Lipase inhibiting composition

Abstract

Pharmaceutical compositions that contain a lipase inhibitor having a melting point ≧37° C., a sucrose fatty acid ester wherein the sucrose fatty acid ester is a mono-, di-, tri- or tetra-ester, and optionally one or more pharmaceutically acceptable excipients, are useful for treatment of obesity.

What is claimed is:  
     
         1 . A pharmaceutical composition comprising a lipase inhibitor having a melting point ≧37° C., a sucrose fatty acid ester wherein the sucrose fatty acid ester is a mono-, di-, tri- or tetra-ester, and one or more pharmaceutically acceptable excipients.  
     
     
         2 . The composition of  claim 1 , wherein the ester is a mono-, di-, or tri-ester.  
     
     
         3 . The composition according to  claim 2 , wherein the ester is a mono- or di-ester.  
     
     
         4 . The composition according to  claim 3 , wherein the ester is a mono-ester.  
     
     
         5 . The composition according to  claim 1 , wherein the fatty acid moieties in the ester are identical.  
     
     
         6 . The composition according to  claim 1 , wherein 0.05 mg to 20 mg sucrose fatty acid ester is used per 1 mg lipase inhibitor.  
     
     
         7 . The composition according to  claim 6 , wherein 0.1 mg to 10 mg sucrose fatty acid ester is used per 1 mg lipase inhibitor.  
     
     
         8 . The composition according to  claim 7 , wherein 0.1 to 2 mg sucrose fatty acid ester is used per 1 mg lipase inhibitor.  
     
     
         9 . The composition according to  claim 8 , wherein 0.15 to 1 mg sucrose fatty acid ester is used per 1 mg lipase inhibitor.  
     
     
         10 . The composition according to  claim 1 , wherein the lipase inhibitor is a lipophilic compound.  
     
     
         11 . The composition according to 10, wherein the lipase inhibitor is orlistat.  
     
     
         12 . The composition according to  claim 1 , wherein the fatty acid moiety of the sucrose fatty acid ester is a C 8  to C 24  saturated or partially non-saturated fatty acid.  
     
     
         13 . The composition according to  claim 12 , wherein the fatty acid moiety of the sucrose fatty acid ester is a C 12  to C 18  saturated fatty acid.  
     
     
         14 . The composition according to  claim 13 , wherein the fatty acid ester is selected from the group consisting of sucroselaurate, sucrosemyristate, sucrosepalmitate, sucrosestearate, sucrosearachidonate and sucrosebehanate.  
     
     
         15 . The composition according to  claim 14 , wherein the fatty acid ester is selected from the group consisting of sucroselaurate, sucrosemyristate, sucrosepalmitate, sucrosestearate.  
     
     
         16 . The composition according to  claim 15 , wherein the fatty acid ester is sucrosepalmitate.  
     
     
         17 . The composition according to  claim 15 , wherein the fatty acid ester is sucrosestearate.  
     
     
         18 . The composition according to  claim 12 , wherein the fatty acid moiety of the sucrose fatty acid ester is a C 12  to C 18  mono- or polyunsaturated fatty acid.  
     
     
         19 . The composition of  claim 18 , wherein the fatty acid moiety is selected from the group consisting of palmitoleic acid, oleic acid, elaidic acid, erucic acid, linoleic acid, gamma-linolenic acid, alpha-linolenic acid and arachidonic acid.  
     
     
         20 . The composition of  claim 19 , wherein the sucrose fatty acid ester is sucroseoleate.  
     
     
         21 . The composition according to  claim 1 , wherein the fatty acid moieties in a di-, tri- and tetra-sucrose fatty acid ester is a mixture of two or more fatty acids.  
     
     
         22 . The composition of  claim 21 , wherein the sucrose fatty acid ester is sucrosepalmitostearate.  
     
     
         23 . The composition according to  claim 11 , wherein the composition comprises 10 to 240 mg orlistat.  
     
     
         24 . The composition according to  claim 23 , wherein the composition comprises 30 to 120 mg orlistat.  
     
     
         25 . The composition according to  claim 24 , wherein the composition comprises 30, 40, 60, 80, 100, or 120 mg orlistat.  
     
     
         26 . The composition according to  claim 11 , wherein the composition comprises 60 to 120 mg orlistat and 20 mg to 100 mg sucrose fatty acid ester.  
     
     
         27 . The composition according to  claim 26 , wherein the composition comprises 120 mg orlistat and 30 mg sucrose ester.  
     
     
         28 . The composition according to  claim 26 , wherein the composition comprises 80 to 120 mg orlistat and 10 to 40 mg sucrose fatty acid ester.  
     
     
         29 . The composition according to  claim 11 , wherein the composition comprises 20 to 60 mg orlistat and 5 to 15 mg sucrose fatty acid ester.  
     
     
         30 . The composition according to  claim 1 , wherein the composition comprises one or more pharmaceutically acceptable excipients selected from the group consisting of mannitol, lactose, HPMC, talcum, sorbitol, polyvinylpyrrolidone, lecithin, polyethylenglycol, polysorbate, polyoxethylenstearate, and dimethicon.  
     
     
         31 . The composition according to  claim 30 , wherein the pharmceutically acceptable excipient comprises lactose.  
     
     
         32 . The composition according to  claim 11 , wherein the composition comprises 10-240 mg orlistat and 0.5-1000 mg sucrose fatty acid ester.  
     
     
         33 . The composition of  claim 32 , wherein the composition comprises one or more excipients selected from the group consisting of maltodextrin, lactose and cellulose.