Preparation and dissolution characteristic evaluation of carvedilol-Kollicoat IR solid dispersions with HPMC and MC as combined carriers

Abstract

In this study, the abilities of hydroxypropyl methylcellulose (HPMC) and methylcellulose (MC) as nonionic surfactants to improve the dissolution rate of carvedilol solid dispersions (CAR SDs) with Kollicoat IR as a carrier were clearly demonstrated. CAR SDs were prepared using the solvent evaporation method, and their physicochemical properties were characterized by scanning electron microscopy (SEM) and Powder X-Ray diffraction (PXRD). The results suggested that CAR in SDs existed in an amorphous form. In vitro dissolution experiments and molecular docking (MD) simulations were conducted to confirm the storage stability of CAR SDs. In order to study the mechanism of solubilization ability, molar solubilization ratio (MSR) and micelle-water partition coefficient (Kmic) were calculated. The results showed that the MSR and lg Kmic values of MC/Kollicoat IR 1:3 were around 30 fold higher than the single surfactant. Above all, HPMC and MC have great potentials to improve the dissolution characteristics of CAR-Kollicoat IR SDs.