Unexpected performance of physical mixtures over solid dispersions on the dissolution behaviour of benznidazole from tablets

DARÍO LEONARDI; CLAUDIO SALOMON

Rosario

Congreso; II Reunión Internacional de Ciencias Farmacéuticas RICIFA 2012; 2012

Universidad Nacional de Rosario/Universidad Nacional de Córdoba

Chagas? disease is an endemic parasitic disease caused by Trypanosoma cruzi and discovered in 1909.(1) Even though the disease was discovered more than 100 years ago, there is still a lack of suitable formulations for the treatment of Chagas disease, as mentioned by the World Health Organization (WHO).(2) Benznidazole (BZL) is the primary drug of choice in the treatment of Chagas disease. According to the Biopharmaceutics Classification System (BCS), BZL belongs to Class III. Although BZL is widely prescribed to treat Chagas disease, the problem of its solubility is still an important challenge for the formulation scientists. One of the most widely applied strategies to increase the solubility/dissolution of poorly water-soluble drugs are the solid dispersions (SDs) (3). This work investigated the feasibility of developing benznidazole (BZL) tablets, allowing fast, reproducible, and complete drug dissolution, by compresing BZL:PEG 6000 physical mixtures (PMs) and solid dispersions.