Method of treating high plasma cholesterol levels

Abstract

A method prevents or treats diseases associated with high plasma cholesterol levels. In addition, this method reduces plasma cholesterol levels. The method comprises administering a lipase inhibitor, e.g. orlistat, and a pharmaceutically acceptable bile acid sequestrant.

What is claimed is:  
     
         1 . A method of reducing plasma cholesterol levels in a hypercholesterolemic patient, which comprises administering to the patient a therapeutically effective amount of a lipase inhibitor and a therapeutically effective amount of a bile acid sequestrant selected from the group consisting of cholestyramine, colestipol, colesevelam, colestimide, sevelamer, DEAE-cellulose, guanidinoethylcellulose, DEAE-Sephadex, β-cyclodextrin, and γ-cyclodextrin.  
     
     
         2 . The method according to  claim 1 , wherein the lipase inhibitor is orlistat.  
     
     
         3 . The method according to  claim 1 , wherein the bile acid sequestrant is selected from the group consisting of DEAE-cellulose, guanidinoethylcellulose, and DEAE-Sephadex.  
     
     
         4 . The method according to  claim 1 , wherein the bile acid sequestrant is selected from the group consisting of cholestyramine, colestipol, sevelamer, DEAE-cellulose, β-cyclodextrin, and γ-cyclodextrin.  
     
     
         5 . The method according to  claim 4 , wherein the bile acid sequestrant is selected from β-cyclodextrin or γ-cyclodextrin.  
     
     
         6 . The method according to  claim 1 , wherein the therapeutically effective amount of a lipase inhibitor and a therapeutically effective amount of a bile acid sequestrant are administered as a medicament that comprises about 5 mg to about 1000 mg lipase inhibitor, about 0.1 g to about 20 g bile acid sequestrant, and one or more pharmaceutically acceptable excipients.  
     
     
         7 . The method according to  claim 6 , wherein the pharmaceutically acceptable excipient is selected from the group consisting of fillers, sugars, sugar alcohols, a mixture of one or more sugars and sugar alcohols, surfactants, disintegrants, binders, lubricants, flowability enhancers, sweeteners, and colorants.  
     
     
         8 . The method according to  claim 7 , wherein the medicament comprises: 
 a) about 5 mg to about 1000 mg lipase inhibitor;    b) about 0.1 g to about 20 g bile acid sequestrant; and    a pharmaceutically acceptable excipients selected from the group consisting of about 0.1 to about 10 g fillers, sugars, sugar alcohols and mixtures thereof, about 0.05 g to about 3.0 g surfactants, about 0.05 g to about 2.0 g disintegrants, about 0.02 g to about 2.0 g binder, about 0.001 g to about 1.0 g lubricants, about 0.1 g to about 5.0 g flowability enhancers, about 0.01 g to about 4.0 g sweeteners, and about 0.001 g to about 0.5 g colorants.    
     
     
         9 . The method according to  claim 6 , wherein the medicament comprises about 10 mg to about 500 mg lipase inhibitor.  
     
     
         10 . The method according to  claim 9 , wherein the medicament comprises about 20 mg to about 100 mg lipase inhibitor.  
     
     
         11 . The method according to  claim 9 , wherein the medicament comprises about 10 mg to about 360 mg orlistat.  
     
     
         12 . The method according to  claim 11 , wherein the medicament comprises about 30 mg to about 120 mg orlistat.  
     
     
         13 . The method according to  claim 12 , wherein the medicament comprises about 40 mg to about 80 mg orlistat.  
     
     
         14 . The method according to  claim 6 , wherein the medicament comprises about 0.5 g to about 10 g bile acid sequestrant.  
     
     
         15 . The method according to  claim 14 , wherein the medicament comprises about 1 g to about 5 g bile acid sequestrant.  
     
     
         16 . The method according to  claim 1 , wherein the lipase inhibitor and bile acid sequestrant are administered simultaneously.  
     
     
         17 . The method according to  claim 1 , wherein the lipase inhibitor and bile acid sequestrant are administered separately.  
     
     
         18 . The method according to  claim 1 , wherein the lipase inhibitor and bile acid sequestrant are administered sequentially.  
     
     
         19 . The method according to  claim 1 , wherein the lipase inhibitor is selected from the group consisting of orlistat, 2-decyloxy-6-methyl-4H-3,1-benzoxazin-4-one, 6-methyl-2-tetradecyloxy-4H-3,1-benzoxazin-4-one, and 2-hexadecyloxy-6-methyl-4H-3,1-benzoxazin-4-one.