药效学的静脉和皮下tinzaparin和肝素在健康志愿者。
文章的细节
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引用
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Fossler MJ,巴雷特JS、海纳JW谜语詹,Ostergaard P, van der Elst E, Sprogel P
药效学的静脉和皮下tinzaparin和肝素在健康志愿者。
J制药健康系统。2001年9月1;58(17):1614 - 21所示。
- PubMed ID
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11556655 (在PubMed]
- 文摘
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静脉输液的药效学和皮下(南)tinzaparin相比,肝素钠在健康的志愿者进行了研究。随机、非盲、five-treatment five-period-crossover研究与拉丁方设计是在30岁健康男性进行估计tinzaparin药效学(anti-Xa anti-IIa活动)单剂静脉输液和南卡罗来纳州政府后,绝对生物利用度进行评估,以确定防腐剂的效果(苯甲醇),评估dose-activity关系,tinzaparin与依诺肝素相比较。南卡罗来纳州治疗是肝素(1)5000台。4500,(2)tinzaparin anti-Xa IU没有防腐剂南卡罗来纳州。4500,(3)tinzaparin anti-Xa IU没有防腐剂注射。12250年,(4)tinzaparin anti-Xa IU南卡罗来纳州防腐剂。,4500 (5)tinzaparin anti-Xa IU南卡罗来纳州防腐剂。血液样本的测量anti-Xa anti-IIa活动超过24小时。Anti-Xa anti-IIa活动显色测定方法;数据分析通过使用noncompartmental方法。基于anti-Xa tinzaparin活动的间隙范围从1.14到2.04 L /人力资源。分布的体积是3.1 - -5.0 L,这表明分子实体负责anti-Xa和anti-IIa活动局限于血管内空间。意味着anti-Xa活动高峰期发生在三到四个小时内注射后,独立的剂量。 The mean half-life of anti-Xa activity after s.c. injection ranged from 3.41 to 4.13 hours and was independent of the dose. The mean absolute bioavailability of s.c. tinzaparin was 86.7%. Intersubject pharmacodynamic variability was low for tinzaparin compared with heparin. Benzyl alcohol did not affect tinzaparin pharmacodynamics. A clear dose-activity relationship was seen for the two fixed doses of tinzaparin (12,250 and 4,500 IU). Single doses of tinzaparin were safe and well tolerated after administration by either route. The anti-Xa profile of tinzaparin supports the pharmacodynamic superiority of low-molecular-weight heparins over standard i.v. heparin administration. This pharmacodynamic study in healthy volunteers indicates that s.c. tinzaparin sodium was well absorbed; the presence of a preservative, benzyl alcohol, did not affect the activity of tinzaparin; and tinzaparin activity is dose-related.
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- 药物