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Interaction between nitroheterocyclic compounds with beta-cyclodextrins: phase solubility and HPLC studies.

作者信息

de Melo Nathalie F S, Grillo Renato, Rosa André Henrique, Fraceto Leonardo Fernandes

机构信息

Departamento de Engenharia Ambiental, Universidade Estadual Paulista Júlio de Mesquita Filho, Campus Sorocaba, Av. Três de Março 511, CEP 18087-180, Sorocaba, São Paulo, Brazil.

出版信息

J Pharm Biomed Anal. 2008 Aug 5;47(4-5):865-9. doi: 10.1016/j.jpba.2008.04.022. Epub 2008 Apr 29.

DOI:10.1016/j.jpba.2008.04.022
PMID:18534804
Abstract

Chagas disease is a serious health problem for Latin America. Nitrofurazone (NF) and Hidroxymethylnitrofurazone (NFOH) are active against Trypanosoma cruzi. The effect of beta-cyclodextrin (beta-CD) and dimethyl-beta-cyclodextrin (DM-beta-CD) complexation on the UV absorption and retention time of nitrofurazone (NF) and its hydroxymethylated analog (NFOH) were studied in solution. The retention behavior was analyzed on a reversed phase C18 column and the mobile phase used was acetonitrile-water (20/80 v/v), in which cyclodextrins (beta-CD or DM-beta-CD) were incorporated as a mobile phase additive. The decrease in the retention times of NF (or NFOH) with increasing concentration of HP-beta-CD enables the determination of the complex stability constants by HPLC. A phase-solubility study was performed, according to the method reported by Higuchi and Connors, to evaluate the changes of NF/NFOH in the complexation state, and the diagrams obtained suggested that it forms complexes with a stoichiometry of 1:1. This is an important study for the characterization of potential formulations to be used as therapeutic options for the treatment of Chagas disease.

摘要

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