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Claims for Patent: 8,784,885

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Claims for Patent: 8,784,885

Title:Controlled release preparation
Abstract: A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient.
Inventor(s): Akiyama; Yohko (Osaka, JP), Kurasawa; Takashi (Osaka, JP), Bando; Hiroto (Osaka, JP), Nagahara; Naoki (Osaka, JP)
Assignee: Takeda Pharmaceutical Company Limited (Osaka, JP)
Application Number:12/839,054
Patent Claims: 1. A pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, which is at least one benzimidazole proton pump inhibitor (PPI) or a salt thereof, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, wherein the release-controlled coating layer comprises a pH-dependently soluble polymer, which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, and wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, and wherein the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, and the first component and the second component individually contain a sufficient amount of the active ingredient to raise a plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

2. The pharmaceutical composition according to claim 1, wherein the pH-dependently soluble release-controlled coating layer comprises one polymeric substance or more than one polymeric substances having different release properties selected from the group consisting of hydroxypropylmethyl cellulose phthalate, cellulose acetate phthalate, carboxymethylethyl cellulose, methyl methacrylate-methacrylic acid copolymer, methacrylic acid-ethyl acrylate copolymer, methacrylic acid-methyl acrylate-methyl methacrylate copolymer, hydroxypropyl cellulose acetate succinate, polyvinyl acetate phthalate and shellac.

3. The pharmaceutical composition according to claim 1, wherein the composition is a capsule containing the tablet, the granules, or the fine granules.

4. The pharmaceutical composition according to claim 3, wherein the composition is a capsule containing the granules.

5. The pharmaceutical composition according to claim 1, wherein the composition releases the active ingredient from the first component and the second component so that the plasma level of at least 100 ng/ml in the mammal continues for at least 8 hours.

6. The pharmaceutical composition according to claim 1, wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level in the mammal to at least 300 ng/ml.

7. A pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, the release-controlled coating layer comprises a pH-dependently soluble polymer which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, and wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core article containing the active ingredient in the second component, and wherein the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, the first component and the second component individually contain a sufficient amount of the active ingredient to raise a plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml, and the active ingredient is represented by formula (I'): ##STR00141## wherein ring C' is an optionally substituted benzene ring or an optionally substituted aromatic monocyclic heterocyclic ring, R.sup.0 is a hydrogen atom, an optionally substituted aralkyl group, acyl group or acyloxy group, R.sup.1, R.sup.2 and R.sup.3 are the same or different and are a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkoxy group or an optionally substituted amino group, and Y represents a nitrogen atom or CH; or a salt thereof or an optically active isomer thereof.

8. A pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, which is at least one benzimidazole proton pump inhibitor (PPI) or a salt thereof, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, the release-controlled coating layer comprises a pH-dependently soluble polymer, which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, and wherein the one polymeric substance or more than one polymeric substances having different release properties are selected from the group consisting of hydroxypropylmethyl cellulose phthalate, cellulose acetate phthalate, carboxymethylethyl cellulose, methyl methacrylate-methacrylic acid copolymer, methacrylic acid-ethyl acrylate copolymer, methacrylic acid-methyl acrylate-methyl methacrylate copolymer, hydroxypropyl cellulose acetate succinate, polyvinyl acetate phthalate, and shellac, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, and wherein the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, and the active ingredient contained in the first component and the second component is released in a pulsatile manner, and wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

9. The pharmaceutical composition according to claim 8, wherein the composition is a capsule containing the tablet, the granules, or the fine granules.

10. The pharmaceutical composition according to claim 9, wherein the composition is a capsule containing the granules.

11. The pharmaceutical composition according to claim 8, wherein the composition releases the active ingredient from the first component and the second component so that the plasma level of at least 100 ng/ml in the mammal continues for at least 8 hours.

12. The pharmaceutical composition according to claim 8, wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise a plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 300 ng/ml.

13. A pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, the release-controlled coating layer comprises a pH-dependently soluble polymer, which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, and wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, and wherein the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, the active ingredient contained in the first component and the second component is released in a pulsatile manner, and the active ingredient is represented by formula (I'): ##STR00142## wherein ring C' is an optionally substituted benzene ring or an optionally substituted aromatic monocyclic heterocyclic ring, R.sup.0 is a hydrogen atom, an optionally substituted aralkyl group, acyl group or acyloxy group, R.sup.1, R.sup.2 and R.sup.3 are the same or different and are a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkoxy group or an optionally substituted amino group, and Y represents a nitrogen atom or CH; or a salt thereof or an optically active isomer thereof, and wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

14. A pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, which is at least one benzimidazole proton pump inhibitor (PPI) or a salt thereof, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, the release-controlled coating layer comprises a pH-dependently soluble polymer, which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, and wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, and wherein the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, and the amount of the active ingredient in the first component is at least 50% more than an amount of the active ingredient in the second component, and wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

15. The pharmaceutical composition according to claim 14, wherein an amount of the active ingredient in the first component is at least twice of an amount of the active ingredient in the second component.

16. The pharmaceutical composition according to claim 14, wherein an amount of the active ingredient in the first component is at least three times an amount of the active ingredient in the second component.

