Purification of the antichagasic benznidazole from the commercial preparation Rochegan®: characterization of inclusion complexes with β-cyclodextrin

Abstract

The Chagas is a endemic disease from the American continent whose etiological agent is the Trypanosoma cruzi. Currently, there is neither a prophylactic vaccine for this disease or a totally effective treatment for the chronic cases. The Nifurtimox and the benznidazole are nitroheterocyclic complexes that have been used since the end of the 60’s and the beginning of the 70’s, mainly for the treatment of congenital and acute infections. However, these medications can cause a wide variety of adverse effects. Especially, in the benznidazole is necessary to develop new therapeutic alternatives which improve its low solubility in water, the limited gastrointestinal absorption, and the high toxicity. Because of the difficulties that often occur in the achievement of pre-synthesis Benznidazole, high costs in the synthesis process and buy the active compound in countries with limited research economics commodities. We have proposed a method of purification in order to facilitate the experimental procedures from the commercial preparation Rochegan®, obtaining BNZ viable for the formation of the controlled release complex with β-cyclodextrin (βCD) and the characterization of the BNZ-βCD inclusion complex.

El Chagas es una enfermedad endémica del continente americano cuyo agente etiológico es el Trypanosoma cruzi. Actualmente, no hay una vacuna profiláctica para esta enfermedad o un tratamiento totalmente eficaz ´ para los casos crónicos. El Nifurtimox y el Benznidazol (BNZ) son complejos nitroheterocíclicos que se han utilizado desde finales de los anos 60 y principios de los a ˜ nos 70, principalmente para el tratamiento de infecciones congénitas y agudas. Sin embargo, estos medicamentos pueden causar una amplia variedad de efectos adversos. Especialmente, en el benznidazol es necesario desarrollar nuevas alternativas terapéuticas que mejoren su baja solubilidad en agua, la absorción gastrointestinal limitada, y su alta toxicidad.