US2004105838A1PendingUtilityA1

Orlistat compositions

56
Priority: Jul 28, 2000Filed: Nov 20, 2003Published: Jun 3, 2004
Est. expiryJul 28, 2020(expired)· nominal 20-yr term from priority
Inventors:Pierre BarbierPaul HadvaryHans Lengsfeld
A61P 3/06A61P 31/18A61P 3/04A61P 43/00A61P 1/16A61P 1/00A61K 45/06A61K 31/785A61K 31/717A61K 31/365A61K 31/721A61K 31/715A61K 31/716A61K 31/70A61K 31/337
56
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Claims

Abstract

A pharmaceutical combination or composition containing a lipase inhibitor, preferably orlistat, and a bile acid sequestrant is useful for treating obesity.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A pharmaceutical composition which comprises orlistat and a pharmaceutically acceptable bile acid sequestrant selected from the group consisting of DEAE-cellulose, guanidinoethylcellulose, and DEAE-Sephadex.  
     
     
         2 . The composition according to  claim 1 , wherein the composition comprises (a) from about 5 to about 1000 mg of orlistat and (b) from about 0.1 to about 20 g of the bile acid sequestrant.  
     
     
         3 . The composition according to  claim 2 , which comprises: 
 (a) from about 5 to about 1000 mg of orlistat;    (b) from about 0.1 to about 20 g bile acid sequestrant selected from the group consisting of DEAE-cellulose, guanidinoethylcellulose, and DEAE-Sephadex;    (c) from about 0.1 to about 10 g of a filler;    (d) from about 0.05 to about 3.0 g of a surfactant;    (e) from about 0.05 to about 2.0 g of a disintegrant;    (f) from about 0.02 to about 2.0 g of a binder;    (g) from about 0.001 to about 1.0 g of a lubricant;    (h) from about 0.1 to about 5.0 g of a flowability enhancer;    (i) from about 0.01 to about 4.0 g of a sweetener; and    (j) and about 0.001 to about 0.5 g of a colorant.    
     
     
         4 . The compositions according to  claim 3 , wherein the orlistat is present in an amount of from about 10 to about 500 mg.  
     
     
         5 . The composition according to  claim 4 , wherein the orlistat is present in an amount of about 120 mg.  
     
     
         6 . The composition according to  claim 4 , wherein the orlistat is present in an amount of from about 20 to about 100 mg.  
     
     
         7 . The composition according to  claim 6 , wherein the orlistat is present in an amount of about 60 mg.  
     
     
         8 . The composition according to  claim 4 , wherein the bile acid sequestrant is present in an amount of from about 0.5 to about 10 g.  
     
     
         9 . The composition according to  claim 8 , wherein the bile acid sequestrant is present in an amount of from about 1 to about 5 g.  
     
     
         10 . A pharmaceutical composition which comprises orlistat and a pharmaceutically acceptable acid sequestrant selected from the group consisting of cholestyramine, colestipol, colestimide, colesevelam, sevelamer, DEAE-cellulose, β-cyclodextrin, and γ-cyclodextrin.  
     
     
         11 . The composition according to  claim 10 , wherein pharmaceutically acceptable bile acid sequestrant is selected from the group consisting of β-cyclodextrin and γ-cyclodextrin.  
     
     
         12 . The composition according to  claim 10 , wherein the bile acid sequestrant is selected from the group consisting of cholestyramine, colestipol, sevelamer, DEAE-cellulose, β-cyclodextrin, and γ-cyclodextrin.  
     
     
         13 . The composition according to  claim 12 , wherein the bile acid sequestrant is selected from the group consisting of cholestyramine, colestipol, and sevelamer.  
     
     
         14 . The composition according to  claim 13 , wherein the bile acid sequestrant is cholestyramine.  
     
     
         15 . The composition according to  claim 13 , wherein the bile acid sequestrant is colestipol.  
     
     
         16 . The composition according to  claim 13 , wherein the bile acid sequestrant is sevelamer.  
     
     
         17 . The composition according to  claim 10 , wherein the composition comprises (a) from about 5 to about 1000 mg of orlistat and (b) from about 0.1 to about 20 g of the bile acid sequestrant.  
     
