Optimization of in situ forming intragastric oral formulations with different grades of PEGs

Abstract

The drug release profiles were optimized using different grades of polyethylene glycols (PEGs). Phase diagrams of ternary mixtures of ethylcellulose, PEG and TEC were obtained and used for optimization of drug release. The phase diagrams showed that addition of higher molecular weight of PEGs increased the phase separation and caused precipitation of ethylcellulose from the ternary mixtures. The effect of different grades and concentrations of PEGs in novel oral intragastric controlled release gel formulations were also investigated. In conclusion, the in situ forming oral controlled release formulations were successfully developed and the formulations were able to control the release of hydrochlorothiazide up to 24 hours.

Los perfiles de liberación farmacológica se optimizaron mediante diferentes grados de glicoles de polietileno (PEGs). Se obtuvieron diagramas de fase de mezclas ternarias de etilcelulosa, PEG y TEC, que se usaron para optimizar la liberación farmacológica. Los diagramas de fase mostraron que la adicción de PEGs de mayor peso molecular incrementaba la separación de fases y causaba precipitación de etilcelulosa de las mezclas ternarias. Se investigó también el efecto de distintos grados y concentraciones de PEGs en nuevas formulaciones de geles orales de liberación controlada intragástrica. En conclusión, las formulaciones orales de liberación controlada in situ se desarrollaron con éxito y fueron capaces de controlar la liberación de hidroclorotiazida hasta 24 horas.