RU2381810C1 - Wound healing gel balm - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to a wound healing agent. The wound healing gel balm containing dihydroquercetin, medicinal glycerine, linseed or cedar oil, aqueous chitosan gel taken in a certain ratio of components.

EFFECT: wound healing and antiinflammatory gel balm.

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Description

The invention relates to medicine, namely to pharmaceutical preparations containing organic active ingredients.

Known means for external use, containing medical phenol, resorcinol, boric acid and distilled water, chitosan, dimethyl sulfoxide, potassium iodide, glacial acetic acid, glycerin and anesthetic in the following ratio, wt.%: Chitosan - 3.0-3.1 medical phenol - 1.0-1.05, resorcinol - 5.0-5.05, boric acid - 1.0-1.05, dimethyl sulfoxide - 7.5-7.55, potassium iodide - 2.0- 2.05, glacial acetic acid - 4.8-5.0, glycerin - 3.0-3.5, anesthetic - 0.5-10.0, distilled water - the rest (see RU 2140264 C1, IPC 6 A61K 31/00, A61K 31/18, A61K 38/02).

A disadvantage of the known means is its relatively low wound healing efficiency.

A known composition having a tonic and antioxidant effect, containing bioflavonoids and vitamins, while it contains dihydroquercetin as bioflavonoids, ascorbic acid as vitamins and additionally microcrystalline cellulose, pectin, sorbitol, dry rosehip extract, sugar substitute and calcium or magnesium in the following proportions, wt.%: dihydroquercetin - 0.5-7.0, MCC - 6.0-42.2, ascorbic acid - 1.0-30.0, pectin - 1.0-15.0, sorbitol - 5.0-30.0, dry rosehip extract - 10.0-50.0, sugar substitute - 0.2-1.0 , calcium or magnesium stearate - 0.1-1.0 (see RU 2187319 C2 7, A61K 35/78, A61P 39/06, A61K 35/78, A61K 31: 351, A61K 31: 047, A61K 33:06 , A61K 31: 375).

A disadvantage of the known agent is its low effectiveness in treating local injuries, since the known agent is a means of internal consumption and is aimed at strengthening the body.

Known drug Lorinden A (ointment for external use) company Elfa A.O. (registration number HN011810 / 01), which is the closest according to the selected mechanism of exposure, containing salicylic acid and a synthetic glucocorticosteroid - flumethasone pivalate, and as auxiliary substances - propylene glycol, anhydrous lanolin and white petrolatum, while salicylic acid in combination with lanolin and provides transport of flumethasone pivalate deep into the surface tissues, where it contributes to its accumulation and implementation of the above action. The presence of lanolin, propylene glycol and petroleum jelly helps to maintain moisture in the tissues and softens the stratum corneum.

The famous drug Lorinden A has anti-inflammatory, decongestant, antibacterial, fungicidal and anti-allergic effects,

Despite the effectiveness of the drug, numerous and rather serious side effects significantly limit its use, these features are determined by the use of synthetic glucocorticosteroid and salicylic acid.

The objective of the invention and the technical result associated with this task is to expand the scope of the gel-balm, by creating an external agent, high biological activity of the components without side effects and high transport properties of chitosan, which has a wide spectrum of action, as well as expanding the arsenal of wound healing and anti-inflammatory decongestants.

To achieve a technical result, a gel-balm having a healing effect contains dihydroquercetin, medical glycerin, linseed or cedar oil, chitosan water gel in the following ratio, wt.%:

dihydroquercetin 1.0-5.0 medical glycerin 1.0-5.0 vegetable oil 2.0-10 chitosan water gel 80.0-96.0.

In addition, gelling agent is food chitosan, the concentration of which is 20-40 g / liter of water.

The basis of most effective treatment methods, in accordance with the principles of "capillary therapy", is to ensure normal blood supply to the affected area or organ.

Dihydroquercetin has powerful antioxidant, capillaroprotective, anti-inflammatory, immunomodulatory and analgesic properties. Dihydroquercetin, also called "Taxifolin", belongs to the group of bioflavonoids. One of the plant sources of dihydroquercetin is shredded wood of Siberian or Daurian larch.

Dihydroquercetin is the most powerful natural antioxidant known today. Dihydroquercetin surpasses ascorbic acid, tocopherol and carotene in its antioxidant effect. The great advantage of dihydroquercetin is its high stability.

Dihydroquercetin has a wide spectrum of pharmacological activity. Its capillary-protective and antioxidant properties are combined with anti-inflammatory, gastro- and hepatoprotective, lipid-lowering (anti-atherosclerotic) and diuretic effects.

