RU2033163C1 - Medicament stimulating healing of wounds and/or improving metabolism in investing tissues - Google Patents

Abstract

FIELD: medicine; cosmetics. SUBSTANCE: healing or cosmetic preparations are enriched with perfluorocarbons. EFFECT: wider range of medicinal and cosmetic agents characterized by wound-healing and metabolism-improving properties. 3 tbl

Description

 The invention relates to medicine and cosmetology and relates to methods for treating injuries of the skin of varying severity, and more particularly the treatment of traumatic, burn and other wounds of the skin and underlying tissues and the elimination of microdamage to the skin of open parts of the body that are in the nature of cosmetic defects.

 There are a number of wound healing medicines known as methyluracil, solcoseryl, collagen sponge, sea buckthorn oil, etc.

 These biologically active substances are used in the form of various dosage forms of ointments, gels, emulsions, solutions, etc. for external applications, enteral and parenteral administration.

 Combined preparations intended for the treatment of wounds and having a wound healing effect are also described.

 One of them, for example, contains carotene and carotenoids, vitamins A, E, K and refined fatty oil.

 Sea-buckthorn oil, which has a healing effect, is used not only in medicine but also in cosmetology for the preparation, in particular, of face cream, which helps to activate regenerative processes in the skin.

 Closest to the invention can be recognized as a block copolymer of ethylene oxide and propylene oxide, which showed a higher multi-healing activity than methyluracil, solcoseryl, collagen sponge, sea buckthorn oil.

 The wound process is complex and multi-stage and the drugs used to treat wounds affect its various stages and according to various mechanisms.

 Methyluracil stimulates the production of antibodies and a phagocytic reaction, has an anti-inflammatory effect, normalizes nucleic acid metabolism in the mucosa and epithelium, and accelerates wound healing.

 Solcoseryl improves metabolic processes, leads to accelerated tissue regeneration, in the first phase of the wound healing process it is used intramuscularly or intravenously, in the second phase it is applied topically, locally.

 Sea buckthorn oil has an analgesic effect, accelerates granulation and epithelization of tissues, and is used in the second phase of the wound healing process. The effectiveness of the drug is largely associated with the presence of vitamins A, E, K, F, C, P and B vitamins in it.

 The collagen sponge is a reinforcing element introduced into the wound area, around which the regeneration process is activated.

 Vitamin A supports the functions of the glands of the epithelial cells of the skin and mucous membranes, increasing the resistance of the latter to various diseases.

 Vitamin E, being an antioxidant, protects biological substrates from oxidative changes.

 Vitamins of group K stimulate the production of prothrombin in the liver and thereby have a hemostatic effect.

 The block copolymer of ethylene oxide and propylene oxide has a wound healing effect in the first phase of the wound process due to a local improvement in microcirculation in the tissues adjacent to the lesion, as well as due to direct biostimulating activity that enhances tissue regeneration.

 The purpose of the invention is to increase the effectiveness of the treatment of wounds and the impact on the regenerative process different from previously used method.

 The goal is achieved through the use of perfluorocarbons as a medicine and cosmetic.

 Perfluorocarbons are a known group of compounds that were considered promising blood substitutes due to their high ability to dissolve oxygen and serve as its carrier.

 These compounds are the product of fluorination of various organic compounds and contain predominantly exhaustive fluorinated substances, as well as small amounts of partially fluorinated compounds and isomers.

Currently, perfluorocarbons are produced by the domestic industry and are inert chemicals with a specific gravity of up to 2 g / cm ³ and high adhesive properties.

 As was first established by the applicant, perfluorocarbons have a pronounced wound healing effect, which may be due to their beneficial effect on the gas exchange of adjacent tissues, since it has long been established that wound damage is accompanied by increasing hypoxia of cells and tissues and increasing acidosis.

 The essence of the proposal is that for the treatment of wound injuries of the skin and adjacent tissues (in medicine), and for the elimination of cosmetic skin defects of wound nature in open areas of the body (in cosmetology), medicinal or cosmetic products based on perfluorocarbons are used.

 In medicine, the use of perfluorocarbons is recommended in the treatment of infected and uninfected injuries of the skin and subcutaneous tissues, thermal and chemical burns, but it is also acceptable and recommended in other cases associated with damage to the skin.

 For these purposes, perfluorocarbons can be included in ointments, emulsions, aerosol formulations, or other dosage forms.

