Cyclodextrin complexation

A method for solubilizing and/or stabilizing a lipophilic and/or water-labile active ingredient which is a drug, cosmetic additive, food additive or agrochemical, in an aqueous medium, said method comprising complexing said active ingredient in an aqueous medium comprising from about 0.1 to about 70% (weight/volume) of cyclodextrin and from about 0.001 to about 5% (weight/volume) of a pharmacologically inactive water-soluble polymer acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition, the polymer and cyclodextrin being dissolved in the aqueous medium before the active ingredient is added, the aqueous medium which comprises the polymer and cyclodextrin being maintained at from about 30.degree. to about 150.degree. C. for a period of from about 0.1 to about 100 hours before, during and/or after the active ingredient is added.

A co-complex of a lipophilic and/or water-labile active ingredient which is a drug, cosmetic additive, food additive or agrochemical with a cyclodextrin and a pharmacologically inactive water-soluble polymer acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition, the ratio by weight of cyclodextrin to polymer being from about 4:1 to about 50,000:1, the molecular ratio of active ingredient to cyclodextrin being from about 0.33 to about 3.0 molecules of active ingredient per molecule of cyclodextrin in the co-complex.

A composition comprising:

• (a) a complex prepared by complexing a lipophilic and/or water-labile active ingredient which is a drug, cosmetic additive, food additive or agochemical in an aqueous medium comprising from about 0.1 to about 70% (weight/volume) of cyclodextrin and from about 0.001 to about 5% (weight/volume) of a pharmacologically inactive water-soluble polymer acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition, the polymer and cyclodextrin being dissolved in the aqueous medium before the active ingredient is added, the aqueous medium which comprises the polymer and cyclodextrin being maintained at from about 30.degree. to about 150.degree. C. for a period of from about 0.1 to about 100 hours before, during and/or after the active ingredient is added, optionally followed by removal of water;
• and
• (b) a non-toxic carrier therefor acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition.

A composition comprising:

• (a) a co-complex of a lipophilic and/or water-labile active ingredient which is a drug, cosmetic additive, food additive or agrochemical with a cyclodextrin and a pharmacologically inactive water-soluble polymer acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition, the ratio by weight of cyclodextrin to polymer being from about 4:1 to about 50,000:1, the molecular ratio of active ingredient to cyclodextrin being from about 0.33 to about 3.0 molecules of active ingredient per molecule of cyclodextrin in the co-complex;
• and
• (b) a non-toxic carrier therefor acceptable for use in a pharmaceutical, cosmetic, food or agricultural composition.