Medicinal agent

FIELD: medicine, pharmacology, pharmacy.

SUBSTANCE: invention relates to a medicinal agent eliciting with the anti-tumor and immunomodulating effect. Agent comprises tetramethyl, pentamethyl or hexamethyl derivative of tri-p-aminotriphenylchloromethane or their mixture with dextrin. Agent elicits enhanced activity and reduced adverse effect.

EFFECT: valuable medicinal properties of agent.

13 cl, 1 tbl, 11 ex

 

The present invention relates to medicine, namely to anticancer medicinal drugs and drugs that affect the immune system.

Known drug “Adriamycin”, representing the antibiotic group anthracyclines and with pronounced anti-tumor activity (see, for example, Medmaravis. Medicinal product. - M.: Medicine, 1985, Vol.2, s-461).

The drug is used in the form of a solution of the hydrochloride strictly intravenously, as when injected under the skin solution possible tissue necrosis. In addition, the drug has a cardiotoxic effect, can cause pain in the heart, heart failure, low blood pressure.

The closest analogue is the prototype drug is the drug Cyclophosphamide, which are produced in the form of white crystalline powder, soluble in water (1:50), easily soluble in alcohol, it is difficult to isotonic sodium chloride solution (see, for example, Medmaravis. Medicinal product. - M.: Medicine, 1985, Vol.2, s-434).

This drug has a relatively broad antitumor spectrum, and is also an immunosuppressive agent, however, its use may experience side effects such as dizziness, nausea and vomiting, often some time after the beginning of the application of the Oia noted hair loss on the head.

The present invention solves the problem of finding drugs with a broad spectrum of effects without side effects.

Known related to diaminodiphenylmethane dyes, representing salt with colored organic cations (see, for example, concise encyclopedia of chemical. - M.: Soviet encyclopedia, 1967, volume 5, s-253), methyl violet dye is a mixture of methylated nitrogen tri-n-aminodiphenylamine (see, for example, Anniesland, Naassenes. Beginning organic chemistry. - M.: Chemistry, 1974, book 2, C), including Tetra-, Penta - and hexamethylene derivatives (see, for example, StainsFile “Methyl Violet 2B, 6B, 10B” http://members.pgonline.com/-bryand/StainsFile/dyes/42535.htm).

The structural formula of tri-n-aminodiphenylamine is:

where, for example, denoted by R1N(CH3)2, R3N, R3N, R4N(CH3)2, R5N, and R6(or NH2or N3or N(CH3)2.

When this Methyl Violet 2B (tetramethyl pararosaniline chloride) - tetramethylene derivative of tri-n-aminodiphenylamine (in the structural formula R6NH2and denote for R1, R2, R3, R4and R5with the Ute above, chemical formula C23H26N3Cl, mol. weight 379, 94) is soluble in water and alcohol, fine-grained crystalline brown powder with a greenish tint. Methyl Violet 6B (pentamethyl of pararosaniline chloride) - pentamethylene derivative of tri-n-aminodiphenylamine (in the structural formula R6NHCH3a notation for R1, R2, R3, R4and R5meet the above chemical formula - C24H28N3CL, mol. weight 393,97) - homogeneous soluble in water and alcohol fine crystalline powder with a greenish-bronze shade - also known as “Basic violet, methyl violet”, a Methyl Violet 10B (HEXAMETHYL of pararosaniline chloride) - hexamethylene derivative of tri-n-aminodiphenylamine (in the structural formula R6N(CH3)3and denote for R1, R2, R3, R4and R5meet the above chemical formula C25H30N3Cl, mol. weight 407,99) - green crystalline soluble in water and alcohol powder is known as Crystal violet (crystal violet), and “Basic violet 3 (see, for example, Harmful substances in industry. Handbook, part 1, Organic matter, GNTI chemical literature, ISD, L., 1963, SS-639, StainsFile “Methyl Volet 2B, 6B, 10B” http://members.pgonline.com/-bryand/StamsFile/dyes/42535.htm and chemist's Handbook. L: Chemistry, 1967, V.6, s). It should be stated that in some sources the above-mentioned derivatives of Methyl Violet are called “Gentian violet” (see, for example, the above StainsFile “Methyl Violet 2B, 6B, 10B” http://members.pgonline.com/-bryand/StainsFile/dyes/42535.htm).

Known dyes mixture of methyl violet with Magenta called “Dahlia purple” - green crystalline powder, soluble in water and alcohol, and a mixture of methyl violet with an equal amount of dextrin, called Gentian violet, which is a brilliant green water-soluble powder (see, for example, “Harmful substances in industry”, Handbook, part 1, “Organic matter”, GNTI chemical literature, ISD, L., 1963, s).

The main use of these dyes in the industry, for example for dyeing, but it is also known the use of Kristalliset (hexamethylene derivative of tri-n-aminodiphenylamine) in gynecology and Pediatrics for the treatment of candidiasis (see, for example, http://www.oncology.com).

Known dextrin, which is a mixture of polysaccharides and used in the manufacture of fabrics (see, for example, Ngling. General chemistry. M.: Chemistry, 1978, s).

The essence of the invention lies in the fact that the drug with immunomodulatory and against the tumor properties, characterized by the fact that it contains pharmacologically acceptable derivatives of tri-n-aminodiphenylamine having the structural formula:

where, for example, denoted by R1N(CH3)2, R2N, R3N, R4N(CH3)2, R5N, and R6or NH2or N3or N(CH3)2.

This medication contains three n-aminodiphenylamine or in the form of its tetramethylene derived, in the structural formula of which R6NH2or as it pentamethylene derived, in the structural formula of which R6N3or as it hexamethylene derived, in the structural formula of which R6N(CH3)2and for the mentioned derivatives of designation for R1, R2, R3, R4and R5meet the above.

In addition, the drug contains three n-aminodiphenylamine or as a mixture of its tetramethylene and pentamethylene derived using the ratio of components,% vol.: tetramethylene derived 2,0-98,0; pentamethylene derivative - else, or a mixture of its tetramethylene and hexamethylene derivatives, when the ratio of the leaves, vol.%: tetramethylene derived 2,0-98,0; hexamethylene derivative - else, or a mixture of its pentamethylene and hexamethylene derivatives, with a ratio of components,% vol.: pentamethylene derived 2,0-98,0; hexamethylene derivative - else, or a mixture of its tetramethylene, pentamethylene and hexamethylene derivatives, with a ratio of components,% vol.: tetramethylene derivative of 1,5-97,0; pentamethylene derivative of 1,5-97,0; hexamethylene derivative - rest.

