的人体相对生物利用度，评价其生物等效性。方法：20名健康男性志愿者按照2制剂2周期的随机交叉试验设计，分别13服单剂量参比制剂和受试制荆，剂量均为20mg，采用液相色谱-串联质谱法测定人血浆中辛伐他汀的浓度，用DAS1．0软件计算各药代动力学参数并进行生物等效性统计分析。结果：受试制剂和参比制剂的主要药动学参数：cmax分别为（3．72±1．77）和（4．02±2．30）ng／ml；tmax分别为（1．5±0．8）和（1．3±0．5）h；AUC0-12h分别为（12．11±7．33）和（12．21±5．92）ng·h·ml^-1；AUC0-∞分别为（15．52±9．79）和（15．48±9．65）ng·h·ml^-1；t1/2分别为（6．5±4．2）和（5．8±4．7）h。两制剂的cmax、tmax、AUC0-12h和AUC0-∞均元显著性差异，双单侧t检验结果表明，受试制剂cmax的90％置信区间落在参比制剂的70％-143％范围内，受试制剂AUC的90％置信区间均落在参比制剂的80％-125％范围内，受试制剂的相对生物利用度为（103．4±32．6）％。结论：两制剂具有生物等效性。Objective：To evaluate the bioequivalenee of two kinds of Simvastatin tablets in healthy male volunteers. Methods：In a randomized crossover design,20 healthy male volunteers were given a single oral dose of 20 mg test or reference Simvastatin tablets. The concentrations of simvastatin in human plasma were determined by a HPLC-MS/MS method. Results：The main pharmaeokinetic parameters of the test and reference Simvastatin tablets were as follows ：cmax were （3.72 ± 1.77 ） and （4.02 ± 2.30 ） ng/ml, tmax were （ 1.5 ± 0.8 ） and （ 1.3 ± 0.5 ） h, AUC0-12; were （12.11 ±7.33） and （12.21 ±5.92） ng·h·ml^-1,AUC0-∞, were （15.52 ± 9.79） and （15.48 ±9.65） ·h·ml^-1, and t1/2 were （6.5 ± 4.2） and （5.8 ± 4.7 ） h,respectively. The relative bioavailability of the test tablets was （103.4 ± 32.6 ）%. There was no significant difference in cmax、tmax、AUC0-12h, and AUC0-∞ between the two preparations. The 90% eonfidential interval of cmax and AUC were between 70% - 143% ,and 80% - 125% respectively according to those of the referenee tablets. Conclusion：The two preparations were bioequivalent.

关 键 词：辛伐他汀 片剂 液相色谱-串联质谱法 生物等效性 

分 类 号：R972.6[医药卫生—药品] R945.2[医药卫生—药学]