RU2286141C1 - Ointment for topical application - Google Patents

Abstract

FIELD: pharmaceutical industry, in particular analgesic, vasodilatation, anti-inflammation ointment for topical application.

SUBSTANCE: claimed ointment is prepared in form of fine dispersed formulation containing bee venom extract melittin, lavender oil, camphor, arnica tincture, rosemary oil, eucalyptus oil, revitalin, carbopol, 30 % solution of sodium hydroxide, hydrophilic anionic ointment, soy lecithin, glycerol, conserving solution, ethanol, distilled water.

EFFECT: reduced toxicity of bee venom, decreased side effects and improved therapeutic effect.

2 tbl, 3 ex

Description

The invention relates to medicine, namely to pharmacy, and for the composition of the ointment for external use.

In medicine, compositions for treating patients with rheumatism, muscle and joint diseases, hypertension, non-specific polyarthritis, myositis, lumbosacral radiculitis, sciatica, neuralgia, polyneuritis, myalgia, such as rubbing "Menovazin" and other compounds containing snake and bee venoms are widely known - “Vipratox”, “Viparin”, “Apizatron”. The disadvantages of the compositions containing snake and bee poisons are high individual intolerance, a large number of contraindications.

The closest to the claimed composition according to the achieved result is Viprosal ointment containing gyurza poison, camphor, salicylic acid, fir oil, petrolatum, glycerin, paraffin, emulsifier and water. However, since gyurza venom is a coagulant (a substance that increases blood coagulability), the disadvantages of the known drug include a narrow therapeutic interval - the difference between safe and toxic doses; the use of petroleum jelly, which forms a thin film on the skin, making it difficult for active drug substances to enter the blood; frequent individual intolerance to the drug, manifested in the form of nausea, vomiting, malaise, chills, fever, swelling, urticaria, pain in the lower back and joints, seizures, fainting, etc. In addition, the drug has numerous contraindications - kidney, liver and pancreas, diabetes, neoplasms, tuberculosis, severe infectious diseases of the hematopoietic system, circulatory failure, etc.

The technical result achieved by the creation of the present invention is to obtain an effective analgesic, vasodilator and anti-inflammatory drug based on the components of bee venom, which has improved tolerance and fewer side effects by reducing the toxicity of bee venom by removing fractions that cause side reactions. The ointment can be used to treat, in particular, patients with rheumatism, muscle and joint diseases, hypertension, non-specific polyarthritis, myositis, lumbosacral radiculitis, sciatica, neuralgia, polyneuritis, myalgia and many other diseases.

This result is achieved by the creation of an ointment of analgesic, vasodilating, anti-inflammatory, the composition of which as a main component includes bee venom extract - melittin, camphor, tincture of arnica, lavender, rosemary and eucalyptus oil, revitalin, and carbopol, 30% sodium hydroxide solution as auxiliary components. hydrophilic anionic ointment, soya lecithin, glycerin, preservative solution, distilled water and ethyl alcohol, in the following ratio of components in g per 100 g of product:

Bee Venom Extract - Melittin (Apis mellifera toxin) 0.003 ÷ 0.010 Lavender Oil (Aetheroleum lavandulae) 1,0 ÷ 5,0 Camphora (Camfora) 3.0 ÷ 5.0 Arnica Tincture (Tinctura amicae) 2.0 ÷ 7.0 Rosemary oil (Aetheroleum rosmarinus) 1,0 ÷ 5,0 Eucalyptus Oil (Aetheroleum eucalyptus) 1,0 ÷ 5,0 Revitalin (Revitalin) 1,0 ÷ 3,0 Carbopol (Carbopol) (934 or 940 or 941) 0.99 ÷ 1.1 Sodium hydroxide solution 30% (Natrium hydroxid 30%) 0.99 ÷ 1.1 Hydrophilic anionic ointment (Natrium laurylsulfuricum, Alkoholum cetylstearilicum, Paraffinum liguidum, Vaselinum album) 19.9 ÷ 20.1 Soya Lecithin (Lecitinum) 0.2 ÷ 0.4 Glycerin (Glycerinum) 6.0 ÷ 10.0 Preserving solution (Methylparahydroxybenzoicum) 0.9 ÷ 1.1 Ethyl Alcohol (Alcoholum 96%) 1,2 ÷ 1,5 Distilled water (Agua destillata) Rest

