RU2299726C2 - Curative-prophylactic anti-infectious labial pomade - Google Patents

Abstract

FIELD: cosmetology.

SUBSTANCE: invention relates to curative-prophylactic anti-infectious labial pomade used in treatment of labial herpes preferably. The proposed curative-prophylactic anti-herpes pomade comprises wax, polyethylene glycol, phosphonoformic acid trisodium salt (phoscarnet), hydroxyethylidene-bisphosphonic acid potassium-sodium salt (xydofon), water, carbon dioxide extracts of medicinal plants, preserving agent and oily base. Pomade can comprise additionally aloe-vera, tea tree oil, lecithin, organic oxyacids, preserving agents, hyaluronic acid and titanium dioxide. Proposed pomade shows high effectiveness as an anti-herpes agent, moistens and softens lips, possesses pretty luster, resistance against rubbing out and possesses the enhanced stability under different climatic conditions.

EFFECT: improved and valuable properties of pomade.

10 cl, 5 ex

Description

The invention relates to medicine, in particular to medical cosmetics, and relates to the composition of anti-infectious lipstick, which can be used for the prevention and treatment of diseases caused primarily by herpes viruses, as well as influenza viruses, rubella, diseases caused by various microbial infections.

As you know, for the treatment of viral diseases, including various forms of herpes, various drugs of both synthetic and natural origin are used. Known antiviral antiherpetic agents, for example, include such well-known chemicals as acyclovir, foscarnet, as well as biologically active substances obtained from raw materials of natural origin, for example interferon, interleukin. One of the most effective antiherpetic drugs can be attributed to the trisodium salt of phosphonoformic acid, which is available as an injection solution called foscarnet or foscavir, as well as in an ointment called foscarnet sodium or triapten. This chemical compound acquired particular importance after reporting its ability to inhibit the reverse transcriptase of human immunodeficiency retrovirus / HIV /, the causative agent of AIDS-a / Lancet, 1985, No. 4, 1480-1482 /. As you know, antiviral drugs come in various dosage forms. One of these forms is lipstick, in particular lipstick, the most convenient in the treatment of such a viral disease as herpes. For example, lipstick with an antiviral effect is known, containing spermaceti, mink, stone fruit, perfume, castor oil, phytosterols, lanolin, ceresin, cocoa butter, beeswax / A.C. SU 1138162, A 61 K 7/025, 1983 /. However, this known composition has a slightly pronounced antiviral effect and is more likely a cosmetic product that heals cracks and wounds on the lips.

An antiviral agent with pronounced antiherpetic activity is another well-known therapeutic and preventive lipstick containing sodium foscarnet / trisodium salt of phosphonoformic acid / as an effective component / patent RU 2093140, A 61 K 7/025, 1997 /. This lipstick, in addition to sodium foscarnet, also contains olive, castor, perfume oils, butyl stearate, lanolin, terlan, larch gum resin, carnauba, candellil and beeswax, calendula or celandine oil extract, paraffin, confectionery fat, ceresin, teresin, teresin, Antal, perfume. Foscarnet sodium in the composition of this lipstick is introduced in the form of a dry crushed product. Lipstick has a fat base that does not contain water at all. The latter fact leads to the underestimated effectiveness of foscarnet due to its weak permeability to the inside of the epidermis. In addition, the absence of moisture in the lipstick reduces its cosmetic effectiveness, since when applied to the lips it does not have sufficient elasticity and therefore it is poorly applied to the lips and quickly erased, which also reduces the time of the therapeutic effect of foscarnet and thus reduces the effectiveness of the whole composition . In addition, the known composition, as shown by additional clinical trials, does not have sufficient resistance to the environment, for example to UV and IR radiation, to moisture, which limits the possibility of its use.

