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Method and composition for treating osteoarthritis

Inactive Publication Date: 2015-06-18
VIREO SYST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is about a new method for treating inflammatory diseases, such as osteoarthritis, using a special anti-inflammatory agent called ethyl (α-guanido-methyl) ethanoate. This agent has unique properties that make it different from other drugs currently on the market. The method involves giving the patient the anti-inflammatory agent either orally or through a skin patch. The treatment can reduce the levels of pro-inflammatory markers like serum amyloid A, pro-inflammatory prostanoids, and tumor necrosis factor alpha in the patient's blood. The effective amount of the anti-inflammatory agent is between 400 mg and 2400 mg per day. The treatment can also involve combining the ethyl (α-guanido-methyl) ethanoate with other compounds like homeopathic compounds, co-medications, nutraceuticals, plant extracts, herbal preparations, and cosmetic agents.

Problems solved by technology

NSAIDs are generally effective but have a number of toxic side effects that compromise the gastrointestinal, renal, and / or cardiovascular health of many patients.
It is clinically known that NSAID side effects include stomach bleeding, heart risks, and liver and kidney toxicity.
Recently, there has also been research that shows current NSAID treatment increases oxidative stress which, in turn, initiates an overall degradation of a person's health and immune system and results in the slowed healing of bones, tendons, ligaments, and muscles.
In addition, NSAIDs may become addictive.
However, attempts to date have been relatively unsuccessful.
Compounds that were considered “safe” for use either did not prove to effectively reduce inflammation in cases like OA or expressed unexpected toxicity in certain situations or among certain groups of patients.

Method used

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  • Method and composition for treating osteoarthritis
  • Method and composition for treating osteoarthritis
  • Method and composition for treating osteoarthritis

Examples

Experimental program
Comparison scheme
Effect test

example 1

Double Blind Randomized Trial in OA Canines

[0040]The following example evaluates the effectiveness of Alpha-GEE on both pain and mobility in a double-blind randomized trial in canines having OA. Results of the study indicate that evaluation of pain and mobility during the course of the trial demonstrated a significant improvement in canines receiving Alpha-GEE compared to canines in the placebo group with score reductions of approximately 50 percent versus 15 percent, respectively. Furthermore, while pedometer measurements showed no significant changes in the mobility of canines in the placebo group, the canines treated with Alpha-GEE showed an approximately 30 percent increase in physical activity during the two-week trial period. No significant differences were observed in prostaglandin E2 (“PGE2”) plasma levels during the trial period in either treatment group; however serum amyloid A (“SAA”) levels were lower in canines in the Alpha-GEE treatment group compared to placebo at the...

example 2

Effects of Alpha-GEE and Ibuprofen on the Release of PGE2 in Brain Endothelial Cells

[0052]In this example, the effects of Alpha-GEE and Ibuprofen on the release of PGE2 from brain endothelial cells were compared. The brain endothelial cells were first exposed to bacterial endotoxin. The effects of Alpha-GEE and Ibuprofen were then measured and the levels of release of PGE2 were compared.

[0053]FIG. 1 demonstrates that the reduction in the release of PGE2 from brain endothelial cells at an Alpha-GEE concentration of about 20 μM or more is about 50 percent or more. The reduction in the release of PGE2 from brain endothelial cells at an Alpha-GEE concentration of about 1000 μM or more greater than about 50 percent. The reduction of PGE2 release observed with Alpha-GEE is similar in magnitude to the reduction of PGE2 release observed with ibuprofen treatment,

example 3

Effects of Alpha-GEE and Ibuprofen on Inhibition of Cyclooxygenase (“COX”) Activity

[0054]The effects of Alpha-GEE and Ibuprofen on the inhibition of cyclooxygenase-1 (“COX1”) and cyclooxygenase-2 (“COX2”) activity were also compared. As shown in FIG. 2, NSAIDs, such as ibuprofen, chemically bind to cyclooxygenase and inhibit prostaglandin production. Specifically, the NSAID, Ibuprofen, produced a concentration dependent inhibition of the COX enzymes when used at concentrations of 0.1-100 μM. For example, greater than about 60 percent of COX-1 and COX-2 activity is inhibited with Ibuprofen. In contrast, Alpha-GEE did not show a concentration dependency on the inhibition of COX enzymes. In other words, Alpha-GEE did not show a mechanistic inhibition of the COX enzymes. This suggests that the anti-inflammatory pathway for Alpha-GEE is different from that of NSAIDs commonly used to treat conditions such as OA.

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Abstract

A method and composition for treating osteoarthritis including administering an anti-inflammatory agent to a patient, wherein the anti-inflammatory agent is ethyl (α-guanido-methyl) ethanoate. Ethyl (α-guanido-methyl) ethanoate provides a safe, non-toxic anti-inflammatory treatment for osteoarthritis.

Description

FIELD OF THE INVENTION[0001]This invention relates to a method for treating osteoarthritis. In particular, the present invention is directed to a safe, non-toxic anti-inflammatory treatment for osteoarthritis. The present invention also relates to the anti-inflammatory agents for use in the method.BACKGROUND OF THE INVENTION[0002]Osteoarthritis (“OA”) is a prevalent, painful, but treatable inflammatory disease that affects millions of Americans. While current treatment modalities include weight reduction and various dietary supplements, such as glucosamine, chondroitin, and green lip mussel, OA is most commonly treated with a class of drugs known as non-steroidal anti-inflammatory drugs (“NSAIDs”), e.g., ibuprofen and Rimadyl. NSAIDs are generally effective but have a number of toxic side effects that compromise the gastrointestinal, renal, and / or cardiovascular health of many patients.[0003]It is clinically known that NSAID side effects include stomach bleeding, heart risks, and li...

Claims

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Application Information

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IPC IPC(8): A61K31/221A61K45/06
CPCA61K45/06A61K31/221A61K31/22
Inventor FAULKNER, MARK C.MILLER, DONALD W.CRAWFORD, GARY
Owner VIREO SYST
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