RU2282473C2 - Curative-prophylactic pomade eliciting antiviral activity and method for its preparing - Google Patents

Abstract

FIELD: medicinal cosmetology.

SUBSTANCE: invention relates to the curative-prophylactic lipstick. The curative-prophylactic pomade comprises aciclovir as an active component, lanolin, castor oil, larch balsam, bee wax, pot-marigold oily extract as accessory substance and, additionally, lecithin, cacao oil, Saint-John's-wort oily extract, retinal acetate (vitamin A), tocopherol (vitamin E) or tycveol or gourd seeds oil, propolis oily extract, nipagin, essential oil wherein components are taken in the definite quantitative ratio. By another variant, alpisarin or flakosid or helepin or hossipol are used as active component and accessory substances as by the first variant. Pomade is prepared by mixing components at heating and pomade sticks are formed and packaged into boxes. Pomade possesses an anti-inflammatory and antiviral effect, provides avoiding herpes appearance on face at the initial stage of disease and to accelerate recovery at later using.

EFFECT: improved, enhanced and valuable medicinal and cosmetic properties of pomade.

3 cl, 2 tbl, 1 ex

Description

The invention relates to cosmetology and medicine, in particular to medical and cosmetic products with anti-inflammatory and antiviral effects.

It is known what troubles people get from a disease that is popularly called a “cold”, and in medicine - a herpes simplex virus. The disease manifests itself in the form of rashes and sores around the mouth, nose and lips, causing pain and discomfort at the most inappropriate moments of life.

In fact, this is not a commonplace malaise, but a rather serious disease of a viral nature. Herpes simplex virus is very common - currently up to 90% of people on Earth are carriers of it. At the same time, about 25% of the population regularly (on average 2 times a year) experiences bouts of “colds”, the manifestations of which are just rashes on the face. The primary infection occurs mainly in childhood through family contacts, and then the virus penetrates through the skin to the nerve endings, where it rests in an inactive state. Colds and flu, emotional upset and stress, upset stomach, fatigue, physical weakness, etc. can cause the virus to become active. The virus returns through the nerves back to the skin, causing a sensation of tingling, burning, numbness. Then other unpleasant and painful symptoms of the “cold” appear in the form of blisters, sores, scabs, which can serve as a source of infection for others, cause eye infection and genital herpes.

Known therapeutic and cosmetic agents for combating the herpes simplex virus using the substance acyclovir - an analogue of the purine nucleoside deoxyguanidine, a normal component of deoxyribonucleic acid (MD Mashkovsky. Medicines. T.2, Kharkov, Torsing, 1997 [1]).

Acyclovir is an antiviral drug that is especially effective against herpes simplex viruses and herpes zoster. With herpes, acyclovir prevents the formation of new elements of the rash, reduces the likelihood of skin dissemination and visceral complications, accelerates the formation of crusts, and alleviates pain in the acute phase of herpes zoster. The drug also has an immunostimulating effect [1].

Along with ingestion, acyclovir is applied topically in the form of ointment or cream for infections of the skin and mucous membranes caused by the herpes simplex virus ([1], Khakhalin LN, Abazova FI Acyclovir in the treatment of acute and relapsing herpes diseases. Clinical Pharmacology and Therapy, 1995, No. 4, pp. 78-81).

In particular, a pharmaceutical composition with antiviral activity (patent of the Russian Federation No. 2175230), which includes acyclovir as an active substance and is made in the form of an ointment based on propylene glycol, also relates to similar preparations. A similar consumer form has a herpes anti-herbal cream based on the acyclovir Zovirax of Glaxo Velkam company, Great Britain.

However, the disadvantage of these drugs is the implementation in the form of an ointment or cream, which creates certain inconvenience when used in various situations. Another disadvantage is the use of ingredients that have an undesirable effect from the point of view of modern cosmetology on the skin. In particular, potentially toxic, but cheap synthetic petrochemical products are used, such as liquid paraffin, propylene glycol, etc., which, "sealing" moisture in the skin, give a temporary effect, but interfere with the normal functioning of the skin.

