RU2093140C1 - Medical-and-prophylactic lipstick and method for its production - Google Patents

Abstract

FIELD: cosmetology. SUBSTANCE: lipstick contains perfumery and castor oils, lanolin, beeswax, paraffin, ceresine and flavor. Additionally lipstick has olive oil, butylstearate, terlan, carnauba and candelilla wax, confectionery fat, twin-60 or twin-80 or sorbitanoleate, antal, larch oleo resin, and biologically-active additive including sodium phoscarnet, or acyclovir, or ferment PHK and oil extract of calendula or celandine. Method involves heating the oil up to 70-80 C, and at mixing the following ingredients are added: carnauba and candelilla wax, ceresine, paraffin, terlan, lanolin, fat, butylstearate, antal. Mixing is conducted till the mixture of auxiliary substances is formed. Then temperature is decreased up to 40-50 C and the following components are added: larch oleo resin, biologically-active additive and flavor. Biologically- active additive is preliminarily activated: dry sodium phoscarnet ground to size of 0.1-3 microns or acyclovir or ferment PHK is mixed with surface-active substance and oil extract of drug plants. Mixture is thoroughly mixed up to forming homogeneous substance in the form of microcapsules, then beeswax is added in it and mixed again, and gradually heated up to 80 C. Dry antiviral substance is ground by ultrasound disintegrator with ultrasound power of 200 db for 5 min. Mixing of antiviral substance, surface-active substances and oil extracts of drug plants are carried out for 1-2 h. EFFECT: higher antiviral and antiherpes effect. 6 cl, 1 tbl

Description

 The invention relates to medicine, namely to the creation of therapeutic agents used in medicine and cosmetics as antiviral antiherpetic agents.

 Currently, a wide range of drugs is known to be used to treat viral diseases such as influenza, acute respiratory viral infections, herpes and shingles. Among them are known chemical agents acyclovir (zovirax), remantadine, arbidol, oxolin; biologically active polypeptides or low molecular weight proteins with antiviral or immunomodulating activity of interferons, interleukins. Medicines isolated from medicinal plants are known and used in medical practice as antiviral agents, helepin (a purified extract of the penny penny) and gossypol (a preparation from cotton roots) (MD Mashkovsky. Medicines, 1993, vol. II, p. 388 403 )

 However, the problem of finding new antivirus agents and how to use them remains relevant. This is due to the fact that some of these drugs act mainly on a certain type of virus. So, remantadine is active against type A influenza virus. Many antiviral drugs have contraindications or cause side effects when taken orally. So, acyclovir can cause an allergic reaction. The use of certain antiviral drugs for external use is difficult due to the instability of antiviral substances (for example, interferon).

 Certain drugs that are effective in various viral infections are known and used by topical application. So, Aciclovir ointment (Zovirax) based on cyclovir and Triapten ointment (based on foscarnet sodium). These ointments contain 5% and 2% of active substances, respectively, and fillers. Foscarnet sodium has antiviral activity against herpes viruses 1 and 2, oncogenic viruses, influenza A virus, hepatitis B virus and some others inhibits the replication and polymerase reactions of viruses. Acyclovir has antiviral activity against herpes simplex virus type 1 and 2, herpes zoster virus, Epstein-Barr virus and cytomegalovirus (Mashkovsky MD Drugs, 1993; "Drugs of foreign firms", 1993).

 However, Zovirax ointment can cause side effects: a skin rash, a painful burning sensation at the site of application of the drug. Treatment with foscarnet sodium is safer, however, the drug is slightly inferior to Zovirax in activity. In addition, the substances acyclovir and foscarnet sodium are hydrophilic substances, which reduces the activity of the active substance in the composition of such dosage forms as ointment and cream.

 Lipsticks are known and used mainly in cosmetics, some of which, due to the biologically active substances contained in them, have anti-inflammatory, antiherpetic effects.

 So, a well-known hygienic lipstick containing distilled monoglycerides, ceresin, lanolin, carbon dioxide extracts of sea buckthorn, sage, carrot seeds, sunflower oil, propylene glycol, propyl ether paraoxybenzoic acid, Antal C, fragrance and perfume oil.

 Due to the presence of a natural complex of biostimulants in her formulation, lipstick has an anti-inflammatory, regenerating effect on the epidermis of the lips (USSR author's certificate 1597193, 1988 A 61 K 7/02).

