Back to results
US 2020/0345751 A1Published application
Fulvestrant compositions and method of use
AssigneeShimoda Biotech (Pty) Ltd
InventorHenk SWART
Life of this patent
Estimating the term…
Abstract
Provided are inclusion complexes comprising fulvestrant and a cyclodextrin. The complexes may be useful for treating various conditions, such as cancer and systemic lupus erythematosus. Also provided are methods of producing the inclusion complexes, methods of using the inclusion complexes in therapy, and kits and unit dosages comprising the complexes.
Claims9
1-76. (canceled)
An inclusion complex comprising an aqueous solution of:
- a) a sulfobutylether beta-cyclodextrin (SBEBCD);
- and b) a compound of the formula (I):
- or a salt thereof or hydrate of the foregoing;
- and c) a carrier
- a Cmax of at least about 2-times greater than administered uncomplexed compound of formula (I) in the same amount and under the same conditions;
- and
- bioavailability at least about 50% over the bioavailability of the uncomplexed compound of formula (I)
- wherein the inclusion complex increases the solubility of the compound of formula (I), in deionized water at 20° C., by at least about 1.5-fold compared to the solubility of the compound of formula (I) in uncomplexed form under the same conditions;
- and wherein the inclusion complex is stable at temperatures of 25° C. to 40° C. for at least 24 months.
6 more elements
A formulation comprising a) a sulfobutylether beta-cyclodextrin (SBEBCD);
- b) a compound of the formula (I):
- or a salt thereof or hydrate of the foregoing;
- and c) water, alone or in combination with a pharmaceutically acceptable carrier.
A method for improving solubility, stability, Cmax, and bioavailability of a compound of the formula (I):
- or a salt, hydrate, or solvate thereof in water, the method comprising:
- complexing the compound of the formula (I) with a sulfobutylether beta-cyclodextrin (SBEBCD) so as to form an aqueous inclusion complex;
- and
- increasing the solubility of the compound of formula (I), in deionized water at 20° C., by at least about 1.5-fold compared to the solubility of the compound of formula (I) in uncomplexed form under the same conditions;
- providing stability of the inclusion complex at temperatures of 25° C. to 40° C. for at least 24 months;
- providing a Cmax of at least about 2-times greater than administered uncomplexed compound of formula (I) in the same amount and under the same conditions;
- and
- providing bioavailability at least about 50% over the bioavailability of the uncomplexed compound of formula (I).
5 more elements
Dependencies are inferred from the claim text.