More convenient to use is the consumer form of the treatment of preventive anti-herpes drugs in the form of cosmetic lipstick containing biologically active antiviral additives.

In particular, there is a well-known anti-herpes anti-herbal lipstick manufactured by NPP “Snow Leopard”, Moscow (RF patent No. 2093140, Mcl. A 61 K 7/025 - prototype), in which acyclovir or foscarnet are used as dietary supplements sodium, or RNase. In addition, it used oil extracts of medicinal plants - calendula or celandine, which enhance the anti-inflammatory and analgesic effects. A number of auxiliary substances used in cosmetics technology are also used: perfume and castor oils, lanolin, beeswax, paraffin, ceresin, olive oil, butyl stearate, terlan, carnauba and candellil wax, confectionery fat, tween-60, or tween-80, or sorbitan oleate, antal SU, larch gum resin, perfume.

However, the disadvantage of the prototype is the use as ingredients of synthetic petrochemical products - paraffin, ceresin, perfume oil, as well as emulsifiers of the tween type - products of interaction with ethylene oxides, the safety of which is doubtful (R.A. Fridman. Cosmetics technology. M .: Food industry, 1964 )

The objective of the present invention is to expand the range of domestic remedies for the fight against herpes simplex, the creation of a highly effective anti-herpes cosmetic product, characterized by a minimum of contraindications and side effects, ensuring ease of use in any environmental conditions.

The technical result is a comprehensive anti-herpes, wound healing and cosmetic effect while eliminating any side effects and harmful effects due to the synergy of specific antiviral agents and agents that positively affect the skin, mainly of natural origin.

The proposed anti-herbal lipstick contains mainly natural ingredients, which avoids the harmful effects on the skin, typical for the use of synthetic products. A convenient consumer form in the form of lipstick in a pencil case allows you to always have the product on hand, carry it in your pocket or purse and use it at any time and in any situation.

The essence of the invention lies in the fact that in one embodiment, therapeutic and preventive lipstick with antiviral activity, including as an active substance acyclovir and as auxiliary substances lanolin, castor oil, larch balm, beeswax, marigold oil extract, additionally contains lecithin, cocoa butter St. John's wort oil extract, retinol acetate (vitamin A), α-tocopherol (vitamin E), or pumpkin, or pumpkin seed oil, propolis oil extract, nipagin, essential oil in the following ratio scientific research institute of components, wt.%: acyclovir 3.0-5.0; larch balm 1.0-3.0; lanolin 7.0-9.0; lecithin 1.0-3.0; beeswax 20.0-25.0; cocoa butter 6.0-8.0; St. John's wort oil extract 1.0-3.0; marigold oil extract 1.0-3.0; retinol acetate (vitamin A) 0.3-0.8; α-tocopherol (vitamin E), or pumpkin, or pumpkin seed oil 0.3-0.8; propolis oil extract 7.0-9.0; nipagin 0.1-0.3; essential oil 0.6-1.0; castor oil - the rest.

In another embodiment, the treatment and prophylactic lipstick with antiviral activity, including the biologically active substance and as adjuvants, lanolin, castor oil, larch balm, beeswax, calendula oil extract, contains alpizarin, or flacoside, or helepin, or gossypol and additionally as adjuvants lecithin, cocoa butter, St. John's wort oil extract, retinol acetate (vitamin A), α-tocopherol (vitamin E), or pumpkin seed oil or t kvy, oil extract of propolis, nipagin, essential oil with the following ratio of components, wt%: alpizarin or flakozid or helepin or gossypol 3.0-5.0;. larch balm 1.0-3.0; lanolin 7.0-9.0; lecithin 1.0-3.0; beeswax 20.0-25.0; cocoa butter 6.0-8.0; St. John's wort oil extract 1.0-3.0; marigold oil extract 1.0-3.0; retinol acetate (vitamin A) 0.3-0.8; α-tocopherol (vitamin E), or pumpkin, or pumpkin seed oil 0.3-0.8; propolis oil extract 7.0-9.0; nipagin 0.1-0.3; essential oil 0.6-1.0; castor oil - the rest.