The essence of the invention lies in the fact that the drug with immunomodulatory and antitumor properties, characterized by the fact that it contains a mixture of dextrin and pharmacologically acceptable derivatives of tri-n-aminodiphenylamine in the form of, for example, or tetramethylene, or pentamethylene, or hexamethylene derivatives, or mixtures tetramethylene and pentamethylene derivatives, or mixtures tetramethylene and hexamethylene derivatives, or mixtures pentamethylene and hexamethylene derivatives, or mixtures tetramethylene, pentamethylene and hexamethylene derivatives, with a ratio of components,% vol.: the corresponding derivative or a corresponding mixture of the corresponding derivatives of tri-n-aminodiphenylamine 10,0-95,5; dextrin - rest.

The mixture tetramethylene and pentamethylene derivatives of tri-n-aminodiphenylamine selected when the ratio of the components (for the mixture), vol.%: tetramethylene derived 2,0-98,0; pentamethylene derivative - rest, a mixture of tetramethylene and hexamethylene derivatives of tri-n-aminodiphenylamine selected when the ratio of the components (for the mixture), vol.%: tetramethylene derived 2,0-98,0; hexamethylene derivative - rest, a mixture of pentamethylene and hexamethylene derivatives of tri-n-aminodiphenylamine selected when the ratio of the components (for the mixture), vol.%: pentamethylene derived 2,0-98,0; hexamethylene derivative - else, and the mixture tetramethylene, pentamethylene and hexamethylene derivatives of tri-n-aminodiphenylamine selected when the ratio of the components (for the mixture), vol.%: tetramethylene derivative of 1,5-97,0; pentamethylene derivative of 1,5-97,0; hexamethylene derivative - rest.

Drugs, containing pharmacologically acceptable derivatives of tri-n-aminodiphenylamine, as well as a mixture of dextrin and these derivatives have antitumor activity, which is accompanied, for example, established by the author dissymmetries therapeutic effect, which is manifested in the difference between the temperature measured at different points of the body, for example, at 2-3° after 0.5-2 hours after taking this drug and duration of 3-4 hours (see, for example, Mevcuttur. The cancer. Healed the e possible. C.-P.: Neva, 2003), and also have anabolic activity, stimulate cellular and humoral defense factors of the organism.

The mechanism of action medicines containing pharmacologically acceptable derivatives of tri-n-aminodiphenylamine, based on the ability of their ions by interacting with phospholipids of the cell membrane to disrupt the balance of transmembrane ion potential, leading to cell death. Conducted by the author studies have also shown that the drug is an inhibitor of enzymes of the mitochondria of malignant cells and cause the death of the mitochondria of cancer cells, for example, due to suppression of NADPH-cytochrome C-reductase activity, which leads to a blockage of energy (see, for example, Shumyantseva V.V., Uvarov V.Yu., Byakova O.E., Archakov, A.I. Biochem. Molec. Biol. Intern., 1996, No. 38, p.p.829-838). It was found that the effectiveness of drugs is higher, the greater the shift of its absorption spectrum towards the UV range. In addition, it was found that the inclusion in the appropriate preparation of dextrin significantly reduces the toxicity of the relevant medicinal product and, accordingly, extends the range of dosage of his admission.

This is confirmed by laboratory studies and examinations of patients by conducting a blood test to check immunol the environmental performance of their (patients) leukocyte and lymphocyte systems.

Derivatives of tri-n-aminodiphenylamine in the form of their mixture, followed by separation tetramethylene, pentamethylene and hexamethylene derivatives obtained by methylation of parafuchsin iodide stands (see, for example, Anniesland, Naassenes. Beginning organic chemistry. - M.: Chemistry, 1974, book 2, C), and pentamethylene derivative (basic violet K) can also be obtained by oxidation of dimethylaniline in the presence of copper salts (see, for example, Harmful substances in industry. Handbook, part 1, Organic matter, GNTI chemical literature, ISD, L., 1963, s), and hexamethylene derivative (crystal violet) in its pure form is obtained by condensation of di-(n-dimethylamino)-benzophenone (michler ketone) with dimethylaniline and subsequent acidification (see, for example, Anniesland, Naassenes. Beginning organic chemistry. - M.: Chemistry, 1974, book 2, s).

Target product in a form suitable for use drugs get through the corresponding cleaning compositions obtained by, for example, recrystallization, and also by means of adsorption chromatography was carried out by passing in the appropriate chromatographic column of aqueous solutions of these salts through the layer of sorbent, for example through or cellulose for chromatography, or bentonite clay.

Dextrinated by heating dry starch to (200-250)° (See, for example, Ngling. General chemistry. - M.: Chemistry, 1978, s).

The desired mixture is obtained by selecting the appropriate components in predetermined proportions.

Made as appropriate or technical salt or chemically pure or purity, or drug chemically pure, or drug purity medicinal product in accordance with pharmacopoeial requirements for medicines (see, for example, the Federal law of the Russian Federation dated 22.06.98, No. 86-FZ “On drugs”, as well as Industry standard OST 91500.05.001-00 “standards for the quality of medicines. General provisions”, published in “Rossiyskaya Gazeta” on 28.11.2001 year) can be administered to the patient, taking into account the purity of the preparation of intravenous isotonic sodium chloride solution, orally in capsules, and is also used in topical compositions, in the form of medicinal enemas or in the form of candles, and its use in these cases does not cause allergic reactions and other side effects, and efficacy in the treatment of relevant diseases) in some cases higher than, for example, a drug, selected as a prototype.

The results of studies of the mechanism of action proposed medicinal product described in examples 1-3, and the possibility of its primeneniya treatment is confirmed by the examples 4-11.

Example 1.

In test tubes (14 tubes of 10 ml each) of the first group with a culture of human melanoma And 375 (human malignant melanoma) in a buffer solution introduced the drug in breeding 10'7mmol/l, respectively in the form of Methyl Violet 2B (tetramethylene derivative of tri-n-aminodiphenylamine), Methyl Violet 6B (pentamethylene derivative of tri-n-aminodiphenylamine), Methyl Violet 10B (hexamethylene derivative of tri-n-aminodiphenylamine), mixtures (equal to the ratio of the components) Methyl Violet 2B, and Methyl Violet 6B, Methyl Violet 2B, and Methyl Violet 10B, Methyl Violet 6B and Methyl Violet 10B, Methyl Violet 2B, Methyl Violet 6B and Methyl Violet 10B, mixtures of dextrin and of these salts, mixtures of dextrin and these mixtures of these salt (in a ratio of components,% vol.: dextrin - 50, a corresponding salt or a mixture (in the above ratio) salt - rest). This is duplicated (14 tubes of 10 ml each) for the medicinal product in dilution 10-9mmol/l

In tubes of the second group are placed in them by fibroblasts HFF (human forskm fibroblast) introduced the drug in the same ways and in the same dilution.

