Methods of administering anti-inflammatory cyclooxygenase-2 selective inhibitors

Abstract

Disclosed are novel anti-inflammatory pharmaceutical compositions and related methods that exhibit potent and selective inhibition of the cycloooxygenase-2 (COX-2) enzyme. The formulation can comprise a hops extract that exhibits COX-2 selectivity as defined by dividing the IC50 COX-2/IC50COX-1 concentrations that are determined by testing with the William Harvey Whole Blood Assay (WHMA), and can fall within the range of 0.011 to 0.2. Such compositions may also optionally contain high levels of alpha acids and low levels of beta acids, some flavonoid compounds, and virtually no essential oils. Such compositions are useful for treating conditions that manifest as inflammatory pain, or are impacted by the COX-2 enzyme. The recited compositions are particularly beneficial for treating osteoarthritis and rheumatoid arthritis, and can be used for chronic pain with reduced gastric side-effects.

1 .- 23 . (canceled)  
   
   
       24 . A pharmaceutical composition comprising a pharmaceutically effective amount of an alpha acid, an iso-alpha acid, and a pharmaceutical excipient.  
   
   
       25 . The pharmaceutical composition of claim  59 , wherein said pharmaceutically effective amount of said alpha acid is at least 20 wt %.  
   
   
       26 . The pharmaceutical composition of claim  59 , wherein said pharmaceutically effective amount of said alpha acid is at least 30 wt %.  
   
   
       27 . The pharmaceutical composition of claim  59 , further comprising xanthohumol.  
   
   
       28 . The pharmaceutical composition of claim  59 , wherein said iso-alpha acid selected from the group consisting of iso-humulone, iso-cohumulone, iso-adhumulone, dihydro-iso-humulone, dihydro-iso-adhumulone, and combinations thereof.  
   
   
       29 . The pharmaceutical composition of claim  59 , wherein said iso-alpha acid selected from the group consisting of trans-iso-humulone, cis-iso-humulone, trans-iso-cohumulone, cis-iso-cohumulone, cis-iso-adhumulone, trans-iso-adhumulone, and combinations thereof.  
   
   
       30 . The pharmaceutical composition of claim  59 , having a WHMA IC50 COX-2/IC50COX-1 ratio of from about 0.011 to 0.20.  
   
   
       31 . A method of making a pharmaceutical composition, said method comprising the step of combining a pharmaceutical excipient and a hops extract, wherein said hops extract comprises from 75 wt % to 99.5 wt % of alpha acid.  
   
   
       32 . The method of claim  62 , wherein said composition is an oral dosage form.  
   
   
       33 . The method of claim  62 , wherein composition is a sustained release composition.