Dissolution enhancement of poorly water-soluble APIs processed by hot-melt extrusion using hydrophilic polymers

Abstract

The aim of this study was to investigate the efficiency of hydrophilic polymers to enhance the dissolution rate of poorly water-soluble active pharmaceutical ingredients (APIs) processed by hot-melt extrusion (HME). Indomethacin (INM) and famotidine (FMT) were selected as model active substances while polyvinyl caprolactam graft copolymer, soluplus (SOL) and vinylpyrrolidone-vinyl acetate copolymer grades, Kollidon VA64 (VA64) and Plasdone S630 (S630) were used as hydrophilic polymeric carriers. For the purpose of the study, drug-polymer binary blends at various ratios were processed by a Randcastle single screw extruder. The physicochemical properties and the morphology of the extrudates were evaluated through X-ray diffraction (XRD), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Increased drug loadings of up to 40% were achieved in the extruded formulations for both drugs. INM and FMT exhibited strong plasticization effects with increasing concentrations and were found to be molecularly dispersed within the polymer blends. The in vitro dissolution studies showed increased INM/FMT release rates for all formulations compared to that of pure APIs alone.

Inkjet printing of transdermal microneedles for the delivery of anticancer agents

“…Interestingly the results showed rapid release rates for all CRC/SOL formulations with 56 -96% release within 1hr. SOL was used a drug carrier due to its amphiphilic nature and proven capacity to increase the solubility and bioavailability of water insoluble drugs by acting as solubilizer (Maniruzzaman et al, 2013;Tian et al, 2014). In our case SOL demonstrated increased solubilisation capacity especially for the CRC/SOL (1:2) ratio where 96% of the drug is release after 1hr.…”

Hot-melt extrusion of polyvinyl alcohol for oral immediate release applications

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Advanced surface chemical analysis of continuously manufactured drug loaded composite pellets

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