Solid pharmaceutical preparation with improved buccal disintegrability and/or dissolubility

• US 5,958,453 A
• Filed: 10/29/1997
• Issued: 09/28/1999
• Est. Priority Date: 10/31/1996
• Status: Expired due to Term

• Current Assignee: Takeda Pharmaceutical Company Limited
• Original Assignee: Takeda Chemical Industries, Ltd. (Takeda Pharmaceutical Company Limited)
• Inventors: Ohno, Yasuo, Kikuta, Junichi, Makino, Tadashi
• Primary Examiner(s): Webman, Edward J.
• Application Number:
  US08/960,353
• Time in Patent Office: 699 Days
• Field of Search: 424/434, 424/464, 424/465, 424/486, 424/488, 514/960-61, 514/772.5, 514/781
• US Class Current: 424/465
• 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 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

A solid pharmaceutical preparation comprising a pharmaceutically active ingredient, erythritol, crystalline cellulose and an disintegrants, which exhibits a fast buccal disintegratability and dissolubility.

Claims

1. A solid pharmaceutical preparation comprising (i) a pharmaceutically active substance, (ii) erythritol, (iii) crystaline cellulose and (iv) crospovidone.

2. A solid pharmaceutical preparation capable of buccal disintegration or dissolution comprising the solid pharmaceutical preparation of claim 1.

3. A solid pharmaceytical preparation as claimed in claim 1, which further comprises mannitol.

4. A solid pharmaceutical preparation as claimed in claim 1, wherein erythritol is contained in a proportion of 5-90 parts by weight, based on 100 parts by weight of the solid pharmaceutical preparation.

5. A solid pharmaceutical preparation as claimed in claim 1, wherein the crystalline cellulose is contained in a proportion of 3-50 parts by weight, based on 100 parts by weight of the solid pharmaceutical preparation.

6. A solid pharmaceutical preparation as claimed in claim 1, wherein crospovidone is contained in a proportion of 1-10 parts by weight, based on the solid pharmaceutical preparation.

7. A solid pharmaceutical preparation as claimed in claim 1, wherein the ingredients, (i) a pharmaceutically active ingredient, (ii) erythritol, (iii) crystalline cellulose and (iv) crospovidone, are uniformly mixed.

8. A tablet comprising the solid pharmaceutical preparation as claimed in claim 1.

10. A solid pharmaceutical preparation as claimed in claim 1, wherein the pharmaceutically active ingredient is an antidinics or a drug for kinetosis or motion sickness.

15. A solid pharmaceutical preparation as claimed in claim 1, wherein the pharmaceutically active substance is acetaminophen.

16. A solid pharmaceutical preparation as claimed in claim 1, which is a fast disintegrating tablet.

9. A solid pharmaceutical preparation capable of buccal disintegration or dissolution, which comprises 0.3-50 parts by weight of (i) pharmaceutically active ingredient, 50-80 parts by weight of (ii) erythritol, and 5-20 parts by weight of (iii) crystalline cellulose and 3-7 parts by weight of (iv) crospovidone.

17. A solid pharmaceutical preparation as claimed in claim 9, wherein the pharmaceutically active substance is acetaminophen.

11. A method of improving buccal disintegration or dissolution of a solid pharmaceutical preparation containing (i) a pharmaceutically active ingredient, which comprises incorporating (ii) erythritol, (iii) crystalline cellulose and (iv) crospovidone into the solid pharmaceutical preparation.

12. A method of making a solid pharmaceutical preparation, which comprises:

blending a mixture of (i) a pharmaceutically active ingredient, (ii) erythritol, (iii) crystalline cellulose and (iv) crospovidone, and producing the solid pharmaceutical preparation from the mixture.

13. The method according to claim 12, wherein the solid preparation dissolves completely in solely buccal saliva within 1 minute of administration to a patient.

18. The method of making a solid pharmaceutical preparation as claimed in claim 12, wherein the pharmaceutically active substance is acetaminophen.

14. A method of inhibiting or treating a disease of a subject in need thereof, which comprises administering to the subject an effective amount of (i) a pharmaceutically active ingredient for the disease as a solid pharmaceutical preparation containing (ii) erythritol, (iii) crystalline cellulose and (iv) crospovidone in addition to the pharmaceutically active ingredient (i), with an improved buccal disintegrability and/or dissolubility.