In addition, there was formed a third (control) group of tubes (6 tubes) with the same pool of cancer cells and fibroblasts, which are introduced in the same dilution respectively the drugs adriamycin and cyclophosphamide, as well as relevant PR the tag, entered saline.

After a temperature above tubes for weeks at a temperature of 37° (in the dark) the analysis of the contents of these tubes.

Examination of the results showed:

In the experimental group with drug in test tubes with dilution 10-7mmol/l the presence of drugs inhibits the proliferation of melanoma cells compared with the result of the proliferation of such cells in vitro with physiological solution (86-93)%, and the proliferation of fibroblasts, respectively (25-27)%, and the picture is almost the same for all variants used medicines.

In the tubes of the control group with drug adriamycin marked decrease in the proliferation of melanoma cells by 42%, with the drug cyclophosphamide, respectively, a decrease of proliferation of melanoma cells by 55%.

In the experimental group with drug in test tubes with dilution 10-9mmol/l the presence of drugs inhibits the proliferation of melanoma cells compared with the result of the proliferation of such cells in vitro with physiological solution (75-90)%, and the proliferation of fibroblasts, respectively (5-10)%, while in test tubes in the control group with drug adriamycin marked decrease in proliferation of the notches melanoma by 30% with the drug cyclophosphamide, respectively, a decrease of proliferation of melanoma cells by 35%.

The data obtained indicate that the proposed drug even at extremely high dilutions has a pronounced antitumor effect and a higher activity than the known anticancer drugs, but it has a weak cytotoxic effect to fireblasts.

Example 2.

In tubes (50 tubes 10 ml) of the experimental group with the “smooth” by microsomes of cancer cells MCF-7 (breast adenocarcinoma) in buffer solution introduced drug dilution 10-5mmol/l, respectively in the form of mixtures of Methyl Violet 2B (tetramethylene derivative of tri-n-aminodiphenylamine) and Methyl Violet 6B (pentamethylene derivative of tri-n-aminodiphenylamine) in two versions ratio of components,%:

1. Methyl Violet 2B - 98,0; Methyl Violet 6B - rest and 2. Methyl Violet 6B - 98,0; Methyl Violet 2B - rest; Methyl Violet 2B and Methyl Violet 10B (hexamethylene derivative of tri-n-aminodiphenylamine) in two versions ratio of components,% vol.: 1. Methyl Violet 2B - 98, rest; Methyl Violet 6B and Methyl Violet 10B also in two versions ratio of components,% vol.: 1. Methyl Violet 6B - 98,0; Methyl Violet 10B - rest and 2. Methyl Violet 10B - 98,0; Methyl Violet 6B - rest, a mixture of Methyl Violet 2B, Methyl Violet 6B and Methyl Violet 10B in four variations is tah components, vol.%: 1. Methyl Violet 2B - 2,0; Methyl Violet 6B - 50,0 and Methyl Violet 10B - rest; 2. Methyl Violet 2B - 50,0; Methyl Violet 6B - 2.0 and Methyl Violet 10B - rest; 3. Methyl Violet 6B - 50,0; Methyl Violet 10B - 2.0 and Methyl Violet 2B - rest; 4. Methyl Violet 2B - 20,0; Methyl Violet 6B - 25,0 and Methyl Violet 10B - rest; and mixtures of dextrin and of these salts, and these mixtures of these salts (in variants of the above ratio of the components in the ratio.%: dextrin - 10,0; 25,0; 75,0; 90,0; the corresponding salt or mixture of salts - the rest). This is duplicated for medicines in dilution 10-9mmol/l

In test tubes (10 ml) of the second group are placed in them by liver microsomes rat entered the drug in the same ways and in the same dilution.

In addition, there was formed a third (control) group of tubes with microsomes same pools of cancer cells and rat liver, which are introduced in the same dilution respectively the drugs adriamycin and cyclophosphamide, as well as the corresponding tubes that have a physiological solution.

In the tubes of the groups defined concentration of cytochrome C, which is 50 µm for cancer microsomes, and 20 µm for microsomes from rat liver.

After a temperature above the tubes for 20 min at a temperature of 25° (in the dark) the analysis of the contents of the test tubes.

Consideration of the results obtained pok is coming:

In vitro experimental group concentration of cytochrome C for tubes entered the medicinal product in the form of mixtures of salts of the specified concentration is determined within the range of 60 μm, and for tubes with the entered medicine in the form of mixtures of salts and dextrin specified concentration determined within 65 microns.

In test tubes with adriamycin and cyclophosphamide concentration of cytochrome-C, respectively 40-45 μm. In the test tube with saline significant changes in the concentration of cytochrome C is not marked. In liver microsomes of rats proposed remedies have not had any effect, the concentration of cytochrome C in all test tubes remained in the range of 19-20 mm.

The results suggest that the proposed drug contributes to the release of the membranes of the mitochondria of cancer cells “aggressive” protein cytochrome C, which, starting the mechanism of destruction of DNA by caspase causes apoptosis of these cells (see, for example, V.E. Wilson, A. Mochon, Boxer L.M. Induction ofbcl-2 expression by phosphorylated CREB proteins during B-cell activation and rescue from apoptosis. Mol. CeU. Biol., 1996, v.16, p.p.5546-5556).

Example 3.

In mice breed-57 audited reactions of the body of the animal by the administration of a medicinal product in the form of salts, Methyl Violet 2B, Methyl Violet 6B and Methyl Violet 10B, as well as mixtures of these salts with dextrin in two versions ratios suitable the salt and dextrin, vol.%: 1. dextrin - 5,0; the corresponding salt of rest and 2. dextrin - 95,0; the corresponding salt of the rest.

Experimental group consisted of 60 mice and was divided into 6 sub-groups of 10 mice in each test group contained 10 mice, with subgroups of the experimental group and control group, respectively isolated from each other, and mouse each subgroup were numbered respectively from 1 to 10 by applying the respective rooms dye composition, in this case the brilliant greens.

