RU2458684C2 - Gel showing anti-inflammatory, analgesic, wound healing action (versions) - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, and concerns more than one version of the compositions showing anti-inflammatory, analgesic, wound healing action which are applicable for treating dermatites, wounds, bruises, and locomotor diseases. All versions of the compositions contain a moulding base, Mumiyo, and also a complex phytoextract.

EFFECT: compositions possess extended pharmacological action and may be applicable in complex therapy of locomotor diseases.

4 cl, 4 tbl, 5 ex

Description

The invention relates to the pharmaceutical industry and relates to a composition that can be used to treat diseases of the musculoskeletal system, osteoarthritis, radiculitis, osteochondrosis with radicular syndrome, muscle pain with bruises and sprains. Known balm, according to patent RU 2231361 analgesic, anti-inflammatory, characterized in that it contains the following components, wt.%:

Thuja essential oil essential (B) 0.19-4.75 Juniper Berry Essential Oil B 0.19-4.75 Cypress B Essential Oil 0.19-4.75 Bergamot B Essential Oil 0.016-0.4 Lemon B Essential Oil 0.02-0.5 Grapefruit B Essential Oil 0.02-0.5 Mandarin B Essential Oil 0.02-0.5 Sweet B Orange Essential Oil 0.01-0.25 Bitter Orange Essential Oil 0.01-0.25 Nerolium B Essential Oil 0.01-0.25 Tauride B essential oil of wormwood 0.01-0.25 Lemon B wormwood essential oil 0.01-0.25 Coriander B Essential Oil 0.01-0.25 Lavender Essential Oil CO ₂ Extraction 0.01-0.25 Petigrene essential oil (lemon leaf) B 0.01-0.25 Catnip B Essential Oil 0.01-0.25 Marjoram B Essential Oil 0.01-0.25 Rosemary B Essential Oil 0.01-0.25 Ylang Ylang Essential Oil 0.1-4.0 Santala essential oil 0.04-1.0 Palmarosa essential oil 0.01-0.25 Rosewood Essential Oil 0.02-0.5 Jasmine essential oil 0.014-0.35 Absolute Rose Oil 0.01-0.25 Absolute Sage Oil 0.04-1.0 Absolute cistus oil absolute 0.01-0.25 Total 1.00-25.00 Odor clamp 1.00-25.00

Known gel balm with a wound healing effect, characterized in that it contains dihydroquercetin, medical glycerin, linseed or cedar oil, chitosan water gel (Patent RU No. 2381810).

Closest to the proposed is a wound healing agent, including a gelling agent and a purified mummy, characterized in that it further contains distilled water (Patent RU No. 2185149).

An object of the invention is the expansion of biological activity and pharmacological action of the proposed composition.

The stated technical problem is achieved due to the synergistic action of the components of the composition options.

The first option contains, in addition to the mummy, a gelling base and purified water, a complex phytoextract from celandine, wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots, fennel, thyme, mint, hypericum, yarrow, caraway seeds, sea buckthorn oil and medicinal plant oil, base, glycerin, PEG-stearate 400, cetyl alcohol, pepper extract, sodium hydroxide 10%, triglyceride caprylate in the following ratio, in wt.%:

Complex phytoextract 0.75 Mummy 0.4 Sea buckthorn oil 2.0 Oil of medicinal plants (Passeriforum) 1,0 Caprylate Triglyceride 20,0 Gel base (carbopol) 0.6 Peg stearate 400 Cetyl alcohol 2.0 Pepper Oil Extract 0.5 Sodium hydroxide 10% 0.6 Purified water rest

The second option contains, in addition to the mummy and the base, a complex phytoextract from celandine, wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots, fennel, thyme, mint, St. John's wort, yarrow, caraway fruits, as well as glucosamine hydrochloride, sea buckthorn oil, flavoring, nipagin, PEG-stearate, Trilon-B, bases, in the following ratio of components, in wt.%:

Complex phytoextract 0.3 Mummy 0.5 Glucosamine hydrochloride 2.0 Sea buckthorn oil 1,0 Flavoring 0.05 Nipagin 0.3 PEG stearate 400 0.5 Trilon-B 0.4 Base (PEG-stearate 1500) rest

The third option contains, in addition to the mummy, a gelling base and purified water, a complex phytoextract from celandine, bitter wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots, fennel, thyme, mint, hypericum, yarrow, caraway seeds, as well as sea buckthorn oil, olive oil, base, glycerin, ammonia water, para-hydroxybenzoic acid methyl ester, para-hydroxybenzoic acid propyl ether, polyethylene glycol stearate, purified water, in%:

