特布他林的药代动力学参数在健康的人。概述。

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尼伯格L

特布他林的药代动力学参数在健康的人。概述。

和说5欧元。1984;134:149-60。

PubMed ID
6586475 (在PubMed
]
文摘

单剂静脉注射后,血浆浓度的特布他林multi-exponential方式。non-compartmental因此最好计算药代动力学参数的方法。直到6 - 12 h后静脉注射特布他林进入mono-exponential下降阶段。玩忽职守的行为产生了终端半衰期的报告文学,是低估了。长期抽样显示,特布他林在健康受试者的终端半衰期大约17 h和主题之间的关于两方面的变化。beplayapp这个半衰期决定,意思是,大约一半的血浆浓度时间曲线下面积。beplayapp大多数研究已经完成了男性受试者。平均而言,他们有一个身体间隙3.0毫升/分钟/公斤,2/3是肾的贡献。根据体重、肾清除率至少在女性像男性那么高,可能有点大。特布他林的体积分布的稳态平均1.6 L /公斤。 The systemic mean residence time of the drug is about 9 h. Terbutaline is little bound to plasma proteins but shows affinity to erythrocytes. However, clearance calculations should probably be based on the plasma concentration, because of a comparatively slow release rate from the erythrocytes. After oral administration, plasma concentration peaks of terbutaline appear within 1-4 h. Food reduces their height by about 40%. Particularly after single doses, more than one concentration peak is observed in plasma. Subjects differ considerably in their oral absorption capacity of the drug; an interindividual range of about 25-80% of the dose can be estimated. This creates a range in the extent of bioavailability of 7-26%, the decrease of the percentages being due to a high first-pass metabolism. There are strong indications that this occurs preferentially in the gut wall. The predominant metabolite of terbutaline formed in man is a sulphate conjugate. Mean bioavailability of oral terbutaline in fasting subjects is 14-15%. Food impairs the bioavailability by about one third because of reduced absorption. Despite the large variation in extent of terbutaline bioavailability between subjects, each individual behaves reproducibly from dose to dose.

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