Titanium compound derivatives, production and uses the same

IPC classes for russian patent Titanium compound derivatives, production and uses the same (RU 2250907):

A61K7/16 -

A61K6 - PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J0003000000; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L)

A61K31 - Medicinal preparations containing organic active ingredients

Another patents in same IPC classes:

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Method for preventing cicatricial commissure process development in epidural space after having removed intervertebral disk hernia at the lumbar level / 2243727

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Method for applying surgical removal and photodynamic prophylaxis of recurrent subretinal neovascular membranes / 2243748

Method involves introducing 0.1-0.3 ml of photosensitizing gel preliminarily activated with laser radiation, after having removed neovascular membrane. The photosensitizing gel is based on a viscoelastic of hyaluronic acid containing khlorin, selected from group containing photolon, radachlorine or photoditazine in the amount of 0.1-2% by mass. The photosensitizing gel is in vitro activated with laser radiation having wavelength of 661-666 nm during 3-10 min with total radiation dose being equal to 100-600 J/cm². The gel is introduced immediately after being activated. To compress the retina, vitreous cavity is filled with perfluororganic compound or air to be further substituted with silicon oil. The operation is ended with placing sutures on sclerotomy and conjunctiva areas. Compounds like chealon, viscoate or hyatulon are used as viscoelastic based on hyaluronic acid. Perfluormetylcyclohexylperidin, perfluortributylamine or perfluorpolyester or like are used as the perfluororganic compound for filling vitreous cavity.

Photodynamic surgical method for treating the cases of choroid hemangioma / 2243753

Method involves making incision in conjunctiva and Tenon's capsule of 3-4 mm in size in choroid hemangioma projection to sclera 3-4 mm far from limb. Tunnel is built between sclera and Tenon's capsule to extrasclerally introduce flexible polymer magnetolaser implant through the tunnel to the place, the choroid hemangioma is localized, after performing transscleral diaphanoscopic adjustment of choroid hemangioma localization and size, under visual control using guidance beam. The implant has permanent ring-shaped magnet in the center of which a short focus scattering lens of laser radiator is fixed. The lens is connected to light guide in soft flexible envelope. The permanent implant magnet is axially magnetized and produces permanent magnetic field of 2-3 mTesla units intensity. It is arranged with its north pole turned towards the choroid hemangioma so that extrascleral implant laser radiator disposition. The other end of the implant is sutured to sclera 5-6 mm far from the limb with two interrupted sutures through prefabricated openings. The implant is covered with conjunctiva and relaxation sutures are placed over it. Light guide outlet is attached to temple using any known method. 0.1-1% khlorin solution is injected in intravenous bolus dose of 0.8-1.1 mg/kg as photosensitizer and visual control of choroid hemangioma cells fluorescence and fluorescent diagnosis methods are applied. After saturating choroid hemangioma with the photosensitizer to maximum level, transscleral choroid hemangioma laser radiation treatment is carried out via laser light guide and implant lens using divergent laser radiation at wavelength of 661-666 nm with total radiation dose being equal to 30-120 J/cm². The flexible polymer magnetolaser implant is removed and sutures are placed on conjunctiva. Permanent magnet of the flexible polymer magnetolaser implant is manufactured from samarium-cobalt, samarium-iron-nitrogen or neodymium-iron-boron system material. The photosensitizer is repeatedly intravenously introduced at the same dose in 2-3 days after the first laser radiation treatment. Visual intraocular neoplasm cells fluorescence control is carried out using fluorescent diagnosis techniques. Maximum level of saturation with the photosensitizer being achieved in the intraocular neoplasm, repeated laser irradiation of the choroid hemangioma is carried out with radiation dose of 30-60 J/cm².

