Desarrollo de una formulación de tabletas revestidas de secnidazol 500 mg / Development of a formulation of coated secnidazole tablets 500 mg

Se describe el desarrollo de una formulación de tabletas revestidas de secnidazol 500 mg. Durante el desarrollo de esta se evaluaron 2 métodos: la granulación seca y la granulación húmeda. En el revestimiento de las tabletas se empleó un sistema hidroalcohólico con el preparado comercial Policoat YS 1-7003 (Opadry)®. Los lotes sometidos a ensayos de estabilidad fueron elaborados a escala piloto, por la vía de granulación húmeda, lo que demostró la factibilidad del proceso de fabricación a esta escala. Las tabletas revestidas presentaron adecuadas propiedades físico-mecánicas y tecnológicas y estas fueron envasadas en frascos de polietileno de alta densidad y en sobres termoconformados de polivinilcloruro/aluminio. La estabilidad química y microbiológica de las tabletas de secnidazol fue estudiada durante 24 meses; los resultados demostraron que estas cumplían con los requisitos establecidos durante este periodo.

The development of a formulation of coated Secnidazole tablets 500mg was described. During its development, 2 methods were evaluated: dry granulation and humid granulation. A hydroalcoholic system was used with the Policoat YS 1-7003 (Opadry)® commercial preparation for coating the tablets. The batches subjected to stability assays were made at pilot scale by humid granulation, which showed the feasibility of the manufacturing process at this scale. The coated tablets had adequate physicomechanical and technological properties and they were packed in polyethylene flasks of high density and in polyvinyl chloride/aluminium thermoconformed envelopes. The chemical and microbiological stability of the secnidazole tablets were studied during 24 months. The results demonstrated that these tablets met the requirements established during this period.

Correlation of biological activity (therapeutic and toxic) with solvochromic properties of metronidazole, emetine hydrochloride and diloxanide furoate.

Goat blood, when incubated for different periods with diloxanide furoate, metronidazole and emetine hydrochloride, underwent changes in fatty acid constituents and their peroxidation products measured as malonaldehyde. These findings, together with the changes noted in the drug-lipid partition coefficient, are discussed in an attempt to correlate the lipid constitution and biological activity of the drugs.