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Pyruvate and related alpha-keto carboxylates as novel adjuvants in the treatment of post tooth whitening sensitivity and the tissue protective effect of pyruvate on the oral soft tissue

a technology of alpha-keto carboxylate and pyruvate, which is applied in the direction of anhydride/acid/halide active ingredients, dentistry, pharmaceutical delivery mechanisms, etc., can solve the problems of irritating many different tissues such as the skin, eyes, esophagus and stomach, and extensive tissue damage, and achieves considerable tooth sensitivity, discomfort or even direct pain

Inactive Publication Date: 2017-08-24
RUSZNAK ZOLTAN +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent aims to provide a pharmaceutical composition that uses pyruvate or related a-keto carboxylates as active ingredients to treat post-tooth-whitening sensitivity. It also seeks to take advantage of the cytoprotective effect of pyruvate in oral soft tissue after application of an external high-concentration-H2O2 insult.

Problems solved by technology

Exogenous Hydrogen Peroxide is known to cause irritation to many different tissues such as the skin, eyes, esophagus and stomach.
Inadvertent exposure of oral soft tissues to a concentrated solution of H2O2 is known to cause extensive tissue damage in the form of vesicle formation and ulceration.
Commonly voiced complaints by patients when treated with bleaching agents at commercially available concentrations are considerable tooth sensitivity, discomfort or even direct pain.
No effective treatment is yet known or in development to mitigate or perhaps abolish the discomfort and pain of current teeth whitening techniques and procedures.
Although fluoridated applications are generally effective, the relief of discomfort and sensitivity is not immediate, as it will take weeks to become effective; this delayed effect is probably due to the slow apposition of the fluoridated compounds in the openings of the dentinal tubules.
This creates an osmotic gradient for and out flux of the dentinal tubular fluid resulting in pain (tooth sensitivity) felt by the patient.
It is this outflow of dentinal fluid that is generally assumed to cause an acute discomfort (tooth sensitivity) for the patient.
The relative sensitivities of pulpal, gingival and periodontal ligament cells to toxic effects of hydrogen peroxide are important given the potential for diffusion of hydrogen peroxide through dentine, and thus resulting in pain.
The reaction between H2O2 and dentin's inorganic compounds could result in the formation of harmful acid by-products such as hydrogen phosphate.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

Novel Dental Applications of Pyruvate and Related Alpha Keto Carboxylates

[0065]As a scavenger of H2O2 and related ROS during and after the process of tooth whitening,

[0066]As an oxidizing redox metabolite: Increased NAD+ / NADH ratio, inhibition of NADHoxidase and hence inhibition of formation of superoxide radical and likely release of inflammatory cytokines,and pyruvate also strengthens the reductive power of the glutathione system, the first line of defense against oxidative stress.

[0067]These two principal effects of pyruvate suggest it could be beneficial in H2O2-based tooth whitening procedures by ameliorating or perhaps even abolishing discomfort and pain of the procedure

[0068]Although deleterious tooth sensitivity is a common side effect of external tooth whitening of otherwise healthy teeth, the etiology is poorly understood.

It is known that dentin hypersensitivity primarily results from the exposure to H2O2 in presence of open dentinal tubules.

[0069]This hydrodynamic theory ...

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Abstract

This invention describes pyruvate and related α-ketocarboxylates as novel adjuvants in the treatment of acute post-tooth-whitening pain and sensitivity; the key feature is the cytoprotective efficacy of pyruvate on oral soft tissue, especially after topical application of high and therefore cytotoxic concentrations of H2O2, currently used in tooth whitening procedures.

Description

I. TECHNICAL FIELD OF THE INVENTION[0001]The invention is in the field of protecting, preserving and restoring normal cell functions. More specifically it is in the field of using alpha-keto carboxylic acid salt compositions as prophylactic and therapeutic agents to prevent the deterioration or promote the restoration and preservation of normal cell functions in the oral cavity.II. BACKGROUND OF THE INVENTION[0002]Hydrogen peroxide (H2O2), carbamide peroxide (CP) and peroxo-adducts of inorganic anions such as peroxoborate, peroxodisulphate and peroxocarbonate as agents for the bleaching of discolored teeth in professional and commercially-available tooth-whitening products such as gels, toothpastes and oral rinses has created much interest regarding their mechanisms of action and redox activity in oral environment as well as adverse effects and safety consideration.[0003]This invention is directed to a novel method of using a therapeutic composition comprising a compound of an α-ket...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K8/365A61K9/00A61K8/22A61K31/19A61Q11/00
CPCA61K8/365A61K31/19A61Q11/00A61K2800/592A61K9/006A61K2800/882A61K2800/74A61K8/22
Inventor RUSZNAK, ZOLTANBUNGER, ROLF
Owner RUSZNAK ZOLTAN