The object of the present invention is a therapeutic and prophylactic anti-infectious lipstick containing, wt.%: Trisodium salt of phosphonoformic acid (foscarnet sodium) 0.1-0.9, waxes 20-40, polyethylene glycol 0.5-5.0, potassium, sodium hydroxyethylidene bisphosphonic acid salt (xidiphon) 0.01-3.0, water 0.5-10.0, carbon dioxide extracts of chamomile and / or calendula 0.01-1.0, preservative 0.01-0.05 and oil base - rest. Additionally, the lipstick may contain 0.02-0.2 wt.% Tea tree oil, 0.5-2.0 wt.% Aloe vera. In addition, the lipstick may also contain, wt.%: Lecithin 0.05-1.0, hydroxy acids 0.01-0.5, hyaluronic acid 0.01-0.1, titanium oxide 0.2-1.0 , fragrance 0-1.5. As waxes, the composition of the new lipstick includes waxes from the following group: Carnauba, Candelillo, Ozokerite, beeswax, ceresin, lanolin, paraffin, spermaceti. The composition of the oil base includes oils selected from the group: liquid paraffin, castor, olive, rosehip oil, rapeseed, peanut, hydrogenated palm oil.

As the main component with anti-infective activity in the new composition, as in the prototype, trisodium salt of phosphonoformic acid is used. However, in the new composition, the content of this salt is only 0.1-0.9 wt.%, While in the prototype - 1.0-3.0 wt.% But, despite the lower content of one of the main components, the effectiveness of the new lipstick as an anti-infectious agent is higher than that of a well-known lipstick. This effect, confirmed by the following data, is achieved, first of all, due to the introduction into the composition of another well-known drug - xidifon, previously not used in lipstick formulations. The introduction of lipid known drug Xidiphon had a significant impact on the effectiveness of lipstick as a medicine. The increase in efficiency can be explained by the biological effectiveness of xidiphon, which when applied to the surface of the lips penetrates through the epidermis and integrates into the structure of cell membranes, which, in turn, enhances the permeability of the phosphonoformic acid salt through the epidermis. The presence of water, which is a solvent of the trisodium salt of phosphonoformic acid and the potassium salt of hydroxyethylidene bisphosphonic acid (xidiphone), also affects the permeability. Another important component of the new composition is polyethylene glycol, which also plays a multifunctional role. On the one hand, it is a solubilizer, miscible with water and promotes emulsification of the aqueous phase in the fat phase, and on the other hand, a softening agent that improves the cosmetic properties of lipstick. Additional lipstick studies have shown that specifically selected amounts of polyethylene glycol help improve lipstick adhesion on the lips. This new product belongs to the category of inverse emulsions "water in oil" and the water content in the lipstick is 0.5-10 wt.%, And the oil phase - the rest is up to 100 wt.%, About 35-80 wt.%, Depending on the amount of basic components and additives.

A significant role in the effectiveness of lipstick as a therapeutic and as a cosmetic product is played by the quantitative content of each of the components. For example, water, polyethylene glycol, waxes are structure-forming components and optimally selected amounts of these components affect the stability of the structure during its molding and storage. The main components of the new lipstick that are present in all variants of the performed composition include waxes and an oil base, which are components of the prototype composition. As you know, waxes are fat-like substances of plant, animal origin and fossils. As components of the new composition, waxes of all three of these types are used. Carnauba and / or Candelilla waxes, ozokerite are introduced as plant waxes in the new composition, beeswax, lanolin, spermaceti as animal waxes, and ceresin and paraffin as fossil waxes. Waxes in the composition simultaneously play the role of both hardener and structure-forming agent. The total wax content in the new tool is a total of 20-40 wt.%. Underestimation or overstatement of the wax content leads to a deterioration in the cosmetic properties of lipstick. In addition, a number of waxes have in the new composition and other useful additional functions. For example, beeswax is a biologically active substance that improves the body's immune system, lanolin, which is also a wax of animal origin, has a softening function. An essential component of lipstick is an oil base, which includes various oils. The oil base may include the following oils: liquid paraffin, castor, olive, peanut, rapeseed, grape seed oil, rosehip oil, hydrogenated palm oil (confectionery fat). The composition of lipstick is conditionally divided into the fat phase (oil base) and the aqueous phase. The composition of the fat phase, in addition to oils, includes waxes, as well as lipophilic additives, for example preservatives, in particular paraoxybenzoic acid esters, essential oils, for example, tea tree oil.

