# US 8,465,767 B2 · Oral administration form for pyridin-2-ylmethylsulfinyl-1H benzimidazoles > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,465,767 B2 - Document ID: US8465767B2 - Status: Granted - Kind: B2 - Application number: 12/153,585 - Filed: 2008-05-21 - Published: 2008-09-18 - Granted: 2013-06-18 - Earliest claimed: 1998-08-12 - Assignees: Takeda GmbH - Applicants: Rango Dietrich; Hartmut Ney - Inventors: Rango Dietrich; Hartmut Ney - Web page: https://patentgrep.com/patent/US8465767B2 ## CPC - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2846: {Poly(meth)acrylates} - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The invention relates to an oral administration form for pyridin-2-ylmethylsulfinyl-1H-benzimidazoles and their salts, which comprises the active compound together with tablet disintegrants and is provided with a film coating customary per se for sustained-release compositions. ## Claims ### Claim 1 An oral fixed combination administration form for an active compound, which is a pyridin-2-ylmethylsulfinyl-1H-benzimidazole or a pharmaceutically acceptable salt thereof, wherein said active compound is in a capsule in two different administration forms which have a different release of the active compound, wherein one administration form comprises the active compound together with a tablet disintegrant and bears a coating film for sustained-release, and an enteric coating film being absent, and wherein the other administration form comprises the active compound and which bears an enteric coating film. ### Claim 2 (depends on 1) An oral fixed combination administration form according to claim 1, wherein the administration form, which comprises the active compound together with a tablet disintegrant and bears a coating film for sustained release will release the active compound only after gastric passage. ### Claim 3 (depends on 2) An oral fixed combination administration form according to claim 2, wherein the release is spontaneous and complete. ### Claim 4 (depends on 1) An oral fixed combination administration form according to claim 1, wherein the pharmaceutically acceptable salts of pyridin-2-ylmethylsulfinyl-1H-benzimidazole are selected from the group consisting of potassium, sodium, calcium and magnesium. ### Claim 5 (depends on 1) An oral fixed combination administration form according to claim 1, wherein the tablet disintegrant is a cellulose derivative, starch, bentonite, sodium alginate, pectin or crosslinked polyvinylpyrrolidone. ### Claim 6 (depends on 1) An oral fixed combination administration form according to claim 1, wherein the tablet disintegrant is selected from the group consisting of sodium cellulose glycolate, a composition based on sodium carboxymethylcellulose and potato starch, sodium carboxymethylstarch, bentonite, sodium alginate, pectin and crosslinked polyvinylpyrrolidone. ### Claim 7 (depends on 1) An oral fixed combination administration form according to claim 1, wherein the pyridine-2-ylmethylsulfinyl-1H-benzimidazole is omeprazole, esomeprazole, lansoprazole, rabeprazole, leminoprazole or nepaprazole. ### Claim 8 (depends on 1) An oral fixed combination administration form according to claim 1, wherein the pyridin-2-ylmethylsulfinyl-1H-benzimidazole is pantoprazole. ### Claim 9 (depends on 1) An oral fixed combination administration form according to claim 1, wherein each administration form is in pellet form. ### Claim 10 (depends on 1) An oral fixed combination administration form according to claim 1, wherein each administration form is in tablet form. ### Claim 11 (depends on 1) An oral fixed combination administration form according to claim 1, wherein the tablet disintegrant is crosslinked polyvinylpyrrolidone. ### Claim 12 (depends on 11) An oral fixed combination administration form according to claim 11, wherein the tablet disintegrant is crosslinked polyvinylpyrrolidone having a proportion in the tablet core of 20-35% by weight. ### Claim 13 (depends on 1) An oral fixed combination administration form according to claim 1, wherein the coating film is a copolymer of acrylic and methacrylic acid esters having quaternary ammonium structures. ### Claim 14 (depends on 1) An oral fixed combination administration form according to claim 1, in combination with or for combined use with an antimicrobial agent. ### Claim 15 (depends on 1) An oral fixed combination administration form according to claim 1, which is suitable for once daily administration of pantoprazole or a pharmaceutically acceptable salt thereof. ### Claim 16 (depends on 1) An oral fixed combination administration form according to claim 1, wherein the coating film is a water-insoluble and physiologically tolerable plastic membrane having low swelling power in water and in which small soluble particles are imbedded. ### Claim 17 (depends on 16) An oral fixed combination administration form according to claim 16, wherein the plastic membrane does not absorb more than 5% by weight of water in an aqueous medium. ### Claim 18 (depends on 17) An oral fixed combination administration form according to claim 17, wherein the plastic is selected from the group consisting of cellulose ethers, cellulose esters, polymers of polyvinylchloride, and copolymers of acrylic and methacrylic acid esters. ### Claim 19 (depends on 16) An oral fixed combination administration form according to claim 16, wherein the small soluble particles are lactose crystals. ### Claim 20 (depends on 16) An oral fixed combination administration form according to claim 16, wherein the weight ratio of plastic to soluble particles is approximately 2:1 to 1:3. ### Claim 21 (depends on 20) An oral fixed combination administration form according to claim 20, wherein the weight ratio of plastic to soluble particles is 4:3 to 4:5.