Solid dosage forms comprising an enteric coating with accelerated drug release

Patent metadata

Field	Value
Publication number	US-10537530-B2
Application number	US-201213603984-A
Country	US
Kind code	B2
Filing date	Sep 5, 2012
Priority date	May 7, 2007
Publication date	Jan 21, 2020
Grant date	Jan 21, 2020

Abstract

The invention provides a gastric resistant, enteric-coated solid dosage form including a core containing a pharmaceutically active ingredient, an inner coating for the core, and an outer enteric coating. The inner coating comprises an anionic polymeric material or a water-soluble neutral polymeric material, and further comprises a water soluble inorganic salt which is not a carbonate or bicarbonates. The outer enteric coating comprises an anionic polymeric material which is less neutralized than the polymeric material comprising the inner coating and disintegrates rapidly at a pH of 5.5 to 7.0 upon entering the small intestine.

First claim

The invention claimed is:

1. A gastric resistant, enteric-coated solid dosage form comprising
an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating;
wherein said inner coating further comprises at least one water soluble inorganic salt, wherein the cation of the inorganic salt is selected from the group consisting of alkali metal, alkaline earth metal, ammonium, manganese, iron, copper, zinc, and molybdenum cations, and the anion of the inorganic salt is selected from the group consisting of chloride, fluoride, bromide, iodide, nitrate, nitrite, and sulphate anions, with the proviso that carbonates and bicarbonates are excluded; and
wherein each of the outer and the inner coatings comprises a partially neutralized anionic (meth)acrylate copolymer consisting of free-radical polymerized units of 25 to 95% by weight C1- to C4-alkyl esters of acrylic or of methacrylic acid and 5 to 75% by weight (meth)acrylate monomers having an anionic group, wherein the outer coating is less neutralized than the inner coating.

2. A gastric resistant, enteric-coated solid dosage form comprising
an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating;
wherein said inner coating further comprises at least one water soluble inorganic salt, wherein the cation of the inorganic salt is selected from the group consisting of alkali metal, alkaline earth metal, ammonium, manganese, iron, copper, zinc, and molybdenum cations, and the anion of the inorganic salt is selected from the group consisting of chloride, fluoride, bromide, iodide, nitrate, nitrite, and sulphate anions, with the proviso that carbonates and bicarbonates are excluded; and
wherein the inner coating comprises a partially neutralized anionic (meth)acrylate copolymeric material and the outer coating comprises the same partially neutralized anionic (meth)acrylate copolymeric material of the inner coating, with the proviso that the partially neutralized anionic (meth)acrylate copolymeric material of the outer coating is less neutralized than the partially neutralized anionic (meth)acrylate copolymeric material of the inner coating.

3. A gastric resistant, enteric-coated solid dosage form comprising
an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating;
wherein said inner coating further comprises at least one water soluble inorganic salt, wherein the cation of the inorganic salt is selected from the group consisting of alkali metal, alkaline earth metal, ammonium, manganese, iron, copper, zinc, and molybdenum cations, and the anion of the inorganic salt is selected from the group consisting of chloride, fluoride, bromide, iodide, nitrate, nitrite, and sulphate anions, with the proviso that carbonates and bicarbonates are excluded; and
wherein each of the outer and the inner coating comprises a partially neutralized anionic (meth)acrylate copolymer consisting of free-radical polymerized units of 25 to 95% by weight C1- to C4-alkyl esters of acrylic or of methacrylic acid and 5 to 75% by weight (meth)acrylate monomers having an anionic group, wherein the outer coating is less neutralized than the inner coating.

4. A gastric resistant, enteric-coated solid dosage form comprising
an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating;
wherein said inner coating further comprises at least one water soluble inorganic salt, wherein the cation of the inorganic salt is selected from the group consisting of alkali metal, alkaline earth metal, ammonium, manganese, iron, copper, zinc, and molybdenum cations, and the anion of the inorganic salt is selected from the group consisting of chloride, fluoride, bromide, iodide, nitrate, nitrite, and sulphate anions, with the proviso that carbonates and bicarbonates are excluded; and
wherein the inner coating comprises a partially neutralized anionic (meth)acrylate copolymeric material and the outer coating consists essentially of the same partially neutralized anionic (meth)acrylate copolymeric material of the inner coating, with the proviso that the partially neutralized anionic (meth)acrylate copolymeric material of the outer coating is less neutralized than the partially neutralized anionic (meth)acrylate copolymeric material of the inner coating.

Assignees

• Liu Fang
• Basit Abdul W
• Lizio Rosario
• Petereit Hans Ulrich
• Meier Christian
• Damm Michael
• Evonik Operations Gmbh

Inventors

• Liu Fang
• Basit Abdul W
• Lizio Rosario
• Petereit Hans-Ulrich
• Meier Christian
• Damm Michael

Classifications

• A61K9/5026

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates · CPC title

• A61K9/5073 Primary

  having two or more different coatings optionally including drug-containing subcoatings · CPC title

• A61K9/28

  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

• A61K47/34 Primary

  Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) · CPC title