Photodynamic surgical method for treating the cases of intraocular neoplasms / 2243754

Method involves creating tunnel between sclera and Tenon's capsule in intraocular neoplasm projection. Intraocular neoplasm localization and size is adjusted by applying transscleral diaphanoscopic examination method. 0.1-0.3 ml of photosensitizing gel based on viscoelastic of hyaluronic acid, selected from group containing chealon, viscoate or hyatulon, is transsclerally introduced into intraocular neoplasm structure using special purpose needle in dosed manner. The photosensitizing gel contains khlorin, selected from group containing photolon, radachlorine or photoditazine in the amount of 0.1-1% by mass. Flexible polymer magnetolaser implant is extrasclerally introduced into the built tunnel in intraocular neoplasm projection zone under visual control using guidance beam. The implant has permanent ring-shaped magnet axially magnetized and producing permanent magnetic field of 3-4 mTesla units intensity, in the center of which a short focus scattering lens of laser radiator is fixed. The lens is connected to light guide in soft flexible envelope. The implant is arranged with its north pole turned towards the intraocular neoplasm so that implant laser radiator lens is extrasclerally arranged in intraocular neoplasm projection zone. The implant light guide is sutured to sclera 5-6 mm far from the limb with single interrupted suture. The implant is covered with conjunctiva and relaxation sutures are placed over it. Light guide outlet is attached to temple using any known method. Visual control of intraocular neoplasm cells is carried out by applying fluorescence and fluorescent diagnosis methods. After saturating the intraocular neoplasm with the photosensitizer to maximum saturation level, transscleral intraocular neoplasm laser radiation treatment is carried out via laser light guide and implant lens using divergent laser radiation at wavelength of 661-666 nm. The treatment course being over, the flexible polymer magnetolaser implant is removed and sutures are placed on conjunctiva. Permanent magnet of the flexible polymer magnetolaser implant is manufactured from samarium-cobalt, neodymium-iron-boron or samarium-iron-nitrogen. 0.1-1% khlorin solution as photosensitizer, selected from group containing photolon, radachlorine or photoditazine, is additionally intravenously introduced in 2-3 days at a dose of 0.8-1.1 mg/kg and repeated laser irradiation of the intraocular neoplasm is carried out with radiation dose of 30-45 J/cm² 15-20 min later during 30-90 s.

Electrochemical destruction and photodynamic surgical method for treating the cases of intraocular neoplasms / 2243755

Method involves applying transscleral diaphanoscopic examination method for adjusting intraocular neoplasm localization and size. Rectangular scleral pocket is built 2/3 times as large as sclera thickness which base is turned from the limb. Several electrodes manufactured from a metal of platinum group are introduced into intraocular neoplasm structure via the built scleral pocket. Next to it, intraocular neoplasm electrochemical destruction is carried out in changing electrodes polarity with current intensity of 100 mA during 1-10 min, and the electrodes are removed. Superficial scleral flap is returned to its place and fixed with interrupted sutures. 0.1-2% aqueous solution of khlorin as photosensitizer, selected from group containing photolon, radachlorine or photoditazine, is intravenously introduced at a dose of 0.8-1.1 mg/kg. Visual control of intraocular neoplasm cells is carried out by applying fluorescence and fluorescent diagnosis methods. After saturating the intraocular neoplasm with the photosensitizer to maximum saturation level, transpupillary laser radiation of 661-666 nm large wavelength is applied at a dose of 30-120 J/cm². the operation is ended with placing sutures on conjunctiva. Platinum, iridium or rhodium are used as the metals of platinum group. The number of electrodes is equal to 4-8. 0.1-1% khlorin solution, selected from group containing photolon, radachlorine or photoditazine, is additionally repeatedly intravenously introduced in 2-3 days at a dose of 0.8-1.1 mg/kg. Visual control of intraocular neoplasm cells is carried out by applying fluorescence and fluorescent diagnosis methods. After saturating the intraocular neoplasm with the photosensitizer to maximum saturation level, repeated laser irradiation of the intraocular neoplasm is carried out with radiation dose of 30-45 J/cm².

FIELD: organometal chemistry, stomatology.

SUBSTANCE: invention relates to titanium compounds of formula [TiF₂L₂] or containing group of formula [TiF_xL_y]^z-, wherein x = 2, 4 or 5; y = 1 or 2; z = 1 or 2; L is group of formula II , wherein m = 1; n = 0, 1 or 2, in enantiomer, diastereomer forms, or mixture thereof, including racemates; as well as free bases or pharmaceutically acceptable salts. Composition containing claimed compounds for buccal application to prevent dental caries also is disclosed.

EFFECT: compounds with improved stability capable to form lacquer on dental surface.

14 cl, 1 ex

The present invention relates to new compounds derived titanium, as well as to receive them.