Dihydroquercetin does not exhibit mutagenic, allergenic or toxic properties.

However, dihydroquercetin is slightly soluble in water and many other traditional solvents, which complicates its delivery to the lesion site.

The properties of the aqueous gel of the marine chitosan polysaccharide are well known; they are used in burn medicine to create artificial skin, which is used for extensive burns, which provides a solution to the problem of disinfection of an open wound surface and its closure with a membrane film that allows air to pass through but retains harmful bacteria and other microorganisms . In addition, chitosan effectively transports various compounds deep into the tissues.

Thus, individually taken components of the gel-balsam do not show strong wound healing properties and a wide range of effects.

So, dihydroquercetin is slightly soluble in water, and its delivery to the affected tissues located in the muscle mass is practically impossible. Healing of surface lesions is accelerated, mainly due to its bactericidal properties. Its powerful capillary-protective and regenerative properties are practically not realized.

Chitosan gel is characterized by the ability to penetrate deep enough into tissues and create a gas-permeable bactericidal membrane on the wound surface, which facilitates accelerated granulation and the volumetric nature of the wound healing process.

In this case, the ultrafine emulsion of dihydroquercetin evenly distributed in the chitosan gel matrix can significantly enhance the wound healing properties of individual components by delivering dihydroquercetin deep into the tissue to the lesion and creating conditions for effective detoxification and reduction of edema. Increasing the permeability of the walls of the capillaries accelerates the processes of regeneration and healing. The synergism of the components is realized.

In order to deliver relatively large amounts of dihydroquercetin using chitosan, it is necessary to evenly distribute it in the gel mass. A thin emulsion of dihydroquercetin dissolved in a mixture of glycerin and vegetable oils is a very stable and effective system that provides the solution to this problem. Obtaining the desired emulsion is achieved, for example, by homogenization.

The dihydroquercetin delivery form proposed by this solution provides a significant increase in its bioavailability. The composition is fully compatible with all tissues of the human body and has the following biomedical properties:

- lack of immunoreactivity;

- the ability to biodegradation and complete removal from the body,

- the ability to form protective films on the wound surface and stimulate the wound healing process;

- the ability to biostimulate regenerative and metabolic processes;

- the ability to enhance the lymphotropic reaction;

- the ability to quickly penetrate into the deeper layers of tissues and transport various nutrients and drugs there;

- the ability to quickly penetrate into the deep layers of tissues.

The proposed gel balm penetrates into the deeper layers of tissues and effectively activates metabolic processes, the permeability of cell membranes and capillary walls, which leads to an improvement in the supply of necessary substances to cells and the removal of waste products. The intensification of blood supply in the affected area increases the efficiency of the body's immune system and significantly accelerates the processes of regeneration and wound healing.

The proposed gel balm promotes the formation on the wound surface of a gas-permeable film that retains moisture, provides bio-barrier functions. Under these conditions, regeneration takes on a voluminous character and allows healing of significant surfaces without adhesions and scars.

The proposed gel balm provides a reduction in pain with all types of mechanical damage to tissues and burns due to the analgesic effect of both major components.

Beneficially affecting the intercellular space and providing powerful detoxification, the proposed gel balm promotes rapid recovery during sprains, dislocations and extensive hematomas.

The claimed gel balm may have the following indications. As a first aid: disinfection, healing and anesthesia for cuts, abrasions and burns (thermal, solar, chemical); restoration of blood circulation during frostbite; reduction of pain, itching and swelling with insect bites.

In general and plastic surgery, according to clinical trials at the Federal State Research Institution Rosmedtekhnologii and the Moscow Polyclinic for Restorative Treatment No. 6, the local application of chitosan gel-balm provides: a significant reduction in pain syndrome, accelerated healing of postoperative sutures (without the formation of a rough scar tissue), cracks, pressure sores, trophic ulcers, resorption of hematomas.

In sports medicine, according to clinical trials at the Moscow Scientific and Practical Center for Sports Medicine, the use of chitosan gel-balm causes accelerated recovery after extreme loads, with bruises, superficial bruises, pains in muscles and joints, and sprains.

When preliminary applying gel-balm to body surfaces that are subject to shock, gel-balm provides a reduction in pain, the absence or significant reduction in the appearance of hematomas, a decrease in damage to periosteal surfaces, and easier wound healing during rehabilitation after competitions.

The use of balsam gel is limited only by the individual intolerance of its components.

The gelling agent is food chitosan, produced under industrial conditions from carapace shells and other marine crustaceans.

The production of balsam gel can be carried out using a ready-made commercial product - chitosan gel - provided that it meets the requirements of regulatory documents or by including the stage of gel preparation in the production cycle.