Phospholipids, for example, lecithin, which is a softener and emulsifier at the same time, are also introduced into the composition of the fat phase as an additive. In addition to the fat phase, the new lipstick, unlike the prototype, also contains the aqueous phase, which additionally makes it a moisturizing lipstick. In the aqueous phase of the lipstick, in addition to the trisodium salt of phosphonoformic acid (sodium foscarnet), xidiphone and polyethylene glycol, various hydrophilic additives, for example, carbon dioxide plant extracts, in particular chamomile, calendula, aloe vera extract, organic hydroxy acids, both synthetic and natural, are introduced origin, for example citric, lactic, salicylic, malic, mandelic, glycolic acids in the form of individual components or as a mixture of the listed hydroxycarboxylic acids in a weight quantity, in total constituting 0.01-0.5 wt.% of the total weight of the composition.

Hydroxy acids used in lipstick help protect the skin from dermatological signs of aging. In combination with other components of lipstick, oxycarboxylic acids increase the body's resistance to viral infections. Hyaluronic acid, which is an animal polysaccharide, can be added to the composition of the aqueous phase as an additive. On the one hand, it is a gelling agent that helps maintain a normal water balance, and on the other hand, it is an additional antiviral, antibacterial component. The selection of the amount of this component was carried out taking into account both its cosmetic and medicinal properties. As an additive, titanium oxide is also introduced into the new composition in a weight amount of 0.2-1 wt.% With respect to the total weight of the mixture. This component is preferably introduced in the form of nanopigments, and in the composition it plays the role of a photoprotective agent, as well as an additional structure former. A tea supplement of natural origin in the new composition is tea tree oil, introduced in an amount of 0.02-0.2 wt.%, Which in the composition performs both cosmetic and therapeutic functions. It, firstly, is a fragrance, and secondly, it is a biologically active additive that enhances the therapeutic effect of the use of lipstick. The amount of essential oil administered is determined based on its cosmetic properties and its biological activity. Additionally, synthetic cosmetic fragrances can be introduced. The amounts of these fragrances are determined by the consumer cosmetic properties of lipstick and make up 0-1.5 wt.% Of the total weight of the mixture. 0.01-0.05 wt.% Of any preservative used in cosmetics for similar purposes, for example, propoxy ester of paraoxybenzoic acid, vitamin E, is introduced into the lipstick. Other components, such as hydroxy acids, such as citric, tartaric, also play the role of preservatives malic acid. In addition to these additives, the composition of lipstick can include in effective quantities organic pigments and flavorings used in cosmetics.

The manufacturing technology of the new therapeutic and prophylactic anti-infectious lipstick is as follows. Separately, by mixing the specific ingredients, two phases are obtained: the fat phase, the so-called oil base, and the aqueous phase. The oil phase is obtained by mixing oils and waxes heated to 75-90 ° C, stirring the mixture until a homogeneous mass is formed, cooling it to 50-60 ° C and adding hydrophobic components, for example, carbon dioxide plant extracts, essential oils, metal oxides, phospholipids, perfumes, preservatives, flavoring. Separately, the aqueous phase is obtained by dissolving in water the trisodium salt of phosphonoformic acid, adding xidiphon in the form of an aqueous solution, polyethylene glycol and then hydrophilic additives, for example hyaluronic acid and / or water-soluble coloring pigments. The water-oil emulsion obtained after mixing the two phases is poured into appropriate forms.

The following are specific examples of the composition of the new lipstick, wt.%.

Composition 1.

Components, wt. share,%:

waxes - 40, including: candelilla - 20.0, carnauba - 5, bee - 5.0, lanolin - 5.0, spermaceti - 5.0;

oils - 56.42, including: petrolatum - 14.92, castor - 25.0, olive - 15.0, hydrogenated palm oil - 1.5;

polyethylene glycol - 0.5, xidiphone - 0.01, foscarnet - 0.9, water - 0.5, paraben - 0.01, carbon dioxide solution of calendula - 0.01, tea tree oil - 0.2, aloe vera - 0.5, lecithin - 0.05, hyaluronic acid - 0.1, lecithin - 0.5, titanium dioxide - 0.3.

