Dental Composition Comprising Potassium Nitrate 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 10% potassium nitrate and 0.5% of propolis; the propolis providing occlusion of tubules and the potassium nitrate providing depolarization of nerve membranes.

Claims

1) A dental formulation for the prevention and treatment of dental caries and dentinal hypersensitivity, the formulation comprising propolis as a first active agent and potassium nitrate 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 potassium nitrate proportion is from about 5 wt. % to about 10 wt. %.

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

8) The dental formulation of claim 6, wherein the potassium nitrate proportion is about 10 wt. %.

9) A dental formulation for the prevention and treatment of dental caries and dentinal hypersensitivity, comprising: about 34.07 wt. % of water; about 31 wt. % of sorbitol; about 18 wt. % of hydrated silica; about 10 wt. % of potassium nitrate; about 1.75 wt. % of glycerin; about 1 wt. % of PVP; about 1 wt. % of CI 77891; about 0.855 wt. % of sodium lauroyl sarcosinate; about 0.8 wt. % of cellulose gum; about 0.5 wt. % of aroma; about 0.5 wt. % of propolis; about 0.3 wt. % of xanthan gum; about 0.2 wt. % of sodium saccharin; and about 0.02174 wt. % of limonene.

Description

DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT

[0027] A novel dental formulation comprising potassium nitrate 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.

[0028] 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.

[0029] 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.

[0030] First, the usefulness of 10% of potassium in toothpaste formulations as a neural desensitization against DH was tested. The goal being to explore modernly the testing of a 10% toothpaste formulation as desensitizing agent and estimate the effect magnitude. The test was designed to observe the effect with cross-over treatments. Twenty patients with DH symptoms were voluntary recruited from two Quebec dental clinics. The criteria for entering the test was a formal dissatisfaction about the perceived effect against their sensitivity (hot/cold food and drink, air, tooth brushing, and sweet and sour food) with their current commercial toothpaste. To be accepted, participants had to provide a score of 7 or less on 10 in which 0 indicated no effects and 10 indicated ideal effects from their current commercial toothpaste against DH. The majority of the patients reported a prior use of Sensodyne® from Glaxo Smith Kline® and a few of them reported a use of Sensitive Pro Relief® from Colgate Palmolive®. The two above-mentioned toothpastes are formulated with 5% of potassium nitrate. All recruited patients reported suffering of DH for an average of 11 years. Their dissatisfaction score prior to the test had an average score of perceived effect of 5.6 on 10. This score expresses a residual lack of ideal effect of about 4.4 out of 10. Participants were then asked to brush twice a day with a formulation comprising 10% of potassium nitrate. Results showed that a positive effect was perceived after 4.1 days on average. From the total of 20 participants, the perceived effectiveness was 7.3 out of 10. Increasing the concentration from 5% to 10% thus increased the effectiveness by 17% compared the previously used commercial toothpastes. All patients further confirmed an interest in switching to the toothpaste formulation comprising 10% potassium nitrate in the future.

[0031] Next, the minimal propolis concentration to have a clinical desensitized effect using an at-home toothpaste vehicle was tested. It is known that pain is a subjective experience and depends on various factors, such as the psychological profile of the individual, his/her previous pain experiences and levels of anxiety. Other aspects that can make the interpretation of alleviating effects of desensitizing agents difficult are the Hawthorne effect. To prevent those potential bias, it was decided to adopt a small randomized control trial as a pilot test. A total of seven different propolis concentrations were tested, though only the results for the first three concentrations are relevant. Ten patients were then recruited that used a commercial toothpaste (mostly Sensodyne®) against DH. The patients were asked to stop the use of the commercial toothpaste until their symptoms were back. All patients were blinded to the exact concentration of propolis and randomly allocated a formulation comprising said concentration of propolis. The first five patients were exposed to three propolis concentrations: 0.25%, 0.50% and 0.75%. Each patient was exposed to all three concentrations. They were asked to qualify, out of 10, the effect of the propolis exposure compared to their actual commercial toothpaste against DH. The score of 10 meant no pain and 0 the highest level of pain. The new toothpaste formulations were tested for three weeks. The concentrations of 0.25% and 0.75% had no reported effect. Formulations with propolis at 0.50% had a significant effect (between 7 and 8 out of 10) and was judged with more impact by patients compared to the commercial toothpastes. Surprisingly, no dose dependent response was observed.

[0032] Given the outcome of two studies related to potassium nitrate at 10% and to propolis at 0.5% both against DH symptoms, a test for the potential synergy and complementarity of both ingredients together was to be undertaken. Testing both treatment approaches is meant to reduce pain by targeting the pulpal nerves directly, typically with potassium nitrate, and at the same time by occluding the dentin tubules with propolis. Again, an observational test with cross-over treatments was used. Ten patients with severe DH symptoms were voluntary recruited from two Quebec dental clinics. Recruiting criteria for the test was a formal dissatisfaction about the perceived of the effect of the commercially used toothpaste of the patients against their sensitivity (hot/cold food and drink, air, tooth brushing, and sweet and sour food). To be accepted, participants had to provide a score of 7 or less out of 10, in which 0 indicated no effect and 10 indicated ideal effects against DH. Furthermore, patients with severe abrasion condition, with pain during orthodontic adjustments and patients under whitening treatment leading to pain were recruited. The majority of them reported a prior use of Sensodyne® from Glaxo Smith Kline® and a few of them, using Sensitive Pro Relief® from Colgate Palmolive®. Their dissatisfaction had an average score of perceived effect of 4.6 out of 10. This score express a residual lack of ideal effect of about 5.4 out of 10. Participants were then asked to brush twice a day with a formulation comprising 10% of potassium nitrate and 0.5% of propolis. Results showed that an effect was perceived after 2.1 days on average. The total of 10 participants gave an average score of 8.2 out of 10, which is an improvement of 36% compared the previous commercial toothpastes effect perception. This increasing of the concentration reduced the ultimate effect goal of 10, by 3.6 units. All patients confirmed their interested to adopt this toothpaste in the future.

[0033] Example 1 provides a representative toothpaste formulation of the invention. The formulation comprises 0.50% of propolis and 10% of potassium nitrate.

TABLE-US-00001 INGREDIENTS % wt Water 34.07 Sorbitol 31 Hydrated silica 18 Potassium nitrate 10 Glycerin 1.75 PVP 1 Cl 77891 1 Sodium lauroyl sarcosinate 0.855 Cellulose gum 0.8 Aroma 0.5 Propolis 0.5 Xanthan gum 0.3 Sodium saccharin 0.2 Limonene 0.02174

[0034] This combination of propolis and potassium nitrate in such concentrations in toothpastes may provide an alternative to patients suffering from severe DH.

[0035] 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.

[0036] 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.