Intrabuccally rapidly disintegrating tablet and a production method of the tablets

• US 8,071,128 B2
• Filed: 06/20/2003
• Issued: 12/06/2011
• Est. Priority Date: 06/14/1996
• Status: Expired due to Fees

• Current Assignee: Kyowa Hakko Kirin Company Limited (Kirin Holdings Company Limited)
• Original Assignee: Kyowa Hakko Kirin Company Limited (Kirin Holdings Company Limited)
• Inventors: Ohta, Motohiro, Hayakawa, Eiji, Ito, Kunio, Tokuno, Sanji, Morimoto, Kiyoshi, Watanabe, Yasushi
• Primary Examiner(s): Tran, Susan
• Assistant Examiner(s): Ahmed, Hasan
• Application Number:
  US10/356,641
• Publication Number:
  US 20030215500A1
• Time in Patent Office: 3,091 Days
• Field of Search: None
• US Class Current: 424/464
• CPC Class Codes: A61J 3/10 into the form of compressed tablets tablet presses B30B11/00
• 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 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00

Abstract

An intrabuccally rapidly disintegrating tablet which is manufactured by a simple method, has an enough practical hardness and is rapidly disintegrated in the buccal cavity and its production method. The intrabuccally rapidly disintegrating tablet is produced by growing a powder material into a granulated material with a fixed particle diameter, the powder material including a sugar alcohol or a saccharide as main ingredient, each of which is first particle having an average particle diameter of not more than 30 μm, by mixing thus obtained granulated material with an active ingredient and a disintegrant, and by compressing the mixture into a predetermined shape.

Claims

1. A method of producing an intrabuccally rapidly disintegrating tablet, said intrabuccally rapidly disintegrating tablet comprising:

a sugar alcohol or saccharide in the form of primary particles having an average particle size of not more than 30 μ

m;

an active ingredient; and

one or more disintegrants selected from the group consisting of crospovidone, croscarmellose sodium, low substituted hydroxypropylcellulose, and a mixture thereof,

said method comprising the steps of;

(a) granulating a powder material comprising the sugar alcohol or saccharide and said one or more disintegrants, thereby producing granulated material having a predetermined size;

(b) mixing said granulated material and said active ingredient; and

(c) compressing the mixture into an intrabuccally rapidly disintegrating tablet.

2. The method of claim 1, wherein the tablet disintegrates within 30 seconds, determined by measuring the time required for the tablet to fall through no. 10 wire mesh when water is added dropwise to the tablet at a rate of 4 mL/min.

3. The method of claim 1, wherein the amount of active ingredient ranges from 0.01-30% by weight of the intrabuccally rapidly dispersing tablet.

4. The method of claim 1, wherein the sugar alcohol or saccharide is pulverized in advance to an average particle size of not more than 30 μ

m.

5. The method of claim 1, wherein the sugar alcohol or saccharide is selected from the group consisting of mannitol, lactose, and mixtures thereof.

6. The method of any one of claims 1-5, wherein said method further comprises mixing the granulated material with a lubricant before said compressing step.

7. The method of any one of claims 1-5, further comprising spraying a lubricant on material contacting surfaces of punches and dies of a tabletting machine before said compressing step.

8. The method of claim 1, wherein said granulating step (a) comprises granulating said sugar alcohol or saccharide, said active ingredient, and said one or more disintegrants to produce a granulated material.

9. The method of claim 1, wherein said intrabuccally rapidly disintegrating tablet comprises about 60-95% by weight of said sugar alcohol or saccharide and about 1-10% by weight of said disintegrant.

10. An intrabuccally rapidly disintegrating tablet, made by the process of any one of claims 1-5.

11. An intrabuccally rapidly disintegrating tablet, made by the process of claim 6.

12. An intrabuccally rapidly disintegrating tablet, made by the process of claim 7.

13. The method of claim 1, further comprising:

(a1) drying the granulated material of step (a);

(a2) mixing the dried granulated material of step (a1) with said active ingredient;

(a3) spraying a lubricant on material contacting surfaces of punches and dies of a tabletting machine before said compressing step (c); and

wherein said compressing of step (c) comprises compressing the mixture of step (a2).

14. The method of claim 13, wherein said granulating of step (a) is wet granulating.

15. The method of claim 1, further comprising:

(a1) drying the granulated material of step (a);

(a2) blending the dried granulated material of step (a1) with one or more additional additives and/or lubricants; and

wherein said granulating of step (a) is wet granulating, and said compressing of step (b) is compressing the blend of step (a2).