Dissolution rate enhancement of 1-(4-acetamide-benzenesulfonyl)-benzimidazole, a new potential antiprotozoal agent, using in situ micronization by solvent change method.

Rosario

Otro; 7ma Reunión Intern Ciencias Farmacéuticas (RICiFa 2023); 2023

1-(4-acetamido-benzenesulfonyl)-benzimidazole (PABZI) is a new benzimidazole derivative which exhibits higher inhibitory activity against Trypanosoma cruzi,1 the causative agent of Chagas disease. However, as many new molecular entities in development, PABZI is a poorly-water soluble compound which exhibits low dissolution rate in physiological media. The objective of this study was to improve the dissolution rate of PABZI by using a simple particle engineering technique such as in situ micronization (ISM). ISM is a technique where microcrystals are obtained during its production itself without the need for any further particle size reduction and the drug is obtained in micron size during the crystal formation.2 There are two ISM methods, by changing the solvent or by changing the pH. The solvent change method involves precipitation in the presence of protective hydrophilic polymers followed by drying, and its was used in this study.