The present invention also relates to compositions for buccal use, containing such compounds - derivatives of titanium.

It is known that tetraploid titanium (TiF₄can contact the tooth surface, forming an amorphous protective layer, also called varnish on the surface of tooth enamel.

The formation of such a protective layer on the tooth surface has led to the consideration of the application of titanium tetrafluoride as an agent for the prevention and treatment of dental caries.

However, tetraploid titanium has the disadvantage that it is strongly acidic in aqueous solution (pH about 1.5), which is aggressive for mineralized tissues and is not compatible with the physiological pH levels.

Its use for the prevention of dental caries, therefore, is still limited to professional use with very short time of application followed by rinsing.

In addition, tetraploid titanium has the disadvantage in its relative instability, especially in aqueous solution.

The present invention is to remedy these disadvantages by offering compounds - derivatives of titanium-IV containing fluorine that SP is able to form a varnish on the surface of the tooth and which can be used in aqueous solution at physiological pH levels, changing from about 6.5 to about 7.5.

Connection - derived titanium according to the present invention correspond to the formula (I)below:

where L is a compound of formula (II)below:

where m is 0 or 1 and n is 0, 1 or 2, and x represents a 2, 4 or 5 and y is 0, 1 or 2.

The compounds of formula (I) can contain one or more than one asymmetric carbon atom. They can therefore exist in the form of enantiomers or diastereoisomers. These enantiomers and diastereoisomers, as well as mixtures thereof, including racemic mixtures, form part of the present invention.

Compounds of the present invention may exist in the form of free bases or salts join pharmaceutically acceptable acids. All these forms are part of the present invention.

According to the present invention compounds L, which can be used are, in particular, derivatives of benzoic acid, in particular 2-hydroxybenzoic acid of the formula:

3-hydroxybenzoic acid of the formula:

4-hydroxybenzoic acid of the formula:

2,3-dihydroxy what sainoi acid of the formula:

3,4-dihydroxybenzoic acid of the formula:

An example of a connection - derived titanium according to the present invention is a compound represented by the following formula (III):

Compounds - derivatives of titanium(IV) of the present invention can be obtained by interaction of solid fluoride titanium IV with a solution of benzoic acid at room temperature in an anhydrous solvent, such as acetonitrile, under nitrogen atmosphere.

Starting materials are commercially available or described in the literature or can be prepared by the methods described therein, or by methods known to experts in this field of technology.

The present invention also relates to protecting compositions for buccal use, containing at least one compound of the present invention, as well as to the use of compounds - derivatives of titanium according to the present invention as agents for protection against dental caries.

The compositions of the present invention contain at least one compound of the present invention in an amount that is equivalent to the amount of fluoride from approximately 10 million^-1(ppm) to about 10000 million^-1and which calculated the molecular weight of the compounds of the present invention.

The compositions of the present invention may be in the usual variety of forms for compositions for buccal use and, in particular, in the form of a toothpaste or tooth gel, liquid mouth rinse, spray, foam, product for rinsing of the mouth or throat, dental gel, or chewing gum, balm, toothpaste, varnish, pellets, tablets, antiseptic preparation for the throat, powder or concentrated or non-concentrated solution, therefore, the carrier is selected depending on the desired application.

The compositions of the present invention in addition to the compound(s) - derivative(nd) titanium may contain as a carrier or for their own activity excipients or ingredients commonly used in compositions for buccal use.

The compositions of the present invention prepared in accordance with conventional ways, which correspond to the selected media. The physiologically acceptable carrier may vary in nature depending on the form selected for composition: an aqueous solution, condensed or not condensed aqueous-alcoholic solution, resin, pasty or solid excipient and so on.

In accordance with the desired form of the composition according to the present invention can also contain at least one polished the third agent in the ratio changing to 80% by weight relative to the total weight of the composition. The polishing agents are, for example, of inorganic or organic origin. Their nature may vary according to the medium used for the selected form.