 The closest in technical essence and the achieved result is a lipstick in the form of a cream containing spermaceti, mink oil, stone seed oil, perfume oil, phytosterols, lanolin, paraffin, ceresin, cocoa butter, beeswax, perfume and castor oil. Lip cream has anti-inflammatory and wound healing (regenerating) effects in case of small lip cracks and herpes. When applying it, healing of cracks and wounds, the elimination of herpetic eruptions is observed (USSR author's certificate N 1138162, 1983 A 61 K 7/025). A disadvantage of the known lipstick is a weak antiviral activity.

 A known method for the manufacture of lipstick, including carnauba wax, candelilla wax, beeswax, paraffin, ceresin, terlan, PES-5 liquid, diisopropyl adipate, butyl stearate, mink fat, coffee oil and fat extract, oil extracts of lily of the valley and bird cherry, Antal C titan, paste and dye, mother-of-pearl paste PPV-1, perfume and perfume oil.

To prepare lipstick, perfume oil is heated to 70 - 80 ^o C and with stirring, wax is added: carnauba, candelilla, bees, as well as ceresin, paraffins, terlan, silicone fluid, mink fat, diisopropyl adipate, butyl stearate, Antal C. In addition, injected white titanium paste, dye and pearlescent paste PPV-1. Stirring is continued until a homogeneous mass is formed. Then the temperature is reduced to 45-50 ^° C and oil extracts of biological active substances and perfume are introduced with constant stirring (USSR copyright certificate N 1708341, 1989b, class A 61 K 7/027).

 An object of the invention is to expand the range of therapeutic and prophylactic agents, the creation of lipsticks with antiviral antiherpetic effect.

 In addition, the objective of the invention is to improve the method of manufacturing lipsticks with antiviral properties, allowing the use of hydrophilic, antiviral substances in the hydrophobic components of lipsticks.

 To solve this problem, a group of inventions is proposed, united by a common inventive concept. The invention includes options for therapeutic lipstick and a method of manufacturing lipstick.

Treatment-and-prophylactic lipstick containing perfume and castor oil, lanolin, beeswax, paraffin, ceresin and perfume, additionally contains olive oil, butyl stearate, terlan, carnauba and candelilla wax, confectionery fat, tween-60 or tween-80 or sorbitanoleate, antal SU, larch gum resin, and biologically active additive foscarnet sodium and calendula or celandine oil extract in the following ratio, wt%
Olive oil 16 19
Castor oil 5 7
Butyl stearate 5 7
Anhydrous lanolin 8 11
Terlan 3 6
Gum resin larch 3 6
Carnauba wax 2 5
Beeswax 2 5
Candelilla Wax 2 4
Foscarnet sodium 1 3
Calendula or celandine oil extract (TU 9154-001-10807755-93) 2 - 5
Paraffin 1 4
Confectionery fat 1 4
Ceresin 1 2.5
Tween-60 or tween-80 or sorbitan oleate 0.8 1.5
Antal SU 0.3 0.7
Fragrance 0.3 0.7
Perfumery oil
In addition, therapeutic and preventive lipstick containing perfume and castor oil, lanolin, beeswax, paraffin, ceresin and perfume, additionally contains olive oil, butyl stearate, terlan, carnauba and candelilla wax, confectionery fat, tween-60 or tween-80 or sorbitan oleate, anta SU, larch gum resin, and a biologically active additive - acyclovir and calendula or celandine oil extract in the following ratio of components, wt
Olive oil 16 19
Castor oil 5 7
Butyl stearate 5 7
Anhydrous lanolin 8 11
Terlan 3 6
Resin leafy gum 3 6
Carnauba wax 3 6
Beeswax 2 5
Candelilla Wax 2 4
Acyclovir 1 3
Calendula or celandine oil extract (TU 9154-001-10807755-93) 2 - 5
Paraffin 1 4
Confectionery fat 1 4
Ceresin 1 2.5
Tween-60 or tween-80 or sorbitan oleate 0.8 1.5
Antal SU 0.3 0.7
perfume 0.3 0.7
Perfumery oil
In addition to these lipsticks, a therapeutic and preventive lipstick is proposed, which contains, in addition to perfume and castor oil, lanolin, beeswax, paraffin, ceresin and perfumes, olive oil, butyl stearate, terlan, carnauba and candelilla wax, confectionery fat, tween 60 or tween-80 or sorbitolate , SU anal, larch gum resin, and biologically active additive RNase enzyme and calendula or celandine oil extract in the following ratio of components, wt
Olive oil 16 19
Castor oil 5 7
Butyl stearate 5 7
Anhydrous lanolin 8 11
Terlan 3 6
Gum resin larch 3 6
Carnauba wax 3 6
Beeswax 2 5
Condellil Wax 2 4
RNase enzyme 0.1 1
Calendula or celandine oil extract (TU 9154-001-10807755-93) 2 - 5
Paraffin 1 4
Confectionery fat 1 4
Ceresin 1 2.5
Tween-60 or tween-80 or sorbitan oleate 0.8 1.5
Antal SU 0.3 0.7
Fragrance 0.3 0.7
Perfumery oil
For the manufacture of therapeutic and preventive lipsticks, the oil is heated to 70 - 80 ^o C and with stirring, carnauba, candellil, ceresin, paraffin, terlan, lanolin, fat, butyl stearate, Antal SU are added, mixing is carried out until a homogeneous mixture is formed, then the temperature is reduced to 40 - 50 ^o C and add to the mixture a biologically active additive and fragrance. In this case, the biologically active additive is pre-activated: dry sodium foscarnet, crushed to a size of 0.1 3 microns, or crushed acyclovir or RNase are mixed with Tween-60 or Tween-80 or sorbitan oleate and an oil extract of medicinal plants, the mixture is thoroughly mixed until homogeneous substances in the form of microcapsules, then beeswax is added to it, re-mixed and gradually heated to 80 ^o C.

