Journal
JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 91, Issue 7, Pages 1659-1668Publisher
JOHN WILEY & SONS INC
DOI: 10.1002/jps.10163
Keywords
danazol; sulfobutylether 7-beta-cyclodextrin; inclusion complex; mucoadhesion; buccal delivery
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The aim of the present work was to develop a mucoadhesive controlled-release formulation of danazol-sulfobutylether 7 beta-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(R),. The increased bioavailability was attributed to the enhanced solubility consequent to complexation, and the possible a-voidance of first-pass metabolism upon buccal administration. (C) 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association.
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