Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Patent
1994-09-09
1998-01-13
Webman, Edward J.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
424458, 424461, 424462, 424486, 424487, 424494, 424495, 424497, 424501, 424502, 424470, 424688, 424691, 424692, 514974, A61K 910, A61K 4732, A61K 4702, A61K 4744
Patent
active
057076464
DESCRIPTION:
BRIEF SUMMARY
This is a national stage application under 35 U.S. 371 of Ser. No. PCT/JP93/00291, filed Mar. 10, 1993 published as WO93/17667 Sep. 16, 1993.
TECHNICAL FIELD
The present invention relates to a composition for preparations of basic drugs which taste unpleasant. More specifically, it relates to a composition for oral preparations, which is excellent in masking unpleasantly tasting basic drugs and has excellent performance in biological use.
BACKGROUND ART
There have been hitherto found a variety of methods for masking the tastes of unpleasantly tasting drugs. For example, JP-A-49-81526 discloses a method in which a macrolide is dissolved in an inert volatile organic solvent in which a coating polymer selected from the group consisting of polyvinylacetal diethylaminoacetate (hereinafter abbreviated as AEA), cellulose acetate dibutylaminohydroxypropyl ether, Eudragit.RTM. E and ethyl cellulose and at least one member selected from the group consisting of wax, higher fatty acid and salt insoluble in higher fatty acid have been dissolved or dispersed, the resultant solution is spray-dried to form coated macrolide particles, and the coated macrolides particles are recovered.
Further, as a pharmaceutical mixture for masking the taste of unpleasantly tasting basic drugs, for example, U.S. Pat. No. 4,656,027 discloses a dry powder for use as a pharmaceutical preparation, which dry powder is prepared by mixing a pharmaceutically acceptable basic substance with a bad tasting pharmaceutical which is in a form insoluble at high pH and encapsulating the mixture.
U.S. Pat. No. 4,994,260 discloses a pharmaceutical preparation for controlled release of a pharmaceutically active substance, which masks bad taste and increases stability of the pharmaceutically active substance and contains an encapsulated active substance in combination with 60 to 99% by weight of a release-controlling substance selected from the group consisting of polysaccharides, oligosaccarides, disaccharides, monosaccharides, polyhydroxy alcohols and mixtures thereof.
In known coating methods using an organic solvent such as methylene chloride, chloroform, cyclohexane, carbon tetrachloride, methyl ethyl ketone, acetone, methyl alcohol or isopropyl alcohol for dissolving a conventional coating agent, it is necessary to remove the solvent by carrying out a drying step, which requires a lot of time, many facilities, much labor and high cost and involves risks of ignition and explosion. Further, the product obtained thereby is of porous coating, and might contain a residual solvent to have a detrimental effect on a human body.
DISCLOSURE OF INVENTION
The present inventors have made an initial study on the masking of taste for overcoming the above-described problems.
At first, a study has been made of the selection of a material. As the material, which is excellent in forming a dense coating is concerned, a substance having a low melting point (wax) is available. Further, as far as a material which is readily soluble at low pH (pH 1-4, endogastric pH) and which is insoluble or hardly soluble in the mouth (pH 5-8) is concerned, a functional polymer may be taken into consideration. However, an organic solvent is required for dissolving the functional polymer, and there might be a risk concerning the toxicity and handling of the solvent. Further, since the functional polymer forms a porous coating or cannot form a dense coating, it is difficult to mask the unpleasant taste sufficiently.
Therefore, studies have been made, and it has been found that, without any organic solvent, a functional polymer can be dissolved or dispersed in a substance having a low melting point when the substance having a low melting point has been melted. It has been also found that the resultant solution or dispersion of the functional polymer can be cooled to give a dense coating and that this can be carried out safely.
Additives for enhancing the masking effect have been studied. Usual additives such as carbonates, phosphates, citrates and hydroxides cannot be said to maintain
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Hayashi Hidefumi
Ishii Kuniaki
Itai Shigeru
Koyama Ikuo
Shimano Kimihide
Taisho Pharmaceutical Co. Ltd.
Webman Edward J.
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