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氯氮䓬经静脉和肌肉注射给药后的药代动力学

Pharmacokinetics of chlorazepate after intravenous and intramuscular administration.

作者信息

Bertler A, Lindgren S, Magnusson J O, Malmgren H

出版信息

Psychopharmacology (Berl). 1983;80(3):236-9. doi: 10.1007/BF00436160.

Abstract

Dichlorazepate (DPC) was given to eight healthy volunteers aged 22-38 years (five males and three females). The dose was 20 mg (48.9 mumol) given either as an IV or an IM injection. The interval between the injections was at least 1 week. Plasma samples were analysed for desmethyldiazepam (DMD) by HPLC before and after acid hydrolysis. The kinetics after both IV and IM administration could be explained by a one or two compartment open model. By comparing values before and after hydrolysis an estimate of di- and/or monopotassiumchlorazepate (MPC) could be made. The bioavailability was almost 100% after IM administration. The plasma half lives of DPC and DMD were independent of the form of administration (2.42 and 46.0 h respectively after IV and 2.29 and 45.1 h respectively after IM injection).

摘要

将二氯氮䓬(DPC)给予8名年龄在22至38岁之间的健康志愿者(5名男性和3名女性)。剂量为20毫克(48.9微摩尔),通过静脉注射或肌肉注射给药。两次注射之间的间隔至少为1周。在酸水解前后,通过高效液相色谱法分析血浆样本中的去甲西泮(DMD)。静脉注射和肌肉注射后的动力学可以用单室或双室开放模型来解释。通过比较水解前后的值,可以估算二氯氮䓬钾和/或一氯氮䓬钾(MPC)。肌肉注射后的生物利用度几乎为100%。DPC和DMD的血浆半衰期与给药方式无关(静脉注射后分别为2.42小时和46.0小时,肌肉注射后分别为2.29小时和45.1小时)。

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