Polishing agents that may be used include, in particular, carbonate or bicarbonate of calcium, magnesium or sodium, phosphates and sulfates of calcium, alumina and hydrated alumina, oxides of silicon, oxides, hydroxides, trisilicate and pyrophosphates magnesium compounds pulp obtained by grinding the cereals, metaphosphate sodium or potassium dihydrate calcium phosphate, calcium phosphate, calcium phosphate, calcium pyrophosphate, in particular trepidatiously aluminum oxide, aluminum silicate or zirconium, bentonite, and orthophosphate magnesium or magnesium phosphate.

When the compositions are in the form of toothpaste, they can contain a polishing agent in proportions of between approximately 2% and approximately 70% by weight, preferably between approximately 15% and approximately 25% by weight. He is usually the inorganic abrasive polishing agent consisting of one or more than one connection, which in most cases insoluble in water. As examples metaphosphate sodium or potassium, Digue is the dratha calcium phosphate, the calcium phosphate, calcium phosphate, calcium pyrophosphate, aluminum oxide, hydrated aluminum oxide and, in particular, trepidatiously aluminium oxides, silicon oxides, silicates of aluminum or zirconium, bentonite, as well as phosphate or magnesium phosphate and magnesium carbonates and bicarbonates of calcium or sodium.

Compositions of the present invention, which are in the form of toothpaste may also contain one or more than one cohesive agent. Such cohesive agents can be included in ratios varying up to about 10% by weight relative to the total weight of the composition, and preferably between approximately 0.5% and approximately 3% by weight. Cohesive agents can be selected, in particular, of natural thickeners, such as alginates or pectins, natural gums, such as tragakant or xanthan gum, guar gum, carob bean gum or carraginanous resin, and synthetic thickeners such as cellulose derivatives such as sodium carboxymethyl cellulose, methyl cellulose, hydroxyethylcellulose, Poperechnaya polyacrylic acid, or synthetic carrageenates.

According to some embodiments of the compositions of the present invention can contain one or more than one stable enough and foaming surface the active substance. Surfactants that can be used may be anionic, amphoteric, zwitterionic, cationic or non-ionic nature.

Typically, surfactants are present in the compositions of the present invention in an amount which varies from approximately 0.01% to approximately 4% by weight, preferably from about 0.1% to about 2% by weight, relative to the total weight of the composition.

In addition, the compositions of the present invention can contain other active agents, which are used in the oral hygiene, in particular agents that reduce bad breath, such as, for example, cyclodextrins or zinc compounds, such as, for example, zinc halides, zinc acetate, zinc citrate or zinc fluoride, chlorhexidine or pyridinium chloride.

The compositions of the present invention can also include various cohesive agents, thickeners, antibiotics, sweeteners, moisturizing or refreshing agents, baptistery, preserving agents, sweeteners, colorants, flavorings, dyes, corrigentov and intensifiers flavoring properties, plasticizers, antimicrobial agents or bactericides, vitamins, agents against Tartar, healing agents, vasomotor agents, hemostatic agents, AG, is, for example, which are active on the resins, anti-inflammatory agents, such as naloxon, benzydamine, allantoin, parmetol and so on.

These various agents present in the compositions of the present invention in accordance with the form of application.

So, when the composition for buccal application is a spray, the carrier may be an aqueous-alcoholic solution, and this composition may also contain flavors, baptistery, and sweetening, refreshing moisturizer or agents.

When the composition for buccal application is in the form of a liquid for rinsing the mouth, the media may be non-aqueous, aqueous or aqueous-alcoholic with one or more than one surface-active substance and/or one or more than one thickening agent and may also contain antibacterial agents, sweetening agents and corrigentov.

For example, when the composition is in the form of a dental gel, it can also contain agents that are active on the tar.

When the composition is in the form of chewing gum, it contains at least one natural or synthetic resin, suitable for chewing, and may also contain plasticizers, vitamins, corrigentov or intensifiers flavoring properties, sweeteners, moisturizing agents, bactericides, preserving AG is, for example, the dyes.

In particular, among the resins suitable for chewing, which can be used are latex rubber, the resin cycle, resin sulong (schulong), polyvinyl acetate and synthetic elastomers, in particular silicone rubber, synthetic butyl rubber and derivatives thereof and/or mixtures.

Compositions for buccal application of the present invention can also contain a sweetening agent. Among sweetening agents which may be used include sucrose, lactose, fructose, xylitol, sodium cyclamate, sodium saccharinate or maltose, glycyrrhizinate ammonium or sodium, a mixture of alpha-glucosyl/steuerklasse, D-mannitol, aspartame, Acesulfame K, sorbitol, limosin and mixtures thereof.

