Microencapsulación de Pamoato de Pirantel de tipo comercial con polímeros Eudragit® como precursor de una nueva presentación de un fármaco antihelmíntico

Abstract

Microencapsulation by spray drying allows the production of amorphous solid dispersions that increase the solubility and stability of the active pharmaceutical ingredient (API) in comparison with its crystalline form, considering that in the pharmaceutical industry about one third of compounds in early development are very poorly soluble in water. The objective of this project was the use of Eudragit enteric-coated polymers to produce microspheres of the broad-spectrum anthelmintic drug Pyrantel Pamoate, at different drug-polymer ratios, evaluated by different methods. The highest yield for microencapsulation was obtained with Eudragit S-100 (25:75) of 57.08 percent, followed by polymers L-100 (25:75) of 56.01 percent and L-100-55 (25:75) of 30.94 percent. In infrared spectroscopy (ATR-FTIR) the infrared spectra of the microencapsulated drug prevail in similarity with the infrared spectra of the polymer, differential scanning calorimetry (DSC) shows the disappearance of the melting peak of the pure drug in the thermograms of the microencapsulated drug and scanning electron microscopy (SEM) shows remarkably spherical and uniform microparticles. The results support the use of spray drying for the microencapsulation of Pyrantel Pamoate with Eudragit enteric-coated polymers to produce exposed microspheres stable against the low solubility of the drug in its crystalline form. In addition, this work serves as a precedent for the development of an oral presentation of the drug with greater efficacy, palatability, solubility, and physical stability.