Lipstatin derivative-soluble fiber tablets
AssigneeSmithKline Beecham Corporation
InventorsBruce P. Daggy, Kenneth G. Mandel
Life of this patent
Estimating the term…
Abstract
The present invention relates to a novel pharmaceutical composition and process for preparing swallowable rapidly disintegrating methylcellulose and lipstatin derivatives together in combination with a suitable diluent and excipients.
Claims24
A pharmaceutical composition for an immediate release tablet comprising:
- (a) at least one water soluble, non-fermentable cellulose derivative which is methylcellulose having a viscosity of >1000 centipoise;
- (b) at least one lipase inhibitor in an amount effective for treating adiposity;
- and
- (c) at least one excipient which is an edible calcium salt which is dibasic calcium phosphate dihydrate, calcium phosphate anhydrous, or tribasic calcium phosphate;
- or mixtures thereof.
A method for the dual treatment of adiposity and the faecal incontinence and steatorrhea associated therewith which method comprises administering to a mammal in need thereof a compressed tablet comprising:
- (a) at least one lipase inhibitor in an amount effective for treating adiposity;
- and
- (b) at least one water soluble, non-fermentable cellulose derivative having a viscosity of >1000 centipoise present in a sufficient amount to reduce the faecal incontinence and steatorrhea associated with coadministration of the lipase inhibitor;
- and
- (c) at least one excipient which is an edible calcium salt which is dibasic calcium phosphate dihydrate, calcium phosphate anhydrous, or tribasic calcium phosphate;
- or mixtures thereof.
A pharmaceutical composition for a tablet comprising:
- (a) at least one water soluble, non-fermentable cellulose derivative which is methylcellulose having a viscosity of >1000 centipoise;
- (b) at least one lipase inhibitor in an amount effective for treating adiposity;
- and
- (c) at least one swellable diluent or filler, selected from the group consisting of microcrystalline cellulose, corn starch, or Starch 1500.
A method for the dual treatment of adiposity and the faecal incontinence and steatorrhea associated therewith which method comprises administering to a mammal in need thereof a compressed tablet comprising:
- (a) at least one water soluble, non-fermentable cellulose derivative which is methylcellulose having a viscosity of >1000 centipoise;
- (b) at least one lipase inhibitor in an amount effective for treating adiposity;
- and
- (c) at least one swellable diluent or filler, selected from the group consisting of microcrystalline cellulose, corn starch, or Starch 1500.
A process for preparing a tablet formulation which process comprises:
- a) blending together to form an intragranular mixture high viscosity methylcellulose of >3000 cps;
- a diluent selected from the group consisting of microcrystalline cellulose, corn starch, or Starch 1500, or a mixture thereof, a lipase inhibitor, a lubricating agent and optionally a disintegrant;
- and
- b) adding to the mixture of step (a), a PVP aqueous solution, or alternatively spraying the mixture of step (a) with a PVP aqueous solution;
- and preparing granulates;
- and
- c) blending together an extragranular mixture of a wetting agent;
- a lubricating agent;
- a diluent;
- and a disintegrant, or a mixture thereof;
- and
- d) compacting the granulates of step (b) with the extragranular mixture of step (c).
A process for the manufacture of a pharmaceutical tablet, which process comprises mixing
- a) granulates comprising high viscosity methylcellulose of >3000 cps;
- at least one edible calcium salt which is dibasic calcium phosphate dihydrate, calcium phosphate anhydrous, or tribasic calcium phosphate;
- or mixtures thereof;
- a lipase inhibitor, and optionally together with an intra-granular disintegrant, and/or wetting agent, and/or colouring agent;
- with
- b) adding to the mixture of step (a), a PVP aqueous solution, or alternatively spraying the mixture of step (a) with a PVP aqueous solution;
- and preparing granulates;
- and
- c) blending together an extragranular mixture of a wetting agent;
- a lubricating agent;
- a diluent;
- and a disintegrant, or a mixture thereof;
- and
- d) compacting the granulates of step (b) with the extragranular mixture of step (c).
A pharmaceutical composition for an immediate release tablet comprising:
- (a) at least one lipase inhibitor in an amount effective for treating adiposity;
- (b) at least one water soluble, non-fermentable cellulose derivative which is methylcellulose having a viscosity of >1000 centipoise present in a sufficient amount to reduce the faecal incontinence and steatorrhea associated with coadministration of the lipase inhibitor;
- and
- (c) at least one excipient which is an edible calcium salt which is dibasic calcium phosphate dihydrate, calcium phosphate anhydrous, or tribasic calcium phosphate;
- or mixtures thereof.
Dependencies are inferred from the claim text.