Polymorphic screen and drug–excipient compatibility studies of the antichagasic benznidazole

The purpose of this study was to investigate the polymorphism and compatibility of benznidazole (BNZ), a drug used in the treatment of Chagas disease. This drug was subjected to a polymorphic screen using a number of solvents and precipitation procedures to explore the possible existence of differen...

Full description

Saved in:
Bibliographic Details
Published in:Journal of thermal analysis and calorimetry 2011-12, Vol.106 (3), p.819-824
Main Authors: Maximiano, Flávia Pires, Novack, Kátia Monteiro, Bahia, Maria Terezinha, de Sá-Barreto, Lívia Lira, da Cunha-Filho, Marcílio Sérgio Soares
Format: Article
Language:English
Subjects:
Analysis
Analytical Chemistry
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Biological and medical sciences
Calorimetry
Chemistry
Chemistry and Materials Science
Crystals
Cyclodextrins
General pharmacology
Infrared spectroscopy
Inorganic Chemistry
Measurement Science and Instrumentation
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Physical Chemistry
Polymer Sciences
Polyols
Rain and rainfall
Structure
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The purpose of this study was to investigate the polymorphism and compatibility of benznidazole (BNZ), a drug used in the treatment of Chagas disease. This drug was subjected to a polymorphic screen using a number of solvents and precipitation procedures to explore the possible existence of different crystal structures of BNZ. The compatibility of BNZ with selected pharmaceutical excipients was evaluated in binary mixtures, in a ratio of 1:1 (w/w). These results were then analyzed with a variety of techniques, including differential scanning calorimetry, Fourier transform infrared spectroscopy, and X-ray powder diffractometry. No polymorphic forms of BNZ were detected despite some observed changes in the DSC profile. The thermal data indicate interaction of the drug with excipients hydroxyethylcellulose, polyethylene glycol, and hydroxypropyl-β-cyclodextrin. Additional studies using infrared spectroscopy confirm the incompatibility of BNZ with only the polyethylene glycol. This excipient should not be used in the development of solid dosage forms containing BNZ.
ISSN:1388-6150
1588-2926
1572-8943
DOI:10.1007/s10973-011-1371-6