Anti-obesity compositions

Abstract

The present invention relates to compositions and methods for treating obesity. More particularly, the invention relates to a composition comprising a lipase inhibitor such as orlistat, and glucomannan such as konjac as well as methods for utilizing such compositions and kits for carrying out this method.

What is claimed:  
     
         1 . A pharmaceutical composition comprising from about 0.1% by weight to about 20% by weight, based upon the weight of the composition, of a lipase inhibitor and from about 10% by weight to about 75% by weight, based upon the weight of the composition, of glucomannan and from about 0.1% to about 90% by weight, based upon the weight of the composition, of one or more pharmaceutically acceptable excipients.  
     
     
         2 . The composition of  claim 1  wherein the glucomannan is present as konjac.  
     
     
         3 . The composition of  claim 2  wherein the konjac is present as konjac flour.  
     
     
         4 . The composition of  claim 2  where in the konjac contains at least 80% by weight of glucomannan.  
     
     
         5 . The pharmaceutical composition of  claim 4  wherein the konjac contains at least 90% by weight glucomannan.  
     
     
         6 . The composition of  claim 1  wherein the lipase inhibitor is present in an amount of from about 0.1% by weight to about 10%, based upon the weight of said composition, and glucomannan is present in an amount of from 20% to 75% by weight, based upon the weight of the composition.  
     
     
         7 . The composition of  claim 1 , wherein the pharmaceutically acceptable excipient is selected from the group consisting of fillers, surfactants, disintegrants, binders, lubricants, flowability enhancers, sweeteners, and colorants.  
     
     
         8 . The composition of  claim 7  wherein the composition comprises 
 a) from about 0.1% to about 20% (w/w) lipase inhibitor;  
 b) from about 10 to about 75% (w/w) glucomannan; and  
 pharmaceutically acceptable excipients selected from the group consisting of, from about 0.1 to about 20% (w/w) fillers, from about 0.1 to about 10% (w/w) surfactants, about 0.1 to about 10% (w/w) disintegrants, from about 0.1 to about 10% (w/w) binder, about 0.1 to about 10% (w/w) lubricants, from about 0.1 to about 10% (w/w) flowability enhancers, about 0.1 to about 10% (w/w) sweeteners, from about 0.1 to about 5% (w/w) colorants and mixtures thereof, with all said weight percents being based upon the weight of the composition.  
 
     
     
         9 . The composition of  claim 1  wherein the composition contains from about 5 mg to about 1,000 mg of said lipase inhibitor and from about 0.5 g to about 10 g of glucomannan.  
     
     
         10 . The composition of  claim 9  wherein said composition is in unit oral dosage form.  
     
     
         11 . The composition of  claim 10  wherein the composition contains from about 0.5 to 6 grams of glucomannan.  
     
     
         12 . The composition of  claim 11  wherein said composition contains from about 10 mg to 500 mg of the lipase inhibitor.  
     
     
         13 . The composition of  claim 12  wherein said composition contains from about 10 mg to about 360 mg of the lipase inhibitor.  
     
     
         14 . The composition of  claim 9 , wherein the pharmaceutically acceptable excipient is selected from the group consisting of fillers, surfactants, disintegrants, binders, lubricants, flowability enhancers, sweeteners, and colorants.  
     
     
         15 . The composition of  claim 14 , comprising 
 a) from about 5 to about 1000 mg of said lipase inhibitor;    b) from about 0.5 to about 10 g glucomannan; and    pharmaceutically acceptable excipients selected from the group consisting of from about 0.1 to about 10 g fillers, from about 0.05 to about 5.0 g surfactants, from about 0.05 to about 2.0 g disintegrants, from about 0.02 to about 5.0 g binder, from about 0.001 to about 1.0 g lubricants, from about 0.1 to about 5.0 g flowability enhancers, from about 0.01 to about 4.0 g sweeteners, from about 0.001 to about 0.5 g colorants and mixtures thereof.    
     
     
         16 . The composition of  claim 1  wherein said lipase inhibitor is orlistat.  
     
     
         17 . The composition of  claim 16  wherein the glucomannan present as konjac.  
     
     
         18 . The composition of  claim 17  wherein the konjac is present as konjac flour.  
     
     
         19 . The composition of  claim 18  where in the konjac contains at least 80% by weight of glucomannan.  
     
     
         20 . The pharmaceutical composition of  claim 19  wherein the konjac contains at least 90% by weight glucomannan.  
     
     
         21 . The composition of  claim 16  wherein the glucomannan is present in said composition in an amount of from about 20% to 75% by weight, based upon the weight of the composition and the orlistat is present in an amount of from 1% to about 10% based upon the weight of the composition.  
     
     
         22 . The composition of  claim 16 , wherein the pharmaceutically acceptable excipient is selected from the group consisting of fillers, surfactants, disintegrants, binders, lubricants, flowability enhancers, sweeteners, and colorants.  
     