17. The pharmaceutical composition according to claim 14, wherein the pH-dependently soluble release-controlled coating layer comprises one polymeric substance or more than one polymeric substances having different release properties selected from the group consisting of hydroxypropylmethyl cellulose phthalate, cellulose acetate phthalate, carboxymethylethyl cellulose, methyl methacrylate-methacrylic acid copolymer, methacrylic acid-ethyl acrylate copolymer, methacrylic acid-methyl acrylate-methyl methacrylate copolymer, hydroxypropyl cellulose acetate succinate, polyvinyl acetate phthalate and shellac.

18. The pharmaceutical composition according to claim 14, wherein the composition is a capsule containing the tablet, the granules, or the fine granules.

19. The pharmaceutical composition according to claim 18, wherein the composition is a capsule containing the granules.

20. The pharmaceutical composition according to claim 14, wherein the composition releases the active ingredient from the first component and the second component so that the plasma level of at least 100 ng/ml in the mammal continues for at least 8 hours.

21. The pharmaceutical composition according to claim 14, wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise a plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 300 ng/ml.

22. A pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, the release-controlled coating layer comprises a pH-dependently soluble polymer, which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, and wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, and wherein the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, the amount of the active ingredient in the first component is at least 50% more than an amount of the active ingredient in the second component, and the active ingredient is represented by formula (I'): ##STR00143## wherein ring C' is an optionally substituted benzene ring or an optionally substituted aromatic monocyclic heterocyclic ring, R.sup.0 is a hydrogen atom, an optionally substituted aralkyl group, acyl group or acyloxy group, R.sup.1, R.sup.2 and R.sup.3 are the same or different and are a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkoxy group or an optionally substituted amino group, and Y represents a nitrogen atom or CH; or a salt thereof or an optically active isomer thereof, and wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

23. A pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, which is at least one benzimidazole proton pump inhibitor (PPI) or a salt thereof, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, the release-controlled coating layer comprises a pH-dependently soluble polymer, which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, and wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, and wherein the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, and the total amount of the active ingredient in the first component and the second component is between 5 mg and 150 mg, and wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

24. The pharmaceutical composition according to claim 23, wherein the total amount of the active ingredient in the first component and the second component is between 30 mg and 90 mg.

25. The pharmaceutical composition according to claim 23, wherein the pH-dependently soluble release-controlled coating layer comprises one polymeric substance or more than one polymeric substances having different release properties selected from the group consisting of hydroxypropylmethyl cellulose phthalate, cellulose acetate phthalate, carboxymethylethyl cellulose, methyl methacrylate-methacrylic acid copolymer, methacrylic acid-ethyl acrylate copolymer, methacrylic acid-methyl acrylate-methyl methacrylate copolymer, hydroxypropyl cellulose acetate succinate, polyvinyl acetate phthalate and shellac.

26. The pharmaceutical composition according to claim 23, wherein the composition is a capsule containing the tablet, the granules, or the fine granules.

27. The pharmaceutical composition according to claim 26, wherein the composition is a capsule containing the granules.

28. The pharmaceutical composition according to claim 23, wherein the composition releases the active ingredient from the first component and the second component so that the plasma level of at least 100 ng/ml in the mammal continues for at least 8 hours.

29. The pharmaceutical composition according to claim 23, wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise a plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 300 ng/ml.

30. A pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, the release-controlled coating layer comprises a pH-dependently soluble polymer, which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, and wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, and wherein the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, the total amount of the active ingredient in the first component and the second component is between 5 mg and 150 mg, and the active ingredient is represented by formula (I'): ##STR00144## wherein ring C' is an optionally substituted benzene ring or an optionally substituted aromatic monocyclic heterocyclic ring, R.sup.0 is a hydrogen atom, an optionally substituted aralkyl group, acyl group or acyloxy group, R.sup.1, R.sup.2 and R.sup.3 are the same or different and are a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkoxy group or an optionally substituted amino group, and Y represents a nitrogen atom or CH; or a salt thereof or an optically active isomer thereof, and wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

31. A method to treat a gastrointestinal disorder in a mammal in need thereof comprising administering to the mammal a pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, which is at least one benzimidazole proton pump inhibitor (PPI) or a salt thereof, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, the release-controlled coating layer comprises a pH-dependently soluble polymer, which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, and wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, and wherein the enteric coating layer comprises one polymeric substance or more than one polymeric substances selected from cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, and the gastrointestinal disorder is caused by at least one selected from the group consisting of ulcer, gastric juice secretion, mucosa damage, and Helicobacter pylori, and wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

32. The method to treat a gastrointestinal disorder according to claim 31, wherein the gastrointestinal disorder is at least one selected from the group consisting of digestive ulcer, Zollinger-Ellison syndrome, gastritis, reflux esophagitis, symptomatic gastroesophageal reflux disease (symptomatic GERD) with no esophagitis, non-ulcer dyspepsia (NUD), gastric cancer, and gastric MALT lymphoma.