Composition 2.

Waxes - 20, including: Candelilla - 6.0, bee - 3.0, ceresin - 3.0, ozokerite - 8.0;

oils - 76.7, including: petrolatum - 40, castor - 30.0, hydrogenated palm - 10.0;

polyethylene glycol - 2.0, xidiphone - 0.3, foscarnet - 0.3, water - 0.5, propyl paraben - 0.02;

carbon dioxide solution of calendula - 0.05, carbon dioxide solution of chamomile - 0.01, tea tree oil - 0.1, lecithin - 0.02, hyaluronic acid - 0.01.

Composition 3

Waxes - 29, including: carnauba - 7.0, bee - 1.0, ceresin - 8.0, spermaceti - 6.0, paraffin - 7.0;

oils - 51.6, including: castor - 31.6, olive - 10, rapeseed - 10.0;

polyethylene glycol - 5.0, xidifon - 3.0, foscarnet - 0.5, water - 10.0 vitamin E (preservative) - 0.05, carbon dioxide solution of chamomile - 0.04, aloe vera - 2.0, oil tea tree - 0.05, lecithin - 1.0, lactic acid - 0.02, titanium dioxide - 1.0.

Composition 4

Waxes - 30, including: Candelilla - 14, ceresin - 5.0, lanolin - 8.0, paraffin - 2.0;

oils - 62.53, including: petrolatum - 36.53, olive - 20.0, rosehip oil - 5.0, hydrogenated palm - 2.0;

polyethylene glycol - 1.0, xidiphone - 1.0, foscarnet - 0.15, water - 2.0, propyl paraben - 0.01, carbon dioxide solution of calendula - 0.5, carbon dioxide solution of chamomile - 0.5, aloe vera - 1.0, citric acid - 0.01, salicylic acid - 0.05, hyaluronic acid - 0.05, titanium dioxide - 0.2, perfume 1.0.

Composition 5

Waxes - 25, including: candelilla - 10.0, bee - 2.0, lanolin - 5.0, paraffin - 8.0;

oils - 68.35, including: liquid paraffin - 35.35, castor - 15.0, peanut - 15.0, hydrogenated palm - 3.0;

polyethylene glycol - 2.5, xidiphone - 0.1, foscarnet - 0.2, water - 1.0, propyl paraben - 0.02, carbon dioxide solution of calendula - 0.05, carbon dioxide solution of chamomile - 0.05, aloe vera - 2.0, tea tree oil - 0.02, lecithin - 0.5, citric acid - 0.2, salicylic acid - 0.1, malic acid - 0.2, hyaluronic acid - 0.01, titanium dioxide - 0 ,5.

The above examples do not limit the possibility of introducing the other components listed above within the indicated weight ranges.

A new therapeutic lipstick was tested at the First Medical Academy. I.M.Sechenova at the Department of Skin and Sexually Transmitted Diseases. Under observation were 20 patients suffering from herpes simplex on the lips. As in the prototype, for a more objective assessment of the effect of lipstick, its effectiveness was evaluated at three stages of the herpetic process on the lips. Lipstick was applied in a thin layer on the affected area of the lips 3-4 times a day.

The first stage of the disease includes a process characterized by subjective sensation, mild swelling and hyperemia, which lasts without treatment on average 1-3 days. 10 out of 20 selected patients had the first stage of herpes disease. Lipstick was applied in a thin layer 3-4 times a day. At the first stage of the disease, the effectiveness of lipstick was observed after 1-2 single application of lipstick and in 9 patients out of 10 by the end of the first day after the 3rd or 4th application, and on the second day, these patients experienced almost complete recovery . The second stage of the disease includes a process that proceeds with the formation of multiple scattered vesicles against the background of increasing swelling and hypermia, which lasts without treatment for up to 5-6 days. To test the effectiveness of the new lipstick at this stage of the disease, 5 patients with the indicated signs of the second stage of the disease were selected. The effect of treatment with daily 3-4-fold application of lipstick was observed in three patients after two days of treatment, in the fourth patient on the 3rd day and in the fifth on the 4th day of treatment. The third stage of the disease includes a process that proceeds without treatment on average from 3 to 8 days and is accompanied by the bursting of vesicles with the formation of erosion or crust, after which all clinical manifestations regress. And to test the effectiveness of the new lipstick for the treatment of the disease at this stage, 5 patients were also selected. Unlike the prototype, the new lipstick is effective at this stage of the disease. The positive effect of applying lipstick in 3 patients at this stage of the disease was already observed on 3-4 days and in 1 patient on the 6th day. Drying was observed, and then the disappearance of the crust.

