Anti-inflammatory and wound-healing drug

 

(57) Abstract:

The invention relates to medicine and pharmaceutical industry. Anti-inflammatory and wound healing agent includes carotenodermia drug, antimicrobial agent, methyluracil, tween-80, synthetic fatty alcohols primary fraction C16-C21, preservative, purified water and propellant Refrigerant-12, and as a preservative - non-aqueous hydrophilic solvent (1,2-propylene glycol or a mixture of glycerol and ethanol 95%). The tool provides a comprehensive impact on the affected tissue and high therapeutic effect while ensuring standards of microbial contamination during production, storage and use of the drug. 5 table.

The invention relates to medicine and pharmaceutical industry, namely to medicines, anti-inflammatory and wound-healing actions that can be used for the treatment of inflammatory diseases.

Known healing agent in the form of microcapsules [1], comprising as a carrier a mixture of magnesium oxide and kaolin, as active ingredients a mixture of carotenodermia raises the vine, water-soluble salt of alginic acid and calcium.

Known wound healing agent applied in the form of foam on the damaged tissue, and represents a combined preparation, which includes sea buckthorn oil, chloramphenicol, benzocaine, boric acid, stearic acid, glycerin, triethanolamine, lanolin, propellant and water.

Known drug "Aerosol nitazola" [2], used for the treatment of acute and chronic trichomoniasis and including nitazol, olive oil, emulsive wax, glycerin, distilled water, alcohol 95%, refrigerant-12.

Closest to the claimed is anti-inflammatory "Hipotel-A [3] , which consists of drugs aekol, etazol-sodium, methyluracil, excipients tween-80, higher fatty alcohols primary fraction C16-C21, propyl ester of p-oksibenzoynoy acid, 95% ethanol, refrigerant-12, distilled water. The drug is intended for treatment of inflammatory diseases in gynecology, proctology, dentistry, dermatology.

The obstacles in the prototype and the analogues of the technical result achieved in the inventive IV is not possible to achieve a high level of anti-inflammatory and wound-healing actions with the present tool synergistic nature while still providing an antimicrobial effect and norms of microbial contamination during production, storage and use of drugs.

The problem to which the invention is directed, is to create drugs with high specific activity.

The invention consists in that the claimed anti-inflammatory and wound healing agent includes carotenodermia drug, antimicrobial agent, methyluracil, tween-80, synthetic fatty alcohols primary fraction C16-C21, preservative, purified water and hladon-12, and as an antimicrobial agent use nitazol, and as preservative - non-aqueous hydrophilic solvent (1,2-propylene-glycol or a mixture of glycerol and ethanol 95%) in the following ratio, wt.%:

Carotenodermia drug - 20-40

Nitazol - 1,0-3,0

Methyluracil - 1,0-3,0

Tween-80 - 2,0-2,8

Alcohols of synthetic primary higher fatty fraction C16-C21- 4,2-5,0

Non-aqueous hydrophilic solvent - 6,0-10,0

Refrigerant-12 - 10-20

Water acidentally the affected tissues and high therapeutic effect while ensuring standards of microbial contamination in the production process, storage and use of the drug.

Example 1. To obtain the claimed medicinal product prepared in a composition containing drugs aekol, nitazol, methyluracil, tween-80, alcohols of synthetic primary higher fatty fraction C16-C21, non-aqueous hydrophilic solvent (a mixture of glycerol and ethanol 95% in sootnoshenii 1:1), purified water and hladon-12 in the following ratio, wt.%:

Aekol - 30,0

Nitazol - 2,0

Methyluracil - 2,0

Tween-80 - 2,4

Alcohols of synthetic primary higher fatty fraction C16-C21- 4,6

A mixture of glycerine and ethyl alcohol 95% (1:) - 8,0

Refrigerant-12 - 14,0

Purified water Up to 100

To obtain the claimed medicinal product in the container 1 is placed higher fatty alcohols, tween-80, methyluracil and purified water. The mixture is heated with stirring to (855)oC. Stirring is maintained till the dissolution methyluracil, tween-80 and melt the alcohol, then the alcohol emuleret using turbomachines, cooling the colloidal disperse system to (555)oC. At this temperature, add Ecol and emuleret the resulting mixture turbomaschinen. In the container 2 is placed non-aqueous hydrofil the rotary pulsation apparatus. The resulting suspension is added to the emulsion ecola cooled to (392)oC, and continue cooling with stirring to (255)oC.

The resulting composition is Packed in aerosol containers, sealcoat valves and injected under pressure refrigerant-12.

Example 2. To obtain the claimed medicinal product prepared in a composition containing sea buckthorn oil, nitazol, methyluracil, tween-80, higher fatty alcohols primary fraction C16-C21, 1,2-propylene glycol, purified water and hladon-12 in the following ratio, wt. %:

Sea buckthorn oil - 40

Nitazol - 3

Methyluracil - 3

Tween-80 - 2,8

Alcohols of synthetic primary higher fatty fraction C16-C21- 5

1,2-propylene glycol - 10

Refrigerant-12 - 20

Purified water Up to 100

Drug get analogously to example 1.

