The composition is in the form of a liquid emulsion of the type oil-in-water for external application

 

(57) Abstract:

The present invention relates to a new composition in the form of a liquid emulsion of the type oil-in-water (M/V) for topical application, containing 30 to 50 wt.% calculated on the total weight of the composition of at least one glycol, appropriate emulsifying system and at least one active agent. The liquid composition according to the invention has preferably a viscosity of from 3 to 10 Pas (3000 - 1000 SDRs), and the viscosity is determined using a Brookfield viscometer model LVDV 11+ N motor 4, when the rotation speed of 30 rpm for 30 s and at a temperature of 253oC. Composition facilitates topical active agent, has adhesive ability while maintaining the properties of the glycol conducive to absorption. 14 C.p. f-crystals.

The invention relates to a new composition in the form of a liquid emulsion of the type oil-in-water (M/V) for external application containing significant amounts of at least one glycol, promote absorption, the appropriate emulsifying system and the active agent.

Currently, there are numerous compositions for topical application containing an active agent and a significant number of glycole, these songs get in the form of emulsions with a high content of fatty phase, which are also commonly called "lipocream", or anhydrous compositions, which are called "Masi", or in the form of liquid formulations with a high content of volatile solvents, such as ethanol or isopropanol, intended for application on hair, also called the "lotions for hair care", or in the form viscous emulsions M/b, which is also called "creams M/B".

Known, for example, creams, M/V, containing corticoid and a high percentage of propylene glycol (47,5%), available in the market under the name TEMOVATEcompany GLAXO. However, the stabilization composition comprising such an amount of glycol, requires the use of emulsifiers and emulsion stabilizers type glyceraldehyde or PEG-100-stearate, and also stabilizers or agents, viscosity type of white wax or cetostearyl alcohol, which lead to the formation of a viscous cream, that is, the viscosity of which is higher than 10 Pas (10000 centipoise, as measured using Brookfield viscometer model LVDV 11+ engine # 4, speed 30 rpm for 30 seconds and at a temperature of 25oC 3oC).

To facilitate the application of the compositions preparational form type emulsion M/, the viscosity of which is intermediate between too liquid capillary lotions that have limited use, and is too viscous creams M/B, which would have a fat character and adhesive ability while maintaining the properties of the glycol conducive to absorption.

The present invention therefore relates to a new composition in the form of a liquid emulsion of the type oil-in-water for external application containing 30 to 50 wt.%, calculated on the total weight of the composition of at least one glycol, appropriate emulsifying system and at least one active agent.

Under liquid emulsion understand preferably the emulsion, the viscosity of which is 3-10 Pas (3000-10000 SDR), and the viscosity is determined using a Brookfield viscometer model LVDV 11+ engine # 4, speed 30 rpm for 30 seconds and at a temperature of 25oC 3oC.

A stable emulsion according to the invention preferably receive, when appropriate emulsifying system at least one polymeric emulsifier. Polymeric emulsifiers are described, in particular, Clymans and Brand in the publication "Cosmetics and Toiletries", 1995, pp. 119-125.

It is one hydrophilic element type of unsaturated olefinic carboxylic acid and at least one hydrophobic link type complex Olkiluoto ether from 10-30 carbon atoms.

According to the invention, under the acrylic parts see parts formula

< / BR>
in which R1means hydrogen or methyl or ethyl, i.e. parts of acrylic acid, methacrylic acid or metacrilato acid.

Also under alkylacrylate links see links patterns

< / BR>
in which R1means hydrogen or methyl or ethyl, i.e. acrylate, methacrylate or ethacrylate links;

R2means an alkyl radical with 10 to 30 carbon atoms, preferably 12-22 carbon atoms.

Acrylates according to the invention include, for example, laurelcrest, stearylamine, dellaquila, isodecyladipate, dodecylamine and the corresponding methacrylates, such as laurenmarie, sterilisability, decylmethacrylate, isabellemadelinet and dodecylmercaptan.

The above anionic amphiphilic polymers are preferably crosslinked with assistance of the polymerized crosslinking monomer containing the group CH2= C < with at least one other polymerized group, unsaturated communication which does not involve one against another.

The polymerized crosslinking monomers are, for example and predpochtitel the polymers of this type are well known; they are described in particular in patents U.S. 3915921 and 4509949.

According to the invention, as anionic amphiphilic polymers can be used polymers, which consist of 95-60 wt.% acrylic links, from 4 to 40 wt.% acrylate units and from 0.1 to 6 wt.% parts of a crosslinking monomer or 98-96 wt.% acrylic links, 1-4 wt.% acrylate units and 0.1 to 0.6 wt.% parts of a crosslinking monomer.