A method of manufacturing a therapeutic and prophylactic lipstick with antiviral activity, comprising mixing the components during heating, forming lipstick pencils and packing them in pencil cases, consists of castor oil, beeswax and cocoa butter being mixed at a temperature of 80-100 ° C, in the molten mixture, crushed larch balm, nipagin and an emulsion of lecithin in lanolin, previously obtained by adding lecithin to a heated lanolin and mixing them for 15 min at a temperature of 80-100 ° C, kneading t weight until smooth for 30 minutes, after cooling the mixture to 60 ° C injected oil extract of propolis, oil extracts of St. John's wort and calendula, vitamins A and E, biologically active substance and essential oil, continue stirring at room temperature for 30-40 min until thickening, the hardened mass is maintained for at least 12 hours until it ripens, after which it is heated to 50-60 ° C.

The ingredients that make up the proposed anti-herbal lipstick have the following properties.

In the first embodiment of the proposed tool as a biologically active substance that determines the anti-herpes properties of the proposed lipstick, is used, as in the prototype, acyclovir (VFS 42-2778-96) in an amount of 3.0-5.0 wt.%, The properties of which are described above .

Larch balm (TU 13-4000177-116-84), introduced into lipstick in an amount of 1.0-3.0 wt.%, Is a natural remedy with protective properties, has phytoncide and antiseptic properties, accelerates wound healing.

Lanolin (FS 42-2420-88), introduced in an amount of 7.0-9.0 wt.%, Is a product of animal origin and is a mixture of fatty acids, wax-like esters of fatty acids, cholesterol, isocholesterol and ceryl alcohol. Gives skin softness, velvety, firmness. Under the action of ultraviolet rays of the sun, vitamin D is formed from cholesterol.

Lecithin (TU 6.02-829-83), administered in an amount of 1.0-3.0 wt.%, Refers to phosphatides. It is a compound close to fats that plays a huge physiological role in animal and plant organisms. Phosphatides are part of the cell membrane and determine its permeability and, therefore, intercellular metabolism. Hydrophilic colloid lecithin is an excellent disinfectant that penetrates deep into the skin and plays the role of an active skin rejuvenator. Lecithin gives firmness and elasticity to weakened skin, stimulates skin activity, especially in combination with lanolin.

Beeswax (GOST 21179-90), introduced in an amount of 20.0-25.0 wt.%, Is an excellent thickening base and plasticizer for lipstick, giving the product a marketable appearance, the necessary hardness. At the same time, it contains lipochromes, carotenoids and biogenic stimulants. Wax has a wonderful effect on the skin, giving it a pleasant softness and velvety, protects against the effects of adverse environmental factors.

Cocoa butter, used in an amount of 6.0-8.0 wt.%, Is a solid low-melting fat, very valuable for lipsticks. Its use normalizes local thermoregulation, contributes to the normal metabolism in these areas. Covering normal or inflamed tissues, protects the exteroreceptors of sensitive nerve endings from the effects of adverse environmental factors. It has photoprotective properties.

St. John's wort oil extract (TU 217 RSFSR 87-89), used in an amount of 1.0-3.0 wt.%, Contains many biologically highly active substances (azulene, flavins, vitamins, etc.). It is used as a hemostatic, anti-inflammatory and disinfectant, soothing skin irritation and promoting healing in purulent inflammatory processes of the skin.

Calendula oil extract (TU 217 RSFSR 87-89), used in an amount of 1.0-3.0 wt.%, Contains protein substances, carotene, phytoncides. It has antiseptic (bactericidal) properties, soothes irritation, relieves inflammation.