     
         18 . The composition according to  claim 17 , which comprises: 
 (a) from about 5 to about 1000 mg of orlistat;    (b) from about 0.1 to about 20 g bile acid sequestrant selected from the group consisting of cholestyramine, colestipol, colestimide, colesevelam, sevelamer, DEAE-cellulose, β-cyclodextrin, and γ-cyclodextrin;    (c) from about 0.1 to about 10 g of a filler;    (d) from about 0.05 to about 3.0 g of a surfactant;    (e) from about 0.05 to about 2.0 g of a disintegrant;    (f) from about 0.02 to about 2.0 g of a binder;    (g) from about 0.001 to about 1.0 g of a lubricant;    (h) from about 0.1 to about 5.0 g of a flowability enhancer;    (i) from about 0.01 to about 4.0 g of a sweetener; and    (j) and about 0.001 to about 0.5 g of a colorant.    
     
     
         19 . The composition according to  claim 14 , wherein the composition comprises (a) from about 5 to about 1000 mg of orlistat and (b) from about 0.1 to about 20 g of the bile acid sequestrant.  
     
     
         20 . The composition according to  claim 19 , which comprises: 
 (a) from about 5 to about 1000 mg of orlistat;    (b) from about 0.1 to about 20 g bile acid sequestrant selected from the group consisting of cholestyramine, colestipol, colestimide, colesevelam, sevelamer, DEAE-cellulose, β-cyclodextrin, and γ-cyclodextrin;    (c) from about 0.1 to about 10 g of a filler;    (d) from about 0.05 to about 3.0 g of a surfactant;    (e) from about 0.05 to about 2.0 g of a disintegrant;    (f) from about 0.02 to about 2.0 g of a binder;    (g) from about 0.001 to about 1.0 g of a lubricant;    (h) from about 0.1 to about 5.0 g of a flowability enhancer;    (i) from about 0.01 to about 4.0 g of a sweetener; and    (j) and about 0.001 to about 0.5 g of a colorant.    
     
     
         21 . The compositions according to  claim 17 , wherein the orlistat is present in an amount of from about 10 to about 500 mg.  
     
     
         22 . The composition according to  claim 21 , wherein the orlistat is present in an amount of about 120 mg.  
     
     
         23 . The composition according to  claim 17 , wherein the orlistat is present in an amount of from about 20 to about 100 mg.  
     
     
         24 . The composition according to  claim 23 , wherein the orlistat is present in an amount of about 60 mg.  
     
     
         25 . The composition according to  claim 17 , wherein the bile acid sequestrant is present in an amount of from about 0.5 to about 10 g.  
     
     
         26 . The composition according to  claim 25 , wherein the bile acid sequestrant is present in an amount of from about 1 to about 5 g.  
     
     
         27 . The compositions according to  claim 19 , wherein the orlistat is present in an amount of from about 10 to about 500 mg.  
     
     
         284 . The composition according to  claim 27 , wherein the orlistat is present in an amount of about 120 mg.  
     
     
         29 . The composition according to  claim 27 , wherein the orlistat is present in an amount of from about 20 to about 100 mg.  
     
     
         30 . The composition according to  claim 29 , wherein the orlistat is present in an amount of about 60 mg.  
     
     
         31 . The composition according to  claim 19 , wherein the bile acid sequestrant is present in an amount of from about 0.5 to about 10 g.  
     
     
         32 . The composition according to  claim 31 , wherein the bile acid sequestrant is present in an amount of from about 1 to about 5 g.  
     
     
         33 . A kit for use in the treatment of obesity, which comprises (a) a first component which is orlistat and (b) a second component which is a bile acid sequestrant selected from the group consisting of cholestyramine, colestipol, colestimide, colesevelam, sevelamer, DEAE-cellulose, β-cyclodextrin, γ-cyclodextrin, guanidinoethylcellulose, and DEAE-Sephadex, present in oral unit dosage form.  
     
     
         34 . A method of treating obesity in an obese patient to achieve a reduction in body weight, which comprises administering to a patient in need of such treatment (a) a therapeutically effective amount of orlistat and (b) a pharmaceutically acceptable bile acid sequestrant selected from the group consisting of cholestyramine, colestipol, colestimide, colesevelam, sevelamer, DEAE-cellulose, β-cyclodextrin, γ-cyclodextrin, guanidinoethylcellulose, and DEAE-Sephadex in an amount effective to reduce gastrointestinal side effects associated with the lipase inhibitor.  
     
     
         35 . The method according to  claim 34 , wherein the orlistat and bile acid sequestrant are administered simultaneously.  
     
     
         36 . The method according to  claim 34 , wherein the orlistat and bile acid sequestrant are administered separately.  
     
     
         37 . The method according to  claim 34 , wherein the orlistat and bile acid sequestrant are administered sequentially.

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