Experimental group of mice within 10 days received the drug, respectively, 1-I subgroup in the form of a mixture of Methyl Violet 2B with dextrin in the ratio of components,% vol.: dextrin - 2,0; Methyl Violet 2B - rest, 2-I subgroup in the form of dextrin - 90,0; Methyl Violet 2B - rest, 3-I subgroup in the form of dextrin - 5,0; Methyl Violet 6B - rest, 4-th subgroup in the form of dextrin - 90,0; Methyl Violet 6B - rest, 5-th subgroup in the form of dextrin - 5,0; Methyl Violet 10B - else, and 6th subgroup in the form of dextrin - 90,0; Methyl Violet 10B - rest, and in each subgroup mouse numbered 1-8 received the appropriate medication in the drinking water (in aqueous solution), and mouse numbers 9-10 - injection into the peritoneum. In each subgroup mouse numbers 1-2 received the appropriate drug dose of 2 mg, mouse, numbers 3-4 received the drug at a dose of 5 mg, the mouse under room is mi 5-6 received the drug at a dose of 10 mg, mouse numbers 7-8 received the drug at a dose of 20 mg and mice at 9-10 injection of the corresponding preparation was carried out in a dose of 15 mg per 1 ml of water for injection.

Mice of the control group of the drug is not received.

Results: one week after starting drug differences in the behavior of animals even subgroups of the experimental group and control groups was not observed. Animals under the numbers 5-6 odd subgroups of the experimental group sedentary, animals, numbers 7-8 odd subgroups of the experimental group were killed.

Mouse with odd numbers in all subgroups scored on day 10, with even numbers on day 21.

Traces the introduction of appropriate drugs detected in kidneys of mice with rooms for 3-6 odd subgroups of the experimental group, mice even subgroups traces the introduction of drug detected in mice with numbers 5-8.

When histology minimal impact medicines discovered during the introduction of the mixture containing Methyl Violet 10B (provisional title OF), the highest for a mixture containing Methyl Violet 2B.

Hence, taking into account the weight ratios can be assumed that the human body is a reasonable dosage of up to 2.0 g single receiving this drug. However, more accurate data can be obtained only when the performance of the relevant studies.

Example 4.

Mice breed-57 experimental and control groups (60 animals in each) vaccinated melanoma - 16.

In the experimental group formed 6 groups control group, three groups of 10 mice in each subgroup.

Mouse each subgroup of the experimental group in the form of a drink in a dose of 5 mg received the drug in the form of aqueous solutions of Methyl Violet 2B, Methyl Violet 6B and Methyl Violet 10B, as well as mixtures of these salts with dextrin in the ratio of the corresponding salt and dextrin, vol.%: 25:75, respectively.

Mouse 1-St and 2-nd subgroups of the control group in the form of drinking received aqueous solutions respectively of adriamycin and cyclophosphamide in single doses of 5 mg of the drug, mouse 3rd subgroups of the control group of drugs was not received.

Results: Of the 60 mice of the experimental group on day 36 of the experiment survived 39. With 11 mice (4 out 1 in 3 of the 2-nd and 3-th subgroup and 1 of 4 subgroups) died on day 19, 5 mice (2 from 1st and 2nd subgroups and 1 of the 3 subgroups) on day 23 and 5 mice (2 of the 1st sub-group and 1 from the 2, 4 and 5 subgroups) on the 34th day after the start of the experiment. Tumors, 17 (1 of the 1st, 3 2nd, 1 3rd, 4 of the 4-th and 5-th subgroup, and 3 of the 6 subgroups) surviving mice of approximately 0,2× 0.2 mm, the remaining mice tumor visually was not determined. Surviving mice were killed at day 36 of the experiment. At autopsy from 9 mice (1 of 1, 4 of the 4th and 2 from the 5-th and 6-podgroup) detected a single metastasis in the lungs, from 4 mice of these 9 (1 of 1 2 of 4 and 1 of 5 subgroups) also metastases in the liver. The rest of metastases not detected, the internal organs without visible changes.

Mouse 1-St and 2-nd subgroups of the control group. Up to 36 days from the start of the experiment survived 2 mouse 1 and 5 mice 2 subgroups. Tumors in average 1.5× 1.5 cm At the opening marked the lungs and liver.

Mouse 3-th subgroup of the control group died, all on 10-12-20-25 day. When viewed from a bleeding tumor on the back, on average 2.5× 2,0 see histology total lysis of the lungs.

Conclusions: the Drug has anti-tumor activity, does not cause side effects.

Example 5.

Dog, 3 years old, weight 16 kg

Diagnosis: non-Hodgkin's lymphoma.

The condition of the dog is severe, shortness of breath, cachexia. Neck tumor - right 7× 5 cm, left 11× 10 see

On the radiograph from 20.10.99, multiple granulomas education in the mediastinum.

Treatment drug started 30.10.99,

Intravenous drip introduced 500 mg Methyl Violet 2 In 500 ml of physiological solution. After 3 days of intravenous administration of a mixture of Methyl Violet 2 b and Methyl Violet 6 (250 mg each) in 500 ml of physiological solution, and admission (per os) no 2 times a day with food in the powder mixture of dextrin and Methyl Violet 2 B, Methyl Violet 6 b and Methyl Violet 10B (one dose of 200 mg 50 mg each pillar is of soup).

After a week of repeated on/in the introduction of a mixture of Methyl Violet 2 b and Methyl Violet 6 B, the reception of the above mixture (dextrin) per os continued.

Two weeks after the start of treatment, marked improvement in General condition, biochemical and clinical indices of blood.

After 3 weeks, the visible tumor has decreased by about 2.5 times.

Treatments/with the introduction of a mixture of Methyl Violet 2 b and Methyl Violet 6 was conducted weekly for 3 months, the reception of the above mixture (dextrin) per os reduced to one a day.

During the examination after the treatment status of the animal is good, weight 19,5 kg, tumors on the neck are not defined. Blood tests without pathology.

On the radiograph from 02.02.2000 a few small metastases in the lungs.

Example 6.

Dog, 6 years old, weight 21 kg

The diagnosis of Sarcoma of the right forearm, metastases in the lungs. On the radiograph from 10.07.2002, the destruction of the periosteum and 1-7 ribs on the right, multiple metastases in both lungs, tumor 10× 15× 12 see

Treatment is begun 12.07.2002 g Intravenously every other day for 2 ml diluted in 250 ml of 0.9% solution of NaCl in water 50 mg Methyl Violet 10B (callout OF). Daily for tumor superimposed ointment bandages (2% Methyl Violet 10B, a children's cream - the rest).

3 weeks after start of treatment, the tumor - 7× 7× 3 cm, in a stable condition after another 2 weeks the condition of the animal is about to be satisfactory, on the radiograph kapsulirovannaja tumor 2× to 2.5× 1 cm, ribs and lungs signs of metastases.

Example 7.

Patient I., aged 35.

Asked in November of 2002.

In 2001 conducted by the extirpation of the uterus and appendages in accordance with the detected cancer in her right ovary. Computer tomogram from 28.08.02 recurrence of the tumor 8,6× 9,8× 14 cm with invasion into the bladder and the rectum.

