Preparation and Characterization of TPGS‐Colloidal Silica Microparticles for Enhancement of Solubility and Oral Bioavailability of Lercanidipine Hydrochloride

摘要

In this study, colloidal silica microparticles containing solubilizing excipient were prepared using the spraya??drying process to enhance dissolution and oral absorption of lercanidipine hydrochloride. Several measurements including scanning electron microscopy, powder Xa??ray diffraction, particle size determination, in vitro dissolution, and pharmacokinetic study were conducted in rats. Among the tested solubilizing excipients, da???±a??tocopheryl polyethylene glycol 1000 succinate (TPGS) dramatically enhanced the solubility of lercanidipine hydrochloride through micelle solubilization. In addition, TPGSa??colloidal silica microparticles at the ratio of 11010 (drugTPGScolloidal silica) showed rapid dissolution rate in all dissolution media and displayed higher area under the curve and maximum plasma concentration values compared with raw lercanidipine hydrochloride. Therefore, amorphous TPGSa??colloidal silica microparticles fabricated using the spraya??drying process have great potential in the clinical application of lercanidipine hydrochloride.