摘要
目的：研究酒石酸美托洛尔片在正常人体的相对生物利用度及药动与药效学。方法：采用配对交叉设计，12名健康男性志愿者随机分成2组，志愿者单次口服酒石酸美托洛尔片 试验制剂或参比制剂后，在不同时间点取静脉血，血药浓度采用高效液相色谱法（HPLC） 测定。以静止心率和血压变化为指标反映美托洛尔的β-受体阻断作用。生物等效性采用双 单侧t检验作判断。结果：志愿者单次服用100 mg酒石酸美托洛尔片试验制剂或参比制剂后的药动学参数AUC0-12 、Cmax、Tmax、T1/2分别为(861.8±431.3)和(8 51.6±457.4) ng·h·ml-1，（173.1±66.7）和（186.2±96.3 ） ng·ml-1,(1.1±0.5)和(1.1±0.5) h、(3.8±1.2)和(4.1±0 .7) h。相对生物利用度为(103.8±17.1)%，血药浓度与心率下降呈正相关，且对正 常人的降压作用均不明显。结论：两种制剂等效，每种制剂均有明显的减慢心率作用。
OBJECTIVE To study the relative bioavailability,pharmacokinetics and pharmacodynamics of m etoprolol tartrate tablet. METHODS In an open randomized cross-over test a single oral dose of metoprolol tartrate reference or test tablet was given to 12 healthy volunteers.The metoprolol conc entrations in plasma were determined by HPLC.The β-blocker of effect metoprolo l was measured by resting heart rate and blood pressure. RESULTS After a single oral dose 100mg of metoprolol tartrate test or reference tablet, the AUC0-12、Cmax、Tmax、T1/2 were(861.8± 431.3) and (851.6±457.4) ng·h·ml-1,(173.1±66.7) and (186.2±96.3) ng·ml-1,(1.1±0.5) and (1.1±0.5) h,（3.8± 1.2） and （4.1±0.7） h respectively,relative bioavailability was （103 .8±17.1）%.Positive correlation was found between metoprolol concentration i n plasma and decreased value of heart rate(P<0.01).No significant decrea sed blood pressure was found in 12 healthy volunteers. CONCLUSIONS Two formulations were bioequivalents.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2001年第10期589-592,共4页
Chinese Journal of Hospital Pharmacy
