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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Bioavailability and pharmacokinetics of lorazepam after intranasal, intravenous, and intramuscular administration.
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Bioavailability and pharmacokinetics of lorazepam after intranasal, intravenous, and intramuscular administration.

机译：劳拉西m经鼻内，静脉内和肌肉内给药后的生物利用度和药代动力学。

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摘要

The purpose of this study was to evaluate the pharmacokinetic profile of intranasal lorazepam in comparison to currently established administration routes. Eleven healthy volunteers completed this randomized crossover study. On three occasions, each separated by a 1-week washout, subjects received a 2 mg dose of lorazepam via the intranasal, intravenous, or intramuscular route. Blood samples were collected serially from 0 to 36 hours. Noncompartmental methods were used to determine pharmacokinetic parameters. Lorazepam was well absorbed following intranasal administration with a mean (%CV) bioavailability of 77.7(11.1). Intranasal administration resulted in a faster absorption rate than intramuscular administration. Elimination profiles were comparable between all three routes. The concentration-time profile for intranasal delivery demonstrated evidence of a double peak in several subjects, suggesting partial oral absorption. Females were found to have significantly higher AUC values than males for all three delivery routes. Overall, this study demonstrated favorable pharmacokinetics of intranasal lorazepam in relation to standard administration methods. Intranasal delivery could provide an alternative, noninvasive delivery route for lorazepam.
机译：这项研究的目的是评估与目前确定的给药途径相比，鼻内劳拉西m的药代动力学特征。 11名健康志愿者完成了这项随机交叉研究。在三种情况下，每次间隔1周，受试者通过鼻内，静脉内或肌内途径接受2 mg剂量的劳拉西m。从0到36小时连续收集血样。非房室方法用于确定药代动力学参数。劳拉西m经鼻内给药后被良好吸收，平均（％CV）生物利用度为77.7（11.1）。鼻内给药比肌肉内给药产生更快的吸收速率。消除曲线在所有三种途径之间是可比的。鼻内给药的浓度-时间曲线证明在几个受试者中出现双峰，表明部分口服吸收。发现在所有三种递送途径中，女性的AUC值均明显高于男性。总的来说，该研究表明与标准给药方法相比，鼻内劳拉西m的药物动力学良好。鼻内给药可为劳拉西m提供另一种非侵入性的给药途径。

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