In vivo buccal delivery of the peptide drug buserelin with glycodeoxycholate as an absorption enhancer in pigs

Pharm Res. 1996 Aug;13(8):1233-7. doi: 10.1023/a:1016024606221.

Abstract

Purpose: 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.

MeSH terms

  • Administration, Oral
  • Animals
  • Buserelin / administration & dosage
  • Buserelin / blood
  • Buserelin / pharmacokinetics*
  • Glycodeoxycholic Acid / metabolism*
  • Injections, Intravenous
  • Male
  • Models, Biological
  • Swine

Substances

  • Glycodeoxycholic Acid
  • Buserelin