Process for preparing water soluble diterpenes and their applications

Abstract

Aqueous solutions of diterpenes such as Forskolin, its congeners, analogs and derivatives, up to approximately 6% concentration, are prepared using suitably substituted cyclodextrin as a solubilizing agents. In the absence of cyclodextrin, some diterpenes such as Forskolin are soluble in water only to concentrations of about 0.001%. Such aqueous solutions find applications in topical and systemic use, as pharmaceutical, cosmeceutical, nutraceutical preparations containing diterpenes such as Forskolin and congeners.

1 . A clear aqueous solution comprising between 0.09% to 6% of at least one natural or synthetic forskolin, isoforskolin, or 7-deacetylforskolin complexed with RAMEBCD.  
   
   
       2 . A method for the treatment of glaucoma in a human or animal comprising administering the clear aqueous solution of  claim 1 .  
   
   
       3 . A method for the treatment of ocular hypertension in a human or animal comprising administering the clear aqueous solution of  claim 1 .  
   
   
       4 . A method for the treatment of dry eye syndrome in a human or animal comprising administering the clear aqueous solution of  claim 1 .  
   
   
       5 . A clear aqueous solution comprising between 0.09% to 6% of at least one natural or synthetic forskolin, isoforskolin, or 7-deacetylforskolin complexed with a cyclodextrin agent, wherein the cyclodextrin agent is the sole complexing/solubilizing agent.  
   
   
       6 . A method for the treatment of glaucoma in a human or animal comprising administering the clear aqueous solution of  claim 5 .  
   
   
       7 . A method for the treatment of ocular hypertension in a human or animal comprising administering the clear aqueous solution of  claim 5 .  
   
   
       8 . A method for the treatment of dry eye syndrome in a human or animal comprising administering the clear aqueous solution of  claim 5 .  
   
   
       9 . The clear aqueous solution of  claim 5 , further comprising one or more anti-glaucoma agents.  
   
   
       10 . A method for the treatment of glaucoma in a human or animal comprising administering the clear aqueous solution of  claim 9 .  
   
   
       11 . The clear aqueous solution of  claim 5 , further comprising hyaluronic acid and/or one or more hyaluronic acid derivatives.  
   
   
       12 . A method for the treatment of dry eye syndrome in a human or animal comprising administering the clear aqueous solution of  claim 11 .  
   
   
       13 . The clear aqueous solution of  claim 5 , further comprising polyvinyl pyrrolidone.  
   
   
       14 . A method for the treatment of dry eye syndrome in a human or animal comprising administering the clear aqueous solution of  claim 13 .  
   
   
       15 . The clear aqueous solution of  claim 5 , further comprising one or more antioxidants.  
   
   
       16 . A method for the treatment of glaucoma or ocular hypertension in a human or animal comprising administering the clear aqueous solution of  claim 15.