GASTRIC RESISTANT PHARMACEUTICAL OR NUTRACEUTICAL FORMULATION COMPRISING ONE OR MORE SALTS OF ALGINIC ACID
First Claim
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 USP with and without the addition of 40% (v/v) ethanol, andwherein 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 30 to 720 cP.
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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
21 Citations
20 Claims
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1. A gastric resistant pharmaceutical or nutraceutical composition, comprising:
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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 USP 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 30 to 720 cP.
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2. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1, wherein a weight gain of the coating layer is at least 2.5 mg/cm2.
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3. 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.
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4. 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.
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5. 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.
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6. The gastric resistant pharmaceutical or nutraceutical composition according to claim 1, wherein the gastric resistant coating layer comprises 0 to 400% by weight of at least one polymer selected from the group consisting of water-insoluble polymers and cellulosic polymers based on the weight of the at least one salt of alginic acid.
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7. The gastric resistant pharmaceutical or nutraceutical composition according to claim 6, wherein the water-insoluble polymers comprise (meth)acrylate copolymers.
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8. The gastric resistant pharmaceutical or nutraceutical composition according to claim 7, wherein the (meth)acrylate copolymer comprises free-radical polymerized units of more than 95 up to 100% by weight of C1- to C4-alkyl esters of acrylic or of methacrylic acid and less than 5% by weight of acrylic or methacrylic acid.
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9. The gastric resistant pharmaceutical or nutraceutical composition according to claim 8, wherein the methacrylate copolymer comprises:
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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.
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10. The gastric resistant pharmaceutical or nutraceutical composition according to claim 7, wherein the (meth)acrylate copolymer comprises:
85 to 98% by weight of free-radical polymerized C1- to C4-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.
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11. The gastric resistant pharmaceutical or nutraceutical composition according to claim 6, wherein the at least one polymer is hydroxypropylmethyl cellulose.
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12. 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 antioxidants, brighteners, binding agents, flavouring agents, flow aids, fragrances, glidants, penetration-promoting agents, pigments, plasticizers, polymers, different from the at least one salt of alginic acid and different from the at least one water-insoluble or cellulosic polymer, pore-forming agents and stabilizers.
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13. 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.
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14. An aqueous coating solution, suspension or dispersion comprising the gastric resistant pharmaceutical or nutraceutical composition according to claim 1.
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15. A process for producing the gastric resistant pharmaceutical or nutraceutical composition according to claim 1, comprising:
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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.
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16. 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.
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17. 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.
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18. The gastric resistant pharmaceutical or nutraceutical composition according to claim 2, wherein the gastric resistant coating layer comprises potassium alginate.
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19. 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 30 to 720 cP.
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20. The gastric resistant pharmaceutical or nutraceutical composition according to claim 17, 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.
Specification