WO2006075236A1

WO2006075236A1 - Dermal lubricant and moisturiser

Info

Publication number: WO2006075236A1
Application number: PCT/IB2006/000045
Authority: WO
Inventors: Ali Altunkaya
Original assignee: Ali Altunkaya
Priority date: 2005-01-13
Filing date: 2006-01-12
Publication date: 2006-07-20
Also published as: WO2006075236B1; GB0500632D0

Abstract

Lubricant and moisturiser compositions for topical application comprising an extract of the seed husk of flax (Linum usitatissimum), optionally in combination with one or more antibacterial, anti-fungal and anti-viral active ingredients, are disclosed.

Description

DERMAL LUBRICANT AND MOISTURISER

This invention relates to an improved lubricant and moisturiser for application to the skin generally and particularly to mucous membranes .

Liquid compositions are known which may be applied topically to human skin to act as a lubricant or to moisturise it . Popular compositions contain a stable mixture of components so as to perform both functions . As the aqueous miscibility of the major components differs the combined moisturiser and lubricant compositions need to be stabilised, usually as a gel or as an emulsion and also need additives to ensure long-term stability from oxidation and other forms of deterioration . Known compositions may form a stable base for infections, bacterial or viral, present on skin and can act as a vector for the infection carrying it to other people .

This invention provides a liquid and gel lubricants and moisturiser compositions , which, are stable, and does not carry viral and bacterial infections .

According to the present invention there is provided a lubricant and moisturiser composition for topical application comprising an extract of the seed husk of flax (Linum usitatissimum) .

Also provided is a lubricant and moisturiser composition for topical application comprising an extract of the seed husk of flax (Linum usitatissimum) in combination with one or more natural and/or nature identical antibacterial, anti-fungal and anti-viral active ingredients .

The composition can be used as a lubricant due to the lubricant properties of the flax husk extract . It also has the added advantage of providing protection against potentially transmitted infections . Such transmission can easily take place where the areas of one or more users to which the lubricant has been applied come in contact, e . g . during sexual relations .

The preferred antibacterial , anti-fungal and anti-viral active ingredient is an antibacterial system based on lactoperoxidase alone or in combination with glucose oxidase and a substrate such as glucose . Such an ingredient is sold under the trademark Biovert . The ingredient is suitably present in a range from 0.5 to 2.5 percent by weight . Preferably the total enzyme levels lie in a range of 0.01 to 0.1 percent by weight .

An alternative antibacterial, anti-fungal and anti-viral active ingredient is Sorbic acid and its sodium and potassium salts . Sorbic acid is suitably present in a range 0.05 to 1.5 percent by weight and preferably in the range 0.1 to 0.5 per cent .

Further antibacterial , anti-fungal and antiviral ingredients include benzoic acid and its sodium and potassium salts . Benzoic acid is suitably present in a range 0.05 to 1.5 percent by weight, preferably 0.1 to 0.5 percent . Cinnamic acid id preferably present in a range 0.05 to 0.4 percent by weight . Salicylic acid or its soluble salts is suitably present in the range 0.1 to 2 percent, more preferably 0.5 to 1 percent . Grapefruit seed extract (sold under a brand name citricidal) in the range of 0.05 to 2.0 percent, more preferably 0.1-0.5 percent .

The formulations made with the flax husk extract may be compounded in known manner to make a gel, a cream or lotions for topical application to skin . For gel preparation xanthan gum, 0.2 to 2 percent by weight, or any other suitable gelling agents such as hydroxy ethyl cellulose or hydroxy propyl ether groups may be added as a gelling agent, to thicken it up to the desired viscosity . The formulations have excellent moisturising and lubricating capability . They are particularly suitable for use as a lubricant and as a moisturiser on any part of the human body including the lips and genital areas .

The flax husks contain compounds . in colloidal form which, when extracted in cold or hot water, yield colloidal ingredients with unique properties . The extracts are available commercially under the trade marks Natunola flax extract 121 and 141 and 160 from Natunola Health of Canada . However these extracts are preserved with synthetic chemical preservatives .

