Pharmaceutical compositions

Abstract

Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.

What is claimed is:  
     
         1 . A substantially pure cocoa extract comprising cocoa polyphenol(s).  
     
     
         2 . The extract of  claim 1  prepared from a process comprising: 
 reducing cocoa beans to powder,  
 defatting the powder, and  
 extracting and purifying the cocoa polyphenol(s) from the powder.  
 
     
     
         3 . The extract of  claim 2  wherein the process of reducing cocoa beans to powder comprises: 
 freeze drying beans and pulp,  
 depulping the freeze dried mass,  
 dehulling the freeze dried cocoa beans, and  
 grinding the dehulled beans.  
 
     
     
         4 . The extract of any one of claims  2  or  3  wherein the process further comprises purifying the extract by gel permeation chromatography and/or by preparative high performance liquid chromatography (HPLC).  
     
     
         5 . The extract of  claim 4  containing polyphenol(s) of at least one cocoa procyanidin selected from the group consisting of: (−)-epicatechin, procyanidin B-2, procyanidin oligomers 4 through 12, procyanidin B-5, procyanidin A-2 and procyanidin C-1.  
     
     
         6 . An antineoplastic composition comprising a substantially pure cocoa extract or synthetic cocoa polyphenol(s) and a suitable carrier.  
     
     
         7 . The antineoplastic composition of  claim 6  which is comprised of a substantially pure cocoa extract containing cocoa procyanidin(s).  
     
     
         8 . The antineoplastic composition of  claim 7  wherein the cocoa procyanidin(s) are prepared from a process comprising: 
 reducing cocoa beans to powder,  
 defatting the powder, and,  
 extracting the cocoa procyanidin(s) from the powder.  
 
     
     
         9 . The antineoplastic composition of  claim 8  wherein the process of reducing cocoa beans to powder comprises: 
 freeze drying beans and pulp,  
 depulping the freeze dried mass,  
 dehulling the freeze dried cocoa beans, and  
 grinding the dehulled beans.  
 
     
     
         10 . The antineoplastic compositions of any one of claims  8  or  9  wherein the process further comprises purifying the extract by gel permeation chromatography and/or by preparative high performance liquid chromatography (HPLC).  
     
     
         11 . The antineoplastic composition of  claim 10  containing polyphenol(s) of at least one cocoa procyanidin selected from the group consisting of: (−)-epicatechin, procyanidin B-2, procyanidin oligomers 4 through 12, procyanidin B-5, procyanidin A-2 and procyanidin C-1.  
     
     
         12 . A method for treating a patient in need of treatment with an antineoplastic agent comprising administering to the patient an antineoplastic composition comprising an effective quantity of a substantially pure cocoa extract or synthetic cocoa polyphenol(s), and a suitable carrier.  
     
     
         13 . The method of  claim 12  wherein the antineoplastic agent is comprised of a substantially pure cocoa extract containing cocoa procyanidin(s).  
     
     
         14 . The method of  claim 13  wherein the cocoa procyanidin(s) are prepared from a process comprising: 
 reducing cocoa beans to powder,  
 defatting the powder, and,  
 extracting the cocoa procyanidin(s) from the powder.  
 
     
     
         15 . The method of  claim 14  wherein the process of reducing cocoa pods to powder comprises: 
 freeze drying beans and pulp,  
 depulping the freeze dried mass,  
 dehulling the freeze dried cocoa beans, and  
 grinding the dehulled beans.  
 
     
     
         16 . The method of any one of claims  14  or  15  wherein the process further comprises purifying the extract by gel permeation chromatography and/or by preparative high performance liquid chromatography (HPLC).  
     
     
         17 . The method of  claim 16  wherein the extract contains polyphenol(s) of at least one cocoa procyanidin selected from the group consisting of: (−)-epicatechin, procyanidin B-2, procyanidin oligomers 4 through 12, procyanidin B-5, procyanidin A-2 and procyanidin C-1.  
     
     
         18 . A kit for treating a patient in need of treatment with an antineoplastic agent comprising a substantially pure cocoa extract or synthetic cocoa polyphenol(s) and a suitable carrier.  
     
     
         19 . The kit of  claim 18  wherein the antineoplastic agent is comprised of a substantially pure cocoa extract containing procyanidin(s); and, the kit includes instructions for admixture of ingredients and/or administration to the patient.  
     
     
         20 . A lyophilized antineoplastic composition comprising a substantially pure cocoa extract or synthetic cocoa polyphenol(s).  
     
     
         21 . The lyophilized antineoplastic composition of  claim 20  wherein the composition is comprised of a substantially pure cocoa extract containing cocoa procyanidin(s).  
     
     
         22 . An antioxidant or preservative composition comprising a substantially pure cocoa extract as claimed in  claim 1  or synthetic cocoa polyphenol(s).  
     
     
         23 . A topoisomerase-inhibiting composition comprising a substantially pure cocoa extract as claimed in  claim 1  or synthetic cocoa polyphenol(s).  
     
     
         24 . A method for preserving or protecting from oxidation a desired item comprising contacting the item with a composition as claimed in  claim 22 .  
     
     
         25 . The method of  claim 24  wherein the item is a foodstuff.  
     
     
         26 . A method for inhibiting topoisomerase which comprises contacting topoisomerase with a composition as claimed in  claim 23.