Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Patent
1997-10-31
1999-10-26
Webman, Edward J.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
424486, 424487, 424501, 514974, A61K 910, A61K 916, A61K 4726, A61K 4732
Patent
active
059723734
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a pharmaceutical composition of an unpleasantly tasting drug, and more particularly, it relates to a composition for oral administration which is excellent in masking a taste of an unpleasantly tasting drug and has a good bioavailability.
BACKGROUND ART
There have been hitherto found various preparations for masking tastes of unpleasantly tasting drugs.
For example, Japanese Patent Kokai 49-81526 discloses a method which comprises dissolving a macrolide antibiotic in an inert volatile organic solvent wherein a wall polymer selected from the group consisting of polyvinylacetal diethylaminoacetate (hereinafter referred to as "AEA"), cellulose acetate dibutylaminohydroxypropyl ether, aminoalkylmethacrylate copolymer E (trade name; Eudragit E) and ethyl cellulose and at least one selected from the group consisting of a wax, a higher fatty acid and a salt insoluble in the higher fatty acid are dissolved or dispersed; spray-drying the solution; and collecting the resulting encapsulated particles of the macrolide antibiotic.
On the other hand, EP Patent No. 37740 discloses a pharmaceutical preparation having an improved stability and content uniformity of drugs, and this preparation can be applied to mask an unpleasant taste, but has a drawback of a bad dissolution because waxes only are used for masking.
As an example of a pharmaceutical mixture for masking a taste of an unpleasantly tasting basic drug, EP Patent No. 69097 discloses that a dry powder for a pharmaceutical mixture comprising an encapsulated bad tasting drug in a form insoluble at high pH.
In addition, EP Patent No. 101418 discloses a pharmaceutical mixture preparation with controlled release of an active substance which includes masking of bad taste and stability increasing of the active substance characterized in that it contains an encapsulated active substance in combination with 40-99% of a release controlling substance, examples of which are a carbohydrate, a carbohydrate-related compound and a mixture of such compounds.
In the past, however, since an inert volatile organic solvent (e.g. methylene chloride, chloroform, cyclohexane, carbon tetrachloride, methylethylketone, acetone, methyl alcohol or isopropyl alcohol) should be used for dissolving coating agents, a drying step for removal of the solvent is required. As a result, the coating layer becomes porous, and the drying step requires a lot of time, equipment, labor, cost, etc. In addition, this step has risks such as inflammation and explosion in work, and the product might contain the residual inert volatile organic solvent which is feared to affect human health, therefore, it has a problem for safety.
In order to mask a taste of an unpleasantly tasting basic drug without using the inert volatile organic solvent, the present inventors disclose in EP. Patent No. 630233 a composition for oral administration comprising a complex formed by dispersing or dissolving the drug and a high polymer soluble in the stomach in a substance having a low melting point of 40 to 120.degree. C., a sugar-alcohol and a basic oxide.
DISCLOSURE OF THE INVENTION
The present inventors researched variously in order to obtain compositions for oral administration for masking a taste of an unpleasantly tasting drug with a good bioavailability. Monoglycerides having a low melting point are superior for making elaborate film, and are easily soluble in the intestines, therefore, they are good materials for formulating.
High polymers soluble in the stomach are useful as materials which are insoluble or hardly soluble in the mouth (pH 5-8), being easily soluble in the stomach (pH 1-4).
Monoglycerides are found to exist in some crystal forms which have different melting points each other, and usually the monoglyceride in the composition for oral administration is in the .alpha.-crystal form immediately after the preparation. The present inventors have found that when a monoglyceride exists in the .alpha.-crystal form, the unpleasant tastes of drugs can not be suffic
REFERENCES:
patent: 3034897 (1962-05-01), Kuhrt et al.
patent: 3034898 (1962-05-01), Kuhrt et al.
patent: 3673106 (1972-06-01), Jones et al.
patent: 4315041 (1982-02-01), Fukuda et al.
patent: 4327077 (1982-04-01), Puglia et al.
patent: 5707646 (1998-01-01), Yajima et al.
Ishii Kuniaki
Itai Shigeru
Nemoto Masami
Suetake Kouji
Tsukui Nobuyoshi
Taisho Pharmaceutical Co. Ltd.
Webman Edward J.
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