In vivo buccal delivery of the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs.
OBJECTIVE
To study the potential of buccal delivery of the peptide drug in pigs.


METHODS
Intravenous administration and buccal delivery without and with 10 mM sodium glycodeoxycholate (GDC) as absorption enhancer were investigated as a randomised cross-over study in six pigs. The buccal delivery device consisted of an application chamber with a solution of buserelin and was attached to the buccal mucosa for 4 hours using an adhesive patch.


RESULTS
Buccal administration of buserelin resulted in rapidly reached steady state plasma levels. The absolute bioavailability of the peptide after buccal delivery for 4 hours could be increased from 1.0 +/- 0.3 to 5.3 +/- 1.1% (mean +/- SD.) by co-administration of 10 mM GDC (0.45% w/v)).


CONCLUSIONS
The results of this study demonstrate that buccal administration with the use of absorption enhancers is a useful approach for the delivery of peptide drugs such as buserelin.
Hoogstraate
A J
AJ
Division of Pharmaceutical Technology, Leiden/Amsterdam Center for Drug Research, Leiden University, The Netherlands.
Coos Verhoef
J
J
Pijpers
A
A
van Leengoed
L A
LA
Verheijden
J H
JH
Junginger
H E
HE
Boddé
H E
HE
D000284:Administration, Oral; D000818:Animals; D002064:Buserelin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D006002:Glycodeoxycholic Acid / Q000378:metabolism*; D007275:Injections, Intravenous; D008297:Male; D008954:Models, Biological; D013552:Swine
D006002:Glycodeoxycholic Acid; D002064:Buserelin