Retinol acetate (vitamin A) according to FS 42-3183-95, FS 42-2403-96 in an amount of 0.3-0.8 wt.% Gives the skin a good color, softens it, ensures normal activity. It is used for sunburn, frostbite, burns, protects the skin from exposure to sunlight.

α-tocopherol (vitamin E) according to FS 42-1642-95 in an amount of 0.3-0.8 wt.% - antioxidant, increases the absorption and effect of vitamin A, softens and improves the nutrition of the skin.

As an alternative, the pumpkin preparation (FS 42-3651-98) can be used - a fatty oil obtained by cold pressing from pumpkin seeds and containing groups of biologically active substances balanced by nature: phosphatides, tocopherols, carotenoids, fatty acids. Tykveolum is independently recommended as an anti-inflammatory and regenerative agent for ordinary and genital herpes. An alternative can also be pumpkin seed oil according to FS 42-3002-97.

Propolis oil extract prepared by extracting propolis (GOST 28886-90) in olive oil (TU 10-04-11 / 13-87) or soybean oil (GOST 7825-76) and introduced into the proposed lipstick in the amount of 7.0-9 , 0 wt.%, Has an anti-inflammatory effect. The antiviral effect of propolis extract on herpes virus infection was noted.

Nipagin (methyl ether of paraoxybenzoic acid) according to TU 18-16-325-80 is a preservative component introduced into lipstick in an amount of 0.1-0.3 wt.%, Which is designed to increase its shelf life.

Essential oil (sage, chamomile, peppermint, etc.), used in an amount of 0.6-1.0 wt.%, Further enhances the anti-inflammatory properties of lipstick. At the same time, it serves as a perfume and is selected taking into account the requirements of modern cosmetics to create a pleasant sensation.

Castor oil according to GF XI or GOST 18102-95 is introduced into the proposed lipstick in an amount in addition to 100 wt.%. It reduces the return of water to the skin and, penetrating into the surface epithelial layer, impregnates, mechanically softens it, imparts elasticity, protects from harmful external influences and sudden changes in temperature.

The use of the ingredients proposed above in the quantitative proportions presented in accordance with the developed technology ensures the production of anti-herbal lipstick according to the first embodiment, the advantage of which with respect to the prototype is the use of natural components (except for the biologically active substance acyclovir), which almost completely eliminates the occurrence of side effects.

A further increase in the level of harmlessness of anti-herbal lipstick due to the use of exclusively natural components can be achieved by the implementation of the proposed second embodiment of the invention, in which 3.0-5.0 wt.% Of a plant substance alpizarin or flacoside are used as a biologically active antiviral ingredient , or helepin, or gossypol.

Alpizarin (mangiferin) according to FS 42-2843-92 is obtained (RF patent 2032413) from the grass of Alpine penny, yellowing penny, as well as leaves of the mango tree.

Flacoside is obtained from Amur velvet leaves and Laval velvet leaves.

Helepin is obtained from the aerial part of the penny penny forest.

Gossypol is obtained by processing cotton seeds or from cotton roots.

In the second embodiment of the invention provides for the use of the same excipients and in the same quantitative proportions as in the first embodiment.

Table 1 shows specific examples illustrating the invention.

Table 1. Name of components Mass fraction (%) Example 1 Example 2 Example 3 Acyclovir - four - Alpizarin 3 - 5 Larch Balm 3 2 one Lanolin 7 8 9 Lecithin 1.8 2 3 Beeswax twenty 22.5 25 Cacao butter 6 7 8 Hypericum oil extract one one 3 Marigold oil extract one one one Vitamin A 0.3 0.6 0.8 Vitamin E 0.8 0.6 0.3 Propolis Oil Extract 9 8 7 Nipagin 0.1 0.2 0.3 Essential oil one 0.9 0.6 Castor oil 46 44 36

The proposed lipstick has been tested at the Center for Beauty and Health. Under observation were 24 patients aged 16 to 62 years with a diagnosis of herpes simplex in various stages of development. Localization of herpetic rash - red border of the lips.