The proposed ointment for physico-chemical properties is a homogeneous fine preparation from white to light yellow in color with the smell of camphor and lavender. The main component of the drug is bee venom extract - melittin. It has an anti-inflammatory, analgesic effect. In addition, it will expand the vessels of the brain and coronary vessels, stimulates the activity of the pituitary-adrenal system. Camphor - a drug from the group of stimulants of nervous activity. Upon contact with the skin, it is well absorbed, has a local irritant effect and has antiseptic and insecticidal properties. Arnica tincture is a locally irritating, anti-inflammatory, antibacterial drug. Promotes the formation and release of physiological stimulants of immunological processes, activates local blood flow, accelerates the resorption of hemorrhages. Lavender, rosemary, eucalyptus oils act on skin receptors, accompanied by the release of endorphins and other substances that regulate pain sensitivity and vascular permeability. They have analgesic and anti-inflammatory effects. Revitalin causes a significant increase in skin temperature, enhances blood supply to the depth of the muscles, which contributes to better penetration into the blood of the active components of the drug. Carbopol is a carboxyacrylic polymer. Used to prepare a suspension. Anionic hydrophilic ointment, sodium hydroxide solution 30%, glycerin are part of the finely dispersed ointment base. Soy lecithin contains common phospholipids, promotes the development of the body, increases physical and mental ability, accelerates the recovery of the body after great efforts. It has the ability to penetrate deep into the skin. Preservative solution is used as an oxidation inhibitor during long-term storage. Ethyl alcohol (96%) is a multifunctional component of the drug. It has good dissolving power. In addition, when applying the ointment to the skin, it promotes a deeper penetration of the components with the simultaneous release of heat (heating the surface of the body).

Testing the therapeutic composition of the ointment as an anesthetic was carried out at the Moscow Institute of Alternative Treatment Methods and the Laboratory of Clinical Pharmacology and Doping Control MNPTSSM.

At the Moscow Institute of Alternative Treatment Methods, the medicinal composition was used as an external agent by rubbing a layer of approximately 1-2 mm in the area of severe pain. Depending on the intensity of the pain, the procedure was repeated up to 3 times a day. With a good result of treatment, pain disappeared, overall health improved, sleep was normalized, neurological symptoms were smoothed out or disappeared. With a satisfactory result of treatment, pain and objective symptoms decreased. In the absence of dynamics in subjective and objective data, the result of treatment was evaluated as without effect. As can be seen from table 1, of the total number of patients who were treated with the proposed drug, 48.6% received a good result, 44.3% - satisfactory, 7.1% - no effect was observed. Thus, the treatment efficiency of the claimed drug was 92.9%.

At the Laboratory of Clinical Pharmacology and Doping Control MNPTSSM the purpose of the study was to evaluate the effectiveness of the drug in the practice of sports medicine. The studies were carried out on athletes, middle-distance runners with traumatic lesions of tissues and the musculoskeletal system (mild and moderate) of the lower extremities.

The total number of subjects: 30 people.

The control group (10 athletes) did not use ointment.

Qualification: msmk-6, ms-12, kmf-12.

Age: 18 to 28 years old.

In accordance with the conditions of the test, all subjects at the beginning and end of the experiment (1st and 20th days) underwent comprehensive testing and medical examination, as well as 5 days after cessation of use. The overall performance of athletes was assessed by performing extreme muscular work of stepwise increasing nature to “failure” on the Quinton running treadmill (USA). Among biochemical parameters, observations were made on the concentration of urea, lactate, glucose, and protein in the blood according to generally accepted methods. The results of the effect of the claimed ointment on physical performance are presented in table 2 (in% of control).

The conclusions of the ISTCM:

- the declared ointment with a course application for 20 days restores the overall athletic performance of athletes;

- revealed the antioxidant effect of the drug at the same time;

- any side effects (allergic reactions, pain, prolonged redness, itching, swelling), as well as negative organoleptic properties of the drug were not found;

- no doping drugs and their metabolites were found in the preparation;

- the drug can be recommended in sports medicine.

The effectiveness of the claimed ointment as a vasodilator is confirmed by the following examples.

Example 1. Patient X, 60 years old.

Was in the therapeutic department of the City Clinical Hospital No. 70 in Moscow in the fall of 2005.

Diagnosis: chronic obstructive bronchitis in the acute stage. IHD: Atherosclerotic cardiosclerosis. Varicose veins of both limbs. Venous insufficiency of 2 stages.

Complaints: shortness of breath, dry wheezing, swelling of the feet of both limbs, trophic ulcer of the right thumb of the left foot, thumb of the left foot.

Objectively: a state of moderate severity. Dry, wheezing in the mediastinum. Hypersthenic. The lower legs are pasty, varicose nodes on both sides, more pronounced on the left lower leg. Feet are swollen, cyanotic. On the left foot of the thumb is a trophic ulcer, 0.5 × 1 cm in size.

Rheography of the lower extremities. Rheographic index (RI) is reduced - 0.5 cm, blood supply is reduced. Venous outflow is difficult.

Appointed: rubbing the claimed ointment five times a day in the feet and lower legs, under the control of the prothrombin index and rheography.

On the 5th day of treatment, edema of the feet subsided, cyanosis almost disappeared.

Rheogram of the lower extremities. RI increased to 1.0, Blood supply increased by 30%, venous outflow and vascular tone improved. Prothrombin 95%.

On the 15th day of treatment: the skin of the lower extremities is elastic, of normal color. Venous nodes were asleep. Prothrombin 85%. The ulcer was epithelized. On the rheogram: RI-2.0. The pulse wave increased to 2.5 cm.

Example 2. Patient Y, 52 years old.

He was in the seventh department of the Infectious Clinical Hospital No. 1 of Moscow in the fall of 2005.

Diagnosis: bronchial asthma, mild course (not hormone-dependent). Flu (N.F. +) mean course; He was admitted with complaints of weakness, fever up to 38 ° C, sweating, shortness of breath.

