Improvement of oral bioavailability of prednisolone by .BETA.-cyclodextrin complexation in humans.

Inclusion complex of prednisolone with beta-cyclodextrin (beta-CyD) in 1:2 molar ratio was prepared and its dissolution, membrane permeation and oral absorption behaviors were examined. The rates of dissolution and permeation through a cellophane membrane in water were significantly increased by beta-CyD complexation. A crossover bioavailability study was performed using human subjects with lower doses of prednisolone tablets, where the plasma levels of the drug were determined by radioimmunoassay. The enhanced bioavailability of prednisolone by beta-CyD complexation suggested the possibility of smaller doses and fewer side effects in prednisolone therapy.