The rash in the patients was represented by vesicular elements against the background of edema and hyperemia, accompanied by itching and a burning sensation. Depending on the time elapsed since the onset of the disease, the phenomena of edema and hyperemia, or vesicles, or erosion and crust predominated in the clinical picture.

Observed were divided into three groups:

the first received therapeutic lipstick with acyclovir, the second - therapeutic lipstick with alpizarin, the third - Zovirax cream (comparison drug).

Lipstick was applied in a thin layer on unchanged or ulcerated areas of the skin and mucous membranes 4-5 times a day (after 4 hours).

For a more objective assessment of the action of the proposed funds, the disease was conditionally divided into two phases, depending on the stage of the herpetic process.

The first phase (three people in each group who started treatment on the first day of the disease) is characterized by subjective sensations of burning and itching, mild swelling and hyperemia in the lesion.

The second phase (6 people in each group who started treatment on the 2nd-3rd day) is characterized by multiple grouped vesicles against the background of swelling and pain, or the vesicles burst with the formation of erosion, or shrink into crusts.

Table 2.
Regression (in percent) of all clinical manifestations of herpes simplex with lipstick and cream Cream "Zovirax" Anti-herpes lipstick with acyclovir Antiherpetic lipstick with alpizarin First phase 100.00% 100.00% 100.00% Second phase 83.00% 83.00% 67.00%

Clinical observations revealed a clear dependence of the results of the use of drugs on the time it started. The table shows that the most effective treatment was in the first phase of the disease. In the second phase, the effect of the use of invented drugs is also comparable in activity with the reference drug - cream "Zovirax".

None of the patients who used anti-herbal lipstick according to the invention had side effects or unpleasant subjective sensations. In 30% of patients who used anti-herbal lipstick, blood tests were taken before and after applying lipstick, which did not reveal the pathological effect of the drugs. All patients note the softness of the red border of the lips, the absence of peeling and unpleasant subjective sensations.

From the above data it is seen that the use of lipstick according to the invention gives a comprehensive anti-herpes, wound healing and cosmetic effect without any side and harmful effects, that is, a technical result is achieved.

The technology for the proposed anti-herbal lipstick is clear from the example below.

EXAMPLE. Before preparing the required mass of anti-herbal lipstick in the amount of 1000 g, an emulsion of lecithin in lanolin is prepared. A container with a weighed portion of 70 g of lanolin is installed in a water bath and heated until it melts. With constant stirring, a portion of lecithin pieces of 10 g is loaded into molten lanolin. Lecithin is dissolved with periodic stirring at a temperature of 80-100 ° C until lecithin is completely dissolved. 517 g of castor oil, 200 g of beeswax and 60 g of cocoa butter are loaded into a container installed in a water bath. The melting of the components is carried out with periodic stirring at a temperature of heating water of 80-100 ° C. Under stirring, the previously prepared emulsion of lecithin in lanolin, 10 g of ground larch balm and 1 g of nipagin are loaded into the molten mixture. With constant stirring and a temperature of heating water of 80-100 ° C, the mass is kneaded to a homogeneous state for 30 minutes. The heating is turned off and, while stirring, when the temperature of the heating water reaches not more than 60 ° C, weighed portions of the remaining components in accordance with the recipe: propolis oil extract 70 g, St. John's wort oil extract 10 g, marigold oil extract 10 g, vitamin A 3 g, vitamin E 3 g, the biologically active substance acyclovir 30 g and sage essential oil 6 g. After loading all the components, stirring is continued for 30-40 minutes at room temperature until thickened. The hardened mass is kept for at least 12 hours until it ripens, after which it is heated in a container in a water bath to 50-60 ° C, periodically mixing. The hot mass is poured into the mold cells, which are placed in the refrigerator for at least 40 minutes. Ready-made lipstick pencils, taken from the injection mold, have a yellowish-green color, a pleasant smell. Next, lipstick pencils are packaged in pencil cases.

