BG65639B1 - Regeneration composition - Google Patents

Abstract

The composition is used in medicine and cosmetics for the prophylaxis and therapy of skin impairments of different etiology. It comprises biologically active components in wt.%: native deproteinaceous polynucleotide having molecular mass over 10 mln. Da in the form of a solution in concentration of 1.0- 2.0 mg/cm? 0.005-0.5, folic acid 0.005-0.5 and inosine 0.005-0.5, which are included in a hydrophilic base with pH 5.5-7.2 û to 100. The hydrophilic base is buffer solution, hydrogel and/or oil/water type emulsion, which can contain, in wt.%: salts of the polyacrylic acid (Na, K, NH3) 0.1-2.0,polyethyleneglycols (PEG) from 10.0 to 60.0, polyalcohols from, 1.0 to 15.0, emulsifiers and preservatives.

Description

Technical field

The invention relates to a regenerative composition, a biologically active ingredient of topical formulations for the prevention and treatment of skin lesions of different etiologies, applicable in medicine and cosmetics.

BACKGROUND OF THE INVENTION

Ionizing radiation UV, gamma, beta, and X-rays are known to cause damage to the dividing cells of the basal epidermal layer, resulting in lipoperoxidation of the cell membranes and direct damage to the genetic material leading to cell death. Radiation-induced dermatitis, acute and tardic, require a course of treatment with known topical agents from 30-40 days to 23 months, necessitating discontinuation of radiation therapy. The natural "aging" of the skin is due to the reduced activity of cellular repair systems and delayed proliferation of the basal cells, leading to thinning of the skin, dryness and susceptibility to external harmful factors.

It is known that exogenous nucleic acids of different origins have a regenerative effect at the subcellular, cellular and organismal level, correlating with the degree of polymerization and naivety (Belous, A.M. et al. , 1974;

Fedorova, TA and others. "Nucleic Kloo ™ and Proteins in Radiation Defeat", M., Medicine, 1972;

Guberniev, MA, et al. COP of General Biology, 1972, Vol. 28, No. 6, 675).

There are formulas and compositions, mainly for cosmetic purposes, containing as active ingredients peptide extracts of the thymus gland, placenta, deoxyribonucleic acid (DNA), DNA synthetic analogues in combination with flavones, vitamins, polysaccharides, etc., aimed at elimination of free radicals in the epidermal layer, stimulating cellular metabolism and reinnervation of the superficial skin layer (CH 678487; WO 2001/068048; WO 2001/074342).

A method of treating skin lesions is also known, in particular radiation dermatitis, containing as a active ingredient a solution of native deoxyribonucleic acid in a hydrogel base (BG 38958). Epithelial activity of the composition has been observed, shortening the duration of treatment for skin lesions to 7-10 days. Clinical observations in patients with skin lesions of different origins prove the efficacy of the polynucleotide composition as a stimulator of tissue regeneration (Pandova V., Marinova Tsv., Stefanova D. et al. Radiobiology, 1986, 28, 3, 23; Stefanova D., Grashev G., Marinova Tsv. Et al., Radiobiology, 1990, 30, 2, 272).

EP 1096938 discloses a composition for the prevention and treatment of inflammation and skin lesions containing a phosphodiesterase inhibitor comprising a cyclic nucleotide having 2 'hydroxyl groups substituted by a hydrogen atom, in particular 2'-eoxyadenosine 3' - cyclic monophos . The composition has an inhibitory effect against the phosphodiesterase activity found in atopic dermatitis.

Substances that directly affect cellular metabolism are known, in particular stimulating the synthesis of specific amino acids, peptides, purine and pyrimidine bases, nucleosides and nucleotides, and other cellular products. The combined action of such substances with the reparative effects of a deproteinized polynucleotide complex at the cellular and tissue levels should stimulate skin regeneration.

SUMMARY OF THE INVENTION

The problem that is solved by the present invention is related to the need to combine different mechanisms of action of the active components aimed at stimulating cell vitality.

The subject of the invention is a regenerative composition for topical application in the prevention and treatment of skin lesions of different etiologies, containing as a biologically active component a native deproteinized po2

65639 Bl linucleotide having a molecular weight exceeding 10 million Da in the form of a solution with a concentration of 1.02.0 mg / cm ³ - from 0.005 to 0.5 wt. %, folic acid from 0.005 to 0.5 wt. %, and inosine from 0.005 to 0.5 wt. %, which are included in the hydrophilic base with a pH of 5.5-7.2 to 100 wt. %.

The hydrophilic base is a buffered solution, hydrogel, and / or an oil / water type emulsion that may contain polyacrylic acid salts (Na, K, NH ₃ ) of 0.1 to 2.0 wt. %, polyethylene glycols (PEG) from 10.0 to 60.0 wt. %, poly alcohols from 1.0 to 15.0 wt. %, emulsifiers, preservatives and other pharmaceutically acceptable substances non-biodegradable.

The biological activity of a buffered deproteinized polynucleotide complex with a molecular weight of over 10 million Da, incorporated into the hydrogel base, is expressed in stimulating cell proliferation, tissue regeneration and enhancing epithelial activity.

Inosine is a purine derivative; stimulates nucleotide synthesis and cellular metabolism, affecting the cyclic adenosine monophosphate system.

Folic acid is involved in the synthesis of purines and pyrimidine bases, which are part of the nucleic acids.

