IN-VIVO BUCCAL DELIVERY OF THE PEPTIDE DRUG BUSERELIN WITH GLYCODEOXYCHOLATE AS AN ABSORPTION ENHANCER IN PIGS

Purpose. To study the potential of buccal delivery of the peptide drug in pigs. Methods. Intravenous administration and buccal delivery with out and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhanc er were investigated as a randomised cross-over study in six pigs. The buccal delivery device consisted of an application chamber with a sol ution of buserelin and was attached to the buccal mucosa for 4 hours u sing an adhesive patch. Results. Buccal administration of buserelin re sulted in rapidly reached steady state plasma levels. The absolute bio availability of the peptide after buccal delivery for 4 hours could be increased from 1.0 +/- 0.3 to 5.3 +/- 1.1% (mean +/- S.D.) by co-admi nistration of 10 mM GDC (0.45% w/v)). Conclusions. The results of this study demonstrate that buccal administration with the use of absorpti on enhancers is a useful approach for the delivery of peptide drugs su ch as buserelin.