US-12622865-B2 - Oral care compositions and methods of use

US12622865B2US 12622865 B2US12622865 B2US 12622865B2US-12622865-B2

Abstract

This invention relates to oral care compositions comprising herbal extracts including, e.g., Gymnema sylvestre, Emblica officinalis, Eugenia jambolana, Azadirachta indica , and combinations thereof and zinc salts, e.g., zinc citrate and zinc oxide. Additionally, the invention relates to methods of using and of making these compositions, e.g., method of using the oral care compositions to treat gingivitis in diabetic consumers.

Inventors

Manas VYAS
Sandip REGE
Ekta MAKWANA
Manish MANDHARE
Manisha JHA
Bernal Stewart
Payal Arora
Bhagyashri CHAVAN

Assignees

COLGATE-PALMOLIVE COMPANY

Dates

Publication Date: 20260512
Application Date: 20211202
Priority Date: 20201202

Claims (16)

1 . An oral care composition comprising: a. an effective amount of a zinc ion source; b. a fluoride source; and c. an herbal extract consisting of: from 0.1 to less than 0.5 wt. % of Gymnema sylvestre extract, based on the weight of the oral care composition, and Eugenia jambolana extract, and optionally melia azadirachta seed oil and/or amla extract, wherein the oral care composition is free of herbal extracts other than Gymnema sylvestre extract, Eugenia jambolana extract, melia azadirachta seed oil and amla extract, and wherein the oral care composition demonstrates at least a 35% reduction in gum sponginess, relative to a control that does not contain the zinc ion source and the herbal extract, wherein the reduction is measured by a Visual Analog Scale.
2 . The oral care composition of claim 1 , wherein the zinc ion source comprises zinc citrate and zinc oxide, where the wt. % ratio of the amount of zinc oxide to zinc citrate is from 1.5:1 to 4.5:1.
3 . The oral care composition of claim 1 , wherein the zinc ion source comprises zinc citrate and zinc oxide, wherein the zinc citrate is present in an amount of from 0.25 to 1 wt. % and zinc oxide is present in an amount of from 0.75 to 1.25 wt. %, based on the weight of the oral care composition.
4 . The oral care composition of claim 1 wherein the fluoride source is selected from: stannous fluoride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, sodium fluorosilicate, ammonium fluorosilicate, amine fluoride, ammonium fluoride, titanium fluoride, hexafluorosulfate, or combinations thereof.
5 . The oral care composition of claim 4 , wherein the fluoride source is sodium monofluorophosphate.
6 . The oral care composition of claim 1 wherein the herbal extract includes amla extract.
7 . The oral care composition of claim 6 wherein the oral care composition includes melia azadirachta seed oil.
8 . The oral care composition of claim 1 , wherein the composition comprises: a. from 0.5 to 1.5 wt. % zinc oxide; b. from 0.25 to 0.75 wt. % zinc citrate; c. from 0.5 to 1.0 wt. % of sodium monofluorophosphate; and d. from 0.2 to 0.5 wt. % of a combination of Gymnema sylvestre extract, Eugenia jambolana extract, melia azadirachta seed oil, and amla extract, wherein all weight percentages are based on the total weight of the oral care composition.
9 . The oral care composition of claim 1 , wherein the composition comprises: a. from 0.5 to 1.5 wt. % of zinc oxide; b. from 0.25 to 0.75 wt. % of zinc citrate; c. from 0.5 to 1.0 wt. % of sodium monofluorophosphate; and d. an herbal extract consisting of: from 0.2 to 0.5 wt. % of Gymnema sylvestre extract, and Eugenia jambolana extract, wherein all weight percentages are based on the total weight of the oral care composition.
10 . The oral care composition of claim 1 , wherein the oral care composition is in a form selected from: a toothpaste, transparent paste, gel, mouth rinse, spray or chewing gum.
11 . The oral care composition of claim 1 , wherein the oral care composition demonstrates at least a 50% reduction in gum bleeding, relative to the control, wherein the reduction is measured by the Loe-Silness Gingival Index.
12 . The oral care composition of claim 1 , wherein the oral care composition demonstrates at least a 25% reduction in gum bleeding, relative to the control, wherein the reduction is measured by a Visual Analog Scale.
13 . The oral care composition of claim 1 , wherein the oral care composition is administered in an amount effective to reduce IL-1β mediated inflammation.
14 . A method for treating or reducing gingivitis in a subject in need thereof, wherein the method comprises administering an oral care composition of claim 1 to the subject in need thereof.
15 . The method of claim 14 , wherein the subject is at risk because the subject is diabetic or has been diagnosed with diabetes.
16 . An oral care composition comprising: a zinc source; a fluoride source; from 20 to 50 wt. % of a calcium carbonate; water; and an herbal extract present in a total amount of 0.2 to 0.5 wt. %, the herbal extract consisting of Gymnema sylvestre extract and amla extract, wherein the oral care composition is free of herbal extracts other than Gymnema sylvestre extract and amla extract, and wherein all weight percentages are based on the total weight of the oral care composition.

