Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules
Reexamination Certificate
1999-03-08
2001-04-10
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Capsules
C424S451000
Reexamination Certificate
active
06214378
ABSTRACT:
FIELD OF THE INVENTION
1. Background of the Invention
This invention relates to capsules for preparations for oral administration and also to capsule preparations for oral administration using said capsules. More particularly, this invention relates to capsules being able to be administered orally in which pharmacologically active substance depending upon the object can be encapsulated and which is firstly disintegrated upon arriving at the large intestine whereby the pharmacologically active substance can be efficiently released therefrom and also relates to capsule preparations using said capsules where said preparations are pharmaceutical preparations useful for colon diseases such as colon cancer, ulcerative colitis, constipation and diarrhea and for systemic diseases such as osteoporosis.
2. Description of Related Art
In recent years, great effort has been made for developing the intestinal delivery art where the preparation after oral administration is not disintegrated in stomach and small intestine but is disintegrated just upon arriving at the large intestine. The reason is that such a method in place of conventional intravenous administration, transnasal administration, rectal administration, etc. greatly reduces the burden of the patients as compared with those conventional methods.
Examples of the known intestinal delivery art which have been known up to now are an oral preparation where a polymer which is soluble only at pH 5.5 or higher and an insoluble polymer are combined whereby large intestine is a target for releasing the drug (European Patent 49,590); a solid oral dosage form coated with an appropriate amount of anionic polymer (trade name: Eudragit S; manufactured by Rohm) which is soluble at pH 7.0 or higher (International Laid-Open Patent WO 83/00435); an oral preparation coated with a composition in an appropriate ratio of anionic copolymer which is soluble at pH 7.0 or higher (trade name: Eudragit S or L; manufactured by Rohm) and a methacrylate copolymer which is hardly soluble in water (trade name: Eudragit RS; manufactured by Rohm) (European Patent 225,189); an osmotic pressure pump preparation which is coated with an enteric coating polymer (Belgian Patent 903,502); and an oral pharmaceutical preparation delivering to large intestine where an internal layer which is soluble at pH 7.0 or higher is coated with a gelled polymer layer as an intermediate layer and then further coated with a stomach-resisting external layer which is soluble at pH 5.5 or higher (Japanese Laid-Open Patent Hei-04/501,411).
However, each of those known art relates to a preparation showing the time-depending release of drugs and their specificity to large intestine is high, cannot be said to be high. Thus, there are problems that, for example, when the staying time in small intestine is long, the preparation is disintegrated in the small intestine while, when the staying time in small and large intestines is short, the preparation is not disintegrated but is excreted outside as it is.
In order to improve such problems, the inventors of this invention proposed an oral pharmaceutical preparation of a type of releasing from lower gastrointestinal tracts having a high specificity to large intestine (International Laid-Open Patent WO 94/10983). This product is characterized in that it is a solid preparation having a double-coated structure where molded tablets or granules with pressure are used as cores and they are coated with an inner layer consisting of a cationic copolymer and an outer layer consisting of an anionic copolymer. This preparation has a very good specificity to large intestine and makes it possible to release the drug to the large intestine as a target in a more reliable manner. However, in spite of such an improvement, satisfactory releasing and absorbing efficiencies are not always achieved in the case of hardly-soluble substances and polymers. Therefore, it has been a very important matter to conduct a drug design depending upon the physical and chemical properties of the drug so that absorbing efficiency of the drug is further improved.
SUMMARY OF THE INVENTION
As a solution for the above-mentioned problems, this invention offers capsules for oral preparations, characterized in that, surface of the capsule base consisting of hydroxypropylmethylcellulose, a mixture of polyethylene glycol with hydroxypropylmethylcellulose, gelatin or agar is successively coated with a cationic copolymer and an anionic copolymer and also offers capsule preparations for oral administration where a pharmacologically active substance is encapsulated in said capsules.
REFERENCES:
patent: 5238686 (1993-08-01), Eichel et al.
patent: 5462951 (1995-10-01), Iwao et al.
patent: 5840332 (1998-11-01), Lerner et al.
Aoki Jun
Nakanishi Masaru
Tanida Norifumi
Hisamitsu Pharmaceutical Co. Inc.
Page Thurman K.
Pulliam Amy E
Wenderoth , Lind & Ponack, L.L.P.
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