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Flavonoid composition for treating oral diseases

A composition and technology of flavonoids are applied in the field of prevention and treatment of diseases and diseases of the oral cavity, teeth and gums, and can solve the problems such as the existence of controversy in the mechanism of action of the anti-inflammatory activity of the unsubstituted B-ring flavonoids

Inactive Publication Date: 2007-12-05
UNIGEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0026] Mechanisms of action of various Free-B-ring flavonoids for anti-inflammatory activity are controversial

Method used

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  • Flavonoid composition for treating oral diseases
  • Flavonoid composition for treating oral diseases
  • Flavonoid composition for treating oral diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 11

[0132] Example 11 shows that UP676 can effectively inhibit the gene expression of a group of pro-inflammatory cytokines including IL-1β, TNFα and IL-6 in human cells. This experiment was performed using lipopolysaccharide (LPS)-stimulated human peripheral blood monocytic cells (PBMC), which is a well-established inflammatory cell model. When cells were co-incubated with different concentrations (0, 10, 30, and 100 μg / mL) of UP676, the gene expression of pro-inflammatory cytokines was inhibited in a dose-dependent manner. (Table 12).

[0133] Pro-inflammatory cytokines, especially IL-1β, TNFα and IL-6, play an important role in chronic infection of periodontal tissues. They not only activate and recruit immune cells at the site of infection, but also induce loss of supporting bone and ligamentous connections. It has been established that the mRNA levels of these cytokine genes are elevated in diseased periodontal tissue and that the synthesis of pro-inflammatory cytokines affec...

Embodiment 14

[0136] Example 14 (Table 13) describes the general procedure for the preparation of UP676 emulsion using pharmacologically, dermatologically and cosmetically suitable excipients. By way of illustration, this example provides a detailed procedure for the preparation of a 0.5% by weight UP676 topical emulsion. The composition of the present invention can also be formulated as a pharmaceutical composition, which includes other ingredients such as pharmaceutically and / or cosmetically acceptable excipients, adjuvants, flavoring agents and / or carriers. For example, compositions of the invention can be formulated in excipients that are tolerated by the subject to be treated. An excipient is an inert substance used as a diluent or carrier for a drug. Examples of such excipients include, but are not limited to, water, alcohol (ethanol or ethylene glycol, propylene glycol), buffer, saline, hydrated silicon dioxide, glucose solution, carboxymethylcellulose (cellulose gum), sorbitol Alc...

Embodiment 15

[0138] Example 15 illustrates the stability of catechins in solutions of different pH and preservatives. Catechin contains four phenolic hydroxyl groups, which make this compound highly acidic and sensitive to oxidative stress. Catechin has an extremely high oxygen radical absorption capacity (ORAC of 20,000), indicating its antioxidant properties. As shown in Figure 15, based on pure catechin in different conditions such as pH, H 2 o 2 and stress experiments in the presence of metal ions, determined that catechins were stable under neutral conditions and at 4°C and 40°C while under alkaline conditions or exposed to metal ions such as Fe 3+ unstable. Even under mildly alkaline conditions (pH=7.5) catechins decompose. However, it can be preserved in a variety of preservatives, including but not limited to stannous chloride (SnCl 2 ), sodium bisulfate / sodium metabisulfite (SBS), and other preservatives listed in Figure 16.

[0139] In a preferred embodiment, an additional ...

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Abstract

The present invention provides a novel composition of matter comprised of a mixture of two specific classes of compounds --Free-B-Ring flavonoids and flavans-- for use in the prevention and treatment of diseases and conditions associated with mouth, gums and teeth. This composition of matter simultaneously inhibits cyclooxygenase (COX) and lipoxygenase (LOX) enzymatic activity and reduces cytokine production at the mRNA level in normal, aged and damaged periodontal cells and tissues. This invention further provides a method for the prevention and treatment of diseases and conditions of the mouth, gums and teeth. The method for preventing and treating diseases and conditions of the mouth, teeth and gums is comprised of administering to a host in need thereof a therapeutically effective amount of a composition comprising a mixture of Free-B-Ring flavonoids and flavans synthesized and / or isolated from a single plant or multiple plants, preferably in the Scutellaria, Oroxylum, Acacia or Uncaria genus of plants and pharmaceutically and / or cosmetically acceptable carriers. Finally the present invention provides a method for the prevention and treatment of diseases and conditions of the mouth, teeth or gums, including but not limited to periodontal diseases, such as gingivitis, periodontitis, pulpitis, periodontal conditions caused by the physical implantation of oral dentures, trauma, injuries, bruxism, neoplastic and other degenerative processes; material alba, pellicles, dental plagues, calculus, and stains. Use of the composition described herein also affords the benefit of maintaining optimum saliva production and pH, minimizing bacterial growth, reducing the formation of pellicles and plague, inhibiting tooth decalcification and tooth caries (decay), promoting remineralization, which yields healthy gums, whitening teeth, maintaining healthy oral hygiene and reducing oral malodour (halitosis).

Description

technical field [0001] The present invention generally relates to novel compositions comprising mixtures of two specific classes of compounds targeting eicosanoid and cytokine pathways, Free-B-Ring flavonoids and flavanoids, for prophylactic and therapeutic Diseases and conditions of the mouth, teeth and gums. Specifically, the diseases and diseases of the oral cavity, teeth and gums include but are not limited to periodontal diseases, such as gingivitis, periodontitis, pulpitis, caused by implantation of dentures (physical implantation of oral dentures), trauma, injury, Periodontal conditions caused by bruxism, tumors and other degenerative processes; white scale, bacterial film, plaque, calculus and tartar. Application of the compositions described herein may also provide the benefits of maintaining optimal saliva production and pH, minimizing bacterial growth, reducing plaque and plaque formation, inhibiting tooth decalcification and dental caries (cavity), promoting miner...

Claims

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Application Information

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IPC IPC(8): A61K31/35A61K9/00A61K9/68A61K47/00A61K8/00A61K9/14A61K8/97
CPCA61K8/602A61K31/353A61K36/484A61K36/48A61K36/54A61K36/9062A61K36/539A61K36/53A61Q11/00A61K31/352A61K36/486A61K36/185A61K45/06A61K36/15A61K31/553A61K36/906A61K36/47A61K36/28A61K31/7048A61K2800/782A61K8/498A61K36/60A61K36/11A61P1/02A61P29/00A61P31/04A61P43/00Y02A50/30A61K2300/00A61K9/14
Inventor 贾琦赵垣
Owner UNIGEN
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