Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1998-03-03
1999-09-14
Spivack, Phyllis G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
A61K 3119
Patent
active
059523832
DESCRIPTION:
BRIEF SUMMARY
This case is a 371 of PCT/EP97/03405 filed Jun. 30, 1997.
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a pharmaceutical composition adapted for oral administration, and more particularly a pharmaceutical composition adapted for an active principle of a medicinal product for human or veterinary use, which is insoluble or sparingly soluble in water and oils, such as diacerein (diacetylrhein), rhein or one of their salts, which allows their bioavalability to be improved.
2. Description of Related Art
Diacerein, described in patent FR-A-2,508,798, is a compound whose pharmacological properties have been known for several years and have allowed it to be used as a non-steroidal antiinflammatory medicinal product applicable in the treatment of diseases such as arthrosis. However, diacerein is virtually insoluble in water and in alcohols, this being a drawback for its administration, in particular by injection. Moreover, when it is administered orally, diacerein is not totally absorbed by the digestive tract, and, on account of this incomplete absorption, undesirable side effects may be observed, for example laxative effects.
Various derivatives, pharmaceutical compositions and pharmaceutical forms intended to improve the properties of diacerein or of other medicinal products which are insoluble or sparingly soluble in water have been described in the literature. Thus, for example, patent EP-A-243,968 describes a water-soluble potassium salt of diacerein which can be used in the preparation of compositions for parenteral administration.
Patent EP-A-598,337 describes a composition comprising an active principle of a medicinal product which is insoluble or sparingly soluble in water, incorporated into a crosslinked polymer, a surfactant and an oil, this composition being of improved bioavailability. U.S. Pat. No. 5,225,192 describes a process for preparing a fast-dissolving medicinal product, which consists in incorporating the medicinal product into crosslinked polymer particles which are insoluble but capable of swelling in water, in leaving the product in contact with an organic solvent and in drying under vacuum.
The subject of the present invention is a pharmaceutical composition adapted for an active principle of a medicinal product for human or veterinary use, containing a medicinal product which is insoluble or sparingly soluble in water and oils, in particular diacerein, rhein or one of their salts, which can be administered orally and affords faster and more complete absorption of the active principle into the body, and being of better bioavailability, thus making it possible to reduce or eliminate the abovementioned side effects.
The subject of the present invention is also a novel pharmaceutical composition based on diacerein, rhein or diacerein or rhein salts, which can be administered orally in the form of a wafer capsule or a gelatin capsule, and which is of improved bioavalability when compared with the usual forms.
DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS
The pharmaceutical composition according to the present invention, which can be administered orally, containing the abovementioned medicinal product that is insoluble or sparingly soluble in water and oils, selected from diacerein, rhein or one of their pharmaceutically acceptable salts, is essentially distinguished in that it comprises
The pharmaceutically acceptable salts which can be used in the invention can be, for example, the sodium or potassium salts of diacerein or of rhein.
The liquid support oil used in the composition of the invention can be selected from a plant oil (for example ground-nut oil, soybean oil or sunflower oil), a mineral oil (for example a paraffin) and an animal oil. It can consist of one or more medium-chain triglycerides. The expression "medium-chain" used here with reference to triglycerides means a linear or branched chain preferably comprising between 8 and 12 carbon atoms approximately. Needless to say, it is possible to use one or more triglycerides in combinati
REFERENCES:
patent: 5225192 (1993-07-01), Lovrecich
patent: 5430067 (1995-07-01), Gallagher et al.
Cohen Avraham
Metziger Pierre
Negma-Steba International Development N.V.
Spivack Phyllis G.
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