Complex phytoextract twenty Mummy 0.1 Perfume 0,03 Sea buckthorn oil 0.5 Olive oil 2.0 Gelling base (arerespol) 1,0 Glycerol 4.0 Ammonia water 0.3 Para-hydroxybenzoic acid methyl ester 0.3 Para-hydroxybenzoic acid propyl ester 0.1 Polyethylene glycol stearate 400 1,0 Purified water rest

The fourth option contains, in addition to the mummy, the gelling base and purified water, a complex phytoextract from celandine, bitter wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots, fennel, thyme, mint, St. John's wort, yarrow, caraway seeds, as well as sea buckthorn oil, cocoa butter, olive oil, a base, glycerin, glucosamine hydrochloride, para-hydroxybenzoic acid methyl ester, para-hydroxybenzoic acid propyl ester, polyethylene glycol stearate, in the following ratio of components, in %:

Complex phytoextract twenty Mummy 0.4 Perfume 0.05 Sea buckthorn oil 1,0 Olive oil 5,0 Gel base (Cibo Salcare SC 91) 1,0 Cacao butter 2.0 Glycerol 6.0 Para-hydroxybenzoic acid methyl ester 0.2 Polyethylene glycol stearate 400 2.0 Para-hydroxybenzoic acid propyl ester 2.0 Purified water rest

All components included are known and used in pharmacy.

An example of a specific implementation No. 1

Phase No. 1: 0.6% of the base is poured into 67.15% of the purified water with the addition of 4.0% glycerol, heated to 70 ° C and allowed to swell, then sodium hydroxide 10% in the amount of 0.6% is added with thorough stirring.

Phase 2: 0.4% of the mummy is crushed and dissolved in 0.75% phytoextract (The extract is obtained from celandine, wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots, fennel, thyme, mint, hypericum, yarrow, caraway seeds. The same number of plants is poured with 70% ethyl alcohol in a ratio of 1: 5 and insisted for 3 days in a dark room, then the finished extract is filtered).

Phase 3: sea buckthorn oil 2.0%, cetyl alcohol 2.0% is fused at 70 ° C.

Phase 4: 1% PEG-stearate 400 is heated in a water bath until melted, then pepper oil extract is added (1 part of pepper is poured with 3 parts of oil and insisted for 3 days in a dark place, then filtered) 0.5% and oil medicinal plants (passeriformes) 1.0%, caprylate triglyceride 20%.

Phase 5: phase 1, 2, 3, 4 are mixed together.

An example of a specific implementation No. 2

Phase 1: 0.5% PEG-stearate is placed in an enameled container, heated in a water bath until melted, then 1.0% sea buckthorn oil is added and mixed until homogeneous, and then 2.0% glucosamine hydrochloride is added in part and mixed until cooling .

Phase 2: 3.0% of the complex extract is mixed in an enameled container (The extract is obtained from celandine, wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots, fennel, thyme, mint, hypericum, yarrow, caraway fruits. The same number of plants is poured with 70% ethyl alcohol in a ratio of 1: 5 and insisted for 3 days in a dark room, then the finished extract is filtered) with crushed mummy in the amount of 0.5%, then 0.3% nipagin and 0.4% are added Trilon B and stirred until dissolved.

Phase 3: phase 1 is mixed with phase 2 and the base is added in parts (pre-melted in an enameled container PEG-stearate 1500) in an amount of 92.25%, thoroughly mixing and flavoring in an amount of 0.05%.

An example of a specific implementation No. 3

Phase No. 1: 1% of the base (arerespol) is poured into 70.67% of the purified water with the addition of 4.0% glycerol, heated to 70 ° C, left to swell, after which 0.3% ammonia water is introduced.

Phase No. 2: 0.1% mummy is crushed and mixed with 20% of the complex extract (The extract is obtained from celandine, wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots, fennel, thyme, peppermint, St. John's wort, yarrow , fruits of caraway seeds The same amount of plants is poured with 70% ethyl alcohol in a ratio of 1: 5 and insisted for 3 days in a dark room, then the finished extract is filtered) and 0.5% sea buckthorn oil.

Phase 3: 1% PEG-stearate is heated in a water bath until melted, then olive oil 2.0% and para-hydroxybenzoic acid methyl ester 0.3% and para-hydroxybenzoic acid propyl ester 0.1% are added.

Phase number 4: connect phase 1, 2, 3 and add fragrance in an amount of 0.03%.

