Injections
AssigneeTakeda Pharmaceutical Company Limited
InventorsTakayuki Doen, Masao Nagao, Naoki Asakawa, Nobuyuki Takechi
Life of this patent
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Abstract
An injectable composition comprises a benzimidazole compound having an antiulcer action and a strong alkali (e.g., an alkali metal hydroxide such as sodium hydroxide) in a proportion of about 1 equivalent of the latter relative to 1 mol of the former, and is substantially free from a nonaqueous solvent. The injectable composition may comprise N-methylglucamine, and a saccharide (such as mannitol). The injectable composition may be a freeze-dried preparation. The freeze-dried preparation is dissolvable in or dilutive with a distilled water for injection or an infusion solution without a nonaqueous solvent. The injectable composition is useful as an antiulcer agent.
Claims29
An injectable composition, comprising:
- a compound represented by the formula (I):
- wherein a ring A represents
- a benzene ring, or a benzene ring having a substituent selected from the group consisting of
- a halogen atom;
- a cyano group;
- a nitro group;
- an alkyl group;
- or an alkyl group having a substituent selected from the group consisting of a halogen atom;
- a hydroxyl group;
- a C1-6alkoxy group;
- a C1-6alkoxy-carbonyl group;
- and a carbamoyl group;
- a hydroxyl group;
- an alkoxy group;
- or an alkoxy group having a substituent selected from the group consisting of a halogen atom;
- a hydroxyl group;
- a C1-6alkoxy group;
- a C1-6alkoxy-carbonyl group;
- and a carbamoyl group;
- an aryl group;
- an aryloxy group;
- a carboxyl group;
- an acyl group;
- an acyloxy group;
- and
- a 5- to 10-membered heterocyclic ring,
- R1 represents
- a hydrogen atom,
- an aralkyl group, or an aralkyl group having a substituent selected from the group consisting of a halogen atom;
- a hydroxyl group;
- a C1-6alkoxy group;
- a C1-6alkoxy-carbonyl group;
- and a carbamoyl group,
- an acyl group, or
- an acyloxy group,
- R2, R3 and R4 are same or different, each representing
- a hydrogen atom,
- an alkyl group, or an alkyl group having a substituent selected from the group consisting of a halogen atom;
- a hydroxyl group;
- a C1-6alkoxy group;
- a C1-6alkoxy-carbonyl group;
- and a carbamoyl group,
- an alkoxy group, or an alkoxy group having a substituent selected from the group consisting of a halogen atom;
- a hydroxyl group;
- a C1-6alkoxy group;
- a C1-6alkoxy-carbonyl group;
- and a carbamoyl group, or
- an amino group, a mono-C1-6alkylamino group, a mono-C6-14arylamino group, a di-C1-6alkylamino group, or a di-C6-14arylamino group,
- X represents a nitrogen atom, and
- Y represents a nitrogen atom;
- N-methylglucamine;
- and a strong alkali,
- wherein the equivalent ratio of the strong alkali relative to 1 mol of the compound represented by the formula (I) is 0.90 to 1.10
- and wherein said composition is dissolvable in or dilutive with a solvent substantially free from a non-aqueous solvent.
Dependencies are inferred from the claim text.