Example 3. To obtain the claimed medicinal product prepared in a composition containing the drug lipohromin, nitazol, methyluracil, tween-80, higher fatty alcohols primary fraction C16-C21, 1,2-propylene glycol, purified water and hladon-12, with the following ratio of components, wt.%:

Lipochrome fraction C16-C21- 4.2V

1,2-propylene glycol - 6

Refrigerant-12 - 10

Purified water Up to 100

Drug get analogously to example 1.

The proposed drug as carotenodermia component, in addition to the above, may contain rosehip oil, oil Rowan ordinary, carotenal and so on, i.e., any drug or substance with the lower limit of the amount of carotenoids in terms of b-carotene-22, 95mm mg in one pack (50 g).

As a non-aqueous hydrophilic solvent used 1,2-propylene glycol or a mixture of glycerine and ethyl alcohol 95% (in the ratio 1: 1).

The resulting tool has been tested in laboratory and clinical settings.

Anti-inflammatory properties of the proposed drug was tested in comparison with the prototype and similar in experimental swelling of the limbs of rats. About the pharmacological action of drugs made the conclusion on their ability to inhibit edema induced vlahogiannis agent Aerosil.

The results are shown in table.1.

As can be seen from the data presented in table. 1, the anti-inflammatory effect of the inventive tool is superior to the object than is claimed in the tool.

Wound-healing properties of the proposed drug was tested in comparison with the prototype and similar experimental screen wounds in rats. A wound healing effect of the drugs made a conclusion on the kinetics of the decrease of the area of the wound surface.

The results are shown in table.2.

As can be seen from the data presented in table.2, in aseptic conditions, naniniwala wounds similar to "Aerosol nidazole" has a weak healing actions. However, in the inventive tool nitazol potentional wound healing effect of the combination of methyluracil with carotenogenesis component, which is especially evident on 5-11 day treatment of animals.

Comparative analysis of microbial obremenjenosti drugs conducted in accordance with the requirements of the State Pharmacopoeia of the USSR XI ed. Conducted research bactericidal and fungicidal action of drugs while infecting them with bacteria (Staphylocoocus aureus was ATSS 25923, Escherichia coli was ATSS 25922, Pseudomonas aeruginosa was ATSS 27853) and fungi (Candida albicans 184) at different microbial load and different exposures.

The results of these studies are reflected in the table.3.

As can be seen from the data presented in table.3, claimed the awn, or are sterile.

These studies indicate that the inventive tool unlike the prototype and its analogues is clostridiosis against pathogenic bacteria and fungi. Thus, it effectively prevents the growth and development of P. aeruoInosa and C. aIs that are not sensitive to native nitazol even with high microbial load 105CFU/g

The claimed aerosol product in accordance with the decision of the pharmacological Committee of the Ministry of health of Ukraine (Protocol # 7 from 03.12.92,) passed clinical trials as anti-inflammatory, wound healing and antibacterial agents. The aggregated results of its clinical use in surgery in 38 patients are presented in table.4.

Compared to similar "Hypothalami " And" inventive tool has provided a more efficient therapeutic effect, which was shown to accelerate the healing time of wounds, reducing the number of pyo-inflammatory complications and associated mortality.

In table. 5 presents the summary of the results of treatment in gynecological inflammatory diseases of the inventive tool and Hypothalami" (similar).

In the treatment gynecologistmothers coloration of the mucous membrane of the vagina, the cervical canal, vulva; was epithelialization of the mucous membrane of the cervix labels, decreased the size of erosions. In 50% of cases there was complete clinical recovery, a positive effect was recorded in 86.5% of cases. No effect was observed in 13.5% of cases. When using "Chipotle" (similar) these figures were, respectively, 30, and 72,5 27,5%.

Thus, the claimed medicinal product in comparison with the known has the following advantages: more effective anti-inflammatory, wound healing and antimicrobial activity, as well as higher quality of drug indicators of microbial purity. All these factors will increase the effectiveness of treatment in surgery, combustology, proctology, gynecology, dentistry.

Literature

1. Auth. St. USSR N 884189, class A 61 K 9/12, 1981.

2. Prospect Aerosol nitazola"): cbti, Minneapol, 1985.

3. Auth. St. USSR N 1681420, class A 61 K 9/12, 1991.

Anti-inflammatory and wound-healing drug, including carotenodermia drug, antimicrobial agent, methyluracil, tween-80, alcohols of synthetic primary higher fatty fraction16- C21, preservative, is the amount of preservative - 1,2-propylene glycol or a mixture of glycerol and ethanol 95% in the ratio of 1 : 1 in the following ratio, wt.%:

Carotenodermia product in the form of oil solution - 20,0 - 40,0

Nitazol - 1,0 - 3,0

Methyluracil - 1,0 - 3,0

Tween-80 - 2,0 - 2,8

Alcohols of synthetic primary higher fatty fraction16- C21- 4,2 - 5,0

1,2-Propylene glycol or a mixture of glycerol and ethanol 95% in the ratio of 1 : 1 - 6,0 - 10,0

Refrigerant-12 - 10,0 - 20,0

Purified water Up to 100

this carotenodermia product is the lower limit of the amount of carotenoids in terms of b-carotene 22, 95mm mg to 50 mg of the drug.

 

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9 cl, 1 tbl, 8 ex

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