Dental formulation comprising xylitol and propolis

Abstract

The present invention provides a dental formulation for the prevention and treatment of dental caries and dental hypersensitivity. The dental formulation is a toothpaste formulation comprising 25% of xylitol and 0.5% of propolis.

Claims

1) A dental formulation for the prevention and treatment of dentinal hypersensitivity, and dental caries, the formulation comprising propolis as a first active agent and xylitol as a second active agent.

2) The dental formulation of claim 1, wherein the propolis proportion is from about 0.25 wt. % to about 2.00 wt. %.

3) The dental formulation of claim 2, wherein the propolis proportion is about 0.50 wt. %.

4) The dental formulation of claim 1, the formulation further comprising at least a carrying agent, a moisturizing agent, a thickening agent, an abrasive agent, a flavor agent, a surfactant agent and a foaming agent.

5) The dental formulation of claim 4, the formulation comprising water, barbadensis leaf juice, propolis, hydroxyethyl cellulose, magnesium aluminum silicate, calcium carbonate, lemon flavor, sodium bicarbonate and sodium lauryl sulfoacetate.

6) The dental formulation of claim 1, wherein the xylitol proportion is from about 5 wt. % to about 25 wt. %.

7) The dental formulation of claim 6, wherein the xylitol proportion is about 5 wt. %.

8) The dental formulation of claim 6, wherein the xylitol proportion is about 25 wt. %.

9) A dental formulation for the prevention and treatment of dental caries and dentinal hypersensitivity, comprising: about 19.83 wt. % of water; about 43 wt. % of sorbitol; about 19 wt. % of hydrated silica; about 7 wt. % of glycerin; about 5 wt. % of xylitol; about 2 wt. % of propolis; about 1.178 wt. % of sodium C14-16 olefin sulfonate; about 1 wt. % of CI 77891; about 0.8 wt. % of cellulose gum; about 0.5 wt. % of aroma; about 0.3 wt. % of xanthan gum; about 0.2 wt. % of sodium saccharin; about 0.17 wt. % of sodium benzoate; and about 0.02174 wt. % of limonene.

10) A dental formulation for the prevention and treatment of dental caries and dentinal hypersensitivity, comprising: about 34.42 wt. % of water; about 25 wt. % of xylitol; about 17.5 wt. % of hydrated silica; about 17.36 wt. % of sorbitol; about 1.75 wt. % of glycerin; about 1 wt. % of CI 77891; about 0.8 wt. % of cellulose gum; about 0.527 wt. % of sodium lauroyl sarcosinate; about 0.5 wt. % of aroma; about 0.5 wt. % of propolis; about 0.3 wt. % of xanthan gum; about 0.17 wt. % of sodium benzoate; about 0.13 wt. % of calcium glycerophosphate; about 0.02 wt. % of sodium saccharin; and about 0.02174 wt. % of limonene.

Description

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT

[0043] A novel dental formulation comprising xylitol and propolis will be described hereinafter. Although the invention is described in terms of specific illustrative embodiment(s), it is to be understood that the embodiment(s) described herein are by way of example only and that the scope of the invention is not intended to be limited thereby.

[0044] As used herein % or wt. % means % by weight as compared to the total weight percent of the phase or composition that is being discussed unless otherwise indicated.

[0045] By “about”, it is meant that the value of weight % can vary within a certain range depending on the margin of error of the method or device used to evaluate such weight %. A margin of error of 10% is generally accepted.

[0046] A total of three different propolis concentrations were first prepared. Five patients using a commercial toothpaste (mostly Sensodyne®) against DH were then recruited. They were asked to stop the use of the commercial toothpaste until the DH symptoms were back. Each patient was then assigned a propolis formulation to use; the exact propolis concentration being unknown to them and randomly allocated. They were asked to qualify the propolis exposure compared to their actual commercial toothpaste against DH. They were then asked to assess the pain from a scale of 1 to 10, with 10 being no pain, the effect using the responsiveness strategy. The new toothpaste was tested for three weeks. The first five patients were exposed to one out of three propolis concentrations at a time: 0.25%, 0.50% and 0.75%. Each patient was exposed to all three concentrations. The concentrations of 0.25 and 0.75 had no reported effect. The formulation with propolis at 0.50% had a significant effect, between 7 and 8 on the pain scale, and was judged as having more impact for the treatment of DH by patients compared to their commercial one. Surprisingly, no dose dependent response was observed.

[0047] Given previous studies outcome related to formulations comprising 25% xylitol and to the new results of the formulation study comprising propolis at 0.5%, both against caries and DH symptoms, the potential synergy and complementarity of both agents now has ground to be tested. No other publications documented this specific benefice of mixing 25% of xylitol to 0.5% of propolis in a dental formulation to combine the anti-caries and anti-sensitivity properties.

