Therapeutic agent for intranasal administration and method of making and using same

Abstract

The present invention provides a composition suitable for intranasal administration comprising capsaicin, dihydrocapsaicin, and nordihydrocapsaicin in the form of capsicum used as a therapeutic agent.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority to U.S. Patent Application No. 61 / 405,390, filed Oct. 21, 2010, and is a continuation-in-part of U.S. patent application Ser. No. 12 / 849,088, filed Aug. 3, 2010, which is a continuation of U.S. patent application Ser. No. 11 / 731,657, filed Mar. 30, 2007, now abandoned, all of which are herein incorporated by reference in their entirety. This application is also related to U.S. patent application Ser. No. 11 / 731,656, filed Mar. 30, 2007, now abandoned, which is herein incorporated by reference in its entirety.FIELD OF THE INVENTION[0002]The present invention relates to a therapeutic agent capable of intranasal administration comprising capsicum and / or capsaicinoids as the therapeutic agent.BACKGROUND OF THE INVENTION[0003]Non-allergic rhinitis (“NAR”) affects millions of Americans, but the mechanism(s) remains unknown. Transient receptor potential vanilloid-1 (“TRPV1”) may be involved, as single dose studie...

AI Technical Summary

Benefits of technology

[0029]An advantage of an embodiment of the present invention is an intranasally administered composition having a quick and / or fast onset of action with an average time to first relief of at least one symptom of less than about thirty minutes, about fifteen minutes, about five minutes, about three minutes, and even less than about one minute.

[0030]An embodiment of the present invention is an intranasally administered composition that provides relief from at least one of nasal congestion, sinus pressure, sinus pain and headache with an improved therapeutic response that continues over time with at least one of nasal congestion, sinus pressure, sinus pain and headache significantly improved at about 5, 10, 15, 30 and / or 60 minutes. An advantage of an embodiment of the present invention is an intranasally administered composition having a rapid onset of action and significant reduction of symptoms that may be an attractive mono-therapy or adjunctive therapy for the management of rhinitis symptoms.

[0031]An embodiment of the present invention is an intranasal composition wherein users experience little to no rebound congestion. An advantage of an embodiment of the present invention is an intranasal composition wherein users experience essentially no alteration, or even an improvement, in olfaction versus placebo after continued use. An advantage of an embodiment of the present invention is a nasally administered composition that provides a rapid onset of relief for rhinitis subjects, while also providing safe, sustained relief over the course of a treatment period.

[0032]An advantage of an embodiment of the present invention is an intranasally administered composition wherein during a treatment period is significantly effective at improving at least one of nasal congestion, sinus pressure, sinus pain and headache compared to placebo.

[0033]An advantage of an embodiment of the present invention is an intranasally administered composition that is well-tolerated and with prolonged treatment results in substantially no reduction in olfaction.

[0034]An advantage of an embodiment of the present invention is an agent that may be used as a mono-therapy comprising capsaicin, dihydrocapsaicin, and nordihydrocapsaicin and other capsaicinoids.

Problems solved by technology

The most popular mechanism postulated for non-allergic rhinitis has been an autonomic imbalance between the sympathetic and parasympathetic nervous system resulting in parasympathetic hyperactivity leading to nasal congestion and drainage.

Because mechanisms of NAR are poorly elucidated, there are still only a few medications approved for the treatment of this condition.

Although clinical studies have found that the intranasal antihistamines, azelastine and olopatidine, intranasal ipratropium bromide and intranasal corticosteroids are relatively effective in relieving symptoms related to NAR, it is unclear how they are mechanistically exerting their effect.

However, the concentration of capsaicin used and found effective in these studies, ranging from 30 ppm to 300 ppm, was very irritating and required a physician to co-administer a local anesthetic making it impractical and intolerable for patients to self-administer the composition or use this treatment long term.

Furthermore, Applicant is not aware of any studies demonstrating clinical efficacy of capsicum / capsaicin at concentrations 10% or less of the dosages used in previous rhinitis clinical trials.

Previously it has not been possible to deliver an effective concentration of capsicum intranasally without causing such discomfort to the user requiring the use of an adjunct to desensitize the nasal membranes in order to administer the capsicum.

In addition, Applicant is not aware of any prior studies disclosing that a low homeopathic dilution of capsicum is clinically effective for the treatment of rhinitis.

Extended use of these known products leads to the occurrence of rebound congestion and the potential for addiction.

These known OTC products are not suitable for use by those with symptoms that last longer than three days, including those suffering chronic conditions, and those suffering from chronic rhinitis symptoms.

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