During the perioperative period, gastric emptying rate and first-pass metabolism limit the use of peroral @entity1286 . Buccal mucosa appears to be a potential site for delivery of @entity1286 as it provides direct entry into the system circulation thereby avoiding the hepatic first-pass effect. However, the low permeability of the buccal epithelium results in a low flux of the drug. The use of a penetration enhancer is required to improve the bioavailability of the drug via buccal route. In this study, the enhancing effect of @entity18034 (GC) used at 10 mM and 100 mM concentrations on permeation of @entity33483 ( @entity7541 ) across the porcine buccal mucosa was studied in vitro. Furthermore, in conjunction with its permeation, accumulation of GC in the tissue with time was also studied in order to elucidate the relationship between GC and enhanced mucosal permeation of the drug. Franz diffusion cells were used in the experiments. Permeation of @entity7541 was increased in the presence of 100 mM GC with an enhancement factor of 9.3 whereas no enhancement was obtained with 10 mM GC. The calculated permeability coefficient for @entity7541 in the presence of 100 mM GC was 2.35 x 10(-5) cm/s. Accumulation of GC at 100 mM in the tissue appears to be more significant at 100 mM concentration which correlated well with the increased permeation of the drug. GC was diffused through the buccal epithelium significantly at 100 mM concentration. Interaction of GC with the tissue appears to be more significant at 100 mM concentration compared to 10 mM concentration, thus resulting in a significant enhancing effect.

In vitro studies on enhancing effect of @entity18034 on transbuccal permeation of XXXX .

@entity7541 :: ('MESH:C041626', 'Chemical') :: ['MPH'] @entity18034 :: ('CHEBI:36273', 'Chemical') :: ['sodium glycocholate'] @entity33483 :: ('CHEBI:55340', 'Chemical') :: ['morphine hydrochloride'] @entity1286 :: ('MESH:D009020', 'Chemical') :: ['morphine']
@entity33483 :: (CHEBI:55340,Chemical) :: ['morphine hydrochloride']
