Non-inclusion cyclodextrin complexes
First Claim
1. 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 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 acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition.
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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.
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Citations
35 Claims
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1. 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 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 acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9)
- -cyclodextrin in an aqueous complexation medium, said medium comprising from about 0.1% to about 80% (weight/volume) of β
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10. 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) of a pharmacologically inactive water-soluble polymer acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition; 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 acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition. - View Dependent Claims (11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
- -cyclodextrin in an aqueous complexation medium, said medium comprising from about 0.1% to about 80% (weight/volume) of β
- 21. A method for enhancing the aqueous solubility of an active ingredient which is insoluble or sparingly soluble in water and which does not readily form an inclusion complex with cyclodextrin, said active ingredient being a drug, cosmetic additive, food additive or agrochemical, said method comprising adding said active ingredient to an aqueous complexation medium which comprises from about 0.1% to about 70% (weight/volume) of said cyclodextrin, said complexation medium being saturated, prior to addition of said active ingredient, with a compound which forms an inclusion complex with said cyclodextrin and which is acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition.
Specification