     
         23 . The composition of  claim 22  wherein the composition comprising from 
 a) about 0.1% to about 20% (w/w) of orlistat;  
 b) about 10 to about 75% (w/w) glucomannan; and  
 pharmaceutically acceptable excipients selected from the group consisting of from about 0.1 to about 20% (w/w) fillers, from about 0.1 to about 10% (w/w) surfactants, from about 0.1 to about 10% (w/w) disintegrants, from about 0.1 to about 10% (w/w) binder, from about 0.1 to about 10% (w/w) lubricants, from about 0.1 to about 10% (w/w) flowability enhancers, from about 0.1 to about 10% (w/w) sweeteners, from about 0.1 to about 5% (w/w) colorants and mixtures thereof wherein the percents are based upon the weight of the composition.  
 
     
     
         24 . The composition of  claim 16  wherein the composition contains from about 5 mg to about 1,000 mg of said lipase inhibitor and from about 0.5 g to about 10 g of glucomannan.  
     
     
         25 . The composition of  claim 16  wherein said composition contains from about 10 mg to 500 mg of orlistat.  
     
     
         26 . The composition of  claim 24  wherein said composition contains from about 10 mg to about 360 mg of orlistat.  
     
     
         27 . The composition of  claim 16 , comprising from: 
 a) about 5 to about 1000 mg orlistat;    b) about 0.5 to about 10 g glucomannan; and    pharmaceutically acceptable excipients selected from the group consisting of from about 0.1 to about 10 g fillers, from about 0.05 to about 5.0 g surfactants, from about 0.05 to about 2.0 g disintegrants, from about 0.02 to about 5.0 g binder, from about 0.001 to about 1.0 g lubricants, from about 0.1 to about 5.0 g flowability enhancers, from about 0.01 to about 4.0 g sweeteners, from about 0.001 to about 0.5 g colorants and mixtures thereof.    
     
     
         28 . A method of combating obesity in human patients comprising administering to said human patients a lipase inhibitor in an amount effective to combat said obesity, said lipase inhibitor being administered in conjunction with glucomannan, said glucomannan being administered in an amount sufficient to reduce the gastro-intestinal adverse events caused after administration of a lipase inhibitor.  
     
     
         29 . The method of  claim 28  wherein the lipase inhibitor is administered for treatment or prevention of obesity.  
     
     
         30 . The method of  claim 29  wherein said lipase inhibitor and glucomannan are administered simultaneously or sequentially or separately.  
     
     
         31 . The method of  claim 30  wherein said lipase inhibitor is administered in an amount of from about 5 mg to 1000 mg per day and the glucomannan is administered in an amount of from 0.5 to 10 g per day.  
     
     
         32 . The method of  claim 31  wherein said lipase inhibitor is administered in an amount of from about 60 mg to 720 mg per day.  
     
     
         33 . The method of  claim 31  wherein said administration is oral.  
     
     
         34 . The method of  claim 33  wherein the glucomannan and the lipase inhibitor are administered within two hours of each other.  
     
     
         35 . The method of  claim 31  wherein the glucomannan is administered for combating gastrointestinal side effects caused by the lipase inhibitor, which side effects are selected from the group consisting of oily spotting, fatty/oily stools, fecal urgency, increased defecation and fecal incontinence.  
     
     
         36 . The method of  claim 33  wherein the combination of lipase inhibitor and the glucomannan are administered from two to three times per day.  
     
     
         37 . The method of  claim 35  wherein the combination is orally administered.  
     
     
         38 . The method of  claim 31  wherein said lipase inhibitor is orlistat.  
     
     
         39 . The method of  claim 38  wherein orlistat is orally administered in an amount of from about 10 mg to about 500 mg per day.  
     
     
         40 . The method of  claim 39  wherein the orlistat is administered in an amount from about 10 mg to 360 mg per day.  
     
     
         41 . The method of  claim 40  wherein the orlistat is administered in an amount from about 30 mg to 120 mg per day.  
     
     
         42 . The method of  claim 41  wherein the orlistat is administered in an amount from about 40 mg to 80 mg per day.  
     
     
         43 . The kit for the treatment of obesity containing as a first component a lipase inhibitor and as a second component glucomannan.  
     
     
         44 . The kit of  claim 43  wherein both of the components within the kit contain unit oral dosage forms to be administered to a human patient.  
     
     
         45 . The kit of  claim 44  wherein said lipase inhibitor is orlistat.  
     
     
         46 . The kit of  claim 45  wherein the oral unit dosage forms which comprise the first component orlistat each contain from about 5 to about 120 mg of the orlistat and the unit oral dosage forms which comprise the second component glucomannan each contain from about 0.5 to about 10 g of glucomannan.  
     
     
         47 . The kit of  claim 45  wherein the oral unit dosage forms which comprise the first component orlistat each contain from about 16 mg to about 720 mg of orlistat and the unit oral dosage forms which comprise the second component glucomannan each contain from about 0.5 to about 10 g of glucomannan.  
     
     
         48 . The kit of  claim 46  wherein each component contains from 1 to 100 oral unit dosage forms of glucomannan and from 1 to 100 oral unit dosage forms of orlistat.  
     
     
         49 . The kit of  claim 47  wherein each component contains from 1 to 100 oral unit dosage forms of glucomannan and from 1 to 100 oral unit dosage forms of orlistat.