Abstract
The aim of the present work was to develop a mucoadhesive controlled‐release formulation of danazol–sulfobutylether 7 β‐cyclodextrin (SBE 7) complex and to evaluate the feasibility of improving the bioavailability of danazol via the buccal route. Different types of polymers, polycarbophil (PC) and hydroxypropylmethyl cellulose (HPMC) were mixed with danazol–SBE 7 complex and compressed into tablets. These tablets were evaluated for their dissolution and mucoadhesion properties and for drug absorption in female beagle dogs. Increased mucoadhesion was observed for PC‐containing tablets compared with HPMC tablets. As the concentration of polymer increased, drug release decreased, and PC‐containing tablets gave slower release compared to HPMC tablets. In vivo bioavailability performed in dogs showed that the perorally administered danazol–SBE 7 complex and the danazol–SBE 7 (in PC matrix) buccal tablets had absolute bioavailabilities of 64% and 25%, respectively, that are significantly greater than 1.8% observed for the commercial formulation Danocrine®. The increased bioavailability was attributed to the enhanced solubility consequent to complexation, and the possible avoidance of first‐pass metabolism upon buccal administration. © 2002 Wiley‐Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 91:1659–1668, 2002
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
