Increasing the Oral Bioavailability of Opioids and Phenolic Bioactives

Uses of Combinations of GRAS and Dietary Substances

The technology

Dr. Gerk has developed methods of enhancing the bioavailability of phenylephrine, buprenorphine, and similar compounds by using a combination of GRAS and dietary substances to inhibit their presystemic metabolism. The approach was developed with FDA qualifications in mind from the beginning, and it is appropriate for FDA applications and regulations. In vitro and in vivo studies indicate the efficacy of the approach.

  • Results from in vivo studies indicate an enhancement in oral bioavailability of buprenorphine by 2-3 fold.
  • Identified agents include a proprietary and unique combination of several GRAS and dietary compounds.
  • Regulatory hurdles will be minimized by the choice of compounds. These compounds are considered GRAS by the FDA, since their safety has been previously demonstrated.
  • In vitro results using single agents and combinations of agents have established potency for defined pathways of metabolism.
  • In vitro-in vivo extrapolation supports the feasibility of the approach for increasing oral buprenorphine bioavailability comparable to the sublingual route.
  • Further mechanistic characterization is desirable to help with development of the technology.
  • Protocols for in vivo testing in small groups of normal healthy subjects are being developed.
  • The selected compounds in appropriate ratios will be identified and validated. The development of marketable dosage forms will require a formulation partner.