The treatment of the enema into the rectum according to the scheme: during the first five days for the 1st time each day, then after 5 treatments a day, and then 15 enemas 1 time in 3 days. Single dose -20 mg of this drug (OF), pre-dissolved in 2 ml of 70(ethyl alcohol, 15-20 ml of water.

Two weeks after the start of treatment based on ultrasound - tumor 3,8× 4,2× 3,1 cm with smooth contours, swelling from the rectal stepped away from the wall, the deformation of the bladder wall is negligible.

After the treatment by ultrasound tumor 1,3× 2,0× 1.6 cm, kapaligiran, the walls of the capsules of 0.5, see no Complaints.

It was recommended to continue treatment with breaks between courses (1.0 to 1.5) months.

In the control ultrasound from 02.03.2004, the tumor is not defined.

Blood tests before starting treatment: Leukocytes to 10 thousand, erythrocytes - 2.5 million, platelet - 110 thousand units.

Blood tests after the end the of treatment: Leukocytes 9 thousand, erythrocytes - 5.5 million, platelet - 300 thousand units.

Example 8.

Patient R., 62.

Diagnosis: Papillary cancer of the thyroid gland.

Turning: the ultrasound showed a tumor in the right lobe 5× 3× 1,7 see

The treatment drug (OFF) for 2 weeks: 2 times a day after meals orally 1 capsule with a shell made of gelatin containing 20 mg of the drug, and daily enema dose to 100 ml of solution containing 50 mg of the powder of the drug dissolved in 2 ml of 70(ethanol, and then dissolved in 100 ml of an aqueous solution of 0.9% NaCl.

During the first 7 days of treatment in a patient after 3 hours after administration of the drug was noted dissymmetrically effect, which was reflected by a sharp chills and over (1.0 to 1.5) hours temperature difference between the right and left halves of the body, respectively (35,4-36,9)° and (37,3-38,6)° . Upon further reception of a preparation the above mentioned differences in temperature has practically disappeared.

After the course on ultrasound primary tumor and metastases are not detected.

At follow-up at two months, the condition is satisfactory, no complaints.

Example 9.

Patient S, 18 years.

In September 2002 a tumor (2× to 2.5× 2) cm3the right breast.

Mammography: fibrous keys the religious breast, right breast.

Biopsy: found atypical cells.

Scheduled lubrication 2-3 times a day area of location of the tumor ointment composition comprising a drug (OF) powder and ointment base (baby oil) in the ratio of components,%: 10% - of the medicinal product and 90% of baby cream.

After 1.5 months of re-treatment biopsy: atypical cells are not detected, the tumor almost no palpable.

Example 10.

Patient Y., 48 years old.

Diagnosis: Adenocarcinoma rectum with metastases in the liver.

In April 1999 was colonectomy removing colostomy. Conducted preventive chemotherapy, because of the inefficiency of which (the appearance of pain in the abdomen, recurrent vomiting, General weakness) in August 2002 and asked for help.

Admission: CT from 21.09.2002 in the area of the splenic angle is defined granulomas education 7,0× 5.5 cm with irregular contours, as well as metastasis in the right lobe of the liver.

The treatment is oral for 10 days dissolved in 100 ml of water the mixture of dextrin and Methyl Violet 2 B, Methyl Violet 6 b and Methyl Violet 10 (in the ratio of components,% vol.: dextrin - 25,0; Methyl Violet 2 B-30,0; Methyl Violet 6 B - 30,0; Methyl Violet 10 (OF) - 15.0) to 1.0 g 2 times a day 30 minutes before meals, as well as in colostomy morning and evening, 0.5 g of the drug OF dissolved in 50 ml of water. In addition, to stand the decision of the effectiveness of treatment and with the consent of the patient is assigned weekly on/in the introduction of 500 ml of 1% solution of the drug OF. The treatment lasted 3 months.

After the treatment the patient was in good condition on CT, the tumor in the abdominal cavity and liver metastases are not detected, the main indicators of blood on the results of clinical and biochemical tests are normal.

Example 11.

Patient P. 25 years.

Turned 23.07.1999, with complaints total alopecia - loss of hair on the whole body, periodic weakness and depression.

The hair loss started after the flue, 6 years ago with lashes and brows, and then six months later appeared foci of alopecia on the scalp.

Within 2 years were treated with hormones, as well as local topical treatment.

From history we found out that at the age of 7 years was ill with ARI and the week after chickenpox, that, apparently, was the beginning of the latent flowed autoimmune diseases.

Diagnosis: Autoimmune disease, complicated by total alopecia. The diagnosis is confirmed by blood tests on cellular and humoral immunity.

Conducted two courses of treatment with medicines. The first course within 3 months of receiving a mixture of dextrin with Methyl Violet 2B, Methyl Violet 6B and Methyl Violet 10B in the ratio of dextrin and the corresponding salt, .%: 25:25:25:25 according to the scheme: 0.2 ml of 1% aqueous solution, 2 times a day for 30 minutes before eating.

After 3 weeks the item is after the beginning of treatment there were nagging pains in the projection of the kidneys. This was interpreted by us as the response of the adrenal glands to suppress drug fixed hyperactive macrophages.

CT of the abdominal cavity, kidneys and adrenal glands showed that the right and left adrenal somewhat enlarged and deformed.

The treatment was continued, and after a week of pain in the projection of the kidneys disappeared.

2 months after the start of treatment appeared vellus hair on the head and legs.

After the first course of treatment was made a two-month break, and then within 2 months conducted an additional course, included the reception Methyl Violet 10B (AF) scheme 0.5 ml of 1% aqueous solution, 2 times a day for 30 minutes before eating.

One year after treatment, the hair on the head has reached normal thickness and structure. Nowadays hair loss is not.

On control CT scan from 12.03.2003, the adrenal glands are not enlarged, triangular in shape. Blood tests are normal.

The results of the study of cellular and humoral immunity are shown in table:

Table
 Before the treatmentafter 4 weeksafter 6 months
Immunoglobulin a60170249
Immunoglobulin M5098 190
Immunoglobulin G80014001750
T-lymphocytes %34,065,074,0
B-lymphocytes %10,014,016,0
Phagocytosis of latex %43,060,067,3
TNFthe 15.623,032.5
T-helper %26,030,038,0
T-suppressors %to 12.018,0of 17.0
T-killers %16,019,019,0

1. Drug with antitumor and immunomodulatory effects, characterized in that it contains pharmacologically acceptable derivatives of tri-n-aminodiphenylamine having the structural formula

where, for example, denoted by R1N(CH3)2, R2N, R3N, R4N(CH3)2, R5N, and R6or NH2or NHCH3or N(CH3)2.

