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HERO ID
668189
Reference Type
Journal Article
Title
Effect of maltosyl-beta-cyclodextrin on drug binding to serum albumin
Author(s)
Miyoshi, T; Matsuda, A; Amino, M; Kataoka, M; Sato, M
Year
1997
Volume
57
Issue
3
Page Numbers
174-180
Abstract
IPA COPYRIGHT: ASHP The effect of maltosyl-beta-cyclodextrin on the serum protein binding of a new triazol antifungal agent MFB-1041 is reported. The bound fraction of MFB-1041 to human serum albumin (HSA) and fatty acid free HSA decreased when the cyclodextrin was added, and similar behavior was observed in mice serum. When MFB-1041 dissolved in a highly concentrated solution of the cyclodextrin was injected into mice, the elimination of the drug from serum was more rapid than when administered without cyclodextrin. The amount of drug distributed to the brain at 15 sec after injection was smaller for injections with cyclodextrin than those without. The clonic convulsion induced by MFB-1041 was blocked by the cyclodextrin. These data indicate that MFB-1041 could be present in serum as a cyclodextrin complex form, and unbound fraction and bound fractions to serum decreased. However, the effect of the cyclodextrin in vitro on the pharmacokinetics of MFB-1041 through serum protein binding could not be explained by the data in this study. It was concluded that solubilizing agents such as maltosyl-beta-cyclodextrin could affect the disposition and pharmacological effect of intravenous drugs into mice.
Keywords
151856-47-2; 104723-60-6
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