Non-inclusion cyclodextrin complexes
AssigneedeCODE Genetics ehf.
InventorThorsteinn Loftsson
Life of this patent
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Abstract
The invention provides a number of methods for enhancing the aqueous solubility of an active ingredient which is insoluble or sparingly soluble in water. In one preferred embodiment, solubilization of the active ingredient is enhanced by combining it with β-cyclodextrin in an aqueous complexation medium comprising β-cyclodextrin and a negatively- or positively-charged compound which forms an inclusion or non-inclusion complex with β-cyclodextrin and its inclusion complexes.
Claims24
A method for enhancing the aqueous solubility of an active ingredient which is insoluble or sparingly soluble in water, said active ingredient being a drug, cosmetic additive, food additive or agrochemical, said method comprising combining said active ingredient with β-cyclodextrin in an aqueous complexation medium, said medium comprising from about 0.1% to about 80% (weight/volume) of β-cyclodextrin;
- from about 0.1% to about 10% (weight/volume) pharmacologically inactive and pharmaceutically, cosmetically or agriculturally acceptable water-soluble polymer which is a polysaccharide, a polypeptide, a cellulose derivative, a polyoxyethylene derivative, a polyvinyl derivative or a copolymer of acrylic acid;
- and from about 0.1% to about 5% (weight/volume) of a negatively- or positively-charged compound which forms an inclusion or non-inclusion complex with β-cyclodextrin and its inclusion complexes, said charged compound being pharmaceutically, cosmetically or agriculturally acceptable, said negatively-charged compound being a salt of a monofunctional carboxylic acid which forms a non-inclusion complex with β-cyclodextrin or a salt of a carboxylic acid having a lipophilic moiety which forms an inclusion complex with β-cyclodextrin.
A method for enhancing the aqueous solubility of a drug which is insoluble or sparingly soluble in water, said method comprising combining said drug with β-cyclodextrin in an aqueous complexation medium. said medium comprising from about 0.1% to about 80% (weight/volume) of β-cyclodextrin;
- from about 0.1% to about 10% (weight/volume) of a pharmacologically inactive pharmaceutically acceptable water-soluble polymer which is a polysaccharide, a polypeptide, a cellulose derivative, a polyoxyethylene derivative, a polyvinyl derivative or a copolymer of acrylic acid;
- and from about 0.1% to about 5% (weight/volume) of a negatively-charged compound which is a salt of a monofunctional carboxylic acid which forms a non-inclusion complex with β-cyclodextrin and which is pharmaceutically acceptable.
A method for enhancing the aqueous solubility of a drug which is insoluble or sparingly soluble in water, said method comprising combining said drug with p-cyclodextrin in an aqueous complexation medium, said medium comprising from about 0.1% to about 80% (weight/volume) of β-cyclodextrin;
- from about 0.1% to about 10% (weight/volume) of a pharmacologically inactive pharmaceutically acceptable water-soluble polymer which is a polysaccharide, a polypeotide, a cellulose derivative, a oolvoxvethvlene derivative, a polyvinyl derivative or a copolymer of acrylic acid;
- and from about 0.1% to about 5% (weight/volume) of an alkali metal, alkaline-earth metal or aluminum salt of acetic acid or of propionic acid.
A method for enhancing the aqueous solubility of a drug which is insoluble or sparingly soluble in water, said method comprising combining said drug with β-cyclodextrin in an aqueous complexation medium, said medium comprising from about 0.1% to about 80% (weight/volume) of β-cyclodextrin;
- from about 0.1% to about 10% (weight/volume) of a pharmacologically inactive pharmaceutically acceptable water-soluble polymer which is a polysaccharide, a polypeotide, a cellulose derivative, a polyoxyethylene derivative, a polyinyl derivative or a copolymer of acrylic acid;
- and from about 0.1% to about 5% (weight/volume) of a negatively-charged compound which is a salt of a carboxylic acid having a lipophilic moiety which forms an inclusion complex with β-cyclodextrin and which is pharmaceutically acceptable.
A method for enhancing the aqueous solubility of a drug which is insoluble or sparingly soluble in water, said method comprising combining said drug with β-cyclodextrin in an aqueous complexation medium, said medium comprising from about 0.1% to about 80% (weight/volume) of β-cyclodextrin;
- from about 0.1% to about 10% (weight/volume) of a pharmacologically inactive pharmaceutically acceptable water-soluble polymer which is a polysaccharide, a polypeptide, a cellulose derivative, a polyoxyethylene derivative, a polvinyl derivative or a copolymer of acrylic acid;
- and from about 0.1% to about 5% (weight/volume) of sodium salicylate, sodium benzoate or sodium gentisate.
A method for enhancing the aqueous solubility of a drug which is insoluble or sparingly soluble in water, said method comprising combining said drug with β-cyclodextrin in an aqueous complexation medium, said medium comprising from about 0.1% to about 80% (weight/volume) of β-cyclodextrin;
- from about 0.1% to about 10% (weight/volume) of a pharmacologically inactive pharmaceutically acceptable water-soluble polymer which is a polysaccharide, a polypeptide, a cellulose derivative, a oolvoxvethvlene derivative, a polyvinyl derivative or a copolymer of acrylic acid;
- and from about 0.1% to about 5% (weight/volume) of amfenac sodium, bromfenac sodium, diclofenac sodium, diflumidone sodium, enolicam sodium, fenoprofen calcium, ibuprofen aluminum, indomethacin sodium, magnesium salicylate, meclofenamate sodium, naproxen sodium, sodium salicylate, tifurac sodium, tolemetin sodium or zomepirac sodium.
Dependencies are inferred from the claim text.