 In cosmetology, perfluorocarbon-based preparations can preferably be used in the presence of microtraumas, microcuts, microcracks of the skin of the face, but it is possible to use them in other cases when cosmetic skin defects occur, for example, with acne.

 Acceptable cosmetic forms of perfluorocarbons can be creams, gels, lotions, means for refreshing the skin after shaving, etc.

 If desired, additional biologically active components may be introduced into the composition of the medicinal or cosmetic products.

 The effectiveness of the biological effect is manifested with single doses of perfluorocarbon preparations of the order of 0.1 g. The optimal content of perfluorocarbons in drugs is 50-60 vol. in cosmetic 5-20 vol. The effect of various doses of perfluorocarbon preparations on the basic physical and mechanical characteristics of the skin can be judged by the data in Table 1.

 Thus, the results indicate that the minimum dosage of the drug onset (0.25 g) has a pronounced therapeutic effect and postoperative scars in this case were more adapted to the loads, the strength of the scars is higher, and the elasticity is higher than the corresponding indicators obtained as a result of treatment with higher doses of the drug.

 To enhance the biological effect of drugs containing perfluorocarbons, the treatment procedure can be carried out at an increased partial pressure of oxygen, as can be concluded from Table 2.

 The presented results show that the perfluorocarbon ointment was an effective wound healing drug and the only drug whose effectiveness increased with an increased partial pressure of oxygen in the gas phase.

 It can be concluded that a special advantage of perfluorocarbon-based preparations is their ability to exhibit maximum wound healing effect under conditions of oxygen aeration. This circumstance can be taken into account in the treatment of traumatic tissue injuries accompanied by an anaerobic infection, oxygenation of a wound treated with a perfluorocarbon-based drug will provide a comprehensive therapeutic effect.

 Perfluorocarbon-based preparations showed an active wound healing effect not only in the treatment of planar muscular skin wounds, but also in relation to thermal burns, which is confirmed by the data in Table. 3.

 It is quite clearly seen that the perfluorocarbon preparation showed a pronounced effect in the treatment of thermal burns, exceeding the effect of solcoseryl.

 To identify the irritating and allergenic effect of perfluorocarbons on the side surface of the skin of male white guinea pigs, the drug was applied in an amount of 0.5 g and skin reactions were observed, evaluating them on a five-point scale. On day 21, the same preparation was once applied to the opposite side surface and after 24 hours the animal was examined. The examination showed that there were no manifestations of a skin reaction, and there were no histochemical differences between the experimental and control areas of the skin: epidermis, appendages (hair follicles), microcirculation vessels, as well as collagen and elastic fibers without changes.

 A morphological study of the internal organs of the animal observed the invariance of the structure of the tissues of the liver, kidneys and other organs when exposed to the perfluorocarbon preparation.

 No negative effect on the body was also detected when studying the effects of perfluorocarbons in cosmetic preparations, while their biological activity was confirmed, which follows from the conclusion of the Beauty Institute, recommending the use of perfluorocarbon preparations in cosmetology.

 The combination of perfluorocarbons with other biologically active substances is especially promising in cosmetology, because, contributing to the processes of blood microcirculation in the subcutaneous tissue, perfluorocarbons locally activate the action of these biologically active substances. It is advisable, in particular, to include in the composition of cosmetics, along with perfluorocarbons, vitamins, plant extracts, oils and other components that affect the metabolism in skin tissue.

 EXAMPLE 1. Sorbitol (12.0), glycerin (6.0), propylene glycol (4.0) are dissolved in 0.4 L of distilled water, and the solution is mixed with 600 ml of a mixture of perfluorocarbons containing lecithin (4, 0) as an emulsifier.

 In this case, the mixture of perfluorocarbons contained perfluorodecalin 89; perfluoroether P-216 6; perfluorotributylamine 5.

 Sorbitol, glycerin and propylene glycol are introduced into the aqueous phase as auxiliary substances exhibiting stabilizing properties.

 The resulting aqueous-organic system is mixed in a mixer and the resulting primary emulsion is repeatedly passed for 30 minutes through a high-pressure homogenizer at 500 atm.

 The finished aqueous emulsion of a mixture of perfluorocarbons has a particle size in the range of 150-350 nm.

 The prepared medical ointment has the following composition, a mixture of perfluorocarbons 60; water emulsion base 40.

 This ointment-based ointment has shown good results especially in the treatment of thermal burns.

