Formulation and research of the solid disper systems of spironolactone

Abstract

Introduction: Starting from the fact that spironolactone is practically insoluble in water, its formulation orodispersible is important to enhance dissolution rapid absorption from the oral cavity. Aim: To increase the solubility of spironolactone was evaluated its association with different solubilized to form solid disperse systems. . Material and method: Preparation o f solid dispersion systems: Solid dispersion was obtained using the combined method: solvent evaporation and melting. Spironolactone and polyvinylpyrrolidone is dissolved in ethyl alcohol 96%. The resulting solution is left to complete evaporation of ethanol. Polyethylene glycol 4000 melts at a temperature of + 60° C, the mixture plus spironolactone and polyvinylpyrrolidone. Stir continuously until completely cooled. Parallel to prepare and physical mixture of spironolactone, polyvinylpyrrolidone and polyethylene glycol. Thermo-gravimetric analysis: Substances studied, physical mixture and solid dispersion were subjected to thermo-gravimetric analysis derivatographic O1500D model MOM (Hungary). Samples were heated to a temperature of 1020° C, the heating rate of 10° C/min. He sought modification of the caloric content of substances and mixtures, recorded temperature variation, in the mass during heat treatment. Results: The dispersed solid is characterized the 3 effects of decomposition in the temperature range 45 to 471° C, the mass loss of 86.96%. At a temperature of about 60° C the degradation of the system is associated with an endothermic effect, characteristic of a melting process which confirms that the system presents a phase change. There follows a series of endothermic and exothermic effects. Total mass loss is 97.91%. Conclusions: The results confirm the formation of a solid dispersed system of spironolactone with polyvinylpyrrolidone and Polyethylene glycol 4000.