From the above crosslinked polymers according to the invention particularly preferred products on sale by the company GOODRICH under the trade names PEMULEN TR1, PEMULEN TR2, CARBOPOL 1342 or CARBOPOL 1382.

The composition according to the invention mainly contains up to 1 wt.% appropriate emulsifying system preferably 0.2 to 0.4 wt.%, calculated on the total weight of the composition.

Glycol, promote absorption, preferably chosen among propylene glycol, dipropyleneglycol, propilenglikolstearat, Laurelville or ethoxydiglycol.

The composition according to the invention preferably contains 40-50 wt.% glycol, contributing to the absorption.

Of active agents as examples, the agents that cause the differentiation and/or proliferation and/or phatnote, those described in the patent application France 2570377, European patent applications 199636, 325540, 402072, vitamin D and its derivatives, oestrogens such as oestradiol, kojic acid or hydroquinone; antibacterial agents such as clindamycine, erythromycin or antibiotics of the class of tetracyclines; antiparasitic agents, in particular metronidazole, crotamiton or pyrethrinoid; antifungal agents, in particular compounds belonging to the class of imidazoles, such as econazole, ketoconazole or miconazole or their salts, polyene compounds such as amphotericin B, compounds of group allylamino, such as terbinafine or octopirox; anti-inflammatory agents, steroids such as hydrocortisone, anthralin (dioxiranes), anthranoid, betamethasone or globalatlanta; or anti-inflammatory agents, non-steroidal type, such as ibuprofen and its salts, diclofenac and its salts, acetylsalicylic acid, acetaminophen or glycyrrhetinic acid; anesthetic agents such as lidocaineydrocortisone and its derivatives; antipruritic agents, as analgin, trimeprazine or cyproheptadine; antiviral agents such as acyclovir; keratolytic agents such qatn, hydroxy acids such as glycolic acid, lactic acid, malic acid, salicylic acid, citric acid and, in General, fruit acids, and n-octanoyl-5-salicylic acid; agents against free radicals, such as alpha-tocopherol or its esters, dissatisfactory, some metalhalide agents or ascorbic acid and its esters; protivoseborainey agents, such as progesterone; agents dandruff, such as octopirox or zinc pyrithione; anti-acne agents like retinoic acid, benzoylperoxide or adapalen; antimetabolite; agents to fight against hair loss, as monoxidil; antiseptics.

The composition according to the invention preferably contains of 0.0001-20 wt. % calculated on the total weight of the composition, the active agent, preferably 0,025-15 wt.%.

Of course, the amount of active agent in the composition depends on the type of active ingredient. Thus, with the use of anti-inflammatory steroids, the compositions may contain less than 1 wt.% active agent, preferably 0,025-0,05 wt.%. When using hydrocinnamic agent composition preferably contains 2-5% of the active agent. In the case of antibacterial or proty="ptx2">

The fatty phase of the emulsion according to the invention may contain fatty substances usually used in this field.

Of them can be called silicone fatty substances, such as silicone oil, and asilicone fatty substances, such as vegetable, mineral, animal or synthetic oils.

Silicone fatty substances can be called

(i) poly (C1-C20) alkylsilane, in particular those that contain trimethylsilyl end groups, and preferably, the viscosity of which is lower by 0.06 m2/s, which can be called linear polydimethylsiloxane and alkildimetilaminooksidy, such as acidisation (CTFA name);

- (ii) volatile silicone oils, such as

- volatile cyclic silicones with 3 to 8 silicon atoms and preferably 4 or 5 silicon atoms. We are talking about, for example, cyclotetrasiloxane, Cyclopentasiloxane or cyclohexasiloxane;

- cyclosporine type dimethylsiloxane/methylalkylcyclenes, such as SILICONE FZ 3109, issued for the sale by the company UNION CARBIDE, which is cyclosporine dimetilsiloksana with metiletilgeksanon;

- volatile linear silicones with 2-9 atom is disiloxane;

(iii) phenylaziridine silicone oils, in particular of the formula

< / BR>
in which R denotes an alkyl radical with 1-30 carbon atoms, aryl radical or arylalkyl radical;

n means an integer from 0 to 100;

m means an integer from 0 to 100, provided that the amount is from 1 to 100.