The treatment process was not accompanied by a regression of the clinical manifestations of herpes.

According to the accepted criterion for evaluating the effectiveness of the prototype, it is believed that lipstick is effective as a herpes medicine in cases where the duration of treatment is reduced by 2 times compared with the course of this disease without treatment. Thus, using this criterion, a new therapeutic and preventive anti-infectious lipstick can be considered a highly effective therapeutic agent at all stages of treatment for herpes on the lips, which cannot be said about the prototype lipstick, which is not at all effective in the treatment of herpes in the third stage of the disease. In addition, the new lipstick has high cosmetic properties, namely it moisturizes and softens the lips, has a pleasant gloss, does not wear off for a long time, and has increased resistance in different climatic conditions (from 6 months to 1 year), including under UV irradiation. Additional studies conducted on the same patients show that the new lipstick also has a prophylactic effect in the case of influenza virus and other viral acute respiratory infections.

Claims (10)

1. Therapeutic and preventive anti-infectious lipstick containing trisodium salt of phosphonoformic acid, wax, as well as plant extracts, preservatives, an oil base, characterized in that it contains carbon dioxide extracts of chamomile and / or calendula as plant extracts, and also additionally contains potassium salt hydroxyethylidene bisphosphonic acid, polyethylene glycol and water in the following weight ratio of mixture components, wt.%: Waxes 20-40 Polyethylene glycol 0.5-5.0 Phosphonoformic acid trisodium salt 0.1-0.9 Potassium salt hydroxyethylidene bisphosphonic acid 0.01-3.0 Carbon dioxide solutions of chamomile and / or calendula 0.01-1.0 Preservative 0.01-0.05 Water 0.5-10.0 Oil base The rest is up to 100% 2. The treatment and prophylactic anti-infectious lipstick according to claim 1, characterized in that the wax contains waxes selected from the group: candelilla wax, carnauba wax, beeswax, lanolin, spermaceti, paraffin, ceresin. 3. The treatment and prophylactic anti-infective lipstick according to claim 1, characterized in that it contains an oil base comprising oils selected from the following group: castor, olive, rapeseed, peanut, petroleum jelly, rosehip oil. 4. The treatment and prophylactic anti-infective lipstick according to claim 1, characterized in that it further comprises tea tree oil in an amount of 0.01 wt.% Of the total weight of the composition. 5. Therapeutic and preventive lipstick according to claim 1, characterized in that it further comprises a herbal supplement - aloe vera in an amount of 0.1-2.0 wt.% Of the total weight of the composition. 6. The treatment and prophylactic anti-infectious lipstick according to claim 1, characterized in that it further comprises lecithin in an amount of 0.05-0.5 wt.% Of the total weight of the composition. 7. Therapeutic prophylactic anti-infectious lipstick according to claim 1, characterized in that it further comprises an organic hydroxy acid or a mixture of organic hydroxy acids selected from the group: citric, milky, salicylic, apple in an amount of 0.01-0.5 wt.% of the total weight of the composition. 8. Therapeutic and preventive anti-infectious lipstick, characterized in that it additionally contains hyaluronic acid in an amount of 0.01-0.1 wt.% Of the total weight of the composition. 9. The treatment and prophylactic anti-infectious lipstick according to claim 1, characterized in that it further comprises titanium oxide in an amount of 0.2 to 1.0 wt.% Of the total weight of the composition. 10. The therapeutic and prophylactic anti-infectious lipstick according to claim 1, characterized in that, as a preservative, it preferably contains paraoxybenzoic acid propyl ester in an amount of 0.01-0.05 wt.% Of the total weight of the composition.