Development and in vitro evaluation of tablets based on the antichagasic benznidazole

Abstract

This work aimed to verify the interferences caused by the use of excipients for immediate release tablets based on benznidazole obtained by direct compression and the accomplishment of a comparative study between the tablets developed and the reference medicine Rochagan TM , obtained by wet granulation. Seven smallscale batches (SSB) were developed and aspects such as compressibility, powder flow, mean weight, friability, disintegration, hardness, assay, content uniformity, kinetic of release in vitro (dissolution) and drug/excipients physical-chemical compatibility were evaluated. Based on the obtained results it can be verified that the analyzed powders presented adequated characteristics for the direct compression process, beyond the inexistent evidence of a physical-chemical interaction between the drug and the tested excipients. The tablets obtained from SSB I and III were chosen for the comparative study with the reference medicine, demonstrating similarity with the statistically treated obtained results, becoming an alternative option of a medicine product for the treatment of Chagas' disease with reduced cost and satisfactory quality.

The Use of Solid Dispersion Systems in Hydrophilic Carriers to Increase Benznidazole Solubility

“…The concentration of BNZ was measured using ultraviolet (UV) spectrophotometry, in accordance with methodology developed and validated by SoaresSobrinho et al 10 with a theoretical concentration of the standard solution and 20 :g/mL samples.…”

“…Samples of 5 mL were taken at fixed intervals of 15 min, for a total of 2 h, from the dissolved medium, filtered through 0.45 :m cellulose filters, and analyzed under UV spectrophotometer Micronal R B582 (Brooklin, São Paulo, Brazil) at 324 nm. 10 Volumes of solvent equal to those of the samples collected were then added to the dissolution vats and the assays were carried out in quadruplicate for each binary system. Table 1 shows the main results related to the structure and energetics of the two complexes formed between PVP or PEG monomers and BNZ.…”

“…4) showed typical characteristics of a crystalline anhydrous product with high purity, with a single endothermic process at about 190 • C related to the melting point of pure substance, 17 with subsequent exothermic process concerning the thermal degradation of the drug at 287.06 • C. Although PVP has several endothermic processes in the range of 50-120 • C due to water loss, showing no melting characteristic endothermic process of the substance as that is an amorphous substance, PEG has a melting endothermic peak at about 65 • C.…”