In the present invention lubricant and moisturiser composition the flax husk extract is preserved using natural and/or nature identical ingredients to control bacteria and also to overcome any fungal spores that may be present in the extract . The preferred natural and/or nature identical antibacterial system is based on Lactoperoxidase . It is able to provide a protective shield to the user of the products from pathogenic bacteria infections such as staphylococcus aureus, widely found on skin and in genital areas, and fungal infections, such as Candida albicans , found mainly in vaginal areas . The Lactoperoxidase is also capable of acting as an anti-viral to give the user of the product a protective shield against these harmful organisms by lowering the population of these organisms by 90% or more within 10 minutes of application and more often within five minutes . It is capable of reducing the population of organisms from several million colony-forming units to a thousand or less colony forming units . This antiseptic property combined with its unique lubricating properties of flax make this combination ideal for use as a sexual aid to give an added protection against potential infections .

Extraction of flax husk can be carried out as outlined below or commercially extracted flax husks could be utilised and preserved using these natural and nature identical preservatives to give flax husks with unique properties with the added benefit of being naturally preserved yet capable of protecting the skin or genital area from harmful pathogenic organisms .

Examples are provided showing the manufacture of a topical gel , lotion and cream with superior moisturising and lubricating capability suitable for use as a skin moisturiser or as a lubricant with added protection against harmful organisms .

1. ) Harvested flax husk is extracted into water at temperatures between 15-85 C or more preferably into warm water heated to between 45-60 C starting from cold. The flax husk extract produced at this stage will contain bacteria and spores capable of growing to become a potential contaminant .

2. ) The flax husk extract is separated from the husk using a filter and the filtrate liquid is then heated to 80-85 C and maintained at that temperature for 1 to 100 minutes , preferably 5 to 10 minutes ,- to effect the killing of some of the organisms and also to assist the spores that are present in the flax husk extract to germinate .

3. ) The flax husk extract from stage 2 or at the end of stage 1 may be preserved with a natural or nature identical preservative such as Cinnamic acid (available under the trade mark Dermasoft 747 from Dr . Straetmans of Germany or the equivalent synthetic material under the trade mark Dermasoft 688 from Dr . Straetmans . ) The manufacturer ' s recommended conditions such as pH of 5 and below allow heating to 60 C without degradation . Any other natural and nature identical preservative capable of withstanding heating to 6OC or higher, for 10 minutes and longer without any maj or degradation of the preservative chosen would be a suitable alternative such as benzoic acid or its salts . Another alternative is to leave the extract un-preserved at this stage . 4. ) The extract from stage 2 or 3 is re-heated after allowing it to stand for 1 hour or longer, ideally for 12-24 hours , back to a temperature of 60-95 C, and preferably 70-85 C . This temperature is maintained for 5 to 60 minutes , preferably 8 to 12 minutes, and then cooled down to a suitable temperature for the addition of any other necessary ingredients, such as buffering agents to adjust pH . A citric acid/sodium citrate combination or a lactic acid/sodium lactate combination are preferred buffers . Other ingredients may be added to make a gel or a lotion .

5. ) Preferred natural and/or nature identical preservative is the Lactoperoxidase based nature identical preservation system sold under the trademark Biovert . The Biovert system alone is capable of preserving the flax extract-as an anti-bacterial and anti-viral agent . However, the antibacterial capability of the Lactoperoxidase system can be enhanced by the addition of 0.05 to 0.5% Cinnamic acid . This may be as supplied under the trade mark Dermasoft 688 and ideally added at a level of 0.1-0.25% . Alternatively the Lactoperoxidase based preservative system can be combined with potassium Sorbate, another nature identical preservative, at 0.01 to 1.0% and ideally at 0.1-0.25% . Cinnamic acid ( Dermasoft 688 ) and potassium Sorbate in any combinations can be added to the Lactoperoxidase system of antibacterial to enhance its capability . It is also possible to combine other suitable nature identical preservatives with the Lactoperoxidase system that are capable of functioning as antibacterial, antifungal or anti-viral agents that are capable of functioning in the pH range of 4-7 and ideally at- pH range of 4.5-6.

