Enhanced oral bioavailability of ATRA by 2-hydroxypropyl-β-cyclodextrin inclusion complex pellets prepared by fluid-bed coating technique

摘要

Purposes: To enhance the oral bioavailability of alltrans-retinoic acid (ATRA) by 2-hydroxypropyl-βcyclodextrin (HPCD) inclusion complex pellets.; Methods: The ATRA/HPCD inclusion complex pellets was prepared with fluid-bed coating technique and characterized in vitro by SEM and dissolution. The oral bioavailability of the ATRA/HPCD inclusion complex pellets was compared with ATRA suspension in beagle dogs with dose of 10 mg/kg.; Results: The resulting pellets were spherical and intact in shape. SEM analysis showed that the pellets were full of crevices on the surface and had a tightly coated inclusion complex layer. In vitro dissolution of ATRA from the inclusion complex pellets was dramatically enhanced as compared with ATRA suspension. Calculated by AUC0-t,the relative bioavailability of the ATRA/HPCD inclusion complex pellets reached 2011.39±1054.64 %. Conclusion: The ATRA/HPCD inclusion complex pellets showed a considerable clinical potential.