Drug – bio-affecting and body treating compositions – Designated organic nonactive ingredient containing other... – Solid synthetic organic polymer
Reexamination Certificate
2000-04-28
2003-06-10
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Designated organic nonactive ingredient containing other...
Solid synthetic organic polymer
C514S974000, C514S963000, C424S441000, C424S480000, C424S495000, C424S489000
Reexamination Certificate
active
06576677
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to a composition or a method for reducing an unpleasant taste of a basic medicament having the unpleasant taste. In addition, the present invention relates to a composition alleviated in the defect of a composition containing a basic medicament, or a method for alleviating the defect.
PRIOR ART
Since oral administration of a medicament having an unpleasant taste such as bitter taste or numbness puts a burden on a patient and lowers compliance, various devices have been made to improve the taste of the medicament. When the medicament is solid such as tablets or granules, a bitter taste or the like can be masked in a relatively easy manner, for example, by coating or incorporation of the medicament in the matrix. For liquids, it is the common practice to conceal a taste of the medicament under a sweet taste substance such as sucrose, which is however only a camouflage. A technique for essentially masking a bitter taste or the like is hardly known. Polyvinylpyrrolidone is known as a binder used for the preparation of tablets or the like. In JP-A 3-287535 and JP-A 4-18015, it is disclosed that a clear and stable aqueous solution is available by the addition of polyvinylpyrrolidone to a medicament sparingly soluble in water.
An object of the present invention is to alleviate an unpleasant taste of an oral medicament and moreover, to suppress the formation of a precipitate or decomposition product.
DISCLOSURE OF THE INVENTION
The present invention is directed to a composition comprising a basic medicament having an unpleasant taste and polyvinylpyrrolidone and/or copolyvidone. In addition, it is also directed to a method for alleviating an unpleasant taste of a basic medicament having the unpleasant taste by adding polyvinylpyrrolidone and/or copolyvidone thereto.
In a further aspect of the present invention, there is also provided a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvidone, and (3) propylene glycol and/or D-sorbitol.
In a still further aspect of the present invention, there is also provided a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvidone, and (4) an antioxidant.
In a still further aspect of the present invention, there is also provided a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvidone, and (5) a colorant or flavor containing a sulfuric acid or sulfurous acid group.
The present invention makes it possible to reduce an unpleasant taste of a basic medicament having the unpleasant taste and this is the first object of the present invention.
Addition of polyvinylpyrrolidone and/or copolyvidone increases analogues to the basic medicament with the passage of time. The second object of the present invention is to suppress this increase of analogues.
Addition of a colorant or flavor having a sulfuric acid or sulfurous acid group happens to form an insoluble precipitate of the basic medicament. To suppress the formation of this precipitate is also an object of the present invention.
The basic medicament having an unpleasant taste in the present invention means a medicament in which a proton exists as a positive charge under acidic conditions and which has an unpleasant taste. Examples include ticlopidine hydrochloride, azelastine hydrochloride, etilefrine hydrochloride, diltiazem hydrochloride, propranolol hydrochloride, indeloxazine hydrochloride, aminoguanidine hydrochloride and donepezil hydrochloride. Among these, effects are particularly remarkable when donepezil hydrochloride is used. Donepezil hydrochloride is chemically named (1-benzyl-4-(5,6-dimethoxyindanon-2-yl)methylpiperidine hydrochloride, and it is a remedy for Alzheimer's disease of a slight to a medium degree. The aqueous solution thereof has a sharp bitterness and numbness.
In the present invention, polyvinylpyrrolidone and/or the like reduces an unpleasant taste. Described specifically, a basic medicament having an unpleasant taste, which the medicament has been positively charged by a proton bound thereto in a solution, is trapped by two pyrrolidone groups, whereby contact of the basic medicament with a taste bud is sterically hindered.
In the present invention, polyvinylpyrrolidone is a linear polymer of 1-vinyl-2-pyrrolidone and that having an average molecular weight ranging from several thousand to several million can be used, with that having an average molecular weight of about 10000 to 2000000 is preferable.
In the Japanese Pharmacopoeia, polyvinylpyrrolidones having an average molecular weight of 25000, 40000 and 1200000 are described as polyvinylpyrrolidone K25, polyvinylpyrrolidone K30 and polyvinylpyrrolidone K90, respectively. They are easily available as Kollidon, the trade name. In the codices of Japan, USA and England, it is officially described as povidone, while in the codex of Europe, it is officially described as polyvidone. Both are embraced in the present invention.
In the present invention, copolyvidone is a (6:4) copolymer of a chain-structured vinyl pyrrolidone and vinyl acetate and for example, it is officially described in the codex of Europe as copolyvidone. In the present invention, polyvinylpyrrolidone and copolyvidone may be used either singly or in combination.
In the present invention, a ratio of a basic medicament having an unpleasant taste to polyvinylpyrrolidone and/or copolyvidone differs depending on the molecular weight or the like and cannot be determined in the wholesale manner. Polyvinylpyrrolidone having an average molecular weight of 40000 is usually added in an amount of 5 to 200 parts by weight, preferably 20 to 200 parts by weight or 100 to 200 parts by weight, more preferably 140 to 200 parts by weight, each based on 1 part by weight of the basic medicament such as donepezil hydrochloride. It is added in an amount of 5 to 100 parts by weight for the solubilization of an insoluble substance, and 50 to 200 parts by weight for masking of a bitter taste. The larger the molecular weight of polyvinylpyrrolidone, the less the amount of it to be added, while the smaller, the more the amount to be added.
Specific examples of the formulated preparation usable in the present invention include water-soluble liquids, syrups, elixirs, jellies, dry syrups, effervescent preparations, lemonades, aerosols, ophthalmic solutions, nasal drops, suppositories, cataplasmas, liniments, lotions and fine granules. Among these, syrups and jellies are particularly preferable. Syrups are each available by adding a sweetener such as sucrose, glucose, mannitol, xylitol, aspartame, saccharin or sorbitol and optionally a taste and smell corrigent. Jellies are usually available by adding, to the composition of the present invention, a gum and then a sweetener such as sucrose, glucose, mannitol, xylitol, aspartame, saccharin or sorbitol and optionally a taste and smell corrigent. The pH of the preparation is usually in the range of from 3 to 7.
The composition of the present invention in the form of an aqueous solution can be produced by weighing necessary amounts of a medicament and polyvinylpyrrolidone and/or copolyvidone, adding a sweetener, flavor or the like as needed and then dissolving the resulting mixture in water. When the medicament is donepezil hydrochloride, the dose is usually 1 to 20 mg/once.
The present invention provides a composition containing a basic medicament. The basic medicament includes the above-mentioned basic medicament having an unpleasant taste and the other basic medicaments. Examples thereof include acebutolol hydrochloride, aprindine hydrochloride, alprenolol hydrochloride, ambroxol hydrochloride, isoprenaline hydrochloride, imipramine hydrochloride, diphenidol hydrochloride, diltiazem hydrochloride, thiamine hydrochloride, trazodone hydrochloride, bunazosin hydrochloride, bunitrolol hydrochloride, ranitidine hydrochloride and midodrine hydrochloride.
In addition, the present invention provides a composition comprising (1) a basic medicament, (2) polyvinylpyrrolidone and/or copolyvi
Harada Tsutomu
Ukai Koji
Eisai Co. Ltd.
Fubara Blessing
Page Thurman K.
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