Anticryptosporidial activity of furan derivative G1 and its inclusion complex with beta-cyclodextrin

被引:23
作者
Castro-Hermida, JA
Gómez-Couso, H
Ares-Mazás, ME
Gonzalez-Edia, MM
Castañeda-Cancio, N
Otero-Espinar, FJ
Blanco-Mendez, J
机构
[1] Univ Santiago de Compostela, Fac Farm, Dept Farm & Tecnol Farmaceut, Santiago De Compostela 15782, Spain
[2] Univ Santiago de Compostela, Fac Pharm, Dept Microbiol & Parasitol, Parasitol Lab, Santiago De Compostela 15782, Spain
[3] Cent Univ Las Villas, Fac Chem & Pharm, Santa Clara, Cuba
关键词
beta-cyclodextrin; G1; inclusion complex; kneading method; suckling murine model; anticryptosporidial in vivo efficacy;
D O I
10.1002/jps.10528
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The capacity of beta-cyclodextrin (PCD) to form a complex with a new furanic derivative, G1, was investigated. Interactions of the drug and betaCD in solution and in the solid state were studied using phase solubility techniques, thermal methods, X-ray, and IR spectroscopy. Preparation of a kneaded mix of G1/betaCD increased both the aqueous solubility and the dissolution rate of the furan derivative. The anticryptosporidial efficacies of the drug and of the inclusion complex were evaluated using a suckling murine model. Oral administration of G1 considerably decreased the intensity of the infection, but PCD showed similar anticryptosporidial activity to that of the betaCD-G1 complex and higher activity than G1 alone. (C) 2004 Wiley-Liss, Inc.
引用
收藏
页码:197 / 206
页数:10
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