33. The method to treat a gastrointestinal disorder according to claim 31, wherein the mammal is human.

34. The method to treat a gastrointestinal disorder according to claim 31, wherein the pH-dependently soluble release-controlled coating layer comprises one polymeric substance or more than one polymeric substances having different release properties selected from the group consisting of hydroxypropylmethyl cellulose phthalate, cellulose acetate phthalate, carboxymethylethyl cellulose, methyl methacrylate-methacrylic acid copolymer, methacrylic acid-ethyl acrylate copolymer, methacrylic acid-methyl acrylate-methyl methacrylate copolymer, hydroxypropyl cellulose acetate succinate, polyvinyl acetate phthalate and shellac.

35. The method to treat a gastrointestinal disorder according to claim 31, wherein the composition is a capsule containing the tablet, the granules, or the fine granules.

36. The method to treat a gastrointestinal disorder according to claim 35, wherein the composition is a capsule containing the granules.

37. The method to treat a gastrointestinal disorder according to claim 31, wherein the composition releases the active ingredient from the first component and the second component of the pharmaceutical composition so that the plasma level of at least 100 ng/ml in the mammal continues for at least 8 hours.

38. The method to treat a gastrointestinal disorder according to claim 31, wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise a plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 300 ng/ml.

39. A method to treat a gastrointestinal disorder in a mammal in need thereof comprising administering to the mammal a pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, the release of the active ingredient in the first component is controlled by a release-controlled coating layer formed on the core particle containing the active ingredient, the release-controlled coating layer comprises a pH-dependently soluble polymer, which comprises one polymeric substance or more than one polymeric substances having different release properties from each other, wherein the elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, and wherein the release-controlled coating layer comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component, the release of the active ingredient in the second component is controlled by an enteric coating layer, wherein the enteric coating layer is formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, and wherein the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, the gastrointestinal disorder is caused by at least one selected from the group consisting of ulcer, gastric juice secretion, mucosa damage, and Helicobacter pylori, and the active ingredient is represented by formula (I'): ##STR00145## wherein ring C' is an optionally substituted benzene ring or an optionally substituted aromatic monocyclic heterocyclic ring, R.sup.0 is a hydrogen atom, an optionally substituted aralkyl group, acyl group or acyloxy group, R.sup.1, R.sup.2 and R.sup.3 are the same or different and are a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkoxy group or an optionally substituted amino group, and Y represents a nitrogen atom or CH; or a salt thereof or an optically active isomer thereof, and wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

40. A pharmaceutical composition containing a tablet, granules, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first component and the second component comprises a core particle containing the active ingredient, which is at least one benzimidazole proton pump inhibitor (PPI) or a salt thereof, the release of the active ingredient in the first component is controlled for delivery at an elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, the first component comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component under the coating layer, a release of the active ingredient in the second component is controlled for delivery, the second component comprises an enteric coating layer formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxyethylcellulose acetate succinate, ethyl acrylate-methyl methacylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, and the first component and the second component individually contain a sufficient amount of the active ingredient to raise a plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml.

41. The pharmaceutical composition according to claim 40, wherein the composition releases the active ingredient from the first component and the second component so that the plasma level of at least 100 ng/ml in the mammal continues for at least 8 hours.

42. The pharmaceutical composition according to claim 40, wherein the first component and the second component individually contain a sufficient amount of the active ingredient to raise the plasma level in the mammal to at least 300 ng/ml.

43. A pharmaceutical composition containing a tablet, granule, or fine granule, in which a release of an active ingredient is controlled, wherein the pharmaceutical composition comprises a first component and a second component, each of which has different release properties of the active ingredient relative to the other component, each of the first and second components comprises a core particle containing the active ingredient, the release of the active ingredient in the first component is controlled for delivery at an elution rate of the active ingredient from the first component is 10% or less for 5 hours in a solution of pH 6.0, and 5% or less for one hour and 60% or more for 8 hours in a solution of pH 6.8, the first component comprises a coating layer, which covers at least about 80% of a surface of the core particle or a layer formed in the first component under the coating layer, the release of the active ingredient in the second component is controlled for delivery, the second component comprises an enteric coating layer formed on an intermediate layer formed on the core particle containing the active ingredient in the second component, the enteric coating layer comprises one or more polymeric substances selected from the group consisting of cellulose acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxymethylcellulose acetate succinate, ethyl acrylate-methyl methacrylate-trimethylammoniumethyl methacrylate chloride copolymer, methyl methacrylate-ethyl acrylate copolymer, carboxymethyl ethylcellulose, methacrylic acid-ethyl acrylate copolymer, and shellac, and the first component and the second component individually contain a sufficient amount of the active ingredient to raise a plasma level of the active ingredient in a mammal to whom the pharmaceutical composition is administered to at least 100 ng/ml, and the active ingredient is represented by formula (I'): ##STR00146## wherein ring C' is an optionally substituted benzene ring or an optionally substituted aromatic monocyclic heterocyclic ring, R.sup.0 is a hydrogen atom, an optionally substituted aralkyl group, acyl group or acyloxy group, R.sup.1, R.sup.2 and R.sup.3 are the same or different and are a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkoxy group or an optionally substituted amino group, and Y represents a nitrogen atom or CH; or a salt thereof or an optically active isomer thereof.
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