United States Patent:  5,958,453

Assignee:  Takeda Chemical Industries, Ltd. (Osaka, JP)

Filed:  October 29, 1997

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

SUMMARY OF THE INVENTION

As a result of intensive studies and researches, the present inventors found that the preparations comprising the particular three ingredients, erythritol, crystalline cellulose and a disintegrant, in addition to a pharmaceutically active or medicinal ingredient, have characteristics of fast disintegrating and/or dissolving in the oral cavity, followed by further studies, which was led to completion of the present invention.

That is, this invention relates to (1) a solid pharmaceutical preparation comprising (i) a pharmaceutically active ingredient, (ii) erythritol, (iii) crystalline cellulose and (iv) a disintegrant; (2) the solid pharmaceutical preparation in (1), which is capable of buccal disintegration or dissolution; (3) the solid pharmaceutical preparation in (1), which further comprises mannitol; (4) the solid pharmaceutical preparation in (1), wherein the disintegrant is crospovidone; (5) the solid pharmaceutical preparation in (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; (6) the solid pharmaceutical preparation in (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; (7) the solid pharmaceutical preparation in (1), wherein the disintegrant is contained in a proportion of 1-10 parts by weight, based on the solid pharmaceutical preparation; (8) the solid pharmaceutical preparation in (1), wherein the ingredients, (i) a pharmaceutically active ingredient, (ii) erythritol, (iii) crystalline cellulose and (iv) a disintegrant, are uniformly mixed, preferably throughout the preparation; (9) the solid pharmaceutical preparation in (1), which is a tablet; (10) a solid pharmaceutical preparation capable of buccal disintegration or dissolution, which comprises 0.3-50 parts by weight of (i) a 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) a disintegrant; (11) the solid pharmaceutical preparation in (1), wherein the pharmaceutically active ingredient is an antidinics or a drug for kinetosis or motion sickness; (12) 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) a disintegrant in combination in the solid pharmaceutical preparation; (13) 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) a disintegrant, and producing the solid pharmaceutical preparation from the mixture; (14) the method according to (13), wherein the solid preparation dissolves completely in solely buccal saliva within 1 minute of administration to a patient; and (15) 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) a disintegrant in addition to the pharmaceutically active ingredient (i), with improved buccal disintegrability and/or dissolubility.

Claim 1 of 18 Claims

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

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