2. The drug according to claim 1, characterized in that it contains three n-aminodiphenylamine in the form of those who retiling derivative, in the structural formula of which R6NH2and denote for R1, R2, R3, R4and R5meet the above.

3. The drug according to claim 1, characterized in that it contains three n-aminodiphenylamine in the form of its pentamethylene derived, in the structural formula of which R6N3and denote for R1, R2, R3, R4and R5meet the above.

4. The drug according to claim 1, characterized in that it contains three n-aminodiphenylamine in the form of its hexamethylene derived, in the structural formula of which R6N(CH3)2and denote for R1, R2, R3, R4and R5meet the above.

5. Medicinal product according to claims 1 to 3, characterized in that it contains three n-aminodiphenylamine in the form of a mixture of his tetramethylene and pentamethylene derivatives with a ratio,%: tetramethylene derivative - 2-98; pentamethylene derivative - rest.

6. Medicinal product according to claims 1 to 3, characterized in that it contains three n-aminodiphenylamine in the form of a mixture of his tetramethylene and hexamethylene derivatives with a ratio,%: tetramethylene derivative - 2-98; hexamethylene derivative else is.

7. Medicinal product according to claims 1, 3 and 4, characterized in that it contains three n-aminodiphenylamine in the form of a mixture of his pentamethylene and hexamethylene derivatives with a ratio,%: pentamethylene derivative - 2-98; hexamethylene derivative - rest.

8. Medicinal product according to claims 1 to 4, characterized in that it contains three n-aminodiphenylamine in the form of a mixture of his tetramethylene, pentamethylene and hexamethylene derivatives with a ratio,%: tetramethylene derivative - 2-98; pentamethylene derivative - 2-98; hexamethylene derivative - rest.

9. Drug with antitumor and immunomodulatory effects, characterized in that it contains a mixture of dextrin and pharmacologically acceptable derivatives of tri-n-aminodiphenylamine in the form of, for example, or tetramethylene, or pentamethylene, or hexamethylene derivative, or mixture tetramethylene and pentamethylene derivatives, or mixtures tetramethylene and hexamethylene derivatives, or mixtures pentamethylene and hexamethylene derivatives, or mixtures tetramethylene, pentamethylene and hexamethylene derivatives with a ratio,%: the corresponding derivative or a corresponding mixture of the corresponding derivatives of tri-n-aminodiphenylamine - 10-95; dextrin - about the Talne.

10. The drug according to claim 9, characterized in that the mixture tetramethylene and pentamethylene derivatives of tri-n-aminodiphenylamine selected with a ratio,%: tetramethylene derivative - 2-98; pentamethylene derivative - rest.

11. The drug according to claim 9, characterized in that the mixture tetramethylene and hexamethylene derivatives of tri-n-aminodiphenylamine selected with a ratio,%: tetramethylene derivative - 2-98; hexamethylene derivative - rest.

12. The drug according to claim 9, characterized in that the mixture pentamethylene and hexamethylene derivatives of tri-n-aminodiphenylamine selected with a ratio,%: pentamethylene derivative - 2-98; hexamethylene derivative - rest.

13. The drug according to claim 9, characterized in that the mixture tetramethylene, pentamethylene and hexamethylene derivatives of tri-n-aminodiphenylamine selected with a ratio,%: tetramethylene derivative - 2-98; pentamethylene derivative - 2-98; hexamethylene derivative - rest.



 

Same patents:

FIELD: organic chemistry, medicine, oncology, pharmacy.

SUBSTANCE: invention relates to new stable crystalline forms of derivative of pyrimidine nucleoside of the formula (I) eliciting the excellent anti-tumor activity. Also, invention relates to pharmaceutical composition eliciting an anti-tumor effect, applying crystalline form for preparing medicinal agent and to a method for prophylaxis or treatment of tumor diseases.

EFFECT: improved method for prophylaxis and treatment, valuable medicinal properties of derivative.

10 cl, 2 tbl, 4 dwg, 9 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to new compound of the formula (I) or its pharmaceutically acceptable salt or solvate wherein X represents CH or nitrogen atom (N); Z represents CH; R1 represents hydrogen atom; R2 and R3 can be similar or different and represent (C1-C6)-alkoxy-group that is optionally substituted with halogen atom, hydroxyl, (C1-C4)-alkoxycarbonyl, amino-group wherein one or two hydrogen atom are optionally replaced for (C1-C4)-alkyl that is optionally substituted with hydroxyl or (C1-C4)-alkoxy-group, the group R12R13N-C(=O)-O- wherein R12 and R13 can be similar or different and represent hydrogen atom or (C1-C4)-alkyl substituted optionally with (C1-C4)-alkoxy-group or the group R14-(S)m- wherein R14 represents phenyl or saturated or unsaturated 5-7-membered heterocyclic group substituted optionally with (C1-C4)-alkyl; m = 0 or 1; R4 represents hydrogen atom; R5, R6, R7 and R8 can be similar or different and represent hydrogen atom, halogen atom, (C1-C4)-alkyl, (C1-C4)-alkoxy-group or nitro-group under condition that R5, R6, R7 and R don't represent hydrogen atom simultaneously; R9 represents hydrogen atom, (C1-C6)-alkyl or (C1-C4)-alkylcarbonyl wherein alkyl fragment of indicated (C1-C6)-alkyl or (C1-C4)-alkylcarbonyl is optionally substituted with (C1-C4)-alkoxy-group; R10 represents hydrogen atom or (C1-C6)-alkyl; R11 represents (C1-C6)-alkyl, (C2-C6)-alkenyl or (C2-C6)-alkynyl (wherein each (C1-C6)-alkyl, (C2-C6)-alkenyl and (C2-C6)-alkynyl is substituted optionally with halogen atom or (C1-C6)-alkoxy-group), or R15-(CH2)n- wherein n is a whole number from 0 to 3; R15 represents naphthyl or 6-membered saturated or unsaturated carbocyclic or saturated or unsaturated 5-7-membered heterocyclic group that are substituted optionally with halogen atom, (C1-C6)-alkyl or (C1-C6)-alkoxy-group. Also, invention relates to variants of compounds of the formula (I). Compounds elicit antitumor activity and don't effect on cytomorphosis. Also, invention relates to pharmaceutical composition based on above described compounds, to a method for treatment of such diseases as malignant tumor, diabetic retinopathy, chronic rheumatism, psoriasis, atherosclerosis, Kaposi's sarcoma, and to a method for inhibition of vascular vessels angiogenesis.

EFFECT: valuable medicinal properties of compounds and composition.

