(189k) In-Line NIR Spectroscopy for Monitoring the Preparation of Ginkgo Biloba Extract Solid Dispersions By Hot-Melt Extrusion

Hot melt extrusion (HME) is regarded as an emerging but promising pharmaceutical technique to enhance drug solubility. The purpose of this study was to prepare the high drug-loading Ginkgo biloba extract solid dispersions (GBE-SD) using HME technique, achieving good dissolution profiles at the same time. Polyethylene glycol (PEG) 4000 was the only-used expicient, and various formulations with varying GBE concentrations (30%, 35% and 40%) were explored. Specific HME parameters setting (e.g. barrel temperature, rotation speed) corresponding to different GBE concentrations was based on the result of rheology testing and differential scanning calorimetry (DSC). Quercetin (QCT), kaempferol (KMF) and isorhamnetin (ISR) were chosen as representative substances to evaluate GBE-SD dissolution profiles via HPLC method. Compared to the marketed dripping pill (DP) formulation, the in vitro dissolution studies indicated that both GBE-SD and DP had good solution performance at 30 min (>85% labeled GBE amount). Near-infrared spectroscopy in the die head was used for monitoring the HME process and assessing extrusion stability, indicating molecular interactions between GBE and PEG4000 as well. Considering that marketed DP was struggling with the poor DP appearance when it came to high GBE loading, GBE-SD could improve GBE concentrations and thus enhanced patient compliance. All these studies show that GBE-SD prepared by HME is a creative and valuable formulation approach.