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地高辛生物利用度:制剂与输注速率

Digoxin bioavailability: formulations and rates of infusions.

作者信息

Marcus F I, Dickerson J, Pippin S, Stafford M, Bressler R

出版信息

Clin Pharmacol Ther. 1976 Sep;20(3):253-9. doi: 10.1002/cpt1976203253.

Abstract

The bioavailability of digoxin (lanoxin) tablets, oral aqueous solution of digoxin, and capsules containing a solution of digoxin was compared with digoxin given intravenously over 1 and 3 hr. The mean peak serum concentration of digoxin after the 1-hr intravenous infusion was 5 ng/ml, after the 3-hr infusion, 3.5 ng/ml, and after the oral solution, 2.0 ng/ml. There was an equivalent bioavailability of the oral solution and reference tablets of digoxin. The digoxin in capsules tended to be better absorbed than the reference tablets. There was 21% more digoxin excreted over 6 days after the 3 hr iv infusion than after the 1 hr iv infusion. This indicates that the calculated bioavailability of an orally administered dose of digoxin may vary with the rapidity of injection of the intravenous standard. It is estimated that an oral tablet of digoxin of 0.5 mg has about the same bioavailability as 0.35 of digoxin given by slow intravenous infusion (or 0.4 mg if calculated against a rapid intravenous injection).

摘要

将地高辛(Lanoxin)片剂、地高辛口服水溶液以及含有地高辛溶液的胶囊的生物利用度与静脉注射1小时和3小时的地高辛进行了比较。静脉注射1小时后,地高辛的平均血清峰值浓度为5纳克/毫升,3小时输注后为3.5纳克/毫升,口服溶液后为2.0纳克/毫升。地高辛口服溶液和参比片剂具有等效的生物利用度。胶囊中的地高辛比参比片剂的吸收倾向于更好。静脉注射3小时后6天内地高辛的排泄量比静脉注射1小时后多21%。这表明口服地高辛剂量的计算生物利用度可能随静脉标准注射的速度而变化。据估计,0.5毫克的地高辛口服片剂的生物利用度与缓慢静脉输注0.35毫克地高辛(或根据快速静脉注射计算为0.4毫克)的生物利用度大致相同。

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