Cyclosporin formulations
OwnerMoshe Flashner-Barak, E. Lerner +2inventors
InventorsMoshe Flashner-Barak, E. Lerner, Vered Rosenberger, Naomi Moldavski
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Abstract
The present invention relates to compositions comprising solutions of drugs in menthol, especially drugs that are poorly soluble in water, and to methods for making such compositions.
Claims34
A composition for reducing the variability of the bioavailability of a drug comprising cyclosporine dissolved in an effective amount of menthol and at least one surface active agent.
A method for reducing the variability of the bioavailability of cyclosporine comprising dissolving cyclosporine in an effective amount of menthol in the presence of at least one surface active agent.
A method for increasing the time that cyclosporine provides a therapeutically significant concentration in blood or plasma comprising dissolving cyclosporine in an effective amount of menthol in the presence of at least one surface active ingredient.
A composition for improving the bioavailability of cyclosporine comprising about 10% by weight cyclosporine dissolved in about 40% menthol, about 34% Tween 80, and about 17% ducosate sodium, wherein the weights are in percents of the composition.
A composition for improving the bioavailability of a drug comprising simvastatin dissolved in an effective amount of menthol.
A composition for improving the bioavailability of a drug comprising simvastatin dissolved in an effective amount of menthol, wherein the composition has an average AUCt of about 181% as compared to a non-menthol containing formulation.
A composition for improving the bioavailability of a drug comprising simvastatin dissolved in an effective amount of menthol, wherein the composition has an average AUCI of about 127% as compared to the sequential administration of simvastatin and menthol.
A composition for improving the bioavailability of an active metabolite of a drug comprising simvastatin dissolved in an effective amount of menthol, wherein the composition has an average AUCt for simvastatin hydroxyacid of about 143% as compared to a non-menthol containing formulation.
A composition for reducing the variability of the bioavailability of an active metabolite of a drug comprising simvastatin dissolved in an effective amount of menthol, where the composition has a % CV for AUCt for simvastatin hydroxyacid which is at least about 30% lower when compared to a non-menthol containing formulation.
A composition for improving the bioavailability of a drug comprising raloxifene HCl and an effective amount of menthol, wherein the raloxifene HCl and the menthol are administered concomitantly.
A composition for improving the bioavailability of a drug comprising raloxifene HCl and an effective amount of menthol, wherein the raloxifene HCl and the menthol are administered concomitantly and the composition has an average AUC of about 108% as compared to a non-menthol containing formulation.
Dependencies are inferred from the claim text.