From fat asilicone substances can be called common oils such as paraffin oil, vaseline, almond oil, perhydrosqualene, apricot kernel oil; oil from sprouted wheat grains, sweet almond, calophylla; palm oil, castor oil, avocado oil, jojoba oil, olive oil or oil from germinated cereals; esters of fatty acids and fatty alcohols, such as octyldodecanol, or (C12-C15- alkylbenzoates alcohols; acetylglycine; octanoate, decanoate or ricinoleate alcohols or polyhydric alcohols; triglycerides of fatty acids; glycerides; hydrogenated polyisobutene; hydrogenated, solid at 25oC oil; lanolin; solid at 25oC fatty esters.

These fatty substances can be chosen by the specialist in various ways, to obtain a composition having the desired characteristics, aprima in number, comprising 5-50 wt. % calculated on the total weight of the composition, and preferably 15-20 wt.%.

The aqueous phase of the emulsion according to the invention may contain water, a floral water such as cornflower water, or medical or natural mineral water, for example, chosen among water Vittel, waters of the Vichy basin, water Uriage, water Roche Posay, water Bourboule, water'enghien-les-Bains, water Saint Gervais-les-Bains, water Neris-les-Bains, water Allevard-les-Bains, water Digne, water Maizieres, water Neyrac-les-Bains, water Lons-le-Saunier, Eaux Bonnes, water Rochefort, water Saint Christau, water Fumades and water Tercis-les-bains, water'avene or water Aix les Bains.

The above aqueous phase may be present in an amount of from 10 to 70 wt.%, calculated on the total weight of the composition, preferably from 20 to 40 wt. %.

The pH of the composition according to the invention is preferably 5 to 7, preferably 5.5 to 6.5. It can be brought to the desired value by adding a regular bases or acids, both mineral and organic.

In addition, the composition according to the invention may contain 0-3 wt.%, preferably 0-2 wt.%, calculated on the total weight of the composition, of at least one simulator, which can be selected among esters of fatty acids saturated or unsaturated, nature is glycerine with ezoterikovou acid, available in the market under the name LAMEFORM TGI firm SIDOBRE-SINNOVA HENKEL; serbianization produced is marketed under the name ARLACEL 987 by the company S; servicesecurity produced is marketed under the name ARLACEL 83 firm S; esters of glycol with ezoterikovou acid, such as PEG-6-isostearate produced is marketed under the name OLEPAL ISOSTEARIQUE by the company GATTEFOSSE; esters of sorbitol with oleic acid, such as Polysorbate produced is marketed under the name TWEEN firm S; ethers of fatty alcohols such as oleic alcohol, in particular esters of glycol and oleic alcohol, for example, simple oleic esters produced is marketed under the name BRIJ company ICI; acetyltyrosine servicemonitor; fatty alcohols such as stearyl alcohol or cetyl alcohol.

In addition, the composition according to the invention it is possible to introduce at least one gelling agent and/or thickener in preferred concentrations of the components of 0-5 wt.% calculated on the total weight of the composition.

Agent gelling and/or thickening agent may be selected from the following agents:

polysaccharide biopolymers, such as xanthan gum, resin fruit of the carob, guar gum, al is concerned, the hypromellose and carboxymethylcellulose;

- synthetic polymers such as polyacrylic acid, for example polymers of glycerol(meth)acrylates, as HISPAGEL or LUBRAGEL manufactured by the companies HISPANO QUIMICA or GARDIAN, polyvinylpyrrolidone, polyvinyl alcohol, crosslinked polymers based on acrylamide and of ammonium acrylate, such as PAS 5161 or BOZEPOL FROM the company HOECHST, crosslinked polymers based on acrylamide and 2-acrylamide-2-methylpropanesulphoacid, partially or completely neutralized, such as SEPIGEL 305 of the company SEPPIC, crosslinked polymers based on acrylamide and methacryloxypropyltrimethoxysilane, such as SALCARE SC 92 company ALLIED COLLOIDS, crosslinked polymers based on acrylic acid and simple alilovic ethers of sucrose or pentaerythritol (carbomer), such as CARBOPOL 910-934 company GOODRICH.

The emulsion may contain, in addition, any additive usually used in cosmetics or pharmaceuticals, such as antioxidants, dyes, fragrances, essential oils, preservatives, cosmetic active substances, hidratante, vitamins, volatile fatty acids, sphingolipids, agents, tanning, such as deshidratada acid, solar filters, fat-soluble polymers, in particular hydrocarbons, substances. Of course, the specialist must choose these optional input connections and their number so that the properties of the composition according to the invention is not deteriorated or is not significantly deteriorated at their introduction.

These additives may be present in the composition in an amount of 0-10 wt.% calculated on the total weight of the composition.

