US 9,314,524 B2 · Topical formulations of Flucytosine

Abstract

The invention relates to topical formulations of flucytosine which demonstrate a clear advantage over currently available therapeutic regimens for the treatment and maintenance of fungal infections, particularly vulvovaginal candidiasis. The invention provides compositions which solve the long-standing need for antimicrobial agents which treat effectively resistant strains of Candida spp., especially C. albicans, C. glabrata, and C. tropicalis, and which pose limited risk of side effects, adverse reactions, or the development of resistant pathogens. The invention provides novel topical formulations of flucytosine designed to allow the active drug to act at the local application area, but which inhibit or moderate transdermal or transmucosal absorption of the drug, thus limiting systemic exposure.

Claims11

Dependent claims

A topical composition for exterior treatment of vulvovaginal candidiasis comprised of flucytosine, a carrier, and poly(lactic acid),

wherein the flucytosine is selected from the group consisting of flucytosine, a flucytosine salt or a mixture thereof and is capable of forming ionized flucytosine;
wherein the poly(lactic acid) reduces permeation of flucytosine across skin and mucosal membrane;
wherein the carrier comprises a pH modulator suitable to establish a pH of the composition of between about 1 to about 5 to control the ratio of ionized flucytosine to unionized flucytosine within the composition and
wherein the topical composition is configured to minimize systemic absorption of the ionized flucytosine in the treatment environment.

1 more element

Dependencies are inferred from the claim text.

Topical formulations of Flucytosine

Life of this patent

Topical formulations of Flucytosine

Life of this patent

Abstract

Claims11