 PRI me R 2. Dissolve sorbitol (15.0), glycerol (8.0), propylene glycol (5.0), proxanol P-268 (40.0) and iodovidone (3) in 0.4 g of distilled water , 0), after which the solution is mixed with 600 ml of a mixture of perfluorocarbons.

 In this case, the mixture of perfluorocarbons contained perfluorodecalin 65; perfluoromethylcyclohexylpiperidine 35.

 Sorbitol, glycerin, propylene glycol are introduced into the aqueous phase as stabilizers and antioxidants, proxanol as an emulsifier, and iodovidone (an aqueous solution of the complex compound of polyvinylpyrrolidone with iodine) as a biologically active substance with a bactericidal effect.

 The resulting aqueous-organic system is mixed in a mixer and the primary emulsion of a mixture of perfluorocarbons is passed through a high-pressure homogenizer at 550 atm for 20 minutes.

 The finished aqueous emulsion has a particle size of 150-250 nm.

 The resulting ointment has the following composition, a mixture of perfluorocarbons 52; iodovidone 0.05; water-emulsion base 47.95.

 This ointment has shown high efficiency in the treatment of wounds, including those infected and accompanied by suppuration.

 PRI me R 3. Propylene glycol (6.0) and glycerol (4.0) are dissolved in 0.4 L of distilled water, and then the solution is mixed with 200 ml of a mixture of perfluorocarbons.

 In this case, the mixture of perfluorocarbons contained perfluoroazabicyclodecane 50; perfluorotributylamine 20; perfluoromethylcyclohexylpiperidine 15; perfluoromethyldibutylamine 10; P-216 perfluoroether 5.

 P-268 proxanol (40.0) is added to the aqueous-organic system as an emulsifier and it is vigorously mixed in a mixer. The primary emulsion is passed for 45 minutes through a high pressure homogenizer at 500 atm.

 The finished aqueous emulsion had a particle size of 120-300 nm.

 Vegetable oil (120.0), mink oil (30.0), perfume oil (20.0), anhydrous lanolin (25.0), cosmetic stearin (25.0), distilled monoglycerides (20.0), synthetic alcohols (15.0) is heated to a temperature of 75 degrees, the VNIIZh emulsifier (5.0) is added and homogenized until a homogeneous mass is obtained.

 An aqueous emulsion of perfluorocarbons is slowly added to the fat base, perfume and stabilizer are introduced into the system and the resulting product is thoroughly homogenized.

 The prepared cosmetic cream had the following composition, a mixture of perfluorocarbons 20; fat base 80.

 The cream is intended for dry skin care, stimulating, in particular, mitotic activity in the basal layer of the dermis and promoting the rapid healing of microdefects of the skin.

 Example 4. Propylene glycol (5.0), glycerin (3.0), vitamin C (3.0) were dissolved in 0.4 L of distilled water, and 150 ml of a mixture of perfluorocarbons were added to the aqueous solution.

 In this case, the mixture of perfluorocarbons contained perfluorooctyl bromide 50; perfluoroazabicyclodecane 30; perfluorotributylamine 20.

 A mixture of egg yolk lipids (3.0) is added to the aqueous-organic system as an emulsifier and it is vigorously mixed in a mixer. The resulting primary emulsion is passed through a high pressure homogenizer for 40 minutes at 600 atm.

 The particle sizes of the resulting emulsions were 140-360 nm.

Vegetable oil (80.0), mink oil (30.0), naphthalan (20.0), anhydrous lanolin (25.0), cosmetic stearin (35.0), distilled monoglycerides (25.0) are heated to a temperature of 75 ^about With, mix thoroughly until a homogeneous mass.

, Cooled to 50 ° ^C added to fat-based flavor, and slowly poured perfluorocarbon emulsion. The resulting product is thoroughly homogenized.

 The prepared cosmetic cream has the following composition, a mixture of perfluorocarbons 20; vitamin C 0.3; naphthalan 2; fat base 77.7.

 This cream is intended for facial skin care and has the ability to stimulate metabolic processes in the dermis and adjacent tissues.

 Thus, the applicant has established a high wound healing activity of drugs and cosmetics based on perfluorocarbons, as well as the beneficial effect of perfluorocarbons on metabolic processes in the skin and subcutaneous tissue, which allows them to be used in cosmetology and in cases where there is no violation of the integrity of the skin.

Claims (1)

 The use of perfluorocarbon as a means of stimulating wound healing and / or improving metabolism in integumentary tissues.

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