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

a technology of intranasal administration and therapeutic agents, which is applied in the field of therapeutic agents, can solve the problems of parasympathetic hyperactivity, nasal congestion and drainage, and poor elucidation of nar, and achieves the effects of improving therapeutic response, rapid onset of action, and quick and/or fast onset of action

Inactive Publication Date: 2013-05-09
HI TECH PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent describes an intranasally administered composition that is well-tolerated and has no effect on olfaction even after prolonged treatment. The composition contains vegetable glycerin, ascorbic acid, sea salt, potassium sorbate, or a combination of these ingredients. The composition provides quick relief from symptoms within a few minutes of administration.

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.

Method used

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

Examples

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Effect test

example 1

[0056]It is hypothesized that capsicum, comprising capsaicinoids, including capsaicin, and possibly other ingredients in Applicant's composition, used for relief of rhinitis and allergic symptoms act via activation of TRP-family receptors. Applicant has developed an in vitro fluorometric assay to measure receptor activity in the presence of various concentrations of capsaicin / capsaicinoids. The activation of the receptors in the in vitro assay correlates with Applicant's demonstrated symptom relief as evidenced in the examples below. Specifically, the goal of the in vitro assay is to quantitatively measure TRPV activation to determine the dose response of airway component cells to Applicant's compositions comprising capsaicin / capsaicinoids. To this end, Applicant developed a new assay for transient receptor protein vanilloid (“TRPV”) activation in cells. The assay is fluorometric in nature, relying upon a calcium-binding fluor, Fura-4. (available from Invitrogen Life Sciences and ot...

example 2

[0060]A clinical study was performed to assess the efficacy and safety of a newly formulated intranasally administered capsicum composition (“ICX”) used continuously over a two week treatment period in chronic rhinitis subjects who have a significant component of NAR. The ICX formulation comprises from about 0.00060% to about 0.010% w / w, or comprising about 0.1 to about 2.0 ppm total capsaicinoids, about 0.0020% to about 0.0080% w / w, resulting in about 0.3 to about 1.5 ppm total capsaicinoids, or preferably about 0.0030% to about 0.0080% w / w, resulting in about 0.5 to about 1.5 ppm total capsaicinoids. The ICX formulation further comprises rosemary extract at a concentration of about 0.02% to about 0.25% w / w, eucalyptol at a concentration of about 0.07 to about 0.15%, vegetable glycerin at a concentration of about 3.5% to about 5.0% w / w, ascorbic acid at a concentration of about 0.10% to about 0.90% w / w and sea salt at a concentration of about 0.40% to about 1.2% w / w. One embodiment...

example 3

[0097]One example of the present invention relates to a headache relief composition. The headache relief composition provides relief of symptoms such as migraines, general headaches, tension, chronic and occasional headaches, and dizziness, and visual distortions associated with headaches. The headache relief composition comprises capsicum comprising capsaicin, dihydrocapsaicin, and nordihydrocapsaicin, feverfew extract, eucalyptol, peppermint oil, rosemary extract, vegetable glycerin, ascorbic acid, citric acid, and sea salt. An embodiment may comprise potassium sorbate at a concentration of about 0.05% to about 0.30% w / w.

[0098]The feverfew extract relieves and prevents headache symptoms. The eucalyptol is used to ameliorate the sensory experience and soothe the nasal mucosa. The peppermint oil relieves and helps prevent headache symptoms. The rosemary extract is an anti-microbial agent and a natural preservative which protects and stabilizes the headache relief composition. In a s...

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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...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K36/81A61K9/00
CPCA61K36/81A61K9/0043A61K47/46A61K47/22A61K9/08
Inventor PERRY, WAYNE JEFFREYMILLHEISER, LYNNE
Owner HI TECH PHARMA
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