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Claims for Patent: 7,396,841

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Claims for Patent: 7,396,841

Title:Injections
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.
Inventor(s): Doen; Takayuki (Suita, JP), Nagao; Masao (Kashiba, JP), Asakawa; Naoki (Takatsuki, JP), Takechi; Nobuyuki (Osaka, JP)
Assignee: Takeda Pharmaceutical Company Limited (Osaka, JP)
Application Number:10/344,805
Patent Claims: 1. An injectable composition, comprising: a compound represented by the formula (I): ##STR00005## 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 C.sub.1-6alkoxy group; a C.sub.1-6alkoxy-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 C.sub.1-6alkoxy group; a C.sub.1-6alkoxy-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, R.sup.1 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 C.sub.1-6alkoxy group; a C.sub.1-6alkoxy-carbonyl group; and a carbamoyl group, an acyl group, or an acyloxy group, R.sup.2, R.sup.3 and R.sup.4 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 C.sub.1-6alkoxy group; a C.sub.1-6alkoxy-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 C.sub.1-6alkoxy group; a C.sub.1-6alkoxy-carbonyl group; and a carbamoyl group, or an amino group, a mono-C.sub.1-6alkylamino group, a mono-C.sub.6-14arylamino group, a di-C.sub.1-6alkylamino group, or a di-C.sub.6-14arylamino 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.

2. An injectable composition according to claim 1, wherein, in the formula (I), the ring A represents a benzene ring which may have substituent(s) selected from the group consisting of a halogen atom, a C.sub.1-4alkyl group which may be halogenated, a C.sub.1-4alkoxy group which may be halogenated and a 5- or 6-membered heterocyclic group; R.sup.1 represents a hydrogen atom; R.sup.2 represents a C.sub.1-6alkyl group, a C.sub.1-6alkoxy group, a C.sub.1-6alkoxy-C.sub.1-6alkoxy group or a di-C.sub.1-6alkylamino group; R.sup.3 represents a hydrogen atom, a C.sub.1-6alkoxy-C.sub.1-6alkoxy group, or a C.sub.1-6alkoxy group which may be halogenated; R.sup.4 represents a hydrogen atom or a C.sub.1-6alkyl group; and X and Y each represent a nitrogen atom.

3. An injectable composition according to claim 1, wherein the compound represented by the formula (I) is a compound represented by the following formula (Ia): ##STR00006## wherein R.sup.1 represents a hydrogen atom; R.sup.2 represents a C.sub.1-3alkyl group or a C.sub.1-3alkoxy group; R.sup.3 represents a C.sub.1-3alkoxy group which may be halogenated or may be substituted with a C.sub.1-3alkoxy group; R.sup.4 represents a hydrogen atom or a C.sub.1-3alkyl group; and R.sup.5 represents a hydrogen atom, a C.sub.1-3alkoxy group which may be halogenated, or a pyrrolyl group.

4. An injectable composition according to claim 3, wherein, in the formula (Ia), R.sup.1 represents a hydrogen atom; R.sup.2 represents a C.sub.1-3alkyl group; R.sup.3 represents a C.sub.1-3alkoxy group which may be halogenated; R.sup.4 represents a hydrogen atom; and R.sup.5 represents a hydrogen atom or a C.sub.1-3alkoxy group which may be halogenated.

5. An injectable composition according to claim 1, wherein the strong alkali is an alkali metal compound.

6. An injectable composition according to claim 1, wherein the strong alkali is sodium hydroxide.

7. An injectable composition according to claim 1, the solution of which has a pH of 10.4 to 12.0 in the case where the injectable composition is dissolved with the use of a physiological saline, or a distilled water for injection in a proportion of 2.5 ml relative to 15 mg of the compound represented by the formula (I).

8. An injectable composition according to claim 1, the solution of which has an osmotic pressure ratio of about 0.3 to 5 against a physiological saline in the case where the injectable composition is dissolved with the use of the physiological saline in a proportion of 2.5 ml relative to 15 mg of the compound represented by the formula (I).