 In addition, the dry antiviral substance foscarnet sodium is ground using an ultrasonic disintegrator with an ultrasonic power of 200 dB for 5 minutes. Mixing foscarnet sodium or acyclovir or RNase, surfactants and oil extracts of medicinal plants is carried out for 1 to 2 hours.

 As an active antiviral substance, antiviral chemical compounds - sodium foscarnet, or acyclovir, or the ribonuclease enzyme (RNase) have been introduced into the composition of therapeutic and prophylactic lipsticks; oil extracts of medicinal herbs (calendula or celandine).

 The molecular mechanisms that determine the antiviral activity of the drugs used are not completely clear, although it can be assumed that in all cases there is a systemic effect, i.e. the effect is directly on replicating viruses, on virus-infected cells, as well as on protective cellular systems.

 In in vitro model experiments, high antiviral activity of these substances was shown. The experiments were carried out at the D.I. Ivanovsky Institute of Virology on a VERO cell culture and on a model of herpetic mouse meningoencephalitis. The experimental results showed that the preparations of RNase, sodium foscarnet and acyclovir provide a high protective effect (100% 60% and 40% of the protective effect, respectively).

Antiviral lipstick is a combined therapeutic and cosmetic product that includes hydrophobic fillers, traditionally used in cosmetics for the manufacture of creams and lipsticks, oils (perfumes, petrolatum, vaseline, olive, castor), butyl stearate, lanolin, terlan, gum leaf resin, beeswax (beeswax , carnauba, candelilla), paraffins, confectionery fat, ceresin, antal, perfume, antiviral biologically active substances:
Foscarnet sodium or acyclovir, or RNase enzyme, calendula or celandine oil extract, substances that activate antiviral substances in lipsticks and creams: Tween-60 or Tween-80 or sorbitanoleate.

A specific example embodiment of the invention:
Name of components Mass fraction (%)
1. Olive oil 18.00
2. Perfume oil 20.00
3. Castor medical oil 7.00
4. Butyl stearate 6.00
5. Lanolin anhydrous 10.00
6. Terlan 5.00
7. Larch gum resin 5.00
8. Carnauba wax 5.00
9. Apiary beeswax production wax 4.00
10. Candelilla Wax 3.00
11. Foscarnet sodium 2.70
12. Calendula oil extract 4.00
13. Solid petroleum paraffins 3.00
14. Cooking confectionery fat 3.00
15. Ceresin grades 65, 70, 75, 80 2.00
16. Tween-60 or Tween-80 or sorbitan oleate 1.30
17. Antal SU 0.50
18. Fragrance 0.50 100.00
The proposed treatment and prophylactic lipstick is a solid lipstick of a light color with a pleasant odor, has an antiviral antiherpetic effect.

 Lipstick, named by the applicant "Hygiene-herpes", passed the test at the 1st Medical Academy. THEM. Sechenov at the Department of Skin and Sexually Transmitted Diseases.

