Aqueous ionic solution, made from dissolved mineral salts, in particular intended for throat care

Abstract

An aqueous ionic solution based on dissolved mineral salts, in particular intended for throat care, especially for the treatment, prevention and relief of manifestations related to sore throats. The aqueous ionic solution includes: by way of aqueous solvent, at least 20% by weight, with respect to the total weight of the composition, of a hypertonic solution of mineral salts having an osmolality greater than 350 mOsm/kg; at least 50% of one or more polyols of plant origin, by weight with respect to the total weight of the ionic solution; at least one sucrose and C8-C24 fatty acid ester, by weight with respect to the total weight of the ionic solution; and a non-alcoholic extract of propolis and/or between 1% and 8% honey, by weight with respect to the total weight of the ionic solution.

Claims

1. Aqueous anionic solution, in particular intended for throat care, comprising: by way of aqueous solvent, at least 20% by weight, with respect to the total weight of the composition, of a hypertonic solution of mineral salts having an osmolality greater than 350 mOsm/kg, at least 50% of one or more polyols of plant origin, by weight with respect to the total weight of the ionic solution, between 0.01 and 1.00% of at least one sucrose and C8-C24 fatty acid ester, by weight with respect to the total weight of the ionic solution, an extract of propolis and/or honey.

2. The aqueous ionic solution according to claim 1, wherein it comprises between 20% and 40%, by weight with respect to the total weight of the ionic solution, of said hypertonic solution of mineral salts having an osmolality greater than 350 mOsm/kg.

3. The Aqueous ionic solution according to claim 1 or claim 2, wherein the mineral salt solution is a solution based on diluted or non-diluted seawater or a saline solution containing between 22 and 25 g/l, of dissolved mineral salts of sodium, chlorine, sulfate, magnesium, calcium and potassium.

4. The aqueous ionic solution according to claim 1, wherein it comprises between 50% and 65% of said polyol or polyols of plant origin, by weight with respect to the total weight of the ionic solution.

5. The aqueous ionic solution according to claim 1, wherein the polyol or polyols of plant origin are glycerol to at least 90%, by weight with respect to the total weight of said polyols, and the sorbitol to 5% to 10% by weight with respect to the total weight of said polyols.

6. The aqueous ionic solution according to claim 1, wherein it comprises between 0.5% and 8% of said extract of propolis and/or between 1% and 8% honey, by weight with respect to the total weight of the ionic solution.

7. The aqueous ionic solution according to claim 1, wherein it also comprises at least one essential oil, in a proportion of between 0.001% and 2%, by weight with respect to the total weight of the ionic solution.

8. The aqueous ionic solution according to claim 7, wherein the essential oils are chosen from essential oils of gaultheria, ravintsara, thyme linalool, niaouli, rosemary, marjoram sylvester or any essential oil rich in 1,8 cineole compound.

9. The aqueous ionic solution according to claim 8, wherein it contains essential oil of gaultheria alone or in a mixture with at least one of said essential oils.

10. The aqueous ionic solution according to claim 1, wherein it also has a pH of between 4 and 6.

11. The aqueous ionic solution according to claim 1, wherein it has a viscosity at 20 of at least 15 mPa.Math.s.

12. The aqueous ionic solution according to claim 1, wherein it comprises, by weight with respect to the total weight of the ionic solution: 25% to 40% hypertonic solution of mineral salts having an osmolality greater than 350 mOsm/kg, based on pure or diluted seawater, at least 50% glycerol, between 0.5% and 8% sorbitol, between 0.5% and 8% hydroglycerine extract of propolis, between 1.0% and 8.0% honey, between 0.01% and 1.00% sucrose and C8-C24 fatty acid ester, between 0.5% and 8% ethyl alcohol (96%), between 0 and 2%, one or more essential oils of gaultheria, thymus zygis, ravintsara, niaouli, rosemary, marjoram sylvester or any essential oil rich in 1,8 cineole compound, between 0.1% and 2% one or more flavourings, between 0.1% and 0.2% pH regulating agent.

13. The aqueous ionic solution according to claim 12, wherein it contains between 0.001% and 0.08% of essential oil of gaultheria, by weight with respect to the total weight of the ionic solution.

14. A method for throat care and treatment of throat pain which comprises spraying an aqueous ionic solution as defined in claim 1.

15. The aqueous ionic solution according to claim 1, wherein it comprises 32% by weight with respect to the total weight of the ionic solution, of said hypertonic solution of mineral salts having an osmolality greater than 350 mOsm/kg.

16. The aqueous ionic solution according to claim 1, wherein the mineral salt solution is a solution based on diluted or non-diluted seawater or a saline solution containing between 22 and 23 g/l of dissolved mineral salts of sodium, chlorine, sulfate, magnesium, calcium and potassium.

