Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
1998-10-21
2002-08-27
Brusca, John S. (Department: 1631)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C514S058000, C514S060000, C562S556000
Reexamination Certificate
active
06441040
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to stable preparations for oral administration comprising S-(3-hydroxypropyl)-L-cysteine useful as an expectorant.
2. Background Art
It has been reported that S-(3-hydroxypropyl)-L-cysteine (hereinafter referred to as “HPCY”) is useful as an expectorant (JP-A-2-3674; the term “JP-A” as used herein means an “unexamined published Japanese patent application”). Examples of the dosage form of HPCY include oral administration preparations, such as tablets, capsules, powders, granules, troches, solutions, and the like; and parenteral administration preparations, such as subcutaneous, intramuscular or intravenous injections, transfusion admixtures, suppositories, and the like. Among these, oral solid preparations are recommendable because of simple handling and easy administration.
HPCY is a compound having excellent stability, because it hardly causes discoloration in the presence of moisture or in the air when it is present alone. However, the discoloration occurs when it is used together with additives which are frequently used in the production of solid preparations, such as various saccharides, sugar alcohols, celluloses, and the like.
Since not only such a discoloration spoils the appearance of medicines but also it sometimes causes reduction of the content, the discoloration should be avoided.
Although there are many means for preventing discoloration of medicines, the countermeasure varies depending on the cause. For example, if moisture is the cause of discoloration, the moisture content of each preparation is reduced by drying or the preparation is blocked from the outside by coating or through a proper design of its packing. Also, if the cause is oxidation reaction, addition of an antioxidant is effective. However, discoloration is generally influenced by the coexisting components and preservation environments in a complicated manner, so that the real cause is not clear in many cases.
SUMMARY OF THE INVENTION
An object of the present invention is to provide an HPCY-containing solid preparation for oral administration which hardly causes discoloration even after a long period of storage due to a pharmaceutical means.
Accordingly, the present invention provides a preparation for oral administration which comprises S-(3-hydroxypropyl)-L-cysteine and an excipient, wherein the excipient is substantially only starch.
Also, the present invention provides a preparation for oral administration which comprises S-(3-hydroxypropyl)-L-cysteine and a cyclodextrin.
DETAILED DESCRIPTION OF THE INVENTION
The present inventors have conducted intensive studies and found as a result of the efforts that a stable oral preparation which causes less discoloration even after a long period of storage can be obtained when HPCY is blended as an excipient with substantially only starch or a cyclodextrin. The present invention has been accomplished on the basis of this finding.
According to the first embodiment of the present invention, substantially only starch should be used as an excipient, because it is not preferred that blending of other excipients excluding cyclodextrins, such as saccharides, sugar alcohols, celluloses, and the like, will cause discoloration.
In the present invention, the expression “the excipient is substantially only starch” means that the excipient is starches alone or that other excipients excluding cyclodextrins are present in such an amount that discoloration of the preparation for oral administration of the present invention is not caused. Preferably, the starches are present in an amount of 90 to 100% by weight of the total excipients.
Examples of the starches for use in the present invention include corn starch, potato starch, wheat starch, rice starch, and the like. These starches may be used alone or as a mixture of two or more. The amount used of these starches is not particularly limited; however, they are preferably used in an amount of 0.01 to 8 parts by weight, more preferably 0.02 to 4 parts by weight, based on 1 part by weight of HPCY.
Furthermore, examples of the cyclodextrins for use in the present invention include &agr;-cyclodextrin, &bgr;-cyclodextrin, and &ggr;-cyclodextrin. These cyclodextrins may be used alone or as a mixture of two or more. The amount used of these cyclodextrins is not particularly limited; however, they are preferably used in an amount of 0.01 to 8 parts by weight, more preferably 0.02 to 4 parts by weight, based on 1 part by weight of HPCY.
When these cyclodextrins are used, other excipients may also be used or the above-described starches may be used as excipients. If the starches coexists, stable preparations can be obtained in any mixing ratios of the cyclodextrins and the starches.
When the preparation for oral administration of the present invention is produced, HPCY is mixed with starches and/or cyclodextrins and, as occasion demands, additives usually used in the production of medicines, and the resulting mixture is made into oral preparations, such as tablets, capsules, powders, granules, troches, and the like, in the conventional way. The conventionally used additives may be selected optionally from correctives, flavors, binders, lubricants, and the like, with the proviso that they do not cause discoloration when coexisted with HPCY. Preferably, these additives are used in an amount of 5% by weight or less, more preferably 2% by weight or less, of the total amount of the preparation.
REFERENCES:
patent: 5614197 (1997-03-01), Pathak et al.
patent: 5626837 (1997-05-01), Shimada et al.
patent: 5846562 (1998-12-01), Yanai et al.
patent: 0 209 957 (1986-07-01), None
patent: 0 346 882 (1989-12-01), None
patent: 0 346 883 (1989-12-01), None
patent: 72.21606 (1974-01-01), None
Iwasa Akira
Kanbe Hideyoshi
Murata Misao
Saito Yukihiro
Yamauchi Shuji
Brusca John S.
Moran Marjorie A.
SSP Co. Ltd.
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