22 cl, 4 tbl, 186 ex

FIELD: medicine, biochemistry.

SUBSTANCE: invention relates to a method for treatment of pathology or disorder taken among inflammatory diseases. Method involves using the simultaneous, separating or distributed by time at least a single substance inhibiting activity of NO-synthase and at least a single substance inhibiting activity of phospholipase A2. Also, invention relates to the composition comprising at least a single substance inhibiting activity of NO-synthase and at least a single substance inhibiting activity of phospholipase A2 for using in the method for treatment of pathology or disorder taken among inflammatory diseases.

EFFECT: improved method for treatment.

21 cl, 4 ex

FIELD: medical engineering.

SUBSTANCE: method involves exposing an intraocular neoplasm after vitrectomy and retinotomy, smoothening retina with perfluororganic compound later substituted with silicon oil. After having removed the neoplasm, intravenous 10% Perfluorane emulsion transfusion is carried out at a rate of 60 drops per 1 min in the amount of 80-100 ml. Next to it, photosensitizer is intravenously drop-by-drop introduced into cubital vein of the same arm. Laser irradiation of blood is carried out with power of 20-50 mW through laser light guide set in advance into cubital vein of the other arm in 5-15 min after starting introducing Perfluorane. When applying 0.1-1% water solution of Khlorine as photosensitizer at a dose of 0.2-0.5 mg/kg, irradiation is carried out at wavelength of 630-633 nm during 10-45 min. The treatment is administered twice with 5 days long pause.

EFFECT: enhanced effectiveness of treatment; reduced risk of tumor cells dissemination and metastases formation.

3 cl

FIELD: medicine, oncology, chemical-pharmaceutical industry and technology, pharmacy.

SUBSTANCE: tablet with antitumor effect contains acceptable carrier on which the following mixture of aqueous-alcoholic tinctures is applied: bloody geranium, penny-cress, common cocklebur and European wild ginger. Tablets by mass 1 g including slipping substance contains the following amounts of indicated tinctures as measure for dry matters, g: bloody geranium, 0.015-0.020; penny-cress, 0.011-0.015; common cocklebur, 0.011-0.017, and European wild ginger, 0.024-0.036. Method for preparing tablet involves applying on carrier the mixture of aqueous-alcoholic tinctures of above indicated plants, the following drying the prepared mass, its granulating and tableting. Method for prophylaxis and treatment of oncological patients involves prescription 0.5-2 tablets with oncological designation, tree times per a day and the treatment course is determined individually based on objective data of treatment. Tablet made by claimed methods shows complex properties: it delays tumor growth and metastazing and can be recommended for treatment and prophylaxis of oncological pathology both independently and in combination with chemo-radiation therapy. Invention can be used in technology for making medicinal formulations of preparations with oncological designation and for treatment of patients with oncological pathology of different organs and body systems.

EFFECT: improved for making tablet, valuable medicinal properties of tablet.

7 cl, 4 ex

FIELD: medicine, oncology, chemical-pharmaceutical technology, pharmacology, pharmacy.

SUBSTANCE: tablet eliciting the antitumor effect comprises active dose of aconite alkaloids in the amount 0.0125-0.0375 mg. Invention relates to a method for making tablet with antitumor effect. Method involves treatment suitable carrier taken in the amount corresponding to the content of alkaloids in tablet 0.0125-0.0375 mg with aconite tincture wherein amount of the total content of alkaloids is determined preliminary. Then carrier treated by such manner is dried at temperature 30-35°C, not above, granulated, granules are powdered and tableted. Also, invention relates to a method for treatment of oncological patients that involves prescription to patient 0.5-2 tablets with oncological designation being this treatment is determined individually. Invention can be used in manufacturing medicinal formulations of preparations used for treatment of patients with oncological pathology.

EFFECT: improved method for treatment and making, valuable medicinal properties of tablet.

8 cl, 2 ex

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to new compounds - pluraflavines of the formula (I): wherein R1 represents sugar group of the formula: ; R2 represents -COOH or -CH2-O-(R7)m wherein R7 represents sugar group of the formula: ; R3 is taken among the groups: and , and to all its stereochemical forms and mixtures of indicated forms in any ratio, and to their physiologically acceptable salts; R5 means hydrogen atom; R4 and R6 represent in common group -X2 with a double bond wherein X2 means oxygen atom (O); R8 and R10 represent in common group -X2 with a double bond wherein X2 means oxygen atom (O), and m = n = 1, and to all its stereochemical forms and mixtures of indicated forms in any ratio and to its physiologically acceptable salts. Invention relates to a method for preparing these compounds from culture of microorganism actinomycetes HAG 003959, DSM 12931 by fermentation, to the strain Actinomycetales HAG 003959, DSM 12931 used for preparing compounds of the formula (I) and to pharmaceutical composition inhibiting transcriptase activity and eliciting cytotoxic effect based on above said compounds. Compounds of the formula (I) are used as medicinal agents, for example, as antitumor agents.

EFFECT: improved method for preparing, valuable medicinal properties of compounds and composition.

19 cl, 3 tbl, 12 ex

FIELD: medicine, oncology.

SUBSTANCE: the present innovation deals with inhibiting the growth of host's cerebral tumors. It deals with introducing therapeutically efficient quantity of integrin αv antagonists being cyclo(Arg-Gly-Asp-D-Phe-[N-Me]-Val). The innovation enables to considerably inhibit cerebral oncogenesis in vivo, moreover, despite antiangiogenesis, due to induction of direct lethality of tumor cells.

EFFECT: higher efficiency of inhibition.

9 dwg, 2 tbl

FIELD: medicine, oncology.

SUBSTANCE: invention relates to a method for assay of efficacy on post-operative intrathecal chemotherapy of patients with intracerebral malignant tumors. Method involves determination of total protein level in cerebrospinal fluid before and after carrying out chemotherapy in autoliquor. Increase of the level of total protein by 5.6-6.3 times indicates on effectiveness of the post-operative chemotherapy. Method provides the objective evaluating dynamic of cytolysis of tumor cells that is the reliable method for estimation of efficacy of indicated treatment.

EFFECT: enhanced and improved method for treatment.

1 ex

FIELD: experimental medicine, oncology, biology.

SUBSTANCE: invention relates to a method for inhibition of tumor growth using radiation therapy as ionizing radiation with additional administration of mixture of octa-4,5-carboxyphthalocyanine sodium cobalt salt or oxocobalamine with sodium ascorbate in the ratio = (1:10)-(1:30). Method of combined using irradiation and indicated mixture of substances provides enhancing the effectiveness of anti-tumor treatment resulting to 70-100% recovery of experimental animals and reducing radiation loading and toxicity.

