RU2445113C2 - Method for producing anti-inflammatory and wound-healing agent - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns pharmaceutical industry, in particular to a method for producing an anti-inflammatory and wound-healing agent. The method for producing the anti-inflammatory and wound-healing agent involving grinding and ethanol extraction of dried leaves of peach in certain environment in percolation-repercolation, extract evaporation to 1/20 of the original volume.

EFFECT: invention provides higher yield of the biologically active substances.

2 cl, 1 tbl, 3 ex

Description

The present invention relates to medicine, namely to the pharmaceutical production and use of extraction preparations from plant materials with a wound healing effect and can be used to treat skin lesions of mucous membranes of various severities (wounds, abrasions, maceration, pressure sores, cracks) and origin (mechanical, thermal , radiation), as well as diseases of the integumentary tissues of the body.

Currently, there is a steady need for effective and safe topical preparations for the treatment of injuries of the skin and mucous membranes. Moreover, of particular interest in the treatment is the use of safe pharmaceutical preparations from plant materials for over-the-counter use.

A known method of using the drug "ERACOND" (Pat. 2053783. Russian Federation. IPC A61K 35/78. Means for the treatment of wounds, ulcers and burns / Lavin P.I .; Slobodenyuk V.K .; Metelkin AB; applicants - Lavin P. I .; Slobodenyuk V.K .; Metelkin A.V .; patent holder - Apt-Ecology Research and Development Enterprise Limited Liability Company - No. 5014937/14; application form 11.27.1991; publ. 02.10.1996 // Bull . - 1996. - No. 4. - 5 p.), Produced from alfalfa hay. The drug is made from alfalfa plants. An extract is prepared from the crushed plant mass, which is then processed at high temperature and pressure. The output remains a concentrated 40% liquid extract, from which, upon drying, a powder or plastic mass of a dark coffee color is obtained, with a characteristic grassy-coffee aroma. The specified preparation is intended for the treatment of surgical and traumatological wounds, thermal, hydrothermal, chemical, radiation burns, and also as a dermatological and antiseptic agent that helps alleviate the severity of the course of infectious processes.

The specified method has the following disadvantages: a) the extraction of the drug is carried out with an extractant with salts of heavy metals, which increases the toxic load on the patient's body; b) the drug is unstable and susceptible to bacterial contamination after dissolution in water; c) the technology of obtaining an aqueous solution requires filtering to clean from mechanical impurities. The method is not effective enough due to these shortcomings and has negative side effects (risk of infectious complications, intoxication).

For the closest analogue adopted "The method of obtaining funds with anti-inflammatory and wound healing effect" [Pat. RU 2062106 C1; Oganesyan E.T., Chomaeva S.Kh., Sarkisov L.S. - No. 5048626/15; declared 04/29/1992; publ. 06/20/1996 // Bull. - 1999. - No. 18. - 6 p.], Which consists in the fact that dry and thick extracts of sage grass, thuja cones, succession grass, cistus grass and onion scales are emulsified in onion oil extract. The preparation technique for this drug is as follows. Dry and thick extracts are obtained by evaporation (full or partial) of the solvent from the corresponding liquid extracts, in turn, obtained by double extraction of medicinal plant materials with 70% or 40% aqueous ethanol each time in a ratio of 1: 5. Separately, an onion oil extract is prepared, in which emulsification of dry and thick extracts is then carried out. They are used to treat mastitis and other inflammatory processes in veterinary medicine.

The specified method has the following disadvantages: a) uses a variety of wild-growing raw materials; b) is an oil extract, which causes instability during storage, ease of bacterial contamination, and the need to use a preservative; c) the production technology provides for a prolonged exposure to high temperatures, which leads to the inactivation of a significant part of biologically active substances.

Tasks: elimination of toxicity, increasing the effectiveness of exposure by reducing treatment time, ensuring the antibacteriality of the drug.