17. The aqueous ionic solution according to claim 1, wherein the polyol or polyols of plant origin are glycerol to at least 95%, by weight with respect to the total weight of said polyols, and the sorbitol to 5% to 10% by weight with respect to the total weight of said polyols.

18. The aqueous ionic solution according to claim 1, wherein it also has a pH of between 4.5 and 5.5.

19. The aqueous ionic solution according to claim 1, wherein it comprises, by weight with respect to the total weight of the ionic solution: 25% to 40% hypertonic solution of mineral salts having an osmolality greater than 350 mOsm/kg, based on pure or diluted seawater, at least 50% glycerol, between 0.5% and 8% sorbitol, between 0.5% and 8% hydroglycerine extract of propolis, between 1.0% and 8.0% honey, between 0.01% and 1.00% sucrose and C8-C24 fatty acid ester, between 0.5% and 8% ethyl alcohol (96%), between 0.001% and 2%, one or more essential oils of gaultheria, thymus zygis, ravintsara, niaouli, rosemary, marjoram sylvester or any essential oil rich in 1,8 cineole compound, between 0.1% and 2% one or more flavourings, between 0.1% and 0.2% pH regulating agent.

Description

(1) The invention is described hereinafter by means of example embodiments.

Example 1: Aqueous Ionic Solutions for Children (Less than 6 Years) or Adults (More than 6 Years)

(2) Aqueous ionic solutions according to the invention are prepared by means of the ingredients mentioned in table 3. The quantities are expressed as a percentage by mass.

(3) TABLE-US-00003 TABLE 3 Ingredients Adult solution Child solution Glycerine (glycerol) Qsp 100 Qsp 100 >50 >50 Propolis 0.5-8.0 0.5-8.0 Neosorb 70/70B (Sorbitol) 0.5-8.0 0.5-8.0 Honey 1.0-8.0 1.0-8.0 Menthol 0.001-0.01 Ethyl alcohol 96% 0.5-8.0 Flavourings 0.1-2.0 0.1-2.0 EO including Gaultheria 0.001-2.000 fragrantissima EO Sucrose esters 0.01-1.00 0.05-1.00 Hypertonic seawater 20.0-40.0 25.0-40.0 pH-regulating agent 0.01-0.20

(4) Preparation of Aqueous Solvent:

(5) A solution based on seawater with a 22 g/l salt content was prepared by electrodialysis, having an osmolality greater 350 mOsm/kg, that is to say a hypertonic solution. The method for producing this seawater-based solution, known from the prior art, is stated below.

(6) Successively: as a raw material, seawater with a salt content greater than 32 g/l is taken, advantageously from a depth of 5 to 10 metres in a zone with strong current movements, for example off Saint-Malo. This water is clarified, filtered and analysed: if the osmolality of the clarified and filtered seawater is higher than the required osmolality, it has soda removed by electrodialysis until the required osmolality is obtained, if the osmolality of the settled seawater is lower than the require osmolality, it is concentrated until the required osmolality is obtained, and then the ionic concentrations of the various ions are adjusted by selective electrodialysis, and the product is filtered and stored under sterile conditions. The ionic concentrations will be adjusted so as to have the characteristics of a reference hypertonic solution as described previously.

(7) Preparation of Ionic Solutions:

(8) After each raw material is weighed, the preparations of the ionic solutions are produced in several phases, these phases being able to be different according to the industrial equipment used.

(9) Preparation of Phase A: Incorporate the glycerine in the mixing vessel. Successively add the following ingredients under stirring: Propolis Neosorb 70/70B Acacia honey Continue the stirring to complete solubilisation.

(10) Preparation of Phase B: In a subsidiary vessel, incorporate the 96% ethyl alcohol and the menthol and then mix until the menthol is dissolved. Next introduce the sucrose ester. Successively add each essential oil and flavouring, taking care to mix thoroughly between each incorporation. In the context of the child solution, only the flavourings are added to the sucrose ester.

(11) Preparation of Phase C: Incorporate the hypertonic seawater (22 g/l of salts) in a 2.sup.nd subsidiary vessel and then add the pH-regulating agent.

(12) Mixing of the Phases: Under screw stirring, gradually incorporate phase B and phase A. Maintain the stirring. Gradually add phase C.

(13) Observations:

(14) The solutions are in the form of stable dispersions or emulsions. The results show the presence of micelles (globule of oil) with a mean size of approximately 0.6 m (diameter). The distribution shows that the smallest micelles have a diameter of around 0.4 m while the largest a diameter of approximately 1.1 m (analysis by the dynamic light scattering granulometric distribution method inspired by ISO 22412:2008 on a Malvern Instruments apparatusZetaSizer NanoZS).