9. An injectable composition according to claim 1, which is a freeze-dried preparation.

10. An injectable composition according to claim 1, wherein the amount of N-methylglucamine is about 0.1 to 1 mg relative to 1 mg of the compound represented by the formula (I).

11. An injectable composition according to claim 1, which further comprises a saccharide.

12. An injectable composition according to claim 11, wherein the saccharide is a sugar alcohol.

13. An injectable composition according to claim 11, wherein the saccharide is mannitol.

14. An injectable composition according to claim 11, wherein the amount of the saccharide is about 0.1 to 20 mg relative to 1 mg of the compound represented by the formula (I).

15. An injectable composition according to claim 1, which comprises the compound represented by the formula (I) and is dissolvable in or dilutive with a solvent substantially free from a nonaqueous solvent, and which further comprises about 0.1 to 0.8 mg of N-methylglucamine and about 1 to 10 mg of a sugar alcohol relative to 1 mg of the compound represented by the formula (I).

16. An injectable composition according to claim 1, which comprises the compound represented by the formula (I) and is dissolvable in or dilutive with a solvent substantially free from a nonaqueous solvent, and which further comprises about 4 to 6 mg of N-methylglucamine, about 25 to 35 mg of mannitol and about 1.5 to 1.8 mg of a sodium hydroxide relative to 15 mg of the compound represented by the formula (I).

17. An injectable composition according to claim 1, which comprises 30 mg of the compound represented by the formula (I), 3.45 mg of a sodium hydroxide, 10 mg of N-methylglucamine and 60 mg of mannitol.

18. An injectable composition according to claim 1, which comprises 15 mg of the compound represented by the formula (I), 1.73 mg of a sodium hydroxide, 5 mg of N-methylglucamine and 30 mg of mannitol.

19. A freeze-dried preparation which is dissolvable in at least one liquid selected from (i) water for injection and (ii) infusion solutions, comprises a compound represented by the formula (I) defined in claim 1 and an alkali metal hydroxide in a molar ratio of 1:0.90 to 1.10, and further comprises about 0.1 to 0.8 mg of N-methylglucamine and about 1 to 10 mg of a sugar alcohol relative to 1 mg of the compound represented by the formula (I).

20. A process for preparing an injectable composition which comprises dissolving a compound represented by the formula (I) defined in claim 1 in an aqueous solution of a strong alkali, wherein the concentration of the aqueous solution of the strong alkali is about 0.15 to 0.25 equivalent/L, and the amount of the aqueous solution of the strong alkali is about 1 equivalent relative to 1 mol of the compound represented by the formula (I).

21. A process according to claim 20, wherein the aqueous solution of the strong alkali is an aqueous solution of sodium hydroxide.

22. A method for improving relief of pain and local irritation by an injectable composition, which comprises preparing the injectable composition with the use of a compound represented by the formula (I) defined in claim 1 and a strong alkali in a proportion of about 1 equivalent of the latter relative to 1 mol of the former without a nonaqueous solvent.

23. A method for improving solubility of a freeze-dried preparation in at least one liquid selected from (i) water for injection and (ii) infusion solutions, without using a nonaqueous solvent, which comprises preparing the freeze-dried preparation with the use of a compound represented by the formula (I) defined in claim 1 and a strong alkali in a proportion of about 1 equivalent of the latter relative to 1 mol of the former.

24. A method for treating digestive ulcer, treating ulcers due to postoperative stress, or ulcer caused by a non-steroidal anti-inflammatory agent, which comprises administering a therapeutically effective amount of an injectable composition recited in claim 1 to a human being.

25. A method for treating digestive ulcer or reflux esophagitis, which comprises administering a therapeutically effective amount of an injectable composition recited in claim 1 to a human being.

26. An injectable composition according to claim 1, wherein the compound represented by the formula (I) is 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-b- enzimidazole.

27. A freeze-dried preparation according to claim 19, wherein the compound represented by the formula (I) is 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-b- enzimidazole.

28. A process according to claim 20, wherein the compound represented by the formula (I) is 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-b- enzimidazole.

29. A method according to claim 23, wherein the compound represented by the formula (I) is 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-b- enzimidazole.
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