Sweetening agents are usually present in amounts varying up to about 2% by weight relative to the total weight of the composition.

As wetting agents can be mentioned sorbitol, glycerol or xylitol, which are present in such concentrations that can reach 70% by mass.

In addition, the compositions of the present invention can be incorporated refreshing agents, such as menthol or eternality.

You can also use preservatives that are selected, in particular, of methylparahydroxybenzoate, propilparagidroksibenzoat, benzoate of sodium and chlorine is hexidine in concentrations components, typically about 1% by weight or less.

The corrigentov, which can be used include all those corrigentov that are registered as additives in the food trade. As an example we can mention the essences of mint, anise seed, eucalyptus, cinnamon, clove, sage and licorice and fruit essences, such as essences of orange, lemon, tangerine or strawberry. The corrigentov are usually present in amounts of about 5% by weight or less.

The compositions of the present invention may also contain an antibacterial agent, preferably selected, in particular, essential oils, plant extracts or substances, such as alexidine, octenidine, hexetidine, Phenoxyethanol, finitely alcohol, triclosan, chlorhexidine, pyridinium chloride and delmopinol, ratios, changing to about 10% by weight relative to the total weight of the composition.

The following example illustrates the connection - derived titanium according to the present invention. Elemental microanalysis, IR and NMR spectra confirm the structure of the compounds obtained.

Example 1

Obtaining the compounds of formula (III):

5 g (0.040 mol) of solid titanium fluoride is added to 10 g (0,072 mol) of a mixture of salici the OIC acid in 100 ml of anhydrous acetonitrile under stirring and in a nitrogen atmosphere. The reaction mixture was quickly painted in orange color, and the mixed solution is kept for 24 hours. After decanting and concentration by evaporation, the solution is cooled during the night and formed a small needle crystals, representing salicylic acid, which has not entered into reaction. The solution is again filtered, concentrated and cooled to 4°With a yellow/orange monoclinic crystals. After filtration and drying under vacuum to obtain the compound of formula (III) with the release of approximately 49%.

Melting point: 157-160°C (decomposition)

Compounds of the present invention were subjected to biological studies, which have demonstrated their properties to form the varnish on the surface of the tooth and their value as agents for treating or preventing dental caries.

A fresh sample of the tooth is placed in a glass vial containing wet cotton and thymol at a temperature of +4°C.

The sample is cleaned from soft tissue, possibly present on the tooth. Then the tooth is polished in a rubber Cup containing pumice, free from fluoride, and then washed in an ultrasonic bath. The sample is treated with an aqueous solution of the compound (III) according to the present invention at pH 5 for 10 minutes at a temperature of 37°C. the sample was Then washed with water for one min is you and the hole, made in the surface of the tooth, see under the microscope.

Demonstrated the formation of amorphous protective layer on the tooth surface after treatment of the sample compound (III).

The results of these biological tests show that the compounds of the present invention have the ability to form a protective varnish on the surface of the tooth.

These compounds can be used for the treatment and prevention of dental caries.

Examples of compositions of the present invention is given below.

1. Compounds of titanium, representing [TiF₂L₂]or containing [TiF_xL_y]^z-where x represents a 2, 4 or 5, y is 1 or 2, z represents 1 or 2, and L is a compound of the formula

where m is 1 and n is 0, 1 or 2,

in the form of enantiomers, diastereoisomers, as well as mixtures thereof, including racemic mixtures, of free bases or pharmaceutically acceptable salts.

2. The compound according to claim 1, characterized in that the compound L is selected from derivatives of benzoic acid, in particular

2-hydroxybenzoic acid of the formula

3-hydroxybenzoic acid of the formula

4-hydroxybenzoic acid of the formula

2,3-dihydroxybenzoic acid formula

3,4-dihydroxybenzoic acid formula

3. The compound according to claim 1, characterized in that it corresponds to the formula (III)below

4. The method of obtaining compounds of titanium according to any one of claims 1 to 3, characterized in that the solid titanium fluoride IV is subjected to interaction with a solution of benzoic acid in an anhydrous solvent, such as acetonitrile, under nitrogen atmosphere.