6. ) Other ingredients may be added to the husk extract at stage 4 such as thickening agents . Xanthan gum, and hydroxyethyl cellulose have been found to be suitable thickening agents .

7. ) To turn the extract into a gel for use as a moisturiser or other practical form it is combined with appropriate ingredients in known manner . The extract may be formed into a lotion or cream, which is found to possess superior moisturising and lubricating capabilities . The gel, lotion or cream all have the added benefit of the very effective natural and/or nature identical antibacterial, anti-fungal and anti-viral protection while remaining very mild to the skin and genital area .

The proposed antibacterial system based on Lactoperoxidase alone or in combination with other natural and nature identical active ingredients is capable of protecting the users from pathogenic organisms found on skin, mouth, lower intestine and vagina as outlined below and hence makes this combination ideal to provide an added protection to users of this combination as a sexual aid to lubricate and protect the user .

++ = nearly 100% + = common +/- = rare potential pathogen

A typical gel according to the invention consists of :

1. ) Flax Husk Extract 1.0% to 98%, typically 75 to 95%

2. ) Sodium Citrate 0.0-5.0% , typically 1-2.5% (any other suitable buffering agent may be used. ) 3. ) Citric acid 0.05- 3.0 , typically 0.1-0.35% (any other suitable buffering agent may be used . )

4. ) Xanthan Gum 0.1- 5% , typically 0.3-1.5%

5. ) Biovert - or any other brand of Lactoperoxidase 1-10% , typically 0.5- 2.5% based enzyme system of preservation- enzyme and substrate part-

6. ) Dermasoft 688 0.01-5.0% , typically 0.1-0.3%

7. ) Potassium Sorbate 0.01- 4.0%, typically 0.05-0.5%

Other ingredients such as antioxidant may be added if desired such as

8. ) Vitamin E 0.01-1.0% , typically 0.05-0.2% (any other suitable antioxidant may be used. )

9. ) Polysorbate 80 0.0-3.0% , typically 0.4-1.5% (any other suitable surfactant may be used to disperse the antioxidant if the antioxidant is an oil soluble material .)

The following examples illustrate further compositions according to the invention.

Preparation of Gel solution from Flaxseed Husks . -

This is then used-to make lubricant gel, fluid or for use in making lubricant creams and lotions .

1 ) Into 5 L container add 2.5 L of Demin water . -Wt of water used=2 , 501g

2) Add 20Og of cleaned oil free flax seed husks (Example- Fortigrad grade of Flaxseed husk) : actual wt used= 201g 3 ) Start the stirring process with medium speed.

4) Start the heating process to take it up to 55-60⁰C . and when the temperature is at ~55°C, stop the heating.

5) Keep the solution at ~55-60°C for 10 minutes .

6) Place the mix into single bag of Polyester cotton filter (or any other suitable filtration equipment) and collect the liquid gel solution.

7) Record the weight to obtain the yield= I₇858g Viscosity

(spindle 5 speed 5 ) = 4520 cps at 24.8 ⁰C

8 ) Heat the solution to 80⁰C and maintain it at 80⁰C for 10 minutes .

The maximum temperature reached in the next ten minutes . The max temperature=82.7°C

9) The actual time the heating kept between 80⁰C to max temperature was lOmin.

10) Add 0.4% equivalent of Benzoic acid (or 4.6% equivalent of 5.2% of Dermasoft 688 solution to make it 0.24% Dermasoft

688 ) in the Gel solution

11) . Adjust pH so that the pH is between 4.5-5.0.

12) 5.1 g of Citric Acid 30%solution were added to bring pH to 4.71.

13) Viscosity 4, 670 cps; pH=4.7-

Typical viscosities of flax husks extract can wary from 800cps to 8, 000cps . The level of gelling agent (Xanthan Gum) that needs to be added in the next stage will change to reflect- the viscosity of the flax husks extract solution made to give the final desired viscosity .

