Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
1999-07-12
2001-06-19
Azpuru, Carlos A. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C514S772500, C514S781000, C514S960000
Reexamination Certificate
active
06248357
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a solid pharmaceutical preparation, especially a buccal dissolution type solid preparation having characteristics of fast disintegration or dissolution in the oral cavity even without water.
2. Description of Related Art
Generally, solid pharmaceutical preparations such as tablets are designed so that after they are orally administered, they disintegrate or dissolve in the digestive organs and the pharmaceutically active ingredients are absorbed. Accordingly, fast disintegration or dissolution in the oral cavity is not a common design feature.
However, in accordance with the increase in the aged population and change in life styles, there has been a need for development of buccal dissolution type solid preparations which can be, if necessary, administered readily even without water, by aged people and children anywhere or anytime, maintaining the convenience typically afforded by pharmaceutical tablets.
As the technique for producing preparations which quickly disintegrate or dissolve in the oral cavity, heretofore, there has been proposed a method for producing preparations by dissolving or suspending pharmaceutical or medicinal ingredients in an aqueous solvent, filling the resultant solution or suspension into a pocket molded beforehand in a blisterpack and reducing water content from the solution by freeze-drying or vacuum drying [USP 4371516(Examined Japanese Patent Application Publication (Kokoku) No. 62(1987)-50445), (W/O 93/12769)(Publication of Translations of International Patent Application. No. 5-812769)]. This method, however, has problems in that it takes time for manufacturing and in that the obtained products have insufficient strength and thus are difficult to handle. There is known another method in which a mixture of a pharmaceutically active ingredient with a low moldability saccharide is granulated with a high moldability saccharide added thereto [EPA 745382, (Publication of Translations of International Patent Application No. 7-820380 (WO 95/20380))]. The product obtained by this method has such hardness that the dosage form remains without being disintegrated in the course of distribution, while the method has a problem that tabletting is not easy, as is often the case with high moldability saccharides, because tabletting is carried out with lower pressure. Also the products have an additional defect that they leave a problem to be solved in terms of buccal fast disintegration and dissolution. On the other hand, have been made of buccal dissolution preparations produced by wetting molding. But, in general, tablets having fast disintegration or dissolution have defects of lack in strength.
From the foregoing view-point, there is a need or demand for development of preparations which exhibit excellent buccal disintegration and dissolution and also an appropriate strength such that the preparations never disintegrate or suffer damage in the course of the production steps or distribution stages. Japanese Patent Applications Laid-open Nos. 1-268627, 1-268628 and 8-27033 describe a pharmaceutical preparation or composition containing erythritol, but fail to describe intrabuccal dissolution type preparations.
This invention provides solid pharmaceutical preparations which can be readily administered even without water, especially solid pharmaceutical preparations which quickly disintegrate and dissolve in the oral cavity.
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.
DETAILED DESCRIPTION OF THE INVENTION
The pharmaceutically active or medicinal ingredient to be used in the present invention may be in any optional form, for example, a solid, powder or granular, crystalline, oily or solution form.
There is no limitation to the pharmaceutically active ingredients to be used. As the pharmaceutically active ingredient, for example, there may be mentioned one or more members selected from the group consisting of nourishing and health-promoting agents, antipyretic-analgesic-antiinflammatory agents, antipsychotic drugs, antianxiety drugs, antidepressants, hypnotic-sedatives, spasmolytics, gastrointestinal function conditioning agents, antacids, antitussive-expectorants, dental buccal drugs, antihistamines, cardiotonics, antiarrhythmic drugs, diuretics, antihypertensive drugs, vasoconstrictors, coronary vasodilators, peripheral vasodilators, cholagogues, antibiotics, chemotherapeutic drugs, antidiabetic agents, drugs for osteoporosis, skeletal muscle relaxants, antidinics or drug for kinetosis or motion sickness and the like.
Examples of the nourishing and health-promoting agents include
Kikuta Junichi
Makino Tadashi
Ohno Yasuo
Azpuru Carlos A.
Takeda Chemical Industries Ltd.
Wenderoth , Lind & Ponack, L.L.P.
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