Pharmacokinetic evaluation of new forms of benznidazole tablets in albino rabbits

• Grant number: 14/13192-8
• Support Opportunities: Regular Research Grants
• Start date: August 01, 2014
• End date: July 31, 2016
• Field of knowledge: Biological Sciences - Pharmacology
• Principal Investigator: Rosangela Gonçalves Peccinini
• Grantee: Rosangela Gonçalves Peccinini
• Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

Chagas disease is an illness that affects millions of people worldwide, especially in developing countries. It is caused by the parasite Trypanosoma cruzi, which causes serious harm to the host, particularly in cardiac tissue. In Brazil, the only drug available to treat Chagas disease is benznidazole. The drug is administered only as immediate release tablets of 100 mg (Ministry of Health) into two or three daily doses for 60 days. Despite the efficacy of this drug, in the acute phase of the disease, the treatment presents many adverse effects that limit its use and it does not show considerable activity in the chronic phase . Furthermore, due to the unavailability of pediatric presentations, the treatment in children is accomplished by extemporaneous solution from 100 mg tablets, resulting in high variability of administered dose. Thus, this project aims to assess the preclinical pharmacokinetics of new benznidazole tablets for the treatment of Chagas disease. Tablets to be evaluated were developed through pharmaceutical technologies for extended-release ( 100 mg ) and pediatric dose of 12.5 mg, aiming the reduction of the frequency of administration of the drug and improvement of treatment in children with more accurate doses. Pharmacokinetic parameters of these new formulations will be compared to the conventional tablet available by the Ministry of Health for the treatment of disease. Through these results it will be possible to define the advantages from the pharmacokinetic and pharmacotecnical points of view for the new formulations and the planning of future clinical trials. (AU)

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

DAVANCO, MARCELO GOMES; CAMPOS, MICHEL LEANDRO; ROSA, TALITA ATANAZIO; PADILHA, ELIAS CARVALHO; ALZATE, ALEJANDRO HENAO; ROLIM, LARISSA ARAUJO; ROLIM-NETO, PEDRO JOSE; PECCININIA, ROSANGELA GONCALVES. Benznidazole Extended-Release Tablets for Improved Treatment of Chagas Disease: Preclinical Pharmacokinetic Study. Antimicrobial Agents and Chemotherapy, v. 60, n. 4, p. 2492-2498, APR 2016. (13/25882-6, 14/13192-8)

MARQUES, LUCAS M. M.; CALLEJON, DANIEL R.; PINTO, LARISSA G.; DE CAMPOS, MICHEL L.; DE OLIVEIRA, ANDERSON R. M.; VESSECCHI, RICARDO; ADHIKARI, ACHYUT; SHRESTHA, RAM L. S.; PECCININI, ROSANGELA G.; LOPES, NORBERTO P.. Pharmacokinetic properties, in vitro metabolism and plasma protein binding of govaniadine an alkaloid isolated from Corydalis govaniana Wall. Journal of Pharmaceutical and Biomedical Analysis, v. 131, p. 464-472, NOV 30 2016. (13/17658-9, 13/16496-5, 14/13192-8, 14/23604-1)