Preparation of gel balm is carried out in accordance with the requirements of GOST 52343-2005.

Characteristics of the final product

Gel balm is intended for external use and has pronounced anti-inflammatory and wound healing properties. Useful additives have a protective, hygienic and bactericidal effect.

Technological scheme of production

The technological process consists of the following stages.

1. Preparation and dosing of raw materials;

2. Preparation of chitosan gel;

3. Preparation of gel balm;

4. Determination of colloidal stability and pH measurement of the finished gel-balm;

5. Packing, packaging, labeling and storage of the finished product.

1. Preparation and dosing of raw materials

All raw materials entering the production should be checked for compliance with GOST and TU, as well as certificates and sanitary and epidemiological conclusions.

1.1. To ensure sanitary and hygienic conditions of production, it is necessary to clean and disinfect the equipment.

The equipment is cleaned mechanically, followed by washing with hot water 80-90 ° C (with a circulating pump).

Disinfection of equipment is carried out with 70% ethyl alcohol.

1.2. Liquid components are dispensed using consumable containers and weighed on a balance. Paste-like and powdery components are weighed on a balance and served with portable containers in the cooking apparatus.

2. Preparation of chitosan gel

2.1. To prepare 1000 ml of chitosan gel, it is necessary to prepare 1000 ml of deionized water and add 10 g of the Argonika silver nanoparticle preparation to it, mix thoroughly and allow to stabilize for one hour. Then add 20 g of glacial acetic acid, qualification grade ХП GOST 61-75.

2.2. 100 g of food chitosan powder obtained under industrial conditions from carapace or other marine crustaceans is poured into 1000 ml of a 2% solution of acetic acid and left to swell for 16-18 hours.

2.3. After preparing the gel, it is necessary to adjust its pH, it should not exceed 7.0.

3. Preparation of gel balm

Example 1

Preparation of gel balm with a dihydroquercetin content of 1.0%.

Gel-balm is prepared in two stages.

First, 1.0 g of dihydroquercetin is poured into a mechanical mortar, then 1.0 g of medical glycerin, 2.0 g of cedar oil and 96.0 g of chitosan gel are added. Grout for 40 minutes at 600 rpm.

Homogenization of the resulting mixture is carried out at 4000 rpm for 1 hour. The final product should be a homogeneous oily-gel mass.

Example 2

Preparation of gel balm with a content of dihydroquercetin 5.0%.

Gel-balm is prepared in two stages.

First, 5.0 g of dihydroquercetin is poured into a mechanical mortar, then 5.0 g of medical glycerin, 10.0 g of cedar oil and 80.0 g of chitosan gel are added. Grout for 40 minutes at 600 rpm.

Homogenization of the resulting mixture is carried out at 4000 rpm for 1 hour. The final product should be a homogeneous oily-gel mass.

4. Determination of colloidal stability and measurement of the pH of the finished product The product must retain its properties for at least one year when stored in a cool place at a temperature not lower than + 5 ° C, the pH of the finished product should not exceed 7.0.

5. Packing, packaging and storage of the finished product

The packaging of the finished product in consumer packaging is carried out using a filling machine. Consumer packaging is packed in shipping containers in accordance with the requirements of GOST 28303-89.

Production control

Quality control of incoming raw materials is carried out in accordance with established standards and specifications.

The control of the technological process is reduced to strict observance of the technological instructions and regulations when conducting the technological process as a whole and each operation separately.

Quality control of the finished product includes the determination of colloidal stability, thermal stability, pH, color matching, odor and product uniformity (control is carried out at the factory).

Microbiological purity of products is carried out in accredited laboratories under an agreement.

The proposed Chitosan gel-balm can be obtained on standard equipment of most pharmaceutical enterprises from standard pharmacological agents supplied to the market, which confirms the compliance of the claimed solution with the condition of industrial applicability.

Thus, the proposed gel balm with a wound healing effect has a very wide field of application due to the high biological activity of the components without side effects and high transport properties of chitosan, which has a wide spectrum of action. Moreover, the components of the balsam gel are synergistic. The proposed gel balm provides an expansion of the arsenal of highly effective wound healing, anti-inflammatory and decongestants.

Claims (1)

Gel-balm with a wound healing effect, characterized in that it contains dihydroquercetin, medical glycerin, linseed or cedar oil, chitosan water gel in the following ratio, wt.%:
dihydroquercetin 1.0-5.0 medical glycerin 1.0-5.0 linseed or cedar oil 2.0-10.0 chitosan water gel 80.0-96.0