The essence of the proposed method for producing the drug for the treatment of wounds, abrasions, maceration, pressure sores, cracks, mechanical and thermal damage, various inflammatory processes is the grinding of dried to atmospheric (~ 40%) moisture of peach leaves, their extraction with 96% ethyl alcohol in the ratio 1: 10 for two hours by continuous filtering (percolation and repercolation). Then the hood at a temperature of 40-50 ° C is evaporated under a pressure of 0.6-0.7 atm to 1/20 relative to the original volume and packaged in a sealed container. Depending on the need, the extract can easily be used as a base for ointments, suppositories, aqueous solutions. Ointments and suppositories are prepared on the basis of indifferent fats (palm, petroleum jelly, etc.) and are used as an application. Aqueous solutions are obtained by diluting the extract in the ratio of water to the extract from the leaves of common peach in a ratio of 1:20 to 1: 5 and take per os in known dosages. The proposed drug, the applicants named "Perlex".

The technical result is a technology for producing an alcoholic extract of peach leaves with a high content of biologically active substances (by increasing the completeness of extraction, inhibiting autolytic processes, preventing the destruction of thermolabile components and autoconservation), which has anti-inflammatory, immunomodulating, regenerative effects with local and systemic methods of application.

Based on the studies [Sadykov A.A., Sadykov A.S. Polyphenolic compounds Persica vulgaris. Chemistry of natural compounds. - 1979. - No. 3. - S. 316-321; Dmitruk S.E., Gergievsky V.P., Komissarenko N.F. Biologically active substances of medicinal plants. - Novosibirsk: Science, Sib. Otdel., 1990. - 333 p.] it is shown that the leaves of common peach contain flavonoids, organic acids, coumarins, tannins and other tannins in significant concentrations. Flavonoids reduce the permeability of capillaries and increase their strength, have an anti-inflammatory effect. Organic acids stimulate regenerative processes. Coumarins exhibit anti-inflammatory and antimicrobial effects. Tannins have antidiarrheal, hemostatic and antihemorrhoidal agents.

The technology for preparing the PERLEX preparation is as follows. The leaves of common peach (Persica vulgaris Mill.) Are dried to atmospheric humidity and ground. The raw materials are subjected to extraction for 24 hours by percolation or repercolation using 96% ethanol as an extractant to obtain an extract that is 10 times the weight of the feedstock by weight. Then the extract is concentrated by gentle evaporation at a temperature of 45-50 ° C and a pressure of 0.6-0.7 atm to obtain an extract (concentration 1:20 by volume). Subsequently, aqueous solutions, ointments and suppositories are obtained from the PERLEX preparation by dilution and mixing with indifferent substances.

The PERLEX preparation was tested on 14 rabbits with a live weight of 5-6 kg each, divided equally into two groups. All animals had standard conditions of feeding and feeding. An aseptic wound of 5 cm ^{2 was} formed for each animal. Sterile rings were sutured to the edges of the wound to prevent contraction, and aseptic conditions were maintained by fixing the sterile film over the wound to the specified ring. Animals of the experimental group were irrigated daily with 10% PERLEX aqueous solution, and the control group with 0.9% sodium chloride solution. Every 48 hours, wound planimetry was performed in animals of both groups. The rate of wound healing in animals of the experimental group exceeded the rate of wound healing in animals of the control group by 39%. Two animals of the control group developed suppuration of wounds after 3 days, while in the experimental group suppuration of wounds was noted.

In addition, the proposed drug was tested on 26 patients with skin lesions of various etiologies: wounds, pressure sores, burns, etc.

Table 1 The results of the use of the drug "PERLEX" results Group A Group B Group C Group D The timing healing 12.1 ± 2.1 10.1 ± 2.3 15.1 ± 3.3 14.1 ± 3.1 days Speed epithelization 0.41 ± 0.06 0.73 ± 0.05 0.25 ± 0.07 0.52 ± 0.06 mm / day Note: Group A (N = 14) - patients of the main group with trophic ulcers, group B (N = 12) - patients of the main group with burns, group C (N = 18) - patients of the control group with trophic ulcers, group D (N = 14) - patients in the control group with burns.

