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地塞米松及其磷酸酯的药代动力学

Pharmacokinetics of dexamethasone and its phosphate ester.

作者信息

Rohdewald P, Möllmann H, Barth J, Rehder J, Derendorf H

出版信息

Biopharm Drug Dispos. 1987 May-Jun;8(3):205-12. doi: 10.1002/bdd.2510080302.

Abstract

Dexamethasone in form of its phosphate was given intravenously in two different doses (1.5 mg kg-1 and 15 mg). Plasma levels of the ester and dexamethasone were measured and pharmacokinetic parameters were calculated. The results indicate no dose-dependency of the pharmacokinetic parameters in the investigated range for dexamethasone. Conversion from the prodrug to the active form was rapid; maximum dexamethasone plasma concentrations were reached after 10 min. The results were verified by dexamethasone level monitoring in patients after chronic dosing. Predicted and achieved steady state levels agreed well.

摘要

以磷酸酯形式存在的地塞米松通过静脉注射给予两种不同剂量(1.5毫克/千克和15毫克)。测量了酯和地塞米松的血浆水平并计算了药代动力学参数。结果表明,在所研究的地塞米松剂量范围内,药代动力学参数不存在剂量依赖性。前药向活性形式的转化迅速;10分钟后达到地塞米松血浆最大浓度。通过对长期给药患者的地塞米松水平监测验证了结果。预测的和实际达到的稳态水平吻合良好。

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