An example of a specific implementation No. 4

Phase 1: 1% of the base (Cibo Salcare SC 91) is poured into 60.35% of water with the addition of 4.0% glycerol, heated to 70 ° C, left to swell, after which 0.3% ammonia water is added with thorough stirring.

Phase 2: 2% PEG-stearate is placed in a container and 2% cocoa butter is heated in a water bath until melted, and 1.0% sea buckthorn oil, 5% olive, oil and para-hydroxybenzoic acid methyl ester in an amount of 0.2% and mix until smooth.

Phase 3: 0.4% of the mummy is crushed and mixed with 20% of the complex extract (The extract is obtained from celandine, wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots, fennel, thyme, mint, St. John's wort, yarrow , fruits of caraway seeds. The same number of plants is poured with 70% ethyl alcohol in a ratio of 1: 5 and insisted for 3 days in a dark room, then the finished extract is filtered).

Phase number 4: connect phase 1, 2, 3 and enter the fragrance in the amount of 0.05%. As the base, any gelling agent or acrylate copolymer can be used. Instead of the red-root passeriformes, clove oil or Chinese magnolia vine can be used.

The wound healing effect was determined by the chemical method of reproducing wounds. The experiments were performed on white rats weighing 200 ± 10 g. Wounds were caused by intraperitoneal administration of 6% dextran solution to animals and subcutaneous administration of 9% acetic acid. We studied 4 groups of animals, which were applied to the injection site of acetic acid, the proposed compositions No. 1, 2, 3, 4 during the appearance of necrotic ulcers on the affected area at a dose of 300 mg / kg of animal body weight.

The criterion for a specific wound healing action was the moment of the appearance of the dividing strip between healthy skin and the necrotic area, the beginning and complete rejection of the scab, the general condition of the animals and the condition of the skin at the wound site after rejection of the scab. Statistically significant differences between treated and untreated animals are noted already after 7 days from the start of treatment, and complete rejection of the scab is observed by 22-27 days. In untreated animals, a similar effect is observed only by 40-49 days.

Thus, the results indicate a pronounced wound healing effect in all the proposed formulations for wounds reproduced using chemicals.

The pharmacological activity of the proposed compounds was tested in the Pyatigorsk Central Military Sanatorium and was prescribed in a comprehensive sanatorium treatment for 30 patients with primary and post-traumatic arthrosis (OA) 1 and 11 of the X-ray stage. The clinical characteristics of the treated are presented in table.№1. A control group of 26 people were patients with OA. The structure of patients with OA is presented in Table 2. The therapeutic effect and tolerability of the compositions was evaluated at the end of a 2-week course compared with the prototype. Used the following indicators:

1) the intensity of pain in the joints according to the patient (0-3);

2) the severity of pain during palpation, active and passive movements;

3) in joints, in points (0-3), synovitis dynamics;

4) assessment of local therapy separately by the patient and the doctor;

5) assessment according to the SAN system.

Compositions were applied with massage movements on 2-3 joints 3 times a day. The course is 2 weeks.

Absorption time ranged from 1-3 minutes. Local action began within 10 to 90 minutes (38 minutes on average) and lasted up to 3 hours on average 1.8 hours. By the end of the 2-week use, quantitative indicators of the severity of the articular syndrome decreased; articular index of 0.8 points, pain and inflammatory index of 0.6 and 0.5 points (Table 3) Individual assessment of the gel by patients as a whole is positive, 63.3% (19 people), noted a noticeable improvement in 7 people, 23.3 % moderate improvement, 4 people (16.4%) did not notice a significant reduction in pain.

Example 5

Patient S., 70 years old, medical history No. 50007, pain in the interphalangeal joints, worried about 10 years. Composition No. 2 was applied to the interphalangeal joints 3 times a day, easily rubbing it in a circular motion. Applied the composition of 18 days. When examined before use, swelling of the interphalangeal joints, synovitis of the proximal phalanx of the middle finger of the right hand were noted. After 4-5 procedures, pain in the joints decreased, after the 5th procedure, the swelling disappeared. The range of motion according to goniometry returned to normal after 10 procedures. The most distinct effect of treatment in the dynamics of synovitis of the proximal phalanx of the middle finger of the right hand.

Thus, the compositions have a wider spectrum of action and can be used in the complex treatment of diseases of the musculoskeletal system.

