Compositions of buprenorphine and μ antagonists

摘要

The invention relates to a composition comprising buprenorphine and a μ opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein;;AAnAI=[Cmax⁡(BUB)BC30][Cmax(ANTAGONIST)IC30].

主权项

1. A composition comprising buprenorphine and a μ opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein;AAnAI=[Cmax⁡(BUP)/EC50][Cmax⁡(ANTAGONIST)/IC50] wherein, EC50 represents the half maximal effective serum concentration of buprenorphine, expressed as nM; IC50 represents the half maximal inhibitory concentration of the μ opioid antagonist in humans, expressed as nM; Cmax(BUP) represents the peak serum or plasma concentration of buprenorphine and/or a μ opioid receptor agonist metabolite of buprenorphine, expressed as nM; and Cmax(ANTAGONIST) represents the peak serum concentration of the μ opioid antagonist and/or a μ opioid receptor antagonist metabolite of said μ opioid antagonist, expressed as nM.