 Under the supervision were 28 patients (age from 18 to 56 years) suffering from herpes simplex with different localization of herpes rash and with different phases of the development of the disease.

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

 Lipstick was applied in a thin layer on the affected skin 3-4 times a day.

 In 8 patients (3 with localization of the rash on the genitals and 5 on the lips) immediately after lubrication, a slight burning sensation was noted, which disappeared after a few minutes and did not significantly disturb the patients.

 Clinical observation revealed a clear dependence of the treatment results on the time it started (data are presented in the table).

For a more objective assessment of the effect of lipstick, depending on the stage of the herpetic process of the disease, it was conditionally divided into three phases:
the first phase is initial, characterized by subjective sensations, mild swelling and hyperemia in the lesion, lasts without treatment for an average of 1 3 days;
the second phase of the developed clinical symptoms continues depending on the location of the rash from 1 to 5 6 days and is manifested by multiple grouped vesicles against the background of increasing swelling and hyperemia;
third phase of the completion of the process. Bubbles burst with the formation of erosion or shrink into crusts, after which there comes a regression of all clinical manifestations. The duration of this phase is on average 3 8 days.

 The results of applying the Hygiene-Herpes lipstick depending on the location of the rash and the phase in which treatment was started in patients with herpes simplex are shown in the table.

 High treatment efficacy was understood to mean rapid relief of subjective sensations and abortion of rashes within 1–2 days of treatment. The use of lipstick was considered effective in cases where the duration of the process as a result of treatment was reduced by about half. The lack of effect was observed in those cases when the use of lipstick did not affect the natural course of the process.

 The table shows that the most effective treatment was at its beginning in the first phase of the process, i.e. in the presence of initial manifestations of the disease.

 In the presence of therapy in the stage of developed clinical symptoms, it was also distinguished by a certain effectiveness.

 The lack of effect in two patients with genital herpes is caused by the late onset of lipstick and the presence of complications in the form of balanoposthitis.

 None of the patients revealed side effects in the form of dermatitis or unpleasant subjective sensations.

 Clinical blood tests were performed in 5 patients before and after treatment, which did not reveal a pathological effect on them.

 Tests of the herbal hygiene lipstick showed that it has a softening and antiseptic effect, as well as high antiviral activity against the herpes virus.

 The test results showed that the proposed lipstick is comparable in activity, and in some cases has a higher activity compared to Zovirax or Triapten creams.

 Lipstick "Hygiene-herpes" can be used for the prevention of other viral diseases, including influenza A. There are no contraindications to the use of lipstick.

 Traditional hydrophobic fillers and hydrophilic antiviral substances were used to make Hygiene-Herpes lipsticks. In the manufacture of the product, it is impractical to use substances containing water and ethyl alcohol.

 To activate hydrophilic antiviral substances in hydrophobic lipsticks, the microencapsulation method was used.

 A specific example of the manufacture of antiviral lipstick.

 The dry antiviral substance of sodium foscarnet is ground on an ultrasonic conical vibrator to a particle size of 0.1 3 microns (particle size is determined under a light microscope) and 1 part by weight of sodium foscarnet is mixed with 0.5 parts by weight surface-active substance (surfactant), namely tween-60 or tween-80 or sorbitan oleate, and 1 part by weight oil extract of medicinal herbs, after which the mixture is thoroughly mixed on a high-speed stirrer for 1 to 2 hours until a homogeneous substance (microcapsules) is formed. Then add 1 vol. beeswax and again mix the mixture by slowly heating to 80. The resulting activated preparation is used to prepare lipsticks according to standard methods.

 Note: in the case of using a lyophilized RNase preparation, the sonication step is skipped.

 Using the microencapsulation method allows evenly introducing a hydrophilic antiviral substance into the hydrophobic lipstick and determines the increased penetration of the active component when applying lipstick to the skin (due to surfactant). In addition, the presence of a hydrophilic antiviral substance in the hydrophobic components of lipstick determines a higher stability of the active substance compared to recipes containing aqueous or alcoholic solutions of an antiviral substance (since the substance is protected in microcapsules). The proposed method also allows you to combine in one recipe several antiviral components such as foscarnet sodium and oil extracts of medicinal herbs.

 Thus, the proposed lipstick is a new form of therapeutic and antiviral drugs, namely lipsticks obtained by introducing water-soluble substances into hydrophobic components by microencapsulation.

