Formulation and Quality – Chemical
2019 PharmSci 360
The impact of surfactants on supersaturation of a model compound solution was evaluated. SDS, vitamin E TPGS, Tween 80 and docusate sodium were studied. The induction time for nucleation and rate of desupersaturation were determined at a constant supersaturation ratio. Measurement was also performed in the presence of pre-dissolved HPMCAS to study the effect of surfactant-polymer interaction on desupersaturation. Tween 80 promoted both nucleation and crystal growth; vitamin E TPGS mainly promoted crystal growth; SDS did not strongly promote desupersaturation by itself but strongly negated the effectiveness of HPMCAS on maintaining supersaturation; docusate sodium provided a stabilization effect on supersaturation. From supersaturation maintenance perspective, when HPMCAS presents, the rank order was found to be: docusate sodium > vitamin E TPGS > SDS > Tween 80. Therefore a careful examination of API, polymer and surfactant interaction on an individual basis is recommended for incorporating a surfactant for ASD development.