(565f) Sublingual Drug Delivery; Will It Always Give ‘Fast Onset'? A Product Enhancement Perspective

In general, absorption of drugs from the oral cavity via solutions, sublingual, fast dissolving, or buccal dosage forms into the mucosal tissues is typically a fast event, while transport of drug from the mucosal tissue into the systemic circulation can be rate limiting to overall systemic bioavailability. While it is common practice to consider administration via the oral mucosa (e.g. sublingual) when a short Tmax or rapid onset is desired, the approach may not always be appropriate depending on the chemical entity.

This presentation will briefly discuss the clinical models available for studying drug transport via the oral mucosa and highlight the similarities and differences to drug absorption via the GI tract. This fundamental understanding of drug transport via the oral cavity is needed to help explain and model pharmacokinetic data that may be generated following administration to the oral cavity. A review of clinical Tmax values for drugs administered via the oral cavity was completed. This data review has allowed for further modeling and correlations to be drawn between chemical structure and Tmax, which may offer the ability to predict a priori certain PK parameters following oral cavity administration based on physiochemical properties alone. If the goal in a drug development program is rapid PK onset, such a model may allow for better prediction of which drug candidates have a higher probability of achieving this goal, and which candidates are likely to be less successful based on physiochemical properties alone.