COMPOSITIONS OF BUPRENORPHINE AND µ ANTAGONISTS
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; A A nAI = [ C m ax ( BUP ) / EC 50 ] [ C ma x ( ANTAGONIST ) / IC 50 ] .
1 - 40 . (canceled)
41 . A method of treating major depressive disorder in a patient in need thereof, comprising administering buprenorphine and Compound-1 or a pharmaceutically acceptable salt thereof to the patient
wherein Compound-1 is administered in a dose of about 0.5 to about 4 mg.
42 . The method of claim 41 , comprising administering the pharmaceutically acceptable salt of Compound-1.
43 . The method according to claim 41 , wherein buprenorphine and/or Compound-1 or pharmaceutically acceptable salt thereof are administered orally or sublingually.
44 . The method according to claim 41 , wherein buprenorphine and/or Compound-1 or pharmaceutically acceptable salt thereof are administered daily.
45 . The method according to claim 41 , wherein buprenorphine and/or Compound-1 or pharmaceutically acceptable salt thereof are in the form of a tablet.
46 . The method according to claim 41 , wherein buprenorphine and Compound-1 or pharmaceutically acceptable salt thereof are in a pharmaceutical composition.
47 . The method according to claim 46 , wherein the composition is administered daily.
48 . The method according to claim 46 , wherein the composition is in the form of a tablet.
49 . The method according to claim 41 , wherein Compound-1 or a pharmaceutically acceptable salt thereof is administered in a dose of about 2 mg.
50 . The method according to claim 41 , comprising 2 mg to 4 mg of buprenorphine.
51 . The method according to claim 41 , comprising 2mg of buprenorphine.
52 . The method according to claim 41 , wherein said major depressive disorder is resistant to two or more antidepressants.
53 . The method according to claim 52 , wherein said antidepressants are selected from the group consisting of selective serotonin reuptake inhibitors (SSRIs), Serotonin-norepinephrine reuptake inhibitors (SNRIs), Monoamine oxidase inhibitors (MAOIs) and Tricyclic antidepressants.
54 . The method according to claim 41 , wherein the method results in the reduction of buprenorphine-induced dopamine release as compared to administration of buprenorphine alone.
55 . The method according to claim 54 , wherein the method results in a reduction in dopamine release of between about 25% to about 75% in comparison with the administration of buprenorphine alone.
56 . The method according to claim 41 , wherein the method reduces the drug liking and addictive potential of buprenorphine while retaining the anti-depressive properties of buprenorphine.