Gastric resistant pharmaceutical or nutraceutical formulation comprising one or more salts of alginic acid

Patent metadata

Field	Value
Publication number	US-9492394-B2
Application number	US-201113086079-A
Country	US
Kind code	B2
Filing date	Apr 13, 2011
Priority date	Aug 18, 2010
Publication date	Nov 15, 2016
Grant date	Nov 15, 2016

Abstract

The invention relates to a gastric resistant pharmaceutical or nutraceutical composition, comprising a core, comprising a pharmaceutical or nutraceutical active ingredient and a gastric resistant coating layer onto the core, wherein the release of the pharmaceutical or nutraceutical active ingredient is not more than 15% under in-vitro conditions at pH 1.2 for 2 hours in medium according to USP with and without the addition of 40% (v/v) ethanol, wherein the gastric resistant coating layer comprises 10 to 100% by weight of one or more salts of alginic acid with a viscosity of 30 to 720 cP of a 1% aqueous solution.

First claim

The invention claimed is:

1. A gastric resistant pharmaceutical or nutraceutical composition, comprising:
a core, comprising:
a pharmaceutical or nutraceutical active ingredient and

a gastric resistant coating layer on the core,
wherein a release of the pharmaceutical or nutraceutical active ingredient is not more than 15% under in-vitro conditions at pH 1.2 for 2 hours in medium according to the method of USP32/NF27 with and without the addition of 40% (v/v) ethanol, and
wherein the gastric resistant coating layer comprises 10 to 100% by weight of at least one salt of alginic acid which provides a 1% aqueous solution having a viscosity of 40 to 720 cP,
wherein the weight gain of the coating layer is at least 3.5 mg/cm 2 ,
wherein the gastric resistant coating layer comprises 0% by weight of water-insoluble polymers other than a water-insoluble polymer selected from the group consisting of a vinyl copolymer and a (meth)acrylate copolymer,
wherein the gastric resistant coating layer comprises 0 to 70% by weight of one or more water-soluble cellulosic polymers, one or more water-insoluble polymers selected from the group consisting of a vinyl copolymer and a (meth)acrylate copolymer, or a mixture thereof, based on the weight of the one or more salts of alginic acid contained, and
wherein said (meth)acrylate copolymer is at least one of:
(a) a methacrylate copolymer comprising free-radical polymerized units of more than 95 up to 100% by weight of C 1 - to C 4 -alkyl esters of acrylic or of methacrylic acid and less than 5% by weight of acrylic or methacrylic acid, and
(b) a methacrylate copolymer comprising 85 to 98% by weight of free-radical polymerized C 1 - to C 4 -alkyl esters of acrylic or methacrylic acid and 15 to 2% by weight of alkyl(meth)acrylate monomers with a quaternary amino group in the alkyl radical.

2. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the coating layer comprises up to 90% by weight of at least one pharmaceutical or nutraceutical acceptable excipient.

3. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein a release of the pharmaceutical or nutraceutical active ingredient is at least 50% under in-vitro conditions at pH 6.8 for one hour in a buffered medium according to USP.

4. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the at least one salt of alginic acid is at least one selected from the group consisting of sodium alginate, potassium alginate, magnesium alginate, lithium alginate and ammonium alginate.

5. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the water-insoluble polymers comprise (meth)acrylate copolymers.

6. The gastric resistant pharmaceutical or nutraceutical composition according to claim 5 , wherein the (meth)acrylate copolymer comprises free-radical polymerized units of more than 95 up to 100% by weight of C 1 - to C 4 -alkyl esters of acrylic or of methacrylic acid and less than 5% by weight of acrylic or methacrylic acid.

7. The gastric resistant pharmaceutical or nutraceutical composition according to claim 6 , wherein the methacrylate copolymer comprises:
20 to 40% by weight of ethyl acrylate;
60 to 80% by weight of methyl methacrylate; and
0 to less than 5% by weight of methacrylic acid.

8. The gastric resistant pharmaceutical or nutraceutical composition according to claim 5 , wherein the (meth)acrylate copolymer comprises:
85 to 98% by weight of free-radical polymerized C 1 - to C 4 -alkyl esters of acrylic or methacrylic acid and 15 to 2% by weight of alkyl(meth)acrylate monomers with a quaternary amino group in the alkyl radical.

9. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the at least one polymer is hydroxypropylmethyl cellulose.

10. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the core or the gastric resistant coating layer further comprises at least one pharmaceutical or nutraceutical acceptable excipient selected from the group consisting of
an antioxidant, a brightener, a binding agent, a flavouring agent, a flow aid, a fragrance, a glidant, a penetration-promoting agent, a pigment, a plasticizer, a pore-forming agent and a stabilizer.

11. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the gastric resistant pharmaceutical or nutraceutical composition is selected from the group consisting of a coated tablet, a coated minitablet, a coated pellet, a coated granule, a sachet, a capsule filled with coated pellets, powder or granules, and a coated capsule.

12. An aqueous coating solution, suspension or dispersion comprising the gastric resistant pharmaceutical or nutraceutical composition according to claim 1 .

13. A process for producing the gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , comprising:
forming the core comprising the active ingredient by at least one method selected from the group consisting of direct compression, compression of dry, wet or sintered granules, extrusion and subsequent rounding off, wet or dry granulation, direct pelleting, by binding powders onto active ingredient-free beads or neutral cores or active ingredient-containing particles and
applying the gastric resistant coating layer in the form of an aqueous dispersion in a spray process or by fluidized bed spray granulation onto the core.

14. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the gastric resistant coating layer comprises 10 to 100% by weight of at least one salt of alginic acid which provides a 1% aqueous solution having a viscosity of 40 to 450 cP.

15. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the gastric resistant coating layer comprises 10 to 100% by weight of at least one salt of alginic acid which provides a 1% aqueous solution having a viscosity of 50 to 300 cP.

16. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the gastric resistant coating layer comprises potassium alginate.

17. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein the gastric resistant coating layer comprises 70 to 90% by weight of at least one salt of alginic acid which provides a 1% aqueous solution having a viscosity of 40 to 720 cP.

18. The gastric resistant pharmaceutical or nutraceutical composition according to claim 15 , wherein the gastric resistant coating layer comprises 70 to 90% by weight of at least one salt of alginic acid which provides a 1% aqueous solution having a viscosity of 50 to 300 cP.

19. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein said gastric resistant coating layer comprises from greater than 0 to 70% by weight of one or more water-soluble cellulosic polymers, one or more water-insoluble polymers selected from the group consisting of a vinyl copolymer and a (meth)acrylate copolymer, or a mixture thereof, based on the weight of the one or more salts of alginic acid contained.

20. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1 , wherein, in gastric resistant coating layer,
the at least one salt of alginic acid is at least one of sodium alginate and ammonium alginate, and
the methacry

Assignees

• Bodinge Shraddha Ashok
• Haksar Priyanka Bansilal
• Gawde Seema Yashwant
• Pagar Hemant Karbhari
• Petereit Hans-Ulrich
• Evonik Roehm Gmbh

Inventors

• Bodinge Shraddha Ashok
• Haksar Priyanka Bansilal
• Gawde Seema Yashwant
• Pagar Hemant Karbhari
• Petereit Hans-Ulrich

Classifications

• A61K9/286 Primary

  Polysaccharides, e.g. gums; Cyclodextrin · CPC title

• A61K9/2866

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• A61K9/2846

  Poly(meth)acrylates · CPC title

• A61P1/04

  for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants · CPC title

• A61K9/28 Primary

  Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)} · CPC title