Description

This invention relates to oral care compositions comprising herbal extracts including, e.g., Gymnema sylvestre, or Emblica officinalis, or Eugenia jambolana, or Azadirachta indica, and combinations thereof and zinc salts, e.g., zinc citrate and zinc oxide. Additionally, the invention relates to methods of using and of making these compositions, e.g., method of using the oral care compositions to treat gingivitis in diabetic consumers. BACKGROUND Gingivitis is an inflammation of gums. If not treated at the early stage it leads to a more severe condition called Periodontitis. Gingivitis occurs in a significant proportion of adults. One of the major risk factors for gingivitis is diabetes. While the mechanisms of action are not completely understood, previous research has demonstrated that there may be a relationship between the degree of hyperglycaemia and severity of periodontitis. There is some understanding in the field that diabetes can have deleterious downstream effects on immune dysfunction, cellular stress and cytokine imbalance (e.g., inflammation). Some of the various inflammatory cytokines that can be increased with the diabetic condition can include, e.g., TNF-alpha, IL-6, and IL-1β. Researchers in the field have posited that diabetes increases the risk for periodontal inflammation then negatively affecting glycaemic control. However, some have indicated that treatment of periodontitis is associated with HbA1c reductions of approximately 0.4%. See e.g., Preshaw, P. et al., Diabetologia. 2012 January; 55(1): 21-31. Accordingly, diabetic individuals can have specific treatment needs that pertain to oral health maintenance. Accordingly, there is a current need for a toothpaste for individuals that have gingivitis, at risk for periodontal disease, diabetes, or that are at risk for diabetes. BRIEF SUMMARY It is believed that the current formulations offer the advantage of treatments that can be beneficial to individuals that have gingivitis, or at risk for gingivitis, in diabetic consumers, or those that are at risk for diabetes, and/or inflammation or gum bleeding in the oral cavity. In one aspect, oral care compositions of the described herein are generally effective for treating inflammation, bleeding and gingivitis in the oral cavity (e.g., specifically acting upon the gingival tissue). In one aspect, the composition is specifically useful to treat inflammation in the oral cavity that is mediated by IL-1β, e.g., in diabetic individuals that have IL-1β mediated inflammation. In one aspect, the application contemplates that a formulation with an herbal extract source comprising, e.g., Gymnema sylvestre, Emblica officinalis, Eugenia jambolana, Azadirachta indica along with zinc salts (e.g., zinc citrate and zinc oxide) can be useful to treat gingivitis, individuals at risk for gingivitis in diabetic consumers, or individuals at risk for diabetes. In one aspect, the inventors have found that gurmar raw material has in-vitro efficacy as an anti-inflammatory compound. In another aspect, it was determined that in toothpastes with gymnema sylvestre could reduce inflammation and gum bleeding significantly in clinical studies, as compared to control samples that did not contain any gymnema sylvestre. In one aspect the invention is an oral care composition (Composition 1.0) comprising: a. an effective amount of a zinc ion source (e.g., a zinc ion source comprising zinc citrate and zinc oxide)b. A fluoride source (e.g., sodium monofluorophosphate); andc. An herbal extract source comprising Gymnema sylvestre, or Emblica officinalis, or Eugenia jambolana, or Azadirachta indica, and combinations thereof. For example, the invention contemplates any of the following compositions (unless otherwise indicated, values are given as percentage of the overall weight of the composition) 1.1 Composition 1.0 further comprising a polyphosphate.1.2 Any of the preceding compositions wherein the zinc ion source comprises zinc citrate and zinc oxide, wherein the ratio of the amount of zinc oxide (e.g., wt. %) to zinc citrate (e.g., wt %) is from 1.5:1 to 4.5:1 (e.g., 2:1, 2.5:1, 3:1, 3.5:1, or 4:1).1.3 Any of the preceding compositions comprising zinc citrate and zinc oxide, wherein the zinc citrate is in an amount of from 0.25 to 1 wt % (e.g., 0.5 wt. %) and zinc oxide may be present in an amount of from 0.75 to 1.25 wt % (e.g., 1.0 wt. %) based on the weight of the oral care composition.1.4 Any of the preceding compositions comprising zinc oxide and zinc citrate wherein the zinc citrate is about 0.5 wt % relative to the total weight of the oral care composition (e.g., zinc citrate trihydrate).1.5 Any of the preceding compositions comprising zinc oxide and zinc citrate wherein the zinc oxide is about 1.0 wt % relative to the total weight of the oral care composition.1.6 Any of the preceding compositions comprising zinc oxide and zinc citrate where the zinc citrate is about 0.5 wt % and the zinc oxide is about 1.0 wt %, relative