Table number 1 Clinical characteristics of the treated compositions. Indicators The main group (n = 30) Control Group (n = 26) Age years 35-79 38-68 Including 57.6 56.4 - men fifteen 12 - women fifteen fourteen Prescription of the disease 7 months 23 years old 1,5-19 years 7.9 8.8 Osteoarthrosis - primary eighteen eighteen - secondary 12 8 R stage of osteoarthrosis one 7 fourteen 2 23 12 The presence of synovitis, people. 5 four

Table number 2 The structure of patients with osteoarthritis (n = 30) Polyosteoarthrosis with a primary lesion of small joints Coxarthrosis Gonarthrosis OA OA of the carpal joints OA of the elbow joints I primary 6 2 10 - - - II post-traumatic - - 6 3 2 one

Table number 3 Dynamics of indicators after treatment. Indicator The main group (n = 30) Control Group (n = 26) BI (0-3) 2,3 1,5 2,3 1.8, SI (0-3) 2,3 1.4 2,3 1,5 VI (n = 5 people) 2.0 1.9 2.0 1,5

Table number 4 Evaluation of the effectiveness of the local use of the compounds in the complex treatment of patients with osteoarthrosis according to the SAN technique Before treatment After treatment Feeling well 4.4 5,0 Activity 4.6 5.8 Mood 5,0 5.5

Claims (4)

1. The composition has anti-inflammatory, analgesic, wound-healing effect, containing a gelling agent, mummy and purified water, characterized in that it additionally contains a complex phytoextract from celandine, bitter wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots , fennel, thyme, mint, St. John's wort, yarrow, caraway seeds, sea buckthorn oil, medicinal plant oil, glycerin, PEG-stearate 400, cetyl alcohol, pepper extract, sodium hydroxide 10%, caprylate trig lyceride in the following ratio, wt.%:
Complex phytoextract 0.75 Mummy 0.4 Sea buckthorn oil 2.0 Herb Oil 1,0 Caprylate Triglyceride 20,0 The basis 0.6 Glycerol 4.0 PEG stearate 400 1,0 Cetyl alcohol 2.0 Pepper extract 0.5 Sodium hydroxide 10% 0.6 Purified water Rest 2. A composition having anti-inflammatory, analgesic, wound healing and bactericidal action, containing a gelling agent and a mummy, characterized in that it additionally contains a complex phytoextract from celandine, bitter wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots, fennel, thyme, mint, St. John's wort, yarrow, caraway seeds, as well as glucosamine hydrochloride, sea buckthorn oil, flavoring, nipagin, PEG stearate 400, trilon-B in the following ratio of components, ma .%:
Complex phytoextract 3.0 Mummy 0.5 Glucosamine hydrochloride 2.0 Sea buckthorn oil 1,0 Flavoring 0.05 Nipagin 0.3 PEG stearate 400 0.5 Trilon-B 0.4 The basis Rest 3. A composition having anti-inflammatory, analgesic, wound healing effect, containing a gel-forming base, mummy and purified water, characterized in that it additionally contains a complex phytoextract from celandine, bitter wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots , fennel, thyme, mint, St. John's wort, yarrow, caraway seeds, as well as sea buckthorn oil, olive oil, glycerin, ammonia water, methyl para-hydroxybenzoic acid, para-o propyl ether sibenzoynoy acid, and polyethylene glycol 400 stearate, perfume components in the following ratio, wt.%:
Complex phytoextract 20,0 Mummy 0.1 Perfume 0,03 Sea buckthorn oil 0.5 Olive oil 2.0 The basis 1,0 Glycerol 4.0 Ammonia water 0.3 Para-hydroxybenzoic acid methyl ester 0.3 Para-hydroxybenzoic acid propyl ester 0.1 Polyethylene glycol stearate 400 1,0 Purified water Rest 4. A composition having anti-inflammatory, analgesic, wound healing effect, containing a gel-forming base, mummy and purified water, characterized in that it additionally contains a complex phytoextract from celandine, bitter wormwood, calendula flowers, pine buds, chamomile flowers, rose hips, licorice roots , fennel, thyme, mint, St. John's wort, yarrow, caraway seeds, as well as sea buckthorn oil, olive oil, glycerin, para-hydroxybenzoic acid methyl ester, para-hydroxybenzoic acid propyl ester, polyethylene glycol stearate 400 and perfume in the following ratio of components, wt.%:
Complex phytoextract 20,0 Mummy 0.4 Perfume 0.05 Sea buckthorn oil 1,0 Olive oil 5,0 The basis 1,0 Glycerol 6.0 Para-hydroxybenzoic acid methyl ester 0.2 Para-hydroxybenzoic acid propyl ester 0.1 Polyethylene glycol stearate 400 2.0 Purified water Rest