5. Composition for buccal application, characterized in that it contains at least one compound of titanium, representing [TiF₂L₂]or containing [TiF_xL_y]^z-where x represents a 2, 4 or 5, y is 1 or 2, z represents 1 or 2, and L is a compound of the formula

where m is 0 or 1, and n is 0, 1 or 2,

in the form of enantiomers, diastereoisomers, as well as mixtures thereof, including racemic mixtures, of free bases or pharmaceutically acceptable salts in an amount that is equivalent to the amount of fluoride from approx the tion 10 million ^-1(ppm) to about 10000 million^-1.

6. Composition for buccal application according to claim 5, characterized in that it is in the form of a toothpaste or tooth gel, liquid mouth rinse, spray, foam, product for rinsing of the mouth or throat, dental gel, or chewing gum, balm, toothpaste, varnish, pellets, tablets, antiseptic preparation for the throat, powder or concentrated or non-concentrated solution.

7. Composition for buccal use according to any one of pp.5 and 6, characterized in that it also contains at least one polishing agent of inorganic or organic origin in ratios varying up to 80% by weight relative to the total weight of the composition.

8. Composition for buccal application according to claim 7, characterized in that the polishing agent contains, in particular, carbonate or bicarbonate of calcium, magnesium or sodium, phosphates and sulfates of calcium, alumina and hydrated alumina, oxides of silicon, oxides, hydroxides, trisilicate and pyrophosphates magnesium compounds pulp obtained by grinding the cereals, metaphosphate sodium or potassium dihydrate calcium phosphate, calcium phosphate, calcium phosphate, calcium pyrophosphate, aluminum oxide, hydrated aluminum oxide and, in particular, trepidatiously OK the IDA aluminum, silicates of aluminum or zirconium, bentonite, and orthophosphate magnesium, or magnesium phosphate.

9. Composition for buccal use according to any one of pp.5-8, characterized in that it also contains one or more than one cohesive agent, in proportions varying up to about 10% by weight relative to the total weight of the composition, selected in particular from natural thickeners, such as alginates or pectins, natural gums, such as tragakant or xanthan gum, guar gum, carob bean gum or carraginanous resin, synthetic carrageenate and synthetic thickeners such as cellulose derivatives such as sodium carboxymethyl cellulose, methyl cellulose, hydroxyethylcellulose or cross-crosslinked polyacrylic acid.

10. Composition for buccal use according to any one of pp.5-9, characterized in that it also contains one or more than one surfactant, anionic, amphoteric, zwitterionic, cationic or non-ionic nature.

11. Composition for buccal use according to any one of pp.5-10, characterized in that it also contains one or more than one active agent used in oral hygiene, in particular, the agent, known as reducing bad breath, such as, for example, chlorhexidine, pyridinium chlorine is d, cyclodextrins or zinc compounds such as zinc halides, zinc acetate, zinc citrate or zinc fluoride.

12. Composition for buccal use according to any one of pp.5-11, characterized in that it also contains one or more than one cohesive agent, a thickening agent, an antibiotic, a sweetening agent, a moisturizing agent or refreshing agent, peptization, a preserving agent, a sweetener, a colorant, flavouring, corrigent and an intensifier of taste and aroma properties, a plasticizer, an antibacterial agent or bactericide, a vitamin agent against Tartar, healing agent, vasomotor agent, hemostatic agent, an agent that is active on the resins, anti-inflammatory agent, such as naloxon, benzydamine, allantoin, parmetol.

13. Composition for buccal application according to item 12, wherein the sweetening agents include sucrose, lactose, fructose, xylitol, sodium cyclamate, sodium saccharinate or maltose, glycyrrhizinate sodium or ammonium, a mixture of alpha-glucosyl/semiglobose, D-mannitol, aspartame, Acesulfame K, sorbitol, limosin and mixtures thereof.

14. Composition for buccal application under section 12, characterized in that the antibacterial agents include essential oils, plant extracts or substances, such as alexidine, octenidine, hexetidine, Hairdryer shall xethanol, finitely alcohol, triclosan, chlorhexidine, pyridinium chloride and delmopinol, ratios, changing to about 10% by weight relative to the total weight of the composition.