Example 2: Analysis of Stability vis--vis Bacterial Contaminations (in Accordance with the European Pharmacopeia 7.SUP.th .Edition 2011 Method) (Tableau 4)

(15) TABLE-US-00004 TABLE 4 Strain tested Adult solution Child solution Pseudomonas aeruginosa A A Staphylococcus aureus A A Escherichia coli A A Candida albicans A A Aspergillus brasiliensis A NC Classification Conformity with Non-conformity criteria A A: result conforming to criteria A B: result conforming to B NC: result non-conforming

(16) The bacteria strains sought are those that are most commonly encountered in production.

(17) The formulae are satisfactory since contamination by Aspergillus brasiliensis is acceptable in production. However, the adult solution 1 is more effective against contaminations. Consequently this formulation makes it possible to dispense with filtration steps during the manufacturing method, which represents a saving in time and equipment.

(18) The performance of the adult solution (according to example 1) is explained by the combination of polyols and essential oils in greater quantity, the presence of alcohol and a more acidic pH buffered at 4.1-4.6. The menthol may also have a slight antimicrobial effect.

(19) It should be noted that the formulation for children, free from essential oils and alcohol, is also effective against contaminations because of the quantity of polyols and the acidic pH.

Example 3: Measurement of the Activity of the Water (Aw) (Tableau 5)

(20) TABLE-US-00005 TABLE 5 Adult solution Child solution Measurement Aw 0.664 0.676

(21) The activity of pure water is 1. The activity of a dehydrated solution is 0. An activity of water less than 0.8 is satisfactory.

(22) The high proportion of polyols in the formula of the adult solution (according to example 1) makes it possible to reduce the activity of the water, which results in auto-protection of the formulae vis--vis the development of microorganisms despite a large quantity of aqueous solvent.

Example 4: Flow Velocity Test

(23) Objective:

(24) Measuring the flow velocity of the adult aqueous ionic solution (according to example 1) compared with demineralised water and 22 g/l hypertonic water in order to show a significant difference in viscosity making it possible to demonstrate the adhesion of the solution to a surface, for example to the surface of the throat mucosa.

(25) Equipment Used: 100 ml decanting bulb Support Chronometer Beakers Scales to 100.sup.th

(26) Operating Method: Place a beaker on the scales and allow for the tare Place the bulb on the support and position it above the beaker Bring the solution to be tested to 20 C. (+/0.5 C.) Fill the decanting bulb with the solution to be tested (lower meniscus) Trigger the chronometer and open the tap of the decanting bulb at the same time Record the time elapsed and the weight delivered into the beaker.

(27) Results: Tableau 6

(28) TABLE-US-00006 TABLE 6 Time Volume elapsed flowrate Product tested Density Quantity in g Quantity in ml (seconds) (ml)/sec Demineralised water 1.00 Test 1 - 139.04 Test 1 - 139.04 21 sec 25 6.543 T: 20 C. Test 2 - 138.98 Test 2 - 138.98 21 sec 03 6.608 Test 3 - 138.96 Test 3 - 138.96 21 sec 34 6.5117 Mean 138.99 138.99 21.206 6.554 22 g/l hypertonic water T 20 C. 1.008 Test 1 - 141.45 Test 1 - 140.33 22 sec 63 6.201 Test 2 - 141.21 Test 2 - 140.09 22 sec 46 6.237 Test 3 - 141.44 Test 3 - 140.32 23 sec 84 5.885 Mean 141.36 140.25 22.976 6.1076 Adult aqueous ionic solution 1.15 Test 1 - 160.55 Test 1 - 139.60 36 sec 89 3.784 T: 20 C. Test 2 - 160.49 Test 2 - 139.55 36 sec 06 3.869 Test 3 - 160.19 Test 3 - 139.30 36 sec 16 3.852 Mean 160.41 139.48 36.37 3.835

(29) Conclusions:

(30) An insignificant difference of 0.4464 ml is noted between the demineralised water and the 22 g/l hypertonic seawater. This difference may be related to the difference in temperature and to the salt content (22 g/l hypertonic).

(31) The difference in flow between the references consisting of demineralised water (2.719 ml) or 22 g/l hypertonic water (2.27 ml) and the adult solution according to the invention (according to example 1) is significant, as well as the time elapsed for the bulb to empty. It is also noted that the adult solution adheres slightly to the wall of the decanting bulb, like an oil.

(32) The adult solution according to the invention has viscosity characteristics superior to those of water or a seawater solution, making it suitable for blanketing the mucosa and adhering for a useful time, enabling the active compounds to exert their actions at the mucosa.

Example 5: Flow Velocity Test n 2

(33) Objective:

(34) Measure the flow velocity of the adult aqueous ionic solution (according to example 1) compared with a solution present on the market and sold under the brand name Pediakid (Laboratoires Ineldea, France) in order to show a significant difference in viscosity, adhesion, flow and coverage making it possible to demonstrate the adhesion and distribution of the solution on the mouth mucosa.

