In a recent study published in Pain Medicine, pharmacokinetic modeling showed that transitioning patients from transdermal to buccal formulations of buprenorphine can be done within 12 hours of patch removal, using the recommended buccal formulation titration doses and schedule.

In this model-based meta-analysis, data were extracted from 6 studies that evaluated mean or median concentration time profiles of transdermal or buccal buprenorphine during at least 6 points in at least 5 adult patients. A meta-model of pharmacokinetics that evaluated absorption rate, apparent clearance, and volume of distribution after buprenorphine administration was developed. The model was then used to simulate the pharmacokinetics of transitioning from transdermal to buccal buprenorphine.

The transdermal absorption model developed in the study was based on a zero-order rate constant that was dependent on the nominal patch delivery rate, the time since patch application, and the time the patch was removed. The delivery rate was dependent on the type of transdermal patch used.

Continue Reading

The buccal absorption model used simple first-order kinetics, incorporating absorption lag and bioavailability.

According to the models developed through the meta-analysis, buccal buprenorphine could be administered 12 hours after removal of 10 or 20 µg/hour transdermal buprenorphine. Dosing could follow the traditional buccal titration schedule, increasing from 75 µg/hour to 300 or 450 µg/hour during a period of 4 days with increments of 10 or 20 µg/hour transdermal buprenorphine, respectively.

Related Articles

Tony Priestley, PhD, lead author on the study and former senior director of pharmacology and drug development with Endo Pharmaceuticals, explained that “the model data suggest that it is feasible and relatively straightforward to convert patients from a transdermal buprenorphine product to [buccal buprenorphine].”

Dr Priestley reports being employed by Endo Pharmaceuticals, Inc.

Follow @ClinicalPainAdv


Priestley T, Chappa AK, Mould DR, et al. Converting from transdermal to buccal formulations of buprenorphine: a pharmacokinetic meta-model simulation in healthy volunteers [published online September 29, 2017]. Pain Medicine. doi: 10.1093/pm/pnx235