Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
1998-10-14
2001-02-13
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S465000, C424S488000, C424S499000
Reexamination Certificate
active
06187336
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a rapidly soluble solid in the oral cavity, particularly, a rapidly soluble preparation in the oral cavity. Also, the present invention relates to a process for producing the same.
2. Background Art
Recently, a novel dose form has been sought for patients having difficulty in swallowing, such as the aged, infants and the like. For example, disintegrating preparations in the oral cavity, jellies, and pastes have been suggested. Particularly, disintegrating preparations in the oral cavity, which can easily be taken without water in any place at any time, would be suitable for the aged, infants and the like.
Generally, disintegration properties and hardness of tablets conflicts with each other. To increase the rate of disintegration for improving disintegration properties leads to decreased tablet hardness. However, it is important for tablets to have a certain degree of hardness while the tablets are transported and packaged in factories or distributed through the market or when a patient takes the tablet out of the package. A tablet having insufficient hardness fails to retain its shape and can crumble in these situations.
Under these circumstances, various techniques for producing rapidly soluble preparations in the oral cavity have been proposed.
For example, JP-B-58-24419 (the term “JP-B” as used herein means an “examined Japanese patent publication”) discloses a process for producing easily disintegrating porous tablets which comprises mixing a pharmaceutical composition with a solvent capable of freezing and inert to the composition, solidifying the solvent in an inert cooling medium, compressing the mixture into tablets at a temperature lower than the freezing point of the solvent, and evaporating the solvent by freeze-drying or spontaneous drying.
Commercially available rapidly soluble preparations in the oral cavity include Zydis (commercial name) produced by R. P Scherer (England), which is produced by dissolving an active ingredient, a polymer, a saccharide, and the like, followed by freeze-drying.
Additionally, JP-A-5-271054 (the term “JP-A” as used herein means an “unexamined published Japanese patent application”) discloses a tablet soluble in the oral cavity and its preparation; JP-A-8-291051 discloses a method for producing rapidly soluble tablet and a rapidly soluble tablet produced by the method; JP-A-8-333243 discloses a tablet having excellent touch in the oral cavity; and JP-A-9-48726 discloses a rapidly disintegrating preparation in the oral cavity and its production.
The techniques disclosed in the above references have their several disadvantages such that the rate of disintegration is insufficient; the tablets, while capable of disintegrating rapidly, fail to have sufficient mechanical strength; or the finished tablets are difficult to handle ordinarily due to high hygroscopicity.
In molding a pharmaceutical composition into solid preparations, such as tablets and the like, a rotary tablet machine is used usually. When a pharmaceutical composition in semi-solid or wet conditions is molded into tablets by using this type of tablet machine, such problems often occur as poor fluidity of the composition to be supplied and adhesion of the composition to a pressing member.
Water-soluble binders (e.g., polyvinylpyrrolidone, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, polyvinyl alcohol, methyl cellulose, gelatin, and the like) are used to increase hardness of tablets. Disintegrants, such as hydroxypropyl cellulose having a low degree of substitution, corn starch, alginic acid, and the like, are used to increase the rate of disintegration. When used in increased amounts; however, the water-soluble binders or disintegrants become sticky as the tablet crumbles in the oral cavity or make the tablet unpleasant to palate.
SUMMARY OF THE INVENTION
To solve the above-described problems of the conventional techniques, the inventors of the present invention have conducted extensive investigations and found, as a result, that preparations obtained by kneading a mixture of erythritol and a drug or the like, together with an appropriate amount of water, molding the mixture into a tablet-like form by means of a single-shot tablet machine, a molding machine or an extrusion molding machine (e.g., extruder), followed by drying in a vacuum drier have sufficient hardness for handling and yet are capable of melting or disintegrating in the oral cavity in an extremely short time (about 10 seconds).
The present invention provides a rapidly soluble solid in the oral cavity comprising erythritol, which has a porous structure or a structure of a porous inside and a dense and hard surface (the solid preferably having a surface hardness of about 3 kg or higher) and is capable of melting or disintegrating in the oral cavity in a short time.
The present invention also provides a process for producing the above-described rapidly soluble solid in the oral cavity comprising erythritol, which comprises the steps of:
preparing a composition comprising erythritol and appropriate moisture,
kneading the composition,
molding the kneaded composition, and
drying the molded composition under reduced pressure.
DETAILED DESCRIPTION OF THE INVENTION
In the present invention, the term “rapidly soluble solid in the oral cavity” means that the time for the solid in the oral cavity of healthy men to completely dissolve or crumble with saliva is about 20 seconds or less, preferable 10 seconds or less, or that the disintegration time of the solid measured with a disintegration tester specified in The Pharmacopoeia of Japan (testing liquid: water at 37° C.) is about 30 seconds or less, preferably 10 seconds or less.
The rapidly soluble solid in the oral cavity according to the present invention is usually intended to be a rapidly soluble preparation in the oral cavity comprising erythritol and a drug, preferably a rapidly soluble tablet in the oral cavity. In addition to the medical use, the rapidly soluble solid in the oral cavity can be made use of as a food. For example, the rapidly soluble solid in the oral cavity can be solid sweeteners, tablet candies, and the like in which erythritol is combined with other sweeteners, flavors, coloring agents, vitamins, acidulants, and the like.
The drug which can be used in the rapidly soluble solid in the oral cavity preparations is not particularly limited so long as it is not affected by erythritol and can be administered orally. Examples of the drugs that especially enjoy the effects of the present invention are drugs for senile dementia, antipyretic, analgesic and anti-inflammatory agents, antitussives, vitamins, psychotropic agents, antivertigo products, hypnotic sedatives, gastrointestinal drugs, antiarrhythmics, hypotensives, and the like.
If the drug is extremely bitter or stinging, it is preferred to mask the particles of the drug with an insoluble or enteric polymer.
The pharmaceutical composition comprising the active ingredient and erythritol can further contain pharmaceutically acceptable additives commonly used in the art, such as sucrose, lactose, xylitol, D-mannitol, maltitol, lactitol, starch, hydroxypropyl cellulose having a low degree of substitution, magnesium stearate, calcium stearate, talc, light silicic acid anhydride, silicon dioxide hydrate, various surfactants, flavors, coloring agents, sweeteners, acidulants, and the like.
The pharmaceutically acceptable additives can be used either individually or as a mixture thereof in arbitrary amounts so long as the disintegrating properties and molding properties are not impaired.
Where the rapidly soluble solid in the oral cavity according to the present invention is a food, such as solid sweeteners, tablet-like candies, and the like, the composition comprises erythritol as a main component and, if desired, other foods or food additives. Examples of useful foods or food additives include high sweetness sweeteners (for example, aspartame, Stevia sweeteners (e.g., stevioside, rebaudioside, enzyme-treated s
Miyazaki Katsuaki
Motegi Sachio
Okumura Mutsuo
Ukigaya Tadashi
Ghali Isis
Nikken Chemicals Co., Ltd.
Page Thurman K.
Sughrue Mion Zinn Macpeak & Seas, PLLC
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