5 Example of different natural and nature identical preservations used for formulations of lubricant fluids are summarised below :

LUBRICANT FLUID

Manufacturing instructions :

Extracted gel solution unpreserved or preserved with Cinnamic acid (or Benzoic acid) can be used to generate lubricant formulation as fluid or gel or varying viscosities . At 0.65% Xanthan Gum (Keltrol SFT type) can be used to give 6-10, 000cps and at higher levels for example at 1.0 to 1.2% it- will give gels with viscosities of 12-18 , OOOcps . At higher levels of gelling agent even higher levels of viscosity lubricant gels can be made if desired^

1) Sprinkle in Xanthan Gum into the Gel solution under medium to high speed of mixing . Allow 10 minutes of mixing prior to starting the heating process;

2) Heat the solution to 80⁰C, and maintain it at ^' 78-83C for lOmin. Then start the cooling process;

3 ) Premix Natural Vit E and Veremul T-80 add to the mix in point 2 when the temperature is about 70⁰C, whilst continuing the cooling process; 4 ) I f Sorbic acid or sodium benzoate is being added it can be added at this stage ;

5 ) I f phytic acid is in the formula it can be added at 5OC and below while continuing to cool down

6) Once the temperature reached ~34°C and below add salicylic acid if the formula calls for it

7 ) Check and Record pH;

8 ) When the solution is at ~30°C, add Potassium Sorbate if it is part of the formula;

9 ) Add Biovert Part 1 if it is part of the formula and mix for 5 minutes ;

10 ) Add the flavour if it is in the formula at this stage , at ~30 °C or below;

11 ) Check the pH and adjust it to about 4.3-5.2 using Citric acid;

12 ) Add Biovert-enzyme part ( if it is in the formula) and mix thoroughly to ensure uniform mixing .

13 ) Check that the final pH is between 4.3 to 5.2 and record the viscosity .

Typically for fluid is between β-12 , 000cps and for gel is 12- 18 , 000cps . Higher viscosity gels up to 45 , 000cps were made and gave satisfactory lubricating properties .

LUBRICANT GEL- An example formula and manufacturing instructions Is given below : To make lOOOg of product ingredients % (w/w) Wt required Wt used Batch number

(g) (g)

Gel solution 98.25 982 .5.5 982 .4

Preserved with Cinnamic acid

( Dermasoft

688 )

Xanthan Gum 1.1 11. 0 11. 05 3G9167K

Manufacturing instructions :

1 ) Mix at medium speed Gel solution and xanthan gum (Keltrol SFT . ) for 10 minutes

2 ) Heat the gel solution rapidly while being mixed and raise the temperature to 80⁰C, for lOmin . Maintain the temperature at 78-82C for 10 minutes . Then start the cooling process .

3) Premix Vit E and Veremul T-80 until it is uniform and when the temperature is about 70⁰C, add to the gel solution .

4 ) Check and Record pH . Adjust to 4.5-5.0 using Citric Acid. • 5 ) When the solution is at ~30°C, add Potassium Soxbate .

6) Check the pH . and viscosity (using Spindle 6, Speed 5 ) at

RT : - initial

Viscosity=14 , 867 cps at Temperature 24.7C Final pH adjusted to 4.7

An Example of a Cosmetic Cream using Lubricant gel solution to give smooth feeling to the touch made with Flax seed husks extract preserved with nature identical preservation system is given below

Manufacturing instructions :

1 ) Into a beaker add Water, Glycerine, gel solution, add the required amount of Carbopol while the water phase is s tirring under high speed. 2 ) Heat the water phase to 80-82 ° C until a clear gel solution forms .