(35) Composition of the Pediakid product: distilled eucalyptus water (Eucalyptus globulus), distilled rosemary water (Rosmarinus officinalis), seawater based on Dead Sea salt, extract of echinacea (Echinacea purpurea), copper, extract of propolis and extract of aloe vera.

(36) Equipment Used Support plate and bracket Box Chronometer Slide gauge Rule 3 bottles of adult solution (according to example 1) packaged batch n 83361 3 Pediakid products with a connecting piece throat spray batch n 12392

(37) Operating Method

(38) Test 1 Place the plate vertically with an inclination angle of 105 mimicking the passage of the oropharyngeal junction. Trace 2 lines horizontally spaced apart by 30 cm. Place 6 points on the top line corresponding to the initial spray point. Measure, using the bracket and rule, a distance of 10 cm between the position of the bottle and the impact zone on the plate. At the same time, trigger the chronometer and spray two sprays onto the impact zone. Record the time elapsed taken by the liquid to reach the bottom line. Repeat the operation for each product 3 times with cleaning of the plate after each series of 6.

(39) Test 2 Place the plate horizontally. Trace 1 vertical line on the box in order to delimit a zone for the adult solution (according to example 1), and a zone for the Pediakid solution. Measure, using the bracket and the rule, a distance of 10 cm between the position of the bottle (mouth connecting piece) and the impact zone on the box. Spray 1 spray on the zone of the box concerned. Surround the zone wet by the spray and take the diameter of the circle thus formed. Repeat the operation for each product.

(40) Results

(41) TABLE-US-00007 TABLE 7 Test 1 Standard Overall Test 1 Test 2 Test 3 Mean deviation mean Adult solution 1 91.47 95.88 94.23 93.86 2.23 93.58 (in seconds) Adult solution 2 96.37 118.83 102.65 105.95 11.59 (in seconds) Adult solution 3 80.97 82.65 79.17 80.93 1.74 (in seconds) Pediakid 1 in 54.77 61.83 58.45 58.35 3.53 60.54 seconds Pediakid 2 in 51.72 78.43 63.12 64.42 13.40 seconds Pediakid 3 in 59.95 62.24 54.32 58.84 4.08 seconds

(42) The two means can be compared in accordance with the Student test with null Ho as the hypothesis: the flow time of the solution adult and Pediakid products is equivalent.

(43) The hypothesis H1 then becomes: the flow time of the solution adult is longer than that of the Pediakid solution.

(44) $t\mathrm{is}\mathrm{given}\mathrm{by}\mathrm{the}\mathrm{formula}\text{:}t=\frac{\left(m1-m2\right)}{\mathrm{ESy}}$$\mathrm{With}{\mathrm{ES}}_v\mathrm{given}\mathrm{by}\mathrm{the}\mathrm{formula}\text{:}\sqrt{\frac{S{1}^2}{n1}+\frac{S{2}^2}{n2}}$

(45) That is to say t=6.78 with ES.sub.v=4.87

(46) Referring to the table of the Student t, and taking as an input the value of t thus calculated and as the number of degrees of freedom the value n1 where n is the number of measurements, that is to say 17 as degrees of freedom, the associated value of p is 2.12 for a of 0.05.

(47) The value of t does not lie in the interval (2.12:2.12), the hypothesis HO is therefore rejected, and the two products are therefore different in terms of flow time.

(48) TABLE-US-00008 TABLE 8 Test 2: Standard Test 1 Test 2 Test 3 Mean deviation Adult solution 8 84 86 86.33 2.52 (in mm) 9 Pediakid 3 25 37 32.33 6.43 (in mm) 5

(49) The two means can be compared in accordance with the Student test with null Ho as the hypothesis: the spreading of the adult solution of example 1 and that of the Pediakid solution are equivalent.

(50) The hypothesis H1 then becomes: the spread of the adult solution of example 1 is greater than that of the Pediakid solution.

(51) The value of t is calculated using the previous formula: t=13.54

(52) Regarding the table of the Student t, taking into account the input of the value of t thus calculated and the value n1 as the number of degrees of freedom where n is the number of measurements, that is to say 5 degrees of freedom, the associated value of p is 2.57 for a of 0.05.

(53) The value of t does not lie in the interval (2.57; 2.57), the HO hypothesis is therefore rejected, and the two products are different in terms of spread.

CONCLUSION

(54) The two tests carried out showed significant differences with regard to flow and dispersion (spread) between the two products.

(55) It is therefore clear from this that, with a better dispersion and a longer flow time, the adult aqueous ionic solution according to the invention can cover a large part of the oropharyngeal mucosa and remain in contact therewith for the time necessary for its action.