Oral administration form for pyridin-2-ylmethylsulfinyl-1H benzimidazoles
View Patent ↗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.
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.
2. 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.
3. An oral fixed combination administration form according to claim 2 , wherein the release is spontaneous and complete.
4. 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.
5. 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.
6. 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.
7. 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.
8. An oral fixed combination administration form according to claim 1 , wherein the pyridin-2-ylmethylsulfinyl-1H-benzimidazole is pantoprazole.
9. An oral fixed combination administration form according to claim 1 , wherein each administration form is in pellet form.
10. An oral fixed combination administration form according to claim 1 , wherein each administration form is in tablet form.
11. An oral fixed combination administration form according to claim 1 , wherein the tablet disintegrant is crosslinked polyvinylpyrrolidone.
12. 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.
13. 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.
14. An oral fixed combination administration form according to claim 1 , in combination with or for combined use with an antimicrobial agent.
15. 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.
16. 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.
17. 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.
18. 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.
19. An oral fixed combination administration form according to claim 16 , wherein the small soluble particles are lactose crystals.
20. 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.
21. 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.