3 ) Dissolve Boswellia serrata ( or Frankincence ) in Caprylic Capfic Triglycerides . 4 ) Prepare Oil phase , by combining the Boswellia serrata dissolved in caprylic Capric with the following ingredients- Ceteareth 20 , Cocoa^' Butter, Myristyl Myristate and Joj oba Oil 5 ) Heat the oil phase to 80-82 " C . 6) Add the Oil phase to Water phase when the 2 phases reach the same temperature ( 80-82 ° C ) . Stir rapidly and maintain the temperature at about 80 ° C . for 10 min . 7 ) Start the cooling process . Add the Dermasoft 688 ( 5% solution) once the temperature reaches 7 OC and below . 8 ) Slow down the speed of stirring .

^■ 9 ) Check and record pH and adj ust that the pH is between 4.9-

5.2 using Citric Acid or sodium citrate . 10 ) Add Citricidal . Check and record final pH, adj ust to 4.9-

5.2. 11 ) Check and record viscosity using spindle 6, speed 5.

For the. above formula the following viscosity and pH were recorded .

Viscosity=171 , 733 cps T ° C=25.9 ° C 22 /07 /05 : viscosity ( spindle 6 , speed 5 ) =188 , 935 cps at T=22.6 ° C

Claims

1. A lubricant and moisturiser composition for topical application comprising an extract of the seed husk of flax

(Linum usitatissimum)

2. A lubricant and moisturiser composition for topical application comprising an extract of the seed husk of flax

(Linum usitatissimum) in combination with, one or more natural and/or nature identical antibacterial , anti-fungal and anti- viral active ingredients .

3. A lubricant and moisturiser composition as claimed in claim

2 , characterised in that the natural and/or nature identical antibacterial, anti-fungal and anti-viral active ingredient is a combination of lactoperoxidase glucose oxidase with a substrate and present in a range from 0.5 to 2.5 percent by weight .

4. A lubricant and moisturiser composition as claimed in claim

3 , characterised in that the total enzyme levels lie in a range of 0.01 to 0.1 percent by weight .

5. A lubricant and moisturiser composition as claimed in claim ^' 2 , characterised in that the natural and/or nature identical antibacterial , anti-fungal and anti-viral , active ingredient is Sorbic acid or a potassium or sodium salts thereof a range of 0.05 to 5 percent by weight .

6. A lubricant and moisturiser composition as claimed in claim 5, characterised in that the ingredient is present in a range of 0.1 to 0.5 percent by weight .

7. A lubricant and moisturiser composition as claimed in claim

2, characterised in that the natural and/or nature identical antibacterial, anti-fungal and anti-viral active ingredient is benzoic acid or a potassium or sodium salt thereof a range of 0.05 to 1.5 percent by weight .

8. A lubricant and moisturiser composition as claimed in claim 7 , characterised in that the ingredient is present in a range of 0.2 to 0.5 percent by weight .

9. A lubricant and moisturiser composition as claimed in claim 2 , characterised in that the natural and/or nature identical antibacterial, anti-fungal and anti-viral active ingredient is Cinnamic acid a range of 0.05 to 0.4 percent by weight .

10. A lubricant and moisturiser composition as claimed in claim 9, characterised in that the ingredient is present in a range of 0.1 to 0.25 percent by weight .

11. A lubricant and moisturiser composition as claimed in claim 2 , characterised in that^" the natural and/or nature identical antibacterial , anti-fungal and anti-viral active ingredient is salicylic acid or a water-soluble salt thereof in a range of 0.1 to 2 percent by weight .

12. A lubricant and moisturiser composition as claimed in claim

11. characterised in that the ingredient is present in a range of 0.5 to 1 percent by weight .

13. A lubricant and moisturiser composition as claimed in claim 2 , characterised in that the natural and/or nature identical antibacterial , anti-fungal and anti-viral active ingredient is Grapefruit seed extract (example Citricidal ) or a water-soluble salt thereof in a range of 0.05 to 2 percent by weight .

14. A lubricant and moisturiser composition as claimed in claim

13, characterised in that the ingredient is present in a range of 0.1 to 1 percent by weight .

15. A lubricant and moisturiser composition as claimed in any of the preceding claims , characterised in that the composition is a fluid or a gel and contains from 0.1 to 20 percent by weight of xanthan gum.