Oxymetazoline for the treatment of ano-rectal disorders
Inventors
Barak, Nir • Rice, Howard Lawrence
Assignees
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Publication Number
US-9849114-B2
Publication Date
2017-12-26
Expiration Date
Abstract
Methods for treating fecal incontinence by administering to a subject in need thereof compositions including oxymetazoline as an active ingredient. Kits including compositions of oxymetazoline suitable for topical application, for the treatment of fecal incontinence.
Core Innovation
The patent describes a method for treating fecal incontinence in a subject by administering a therapeutically effective amount of a composition consisting essentially of oxymetazoline or a pharmaceutically acceptable salt thereof to the subject’s anal cavity. The composition consists essentially of 0.1% to 1% of oxymetazoline or the pharmaceutically acceptable salt thereof, and the disclosed approach is directed to ano-rectal disorders with an emphasis on increasing resting anal pressure.
The background problem addressed is fecal incontinence, which requires a treatment that can increase resting anal pressure in the anal canal. The patent associates the treatment effect with low-concentration α-adrenergic activity of topical oxymetazoline, including oxymetazoline hydrochloride, to increase resting anal pressure and improve anal sphincter function related to resting pressure.
The disclosed compositions are administered topically into the anal cavity and include controlled release, long acting, slow release, sustained release, bioadhesive, and mucoadhesive formulations. The document further describes dosage forms and optional extended efficacy, with examples reporting pronounced increases in resting anal pressure maintained for at least 5 hours for a ~0.1% oxymetazoline condition, while low doses do not significantly alter blood pressure or heart rate in the evaluated human subjects.
Claims Coverage
Independent claim coverage centers on a single method for treating fecal incontinence via anal-cavity administration of a composition consisting essentially of oxymetazoline or a pharmaceutically acceptable salt at 0.1% to 1%. The claim set includes multiple refining inventive features, with a total of 1 independent claim.
Anal-cavity oxymetazoline composition for fecal incontinence
Treating fecal incontinence in a subject in need thereof by administering a therapeutically effective amount of a composition consisting essentially of oxymetazoline or a pharmaceutically acceptable salt thereof to the subject’s anal cavity, wherein the composition consists essentially of 0.1% to 1% of oxymetazoline or the pharmaceutically acceptable salt thereof.
Oxymetazoline hydrochloride salt administration
The method specifies oxymetazoline hydrochloride as the pharmaceutically acceptable salt under the composition framework.
Concentration range of 0.1% to 0.8% oxymetazoline
The method specifies that the therapeutically effective amount of the composition essentially contains 0.1% to 0.8% oxymetazoline or a pharmaceutically acceptable salt of oxymetazoline.
Long acting and adhesion-capable formulation categories
The method is carried out using a composition selected from long acting, controlled release, slow release, sustained release, bioadhesive, or mucoadhesive formulations.
Selected dosage forms for anal administration
The composition is provided in one of several listed dosage forms including gel, cream, paste, spray, suppository, mousse, emollient, powder, solution, suspension, or foam.
Efficacy lasting at least 4 hours
The method uses a therapeutically effective amount of the composition to treat fecal incontinence in a subject for at least 4 hours.
Overall, the claims cover treating fecal incontinence by administering an essentially oxymetazoline composition to the anal cavity with 0.1% to 1% active content, and refining embodiments specify oxymetazoline hydrochloride, a narrower 0.1% to 0.8% range, long acting, controlled release, slow release, sustained release, bioadhesive, and mucoadhesive formulations, enumerated dosage forms, and at least 4 hours of treatment efficacy.
Stated Advantages
Increases resting anal pressure.
Efficacy is maintained for at least 4 hours, and at least 5 hours in the examples.
Low doses do not significantly alter blood pressure or heart rate in the evaluated human subjects.
Documented Applications
Topical treatment of fecal incontinence by administering an oxymetazoline composition to a subject’s anal cavity.
Use of the disclosed oxymetazoline composition to increase resting anal pressure related to anal sphincters and anal canal function in ano-rectal disorders.
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