EFFECT: improved method for inhibition.

2 tbl, 3 dwg, 3 ex

FIELD: medicine, gynecology, contraceptives, pharmaceutical chemistry.

SUBSTANCE: invention proposes vaginal suppository comprising benzalconium chloride, benzoic acid, purified water and the preparation vitespol taken in the definite content of components. Invention provides the reliable inhibition of fungal microflora being especially against fungus Candida albicans and the absence of irritation and symptoms in vagina drying. Invention can be used as an individual agent for prophylaxis of undesirable pregnancy.

EFFECT: valuable properties of suppository.

5 tbl

FIELD: organic chemistry.

SUBSTANCE: invention relates to compounds of the general formula: wherein R means ethyl or benzyl; X means chlorine atom (Cl) or bromine atom (Br). Invention provides preparing quaternary ammonium compounds eliciting fungicide, bactericidal and surface-active properties.

EFFECT: valuable properties of compounds.

2 tbl, 4 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention proposes an agent for removing the post-narcosis depression after combined anesthetic assistances with applying sedative and narcotic preparations. As such agent the preparation "Reamberin" is used based on succinic acid that is a natural metabolite in human body. The preparation provides reducing time for adequate spontaneous breathing and awaking time by 1.5-fold and the absence of complications and negative adverse responses.

EFFECT: valuable properties of agent.

4 dwg, 3 ex

FIELD: medicine.

SUBSTANCE: the suggested disinfectant contains glutaric aldehyde, didecyldimethylammonium chloride, ethoxylated alcohol, propylene glycol and water at certain ratios. The method to treat objects, those of medicinal indications, among them, deals with treating an object with the above-mentioned disinfectant followed by keeping disinfectant on the object during the time and at temperature to provide disinfection and/or sterilization of the object followed by washing disinfectant off. The present innovation provides hermetic nature of elements and connective elements of flexible and rigid endoscopes, soldered and glued sites in the course of disinfection.

EFFECT: higher efficiency of application.

10 cl, 3 ex

FIELD: organic synthesis.

SUBSTANCE: invention provides group of novel antiviral nitrogen-containing compounds, in particular adamantane derivatives having general formula:

, wherein R represents chlorine or ethyl.

EFFECT: increased choice of biologically active compounds suitable for use in medicine as antiherpetic agents.

2 cl, 6 tbl, 3 ex

Antibacterial gel // 2247555

FIELD: cosmetology.

SUBSTANCE: the present innovation deals with cosmetic preparation for taking care of skin, in particular. The suggested antibacterial gel consists of either hydroxypropylcellulose or hydroxyethylcellulose, propylene glycol or diethylene glycol compound, polyguanidine or its synergistic mixture with quaternary ammonium compound, chitosan, oxyethylated ether of sorbitane, polyvinyl pyrrolidone at molecular weight ranged 10000 - 40000 or copolymer of polyvinylpyrrolidone, trilon-B - sodium salt of ethylene diamintetraacetic acid, perfumery composition, vitamin constituent and water. The present innovation provides increased regenerating formula of skin and its enhanced barrier function, improves homogeneity of the composition mentioned and its stability.

EFFECT: higher efficiency of application.

5 cl, 4 ex, 3 tbl

FIELD: agriculture, animal husbandry, organic chemistry.

SUBSTANCE: antiseptic ointment comprises cationic surface-active substance, lower glycols, polyethylene glycols, water and ethylene glycol monophenolic ester and higher polyethylene glycols taken in the definite ratio of components. As cationic surface-active substance ointment comprises N-alkyl-N-alkoxycarbonylmethylhexahydroazipinium chloride or alkyldimethylbenzylammonium chloride, or cetylpyridinium bromide, or cetylpyridinium chloride, or 1,2-ethylenebis-(N-methylcarbdecyloxymethyl)ammonium dichloride, or ethylhexadecyldimethylammonium chloride, or chlorhexidine; as lower glycol ointment comprises 1,2-propylene glycol or polyethylene glycol-300, or polyethylene glycol-400; as higher polyethylene glycol ointment comprises polyethylene glycol-1500 or polyethylene glycol-3000, or polyethylene glycol-4000, or polyethylene glycol-6000. Ointment elicits the high antibacterial activity, broad spectrum of bactericidal effect and low irritating effect with respect to udder skin. Invention can be used for sanitary-hygienic treatment of udder of lactating cows for prophylaxis and rapid healing external damages of udder and nipples (arising cracks), prophylaxis of mastitis, enhancing milk purity by microbiological indices.

EFFECT: valuable antiseptic properties of ointment.

2 cl, 1 tbl, 22 ex

The invention relates to chemical-pharmacological industry and relates to an inhibitor of the expression of integrin, comprising as active ingredient a compound sulfonamida formula IaIbthat means, containing an inhibitor of the expression of integrin formula IaIbfor the treatment of arteriosclerosis, psoriasis, osteoporosis, angiogenesis, retinal angiogenesis, diabetic retinopathy, inflammatory diseases, and how to prevent, treat or alleviate disease associated with increased expression of integrin
The invention relates to veterinary medicine, in particular for the treatment of hypothyroidism in rabbits
The invention relates to the field of veterinary medicine

FIELD: agriculture, animal husbandry, organic chemistry.

SUBSTANCE: antiseptic ointment comprises cationic surface-active substance, lower glycols, polyethylene glycols, water and ethylene glycol monophenolic ester and higher polyethylene glycols taken in the definite ratio of components. As cationic surface-active substance ointment comprises N-alkyl-N-alkoxycarbonylmethylhexahydroazipinium chloride or alkyldimethylbenzylammonium chloride, or cetylpyridinium bromide, or cetylpyridinium chloride, or 1,2-ethylenebis-(N-methylcarbdecyloxymethyl)ammonium dichloride, or ethylhexadecyldimethylammonium chloride, or chlorhexidine; as lower glycol ointment comprises 1,2-propylene glycol or polyethylene glycol-300, or polyethylene glycol-400; as higher polyethylene glycol ointment comprises polyethylene glycol-1500 or polyethylene glycol-3000, or polyethylene glycol-4000, or polyethylene glycol-6000. Ointment elicits the high antibacterial activity, broad spectrum of bactericidal effect and low irritating effect with respect to udder skin. Invention can be used for sanitary-hygienic treatment of udder of lactating cows for prophylaxis and rapid healing external damages of udder and nipples (arising cracks), prophylaxis of mastitis, enhancing milk purity by microbiological indices.

EFFECT: valuable antiseptic properties of ointment.

2 cl, 1 tbl, 22 ex

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