Below are examples of preparative production of forms, illustrating the composition according to the invention, but not limiting the invention. The number of components are expressed in wt.% calculated on the total weight of the composition.

Example 1: Example compositions according to the invention, wt.%:

purified water to total amount 100

the hypromellose - 0,10

propylene glycol - 47,50

the active agent - 0,05

liquid paraffin 110-230 - 20,00

cross-linked polymer based on acrylate and (C10-C30)-alkylacrylate (available in the market under the name PEMULEN TR-2 by the company GOODRICH) - 0,30

PEG-6-isostearate - 2,00

10% sodium hydroxide solution to pH 6.

In this composition, the active agent is stable for at least three months at a temperature of 40oC.

Example 2: Activity of the composition with globalatlanta.

Were carried out comparative tests on the vasoconstrictor effect according to a modified method Stoughton with this song and with a matching cream M/manufactured is marketed under the name TEMOVATE company GLAXO.

The results showed the activity that is identical for both formulations, as evidenced by the fact that, despite the change in the viscosity of the composition according to the invention and the use of other emulsifying systems, glycol conducive to the absorption retains these properties in the proposed composition.

1. The composition is in the form of a liquid emulsion of the type oil-in-water (M/C) for outdoor application, characterized in that it contains 30 to 50 wt.%, calculated on the total weight of the composition, of at least one glycol, appropriate emulsifying system and at least one active agent.

2. The composition according to p. 1, characterized in that its viscosity is 3 to 10 PA (3000 - 10000 centipoise), and the viscosity is determined using a Brookfield viscometer model LVDV 11+ engine N4, when the rotation speed of 30 rpm for 30 s and at a temperature of 25 3oC.

3. Composition under item 1 or 2, characterized in that the emulsifying system comprises at least one polymer of the first amphiphilic polymer, more specifically, the anionic amphiphilic polymer containing at least one hydrophilic element type of unsaturated olefinic carboxylic acid and at least one hydrophobic link type complex (C10- C30)-Olkiluoto ether.

5. The composition according to p. 4, characterized in that the anionic amphiphilic polymers crosslinked using a crosslinking polymerized monomers containing the group CH2With < and at least one other polymerized group, unsaturated communication which does not involve one against another, in particular, using a simple polyallylamine esters, such as polyallylamine and polyethylentereftalat.

6. The composition according to p. 4 or 5, characterized in that the anionic amphiphilic polymer is selected from polymers that are composed of 95 to 60 wt.% acrylic links, 4 to 40 wt.% acrylate units and 0.1 - 6 wt.% parts of a crosslinking monomer, or which consist of 96 to 98 wt.% acrylic links, 1 to 4 wt.% acrylate units and 0.1 to 0.6 wt.% parts of a crosslinking monomer.

7. The composition according to PP.1 - 6, characterized in that it contains up to 1 wt.% appropriate emulsifying system, preferably 0.2 to 0.4 wt.%.

8. The composition according to PP.1 to 7, characterized in that targanta, Laurelville and ethoxydiglycol.

9. The composition according to PP.1 to 8, characterized in that it contains 40 - 40 wt.% glycol.

10. The composition according to PP.1 to 9, characterized in that the active agent is selected from agents modulating the differentiation and/or proliferation and/or pigmentation of the skin, antibacterial agents, antiparasitic agents, antifungal agents, anti-inflammatory agents, steroidal or non-steroidal type, anesthetic agents, antipruritic agents, antiviral agents, keratolytic agents, agents against free radicals, protivoseborainey agents, protivoprigarnykh agents, anti-acne agents, antimetabolites, agents to combat hair loss and antiseptics.

11. The composition according to PP.1 to 10, characterized in that it contains of 0.0001 - 20 wt.%, calculated on the total weight of the composition, of at least one active agent, preferably 0,025 - 15 wt.%.

12. The composition according to PP.1 - 11, characterized in that the oil phase is present in an amount of 5 to 50 wt.%, calculated on the total weight of the composition, preferably 15 to 25 wt.%.

13. The composition according to PP. 1 - 12, characterized in that the aqueous phase is present in an amount of 10 to 75 wt.%, in calculating what it contains up to about 3 wt. % calculated on the total weight of the composition, of at least one simulator, preferably up to 2 wt.%.

15. The composition according to PP. 1 to 14, characterized in that it further comprises at least one gelling agent and/or thickening agent in concentrations up to 5 wt.%, calculated on the total weight of the composition.

 

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EFFECT: improved preparing method.

6 cl, 1 tbl, 8 ex

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