Preparation of 1-Deoxynojirimycin (cas 19130-96-2) controlled release matrix pellets of capsules and evaluation in vitro-in vivo to enhance bioavailability

Add time:07/23/2019    Source:sciencedirect.com

1-Deoxynojirimycin (cas 19130-96-2) was used for the treatment of type II diabetes. However, due to its poor water solubility and low oral bioavailability, clinical application was limited. This study aimed to prepare controlled release matrix pellets of 1-deoxynojirimycin to enhance its oral bioavailability. The pellets composed of a solid dispersed 1-deoxynojirimycin made with hydroxypropyl cellulose (HPMC) and microcrystalline cellulose (MCC) and subsequently coated with hydroxypropyl methylcellulose phthalate (HMNCP) were manufactured by extrusion/spheronization and fluidized bed processes. Evaluation of physicochemical properties of pellets by scanning electron microscopy (SEM) and the yield, friability, tapped density, bulk, moisture content, and particle size distribution were also detected. In addition, the release in vitro, absorption in vivo, and in vitro-in vivo correlation were assessed. More importantly, the bioavailability of the solid dispersion (SDD) and controlled release matrix pellets of 1-deoxynojirimycin (CMPD) were studied in beagle dogs after oral administration using free 1-deoxynojirimycin as a reference. The results indicated that SDD and CMPD enhanced bioavailability of 1-deoxynojirimycin by 186.30% and 235.47%, respectively, compared with free 1-deoxynojirimycin. Furthermore, the correlation analysis in vitro-in vivo studies for CMPD demonstrated good linear relationships between dissolution in vitro and absorption in vivo.

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