It is recommended to apply lipstick in a thin layer on unchanged or ulcerated areas of the skin and mucous membranes 4-5 times a day (after 4 hours). The use of anti-herpes lipstick in the early stages of herpetic manifestations increases its antiviral effect and can completely prevent the appearance of rashes. Contraindication is individual intolerance. The shelf life of anti-herpes lipstick is 12 months.

The proposed treatment-and-prophylactic lipstick was tested at the Center for Cosmetic Correction of the Central Clinical Hospital of the Russian Academy of Sciences (Conclusion No. 10135/5 of 01/12/2000), was recognized in terms of quality and safety to meet the standards and requirements for perfumes and cosmetics, and recommended (Hygienic conclusion of the Ministry of Health RF №77.01.06.915.Т.00846.01.0 dated January 18, 2000) for production under the conditions of ZAO Evalar (Biysk).

Claims (3)

1. Treatment and prophylactic lipstick with antiviral activity, including as an active substance acyclovir and as auxiliary substances lanolin, castor oil, larch balm, beeswax, marigold oil extract, characterized in that it additionally contains lecithin, cocoa butter, oil extract St. John's wort, retinol acetate (vitamin A), α-tocopherol (vitamin E), or pumpkin, or pumpkin seed oil, propolis oil extract, nipagin, essential oil in the following ratio, wt.%: Acyclovir 3.0-5.0 Larch Balm 1.0-3.0 Lanolin 7.0-9.0 Lecithin 1.0-3.0 Beeswax 20.0-25.0 Cacao butter 6.0-8.0 Hypericum oil extract 1.0-3.0 Marigold oil extract 1.0-3.0 Retinol Acetate (Vitamin A) 0.3-0.8 α-Tocopherol (Vitamin E), or pumpkin, or pumpkin seed oil 0.3-0.8 Propolis Oil Extract 7.0-9.0 Nipagin 0.1-0.3 Essential oil 0.6-1.0 Castor oil Rest 2. Treatment and prophylactic lipstick with antiviral activity, including biologically active substance and as adjuvants lanolin, castor oil, larch balm, beeswax, calendula oil extract, characterized in that it contains alpizarin or flacoside as a biologically active substance, or helepin, or gossypol, and additionally as adjuvants lecithin, cocoa butter, St. John's wort oil extract, retinol acetate (vitamin A), α-tocopherol (vitamin E), or pumpkin, or oil o pumpkin seeds, propolis oil extract, nipagin, essential oil in the following ratio, wt.%: Alpizarin, or flacoside, or helepin, or gossypol 3.0-5.0 Larch Balm 1.0-3.0 Lanolin 7.0-9.0 Lecithin 1.0-3.0 Beeswax 20.0-25.0 Cacao butter 6.0-8.0 Hypericum oil extract 1.0-3.0 Marigold oil extract 1.0-3.0 Retinol Acetate (Vitamin A) 0.3-0.8 α-Tocopherol (Vitamin E), or pumpkin, or pumpkin seed oil 0.3-0.8 Propolis Oil Extract 7.0-9.0 Nipagin 0.1-0.3 Essential oil 0.6-1.0 Castor oil Rest 3. The method of preparation of therapeutic and preventive lipstick with antiviral activity, which consists in mixing the components during heating, forming lipstick pencils and packing them in pencil cases, characterized in that at a temperature of 80-100 ° C castor oil, beeswax and cocoa butter are mixed, add crushed larch balm, nipagin and an emulsion of lecithin in lanolin to the molten mixture, previously obtained by adding lecithin to the heated lanolin and mixing them for 15 min at a temperature of 80-100 ° C, knead assu to a homogeneous state for 30 minutes, then after cooling the mixture to 60 ° C, injected oil extract of propolis, oil extracts of St. John's wort and calendula, vitamins A and E, biologically active substance and essential oil, continue stirring at room temperature for 30- 40 minutes before thickening, the hardened mass is held for at least 12 hours until it ripens, after which it is again heated to 50-60 ° C.