[0048] In order to test the obtained formulation, an observational test with cross-over treatments was performed. Ten patients, with the intention to use toothpaste comprising 25% xylitol, were complaining about the absence of anti-sensitive agents in the formulation. They all had a history with DH symptoms and were voluntarily recruited from two Quebec dental clinics. Having a desensitizing agent was a criteria for the treatment of DH with their current commercial toothpaste. All participants were evaluated using a scale from 0 to 10, in which 0 indicated no effect and 10 indicating an optimal effect. The majority of them reported the use of a commercially available Sensodyne® from Glaxo Smith Kline™. Their actual satisfaction with their commercially available toothpaste generated an average score of 7.0 out of 10. Participants were then asked to brush twice a day with the formulation samples of 25% xylitol and 0.5% propolis. Results showed that a positive effect was perceived within 3 days on average. On average, the participants gave a score of 8.0 out of 10, which firmly proves that the formulation provides benefits against both dental caries and DH. Furthermore, all recruited patients confirmed their interested to adopt this toothpaste in the future.

[0049] Another trial with five other patients and a similar approach was also conducted. In this trial, each patient was exposed to four concentrations of propolis: 1.00%, 1.25%, 1.50% and 2.00%. The trial lasted for 2 months before the results were compiled. This time, the results were the most promising with a concentration of 2.00% which resulted in a rating average of 7.7 out of 10.

[0050] These results support the effectiveness of a propolis-based toothpaste. More so, those results prove that simply increasing the propolis concentration does not automatically equate to increased positive results. Increasing the concentration from 0.5% to 0.75% did, in fact, diminish the positive impacts of the formulation. It is therefore important to have a specific concentration of propolis in a given formulation that was pre-emptively tested so as to ensure desired performance. Furthermore, most patients were interested in replacing their present commercially available toothpaste with a natural one having propolis as the active agent against DH.

[0051] Example 1 provides a representative toothpaste formulation of the invention which comprises 2% of propolis as the only active agent against DH.

TABLE-US-00001 INGREDIENTS % wt Water 19.83 Sorbitol 43 Hydrated silica 19 Glycerin 7 Xylitol 5 Propolis 2 Sodium C14-16 olefin sulfonate 1.178 Cl 77891 1 Cellulose gum 0.8 Aroma 0.5 Xanthan gum 0.3 Sodium saccharin 0.2 Sodium benzoate 0.17 Limonene 0.02174

[0052] In a further embodiment, the toothpaste formulation may comprise propolis and a high amount of xylitol. The formulation may comprise 0.5% or propolis and about 25% of xylitol. Xylitol is an ingredient that has proven its effectivity against cavities, especially in commercially available toothpastes such as Cari0®.

[0053] Example 2 provides a representative toothpaste formulation of the invention. The formulation comprises 0.5% of propolis and 25% of xylitol.

TABLE-US-00002 INGREDIENTS % wt Water 34.421 Xylitol 25 Hydrated silica 17.5 Sorbitol 17.36 Glycerin 1.75 Cl 77891 1 Cellulose gum 0.8 Sodium lauroyl sarcosinate 0.527 Aroma 0.5 Propolis 0.5 Xanthan gum 0.3 Sodium benzoate 0.17 Calcium glycerophosphate 0.13 Sodium saccharin 0.02 Limonene 0.02174

[0054] Furthermore, the tested toothpaste formulations had the following characteristics. Tested with a PHmetry test diluted at 25%, the pH value of each formulation varied between 6 to 8. A densimeter test revealed a density of about 1.35 g/mL for each formulation. Both tests of aerobic mesophilic flora and moulds and yeasts resulted in under 100 Ufc/g as per rapid microbiological method and/or UNE/EN/ISO 21149:2017 and UNE/EN/ISO 16212:2017. More so, there was an absence of pathogenic microorganisms in the formulations from the tests of absence/presence, rapid microbiological method and/or UNE/EN/ISO 21150:2016, UNE/EN/ISO 22717:2016, UNE/EN/ISO 22718:2016 and UNE/EN/ISO 18416:2016. Additionally, each toothpaste formulation had the following characteristics based on sensorial testing methods: they had a pasty texture, their color was a slightly yellowish white and they tasted like sweet mint. These characteristics are further proof that the different formulations, representing different aspects of the invention, are well suited for at-home usage.

[0055] While illustrative and presently preferred embodiment(s) of the invention have been described in detail hereinabove, it is to be understood that the inventive concepts may be otherwise variously embodied and employed and that the appended claims are intended to be construed to include such variations except insofar as limited by the prior art.