Endometriosis treatment
AssigneeDrugtech Corporation
InventorsDaniel J. Thompson, Robert C. Cuca, Thomas C. Riley, JR., Jonathan David Bortz
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Abstract
A pharmaceutical composition comprises at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprises danazol in an amount of about 3% to about 30% by weight of the composition, wherein upon application of the composition to the vaginal mucosal surface the danazol is released over a period of about 1 to about 10 days. The composition is useful for intravaginal administration to treat a condition such as endometriosis for which danazol is indicated.
Claims57
A pharmaceutical composition comprising at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprising danazol in an amount of about 1% to about 30% by weight of the composition, wherein upon application of the composition to the vaginal mucosal surface the danazol is released over a period of about 1 to about 10 days.
A pharmaceutical composition comprising at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprising about 20% danazol, wherein the internal phase comprises about 45% water and about 20% sorbitol and the external phase comprises about 8% mineral oil, about 2.8% polyglyceryl-3-oleate, about 2.8% glyceryl monoisostearate, about 0.5% microcrystalline wax and about 1% hydrophobic silica, all percentages being by weight of the composition as a whole;
- or a composition substantially bioequivalent thereto when administered intravaginally.
A process for preparing a danazol vaginal cream composition, comprising
- (a) admixing one or more hydrophilic ingredients including at least one pharmaceutically acceptable polyol with water to provide an aqueous phase;
- (b) admixing one or more hydrophobic ingredients including at least one emulsifying agent and optionally at least one viscosity modulating agent with at least one pharmaceutically acceptable oil to provide a lipoidal phase;
- (c) admixing a first portion of the aqueous phase to the lipoidal phase to form an intermediate dispersion;
- (d) adding micronized particulate danazol to the intermediate dispersion with mixing to provide a uniform premix;
- and
- (e) admixing the balance of the aqueous phase to the premix with mixing to provide the finished composition;
- wherein the ingredients and relative amounts thereof are selected to provide a finished composition having the lipoidal phase continuous and external to the aqueous phase;
- and
- wherein the danazol is added in an amount of about 1% to about 30% by weight of the finished composition.
A vaginal danazol delivery system comprising (a) a pharmaceutical composition comprising at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprising danazol in an amount of about 1% to about 30% by weight of the composition, wherein upon application of the composition to the vaginal mucosal surface the danazol is released over a period of about 1 to about 10 days;
- and (b) an applicator.
A method for treating a condition in a female subject for which danazol is indicated, comprising administering intravaginally to the subject a therapeutically effective amount of a pharmaceutical composition comprising at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprising danazol in an amount of about 1% to about 30% by weight of the composition, wherein upon application of the composition to the vaginal mucosal surface the danazol is released over a period of about 1 to about 10 days.
A contraceptive method comprising administering intravaginally to a female subject a contraceptively effective amount of a pharmaceutical composition comprising at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprising danazol in an amount of about 1% to about 30% by weight of the composition, wherein upon application of the composition to the vaginal mucosal surface the danazol is released over a period of about 1 to about 10 days.
A pre-operative endometrial thinning method comprising administering intravaginally to a female subject prior to surgery an endometrial thinning effective amount of a pharmaceutical composition comprising at least one nonlipoidal internal phase and at least one lipoidal external phase that is bioadhesive to a vaginal mucosal surface, and comprising danazol in an amount of about 1% to about 30% by weight of the composition, wherein upon application of the composition to the vaginal mucosal surface the danazol is released over a period of about 1 to about 10 days.
Dependencies are inferred from the claim text.