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

Publisher Website
Google Scholar
Abstract
An inclusion complex of prednisolone [an antiinflammatory agent] with .beta.-cyclodextrin (.beta.-CyD) in a 1:2 molar ratio was prepared and its dissolution, membrane permeation and oral absorption behaviors were examined. The ralution 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.