Using the proposed extract of peach leaves ordinary allowed to obtain the following effect:

- acceleration of healing of wounds, burns, maceration, pressure sores, cracks in the skin and mucous membranes of various origins and localization due to regenerative, anti-inflammatory, immunomodulating effects on average by 39%;

- reduction of the drug load associated with the use of synthetic drugs for patients with wounds, burns, maceration, pressure sores, cracks in the skin and mucous membranes;

- preservation of the pharmaceutical properties of the drug for a long time due to its high concentration and the use of ethyl alcohol as an extractant and preservative;

- increasing the effectiveness of treatment in connection with the preservation of the active principles of the target components due to the sparing modes of their extraction from the leaves of common peach.

Example 1

A weighed portion of 100 g of ordinary peach leaves was dried to a moisture content of 40%, crushed, filled with 1 liter of 96% ethanol and extracted within 24 hours by percolation and re -colation, then the obtained extract was evaporated under a pressure of 0.6 atm at a temperature of 40-50 ° C to a volume of 50 ml and packaged in a bottle of 50 ml. Upon receipt of the victim with a burn of boiling water 2 tbsp. prepared an ointment based on pre-boiled olive oil for 15 minutes, adding 50 ml of extract to 500 ml of oil. Daily, a sterile bandage dipped in the preparation was applied to the burn. The very next day, a decrease in inflammatory reactions on the burn surface was noted, and after 3 days an acceleration of edge epithelization was noted by 35%. The burn completely epithelized 29% faster than a similar victim treated with well-known drugs.

Example 2

A weighed portion of 100 g of ordinary peach leaves was dried to a moisture content of 40%, crushed, filled with 1 liter of 96% ethanol and extracted within 24 hours by percolation and re -colation, then the obtained extract was evaporated under a pressure of 0.6 atm at a temperature of 40-50 ° C to a volume of 50 ml. 6 ml of the resulting solution was mixed with 54 ml of cocoa butter until smooth and 20 candles of 3 g each were made from the resulting mixture. The prepared candles were applied rectally to a patient with an acute rectal fissure in a dosage of 1 candle twice a day (morning and night). After 2 days, the pain syndrome decreased. By 5 days, pain, discomfort, perianal itching regressed. At 9 days of examination, a good epithelization of an acute rectal fissure was observed, which is almost twice as fast as in a similar contingent of patients treated with well-known drugs.

Example 3

A weighed portion of 100 g of ordinary peach leaves was dried to a moisture content of 40%, crushed, filled with 1 liter of 96% ethanol and extracted within 24 hours by percolation and re -colation, then the obtained extract was evaporated under a pressure of 0.6 atm at a temperature of 40-50 ° C to a volume of 50 ml and packaged in a bottle of 50 ml. Upon receipt of a patient with a trophic ulcer of the lower leg, in the complex therapy of complications of chronic venous insufficiency, the resulting solution was used as a local therapy. A gauze napkin was placed on the ulcer defect along the perimeter and soaked with PERLEX solution 4-5 times a day from a syringe. After 2 days, there was a decrease in inflammatory reactions, a decrease in perivular edema, and after another 5 days, an acceleration of edge epithelization was noted by 25%. A peptic ulcer completely epithelized 24% faster than a similar patient treated with well-known drugs.

Claims (2)

1. A method of obtaining anti-inflammatory and wound healing agents, including alcohol extraction of herbal medicinal products and evaporation in vacuum to obtain a thick extract, characterized in that the leaves of ordinary peach are pre-dried to atmospheric humidity, crushed and extracted for 24 hours with 96% ethyl alcohol in the ratio raw materials and extractant 1:10 in the mode of percolation-repercolation, then under a pressure of 0.6-0.7 atm at a temperature of 40-50 ° C, the hood is evaporated to 1/20 relative to the original volume . 2. The method according to claim 1, characterized in that on the basis of the obtained extract prepare aqueous solutions, ointments and suppositories with a final extract content of from 5 to 20 vol.%.