Rapidly disintegrable solid preparation

• US 20010010825A1
• Filed: 03/07/2001
• Published: 08/02/2001
• Est. Priority Date: 07/28/1998
• Status: Active Grant

• Current Assignee: Takeda Pharmaceutical Company Limited
• Original Assignee: Takeda Pharmaceutical Company Limited
• Inventors: Shimizu, Toshihiro, Nakano, Yoshinori, Sugaya, Masae
• Granted Patent: US 7,070,805 B2
• Time in Patent Office: Days
• US Class Current: 424/465
• CPC Class Codes: A61K 31/13 Amines A61K31/04 takes precedence
• CPC Class Codes: A61K 31/41 having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
• CPC Class Codes: A61K 31/717 Celluloses
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 13/00 Drugs for disorders of the urinary system
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/12 Antihypertensives

Abstract

A rapidly disintegrable solid preparation which comprises (i) a pharmacologically active ingredient, (ii) a sugar and (iii) a low-substituted hydroxypropylcellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group. The rapidly disintegrable solid preparation has fast disintegrability, suitable strength and no roughness.

Claims

1. A rapidly disintegrable solid preparation which comprises (i) a pharmacologically active ingredient, (ii) a sugar and (iii) a low-substituted hydroxypropylcellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group.

2. A preparation of

claim 1

, which is an orally rapidly disintegrable solid preparation.

3. A preparation of

claim 1

or

2

, which is a tablet.

4. A preparation of

claim 1

, wherein the sugar is a sugar alcohol.

5. A preparation of

claim 4

, wherein the sugar alcohol is mannitol or erythritol.

6. A preparation of

claim 1

, wherein the sugar is in an amount of 5 to 97 parts by weight per 100 parts by weight of the solid preparation.

7. A preparation of

claim 1

, wherein the low-substituted hydroxypropylcellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group is used in an amount of 3 to 50 parts by weight per 100 parts by weight of the solid preparation.

8. A preparation of

claim 1

, wherein the pharmacologically active ingredient is lansoprazole.

9. A preparation of

claim 1

, wherein the pharmacologically active ingredient is voglibose.

10. A preparation of

claim 1

, wherein the pharmacologically active ingredient is manidipine hydrochloride.

11. A preparation of

claim 1

, wherein the pharmacologically active ingredient is pioglitazone hydrochloride.

12. A preparation of

claim 1

, wherein the pharmacologically active ingredient is candesartan cilexetil.

13. A preparation of

claim 3

which comprises fine granules.

14. A preparation of

claim 13

, wherein the pharmacologically active ingredient is comprised in fine granules of the solid preparation.

15. A preparation of

claim 14

, wherein (i) a sugar and (ii) a low-substituted hydroxypropylcellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group are comprised in the solid preparation separately from fine granules.

16. A preparation of

claim 15

, wherein the sugar is in an amount of 5 to 97 parts by weight per 100 parts by weight of the rest of the solid preparation other than the fine granules.

17. A preparation of the

claim 15

, wherein the low-substituted hydroxypropylcellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group is in an amount of 3 to 50 parts by weight per 100 parts by weight of the rest of the solid preparation other than the fine granules.

18. Use of a low-substituted hydroxypropylcellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group for producing a rapidly disintegrable solid preparation comprising a pharmacologically active ingredient and a sugar.

19. A method for improving fast disintegrability of a solid preparation comprising a pharmacologically active ingredient and a sugar which is characterized in that a low-substituted hydroxypropylcellulose having 5% by weight or more to less than 7% by weight of hydroxypropoxyl group is contained therein.