Compositions and methods for inhibiting 5-alpha reductase

Abstract

Disclosed herein are compositions for controlling androgen activity in target organs and cells through the modulation of a 5-α-reductase activity. In certain aspects, these compositions are employed to modulate androgenic activity by inhibiting the formation and availability of active androgen in target cells. As a result, the present invention is directed toward the treatment of a wide variety of conditions including, but not limited to, the treatment of prostatic hyperplasia, prostatic cancer, hirsutism, acne, male pattern baldness, seborrhea, and other diseases related to androgen hyperactivity. Several of these compositions have been shown to effectively decrease body weight, and in some cases, to decrease the weight of an androgen-dependent body organ, such as the prostate and other organs.

1 . A composition for modulating 5-α-reductase activity comprising a supercritical fluid isolate of Saw Palmetto, Sperol, their respective analogs or derivatives.  
     
     
         2 . The composition of  claim 1 , wherein said analogs or derivatives have a similar function as compared to their parent compound.  
     
     
         3 . The compound of  claim 2 , wherein said similar function include the inhibition of 5-α-reductase.  
     
     
         4 . A method of preparing one or more active 5-α-reductase inhibitor preparations, comprising the following steps: 
 (a) preparing a fine powder of a sample;    (b) transferring said sample fine powder to a cartridge, wherein said cartridge comprises a filler to reduce dead volume;    (c) performing a sequential procedure comprising extraction and fractionation employing carbon dioxide and an appropriate alcohol, wherein pressure is set to around 3000 psig and temperature set to around 40° C.; and    (d) collecting individual fractions.    
     
     
         5 . The method of  claim 4 , wherein said sample is selected from the group consisting of Saw Palmetto, Sperol, their respective analogs or derivatives.  
     
     
         6 . The method of  claim 4 , wherein said filler is selected from the group consisting of glass wool, beads, or alike.  
     
     
         7 . The method of  claim 4 , wherein said appropriate alcohol is either methanol or ethanol.  
     
     
         8 . The method of  claim 4 , wherein step (c) includes step extractions employing either methanol or ethanol.  
     
     
         9 . The method of  claim 8 , wherein said step extractions includes extractions with said appropriate alcohol, wherein individual steps include 5, 10, 20, 30, or 40% alcohol volume.  
     
     
         10 . A method of modulating 5-α-reductase in an individual, comprising administering to said individual a therapeutically effective amount of a supercritical fluid isolate of Saw Palmetto, Sperol, their respective analogs or derivatives.  
     
     
         11 . The method of  claim 10 , wherein said modulation is inhibition.  
     
     
         12 . The method of  claim 10 , wherein said administration includes an additional pharmaceutical agent.  
     
     
         13 . The method of  claim 12 , wherein said pharmaceutical agent includes oncolytic pharmaceuticals.  
     
     
         14 . The method of  claim 10  further comprising the administration of either resection or radiation therapy.  
     
     
         15 . The method of  claim 10 , wherein said administration is effectuated through topical application.  
     
     
         16 . A method of treating benign prostate hyperplasia, comprising administering to a subject in need thereof an effective amount of a supercritical fluid isolate of Saw Palmetto, Sperol, their respective analogs or derivatives.  
     
     
         17 . A method of treating hirsutism, comprising administering to a subject in need thereof an effective amount of a supercritical fluid isolate of Saw Palmetto, Sperol, their respective analogs or derivatives.  
     
     
         18 . A method of treating acne, comprising administering to a subject in need thereof an effective amount of a supercritical fluid isolate of Saw Palmetto, Sperol, their respective analogs or derivatives.  
     
     
         19 . A method of treating benign prostate hyperplasia, comprising administering to a subject in need thereof an effective amount of a supercritical fluid isolate of Saw Palmetto, Sperol, their respective analogs or derivatives.  
     
     
         20 . A method of treating male pattern baldness, comprising administering to a subject in need thereof an effective amount of a supercritical fluid isolate of Saw Palmetto, Sperol, their respective analogs or derivatives.  
     
     
         21 . A method of treating seborrhea, comprising administering to a subject in need thereof an effective amount of a supercritical fluid isolate of Saw Palmetto, Sperol, their respective analogs or derivatives.