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伊曲康唑口服溶液和静脉制剂:药代动力学与药效学综述

Itraconazole oral solution and intravenous formulations: a review of pharmacokinetics and pharmacodynamics.

作者信息

Willems L, van der Geest R, de Beule K

机构信息

University Hospital Gasthuisberg, Herestraat 49, B-3000 Leuven, Belgium.

出版信息

J Clin Pharm Ther. 2001 Jun;26(3):159-69. doi: 10.1046/j.1365-2710.2001.00338.x.

Abstract

Itraconazole is a triazole antifungal agent with a broad spectrum of activity. It is well tolerated and highly efficacious, particularly because its main metabolite, hydroxy-itraconazole, also has considerable antifungal activity. Two new formulations of itraconazole, an oral solution and an intravenous formulation, have recently been developed, which combine lipophilic itraconazole with cyclodextrin. These formulations have improved the solubility of itraconazole, leading to enhanced absorption and bioavailability compared with the original capsule formulation, without having an impact on the tolerability profile of itraconazole. The oral solution and intravenous formulations of itraconazole produce consistent plasma concentrations and are ideal for the treatment of systemic fungal infections in a wide range of patient populations. The additional flexibility offered by the different routes of administration means that itraconazole treatment can be specifically tailored for use in all patients, including children and those requiring intensive care.

摘要

伊曲康唑是一种具有广谱活性的三唑类抗真菌药。它耐受性良好且疗效显著,特别是因为其主要代谢产物羟基伊曲康唑也具有相当强的抗真菌活性。最近开发了两种伊曲康唑的新剂型,即口服溶液和静脉制剂,它们将亲脂性伊曲康唑与环糊精结合在一起。这些剂型提高了伊曲康唑的溶解度,与原胶囊剂型相比,吸收和生物利用度得到增强,且对伊曲康唑的耐受性没有影响。伊曲康唑的口服溶液和静脉制剂可产生一致的血浆浓度,是治疗广泛患者群体中系统性真菌感染的理想药物。不同给药途径提供的额外灵活性意味着伊曲康唑治疗可专门针对所有患者进行定制,包括儿童和需要重症监护的患者。

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