Anamnesis: Ill sharply in October 2005. The temperature rose to 38.2 ° C. It became difficult to breathe. It was treated symptomatically: breast collection, aminophylline 1 t. × 3 times a day. There were no improvements. He went to the clinic, was hospitalized in the hospital №1-7 det.

Fluoroscopy. Signs of pneumosclerosis: the roots are dilated; bronchial tree with a sign of obstruction. Blood test: HB-12.0, L-5.6, Er-5.02, p-8, s-60, e-2. ESR-8 mm / h.

At the first stage of treatment, along with the usual treatment regimen, ointment therapy of the claimed composition was added by rubbing it on the front surface of the chest 3 times a day and the back surface 2 times a day. On the 5th day of treatment, due to a significant improvement in respiratory functions, shortness of breath stopped, body temperature returned to 36.5 ° C, it was decided to continue treatment with the ointment of the claimed composition with the complete abolition of the previous drug therapy. Ointment treatment lasted 15 days.

X-ray of the chest after the procedures: the bronchopulmonary tree was almost completely structured, hemodynamics in the small circle returned to normal, signs of overload of the right atrium disappeared. Urinalysis from 10/29 without pathology.

The effectiveness of the claimed ointment as an anti-inflammatory agent is confirmed by the following.

Example 3. Patient Z, 28 years old.

He was in October 2005 in the second trauma unit of the Moscow Scientific and Practical Center for Sports Medicine.

He was admitted with complaints of pain in the right knee joint, his swelling, inability to move freely, pulling pains in the lumbar spine with radiation to the right lower limb.

Anamnesis: up to 25 years of age he was actively involved in sports - the backup team of Dynamo (Moscow). Repeatedly treated for various injuries of the lower extremities (ankle fracture of the left ankle joint in 2002). In October 2005, during an amateur game in a collision, he fell sharply on the right side of his body. It was treated independently: compresses, analgesics - without a pronounced effect.

Objectively: The right knee joint is swollen, painful on deep palpation. Movements in it are saved, but limited.

X-ray: crack of the lateral margin of the patella, accumulation of synovial fluid in the cavity of the joint bag

Ultrasound: tears of the material ligaments.

Diagnosis: traumatic arthritis of the right knee joint, lumbishialgia.

The department actively conducted course treatment with ointment of the claimed composition - three times a day, application of the joint zone and paravertebral departments, as well as electrophoresis with ointment of the claimed composition in the lumbar region and the right knee joint every other day. On the 2nd day of the therapy, the pain was significantly weakened, on the 4th day the swelling of the joint was gone. On the 10th day, a complete restoration of the motor activity of the joint.

X-ray after treatment: no visible changes in the patella.

Discharged with a good effect of the treatment.

Table 1 Name Number of patients Significant Improvement No change Worsening diseases improvement Rheumatoid Polyarthritis twenty 12 7 one - Rheumatic fifteen 8 6 one - polyarthritis Deforming twenty 5 13 2 - osteoarthrosis Neuralgia and fifteen 9 5 one - myositis Total: abs. 70 34 31 5 - % one hundred 48.6 44.3 7.1 -

table 2 Groups The initial state On the 20th day 5 days after taking Healthy athletes 100,2 99.1 100.3 The control 79.3 83.1 94.9 Experiment 75,4 119.1 102,4

Claims (1)

The ointment is analgesic, vasodilating, anti-inflammatory, containing bee venom extract - melittin, camphor, tincture of arnica, lavender, rosemary and eucalyptus oil, revitalin, carbopol, 30% sodium hydroxide solution, hydrophilic anion ointment, soya lecerin, preservative lecithin, soy lecithin distilled water and ethyl alcohol, in the following ratio of components, g per 100 g of product: Bee Venom Extract - Melittin (Apis mellifera toxin) 0.003 ÷ 0.010 Lavender oil (Aetheroleum lavandulae) 1,0 ÷ 5,0 Camphora (Camfora) 3.0 ÷ 5.0 Arnica Tincture (Tinctura arnicae) 2.0 ÷ 7.0 Rosemary oil (Aetheroleum rosmarinus) 1,0 ÷ 5,0 Eucalyptus oil (Aetheroleum eucalyptus) 1,0 ÷ 5,0 Revitalin (Revitalin) 1,0 ÷ 3,0 Carbopol (934 or 940 or 941) 0.99 ÷ 1.1 Sodium hydroxide solution 30% (Natrium hydroxid 30%) 0.99 ÷ 1.1 Hydrophilic anionic ointment (Natrium layrylsulfuricum, Alkoholum cetylstearilicum, Paraffinum liguidum, Vaselinum album) 19.9 ÷ 20.1 Soya Lecithin (Lecitinum) 0.2 ÷ 0.4 Glycerin (Glycerinum) 6.0 ÷ 10.0 Preserving solution (Methylparahydroxybenzoicum) 0.9 ÷ 1.1 Ethyl Alcohol (Alcoholum 96%) 1,2 ÷ 1,5 Distilled water (Agua destillata) Rest