 This made it possible to combine hydrophilic and hydrophobic biologically active substances in one preparation while maintaining their activity; get a convenient form of antiviral drugs; to achieve the possibility of stabilization (i.e. long-term activity preservation) of antiviral biologically active substances in neutral hydrophobic lipstick fillers.

Claims (3)

 1. Therapeutic and preventive lipstick containing perfume and castor oil, lanolin, beeswax, paraffin, ceresin and perfume, characterized in that it additionally contains olive oil, butyl stearate, terlan, carnauba and candelilla wax, confectionery fat, twin-60, or tween-80, or sorbitan oleate, SU antal, gum resin and biologically active additives, including sodium foscarnet and calendula or celandine oil extract, in the following ratio, wt. Olive oil 16 19
Castor oil 5 7
Butyl stearate 5 7
Anhydrous lanolin 8 11
Terlan 3 6
Gum resin larch 3 6
Carnauba wax 3 6
Beeswax 2 5
Candelilla Wax 2 4
Foscarnet sodium 1 3
Calendula or celandine oil extract 2 5
Paraffin 1 4
Confectionery fat 1 4
Ceresin 1 2.5
Tween-60, or tween-80, or sorbitan oleate 0.8 1.5
Antal SU 0.3 0.7
Fragrance 0.3 0.7
Perfumery oil
2. Treatment-and-prophylactic lipstick containing perfume and castor oil, lanolin, beeswax, paraffin, ceresin and perfume, characterized in that it additionally contains olive oil, butyl stearate, terlan, carnauba and candelilla wax, confectionery fat, twin-60, or tween-80, or sorbitan oleate, SU antal, larch gum resin and dietary supplement, including acyclovir and calendula or celandine oil extract, in the following ratio, wt. Olive oil 16 19
Castor oil 5 7
Butyl stearate 5 7
Anhydrous lanolin 8 11
Terlan 3 6
Gum resin larch 3 6
Carnauba wax 3 6
Beeswax 2 5
Candelilla Wax 2 4
Acyclovir 1 3
Calendula or celandine oil extract 2 5
Paraffin 1 4
Confectionery fat 1 4
Ceresin 1 2.5
Tween-60, or tween-80, or sorbitan oleate 0.8 1.5
Antal SU 0.3 0.7
Fragrance 0.3 0.7
Perfumery oil
3. Treatment-and-prophylactic lipstick containing perfume and castor oil, lanolin, beeswax, paraffin, ceresin and perfume, characterized in that it additionally contains olive oil, butyl stearate, terlan, carnauba and candelilla wax, confectionery fat, twin-60, or tween-80, or sorbitan oleate, SU antalum, larch gum resin and biologically active additive, including the RNase enzyme and calendula or celandine oil extract, in the following ratio of components, wt. Olive oil 16 19
Cator oil 5 7
Butyl stearate 5 7
Anhydrous lanolin 8 11
Terlan 3 6
Gum resin larch 3 6
Carnauba wax 3 6
Beeswax 2 5
Candelilla Wax 2 4
RNase enzyme 0.1 1
Calendula or celandine oil extract 2 5
Paraffin 1 4
Confectionery fat 1 4
Ceresin 1 2.5
Tween-60, or tween-80, or sorbitan oleate 0.8 1.5
Antal SU 0.3 0.7
Fragrance 0.3 0.7
Perfumery oil
4. A method of manufacturing a therapeutic and preventive lipstick, according to which the oil is heated to 70 80 ^o C and with stirring, carnauba, candellil, ceresin, paraffin, terlan, lanolin, fat, butyl stearate, SU anal are added, mixing is carried out to form a mixture of excipients with followed by temperature reduction to 40 50 ^o C and introducing a mixture of biologically active additives and perfumes, characterized in that larch gum resin are applied simultaneously with waxes and the biologically active additive is preactivated n and this dry sodium foscarnet, crushed to a size of 0.1 3 μm, or crushed acyclovir, or RNase is mixed with a surfactant and an oil extract of medicinal plants, the mixture is thoroughly mixed until a homogeneous substance in the form of microcapsules is formed, then beeswax is added to it , re-mixed and gradually heated to 80 ^o C.  5. The method according to p. 4, characterized in that the dry antiviral substance foscarnet sodium is ground using an ultrasonic disintegrator with an ultrasonic power of 200 dB for 5 minutes  6. The method according to p. 4, characterized in that the mixing of the antiviral substance, surfactants and oil extracts of medicinal plants is carried out for 1 to 2 hours

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