Benznidazole microcrystal preparation by solvent change precipitation and in vivo evaluation in the treatment of Chagas disease
| Autor: | Isabel Mayer de Andrade, Marcilio Cunha-Filho, Maria Terezinha Bahia, Vivian Paulino Figueiredo, Lívia Cristina Lira de Sá-Barreto, André Talvani, Lívia Maria de Paula, Flávia Pires Maximiano |
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| Jazyk: | angličtina |
| Rok vydání: | 2011 |
| Předmět: |
Dissolution rate
Chagas disease Polymers Drug Compounding Trypanosoma cruzi Pharmaceutical Science Methylcellulose Microcrystals Excipients Mice Drug Delivery Systems Hypromellose Derivatives In vivo medicine Animals Chemical Precipitation Chagas Disease Hardness Tests Dissolution Aqueous solution Precipitation (chemistry) Chemistry General Medicine Trypanocidal Agents Bioavailability Solvent Crystallography Disease Models Animal Solubility Benznidazole Nitroimidazoles Solvents Solvent change precipitation Female Particle size Biotechnology medicine.drug Nuclear chemistry Tablets |
| Zdroj: | Repositório Institucional da UFOP Universidade Federal de Ouro Preto (UFOP) instacron:UFOP |
| Popis: | Benznidazole (BNZ) is traditionally used to treat Chagas disease. Despite its common use, BNZ has a poor water solubility and a variable bioavailability. The purpose of this study was to prepare BNZ microcrystals by solvent change precipitation and to study the effects of BNZ micronisation on therapeutic efficiency using a murine model of Chagas disease. The solvent change precipitation procedure was optimised in order to obtain stable and homogeneous particles with a small particle size, high yield and fast dissolu- tion rate. The thermal and crystallographic analysis showed no polymorphic change in the microcrystals, and microscopy confirmed a significant reduction in particle size. A marked improvement in the drug dis- solution rate was observed for micronised BNZ particles and BNZ tablets in comparison with untreated BNZ and commercial Rochagan . In vivo studies showed a significant increase in the therapeutic efficacy of the BNZ microparticles, corroborating the dissolution results. |
| Databáze: | OpenAIRE |
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