The combination of the biological effects of the three active components results in synergism with the effects of cellular repertoire systems and cellular metabolism, thereby enhancing skin regeneration in various tissue lesions. The hydrophilic base guarantees the stability of the biologically active components and ensures their storage activity.

The regenerative composition is applicable in therapeutic and cosmetic preparations intended for the treatment and prevention of skin lesions by thermal, mechanical and radiation factors.

Examples of carrying out the invention

The invention is illustrated by the following examples without limitation:

Example 1

The regenerative composition for topical application contains in wt. %:

native deproteinized polynucleotide, isolated of thymus (solution with concentration of 1 mg / cm ³ ) 50.0 inosine 0.10 folic acid 0.05 polyacrylic acid (Carbomer 940) 1.00 sodium hydroxide 0.2 propylene glycol (GHG) 10,0 preservatives 0.10 distilled water up to 100.0

Method of preparation

The weighed amount of Carbomer 940 was homogenized with 1/2 of the amount of water, after which the sodium hydroxide solution was dissolved in water and added dropwise to the solution of Carbomer 940 to give a colorless clear gel. Propylene glycol dissolves inosine and preservatives at gentle warming to 20-40 ° C and after cooling to room temperature with stirring the resulting solution is added to the gel. A solution of native deproteinized polynucleotide and folic acid solution were added sequentially. Stirring is continued until complete homogenization. At the end of the process, the mixture was vented. A clear gel was obtained with a pH of 10% solution of 6.2-6.8.

The composition is used to treat damaged skin areas.

The hydrogel is applied in a thin layer on the affected areas. It is recommended to apply it immediately after the end of the radiotherapy procedure and re-administration after an 8-10 hour interval during the course of radiation therapy. Skin regeneration and epithelialization occur on the fifth to the tenth day, depending on the degree of damage.

In the presence of bacterial contamination and / or necrotic matter (in decubitus, diabetic ulcers, postoperative fields, etc.), the wound sections are pre-treated with saline, 3% oxygen water and / or mechanical removal of the formations. The preparation is applied to the fields thus cleared in the form of a sterile dressing once per 24-hour interval.

Example 2

The regenerative composition for topical application contains in wt. %:

65639 Bl native deproteinized polynucleotide (solution with

concentration of 2 mg / cm ³ ) 15.0 inosine 0.05 folic acid 0.05 Carbomer 940 0.2 sodium hydroxide 0.04 GHG 5.0 PEG 5.0 preservatives 0.10 lecithin 1.0 nicotinic acid 0.02 silicone oil 5.0 distilled water up to 100.0 Method of preparation The receipt is carried out in a similar manner

of Example 1 method. To the hydrogel containing the active components of Example 1 was added, with continuous stirring, an emulsion of PEG, a preservative, water and silicone oil. Finally, a solution of nicotinic acid is added to the emulsion. The composition is in the form of an opalescent emulsion with a pH of 10% solution - 6.0-6.6.

The composition is intended for the treatment of hair in order to strengthen the hair.

Example 3

The regenerative composition for topical application contains in wt. %: native deproteinized polynucleotide (solution with

concentration of 1.5 mg / cm ³ ) 20,0 inosine 0.10 folic acid 0.05 Carbomer 940 0.10 sodium hydroxide 0.02 GHG 5.0 PEG 20,0 preservatives 0.10 lecithin 1.0 glycerol stearate 1.0 Vitamin E. 1.0 flavontioglycolic acid 2.0 olive oil 5.0 silicone oil 5.0 distilled water up to 100.0

Method of preparation

The preparation was performed in a manner analogous to Example 1. To the hydrogel containing the active components of Example 1, 5 PEG emulsions, emulsifiers, water, vitamin E, silicone oil and olive oil were added. An aqueous solution of flavonthioglycolic acid was added to the mass thus obtained and the composition was vented. The final product is a white hydrophilic emulsion. Finds an app for third-

0 skin wound after sun and radiation burns.

The above examples do not exclude the possibility of combining the regenerative composition according to the invention with other substances15 relevant to the treatment and prophylaxis of the skin from adverse effects, especially flavones, isoflavones, and their Mg, Se, Zn derivatives (antioxidants), cellular protectors , for example sulfur-containing amino acids such as methionine, cysteine and their metal salts, alcohols, anti-inflammatory agents, plant, tissue and cellular extracts.

Claims (2)

Claims 1. A regenerative composition for the prevention and treatment of skin lesions based on native deproteinized polynucleotide, characterized in that it contains biologically active components of native deproteinized polynucleotide; 2 0 leotide having a molecular weight exceeding 10 million Da in the form of a solution with a concentration of 1.0-2.0 mg / cm ³ from 0.005 to 0.5 wt. %, folic acid from 0.005 to 0.5 wt. % and inosine from 0.005 to 0.5 wt. % incorporated in the hydrophilic base with a pH of 5.5-7.2 to 100%. The regenerating composition of claim 1, wherein the hydrophilic base is a buffered solution, hydrogel and / or an oil / water emulsion, which may contain: salts of polyacrylic acid of 0.1 to 2 wt. %, 40 polyethylene glycol from 10 to 60 wt. %, poly alcohols from 1.0 to 15.0 wt. %, emulsifiers, preservatives up to 100 wt. %.