Drug and method thereof

 

(57) Abstract:

The invention relates to medicine. Sodium salt chlororesorcinol acid is contained in a medicinal drug with immunomodulatory, anti-inflammatory and antitumor properties. Spend bubbling resocialise acid chloride with subsequent exposure to an aqueous solution of sodium bicarbonate. Received after ozonation chlororesorcinol acid is added at a temperature of (80-100)oWith distilled water, kept at this temperature until a dark precipitate. After decanting mixed with an aqueous solution of sodium bicarbonate. The resulting composition is cooled to a temperature of (4-10)oWith and obtain the target product in the form of loose then as a precipitate of white or slightly yellowish crystalline powder. When heated add distilled water in the ratio, wt.%: harrisoniana acid of 0.002 to 0.2, the water - the rest. The invention allows to realize the specified destination. 2 S. and 1 C.p. f-crystals.

The present invention relates to medicine, namely to drugs that affect the immune system, and t is islote, which drug immunological actions, representing white or slightly yellowish, easily soluble in water with formation opalestsiruyuschih solutions powder, possessing the ability to stimulate migration and cooperative T - and b-lymphocytes, increase the phagocytic activity of macrophages and the activity factors of nonspecific resistance (see , for example, M. D. Mashkovsky "Drugs". M, Medicine, 1985, so 2, S. 172).

This drug has a broad spectrum of biological activity, but injecting this drug causes pain, which leads to the need for simultaneous administration to patients of painkillers.

The closest analogue prototype is the drug "Leykomaks" (Leucomax), produced as a sterile, lyophilized water-soluble powder, which have significant influence on the blood and the functional activity of leukocytes, stimulating the growth of granulocytes, monocytes and T-lymphocytes without affecting the growth of b-lymphocytes (see, for example, reference to "drugs of foreign firms in Russia", M, Attraversare, 1993, S. 351).

This drug is used in the treatment of leukopenia with insufficient speed up blood after chemotherapy, in AIDS, but it causes fever and allergic reactions.

Known sodium salt chlororesorcinol acid, part of the adduct of crystalline sodium salts chlororesorcinol, crotoxyphos acid and sodium bicarbonate, with biostimulating properties, but because of its toxicity limited in application (see, for example, USSR author's certificate 614087 priority from 30.12.75,, IPC: 01 N 9/24, bull. 25 from 05.07.78 year). While the info about the sodium salt chlororesorcinol acid out of the above adduct in the relevant sources of information not found.

A method of obtaining drug - 2-amino-1,2,3,4-tetrahydropyrazin-1,4-dione sodium salt dihydrate, which includes the receipt of the original product, such as 3-aminophthalhydrazide, which is subjected to the reaction of molecular rearrangement with subsequent exposure to sodium hydroxide and isolation of the target product (see, for example, the patent of the Russian Federation 2138264 priority from 06.05.99 year, the IPC: a 61 K 31/50, bull. 27 from 27.09.99 year).

This method can improve the yield of the target product, but its use is limited by the ability of polucheniya of crystalline sodium salts chlororesorcinol, resocialise acid and sodium bicarbonate (see, for example, ABT.the certificate of the USSR 614087 priority from 30.12.75,, IPC: 01 N 9/24, bull. 25 from 05.07.78, including the transmission (bubbling through the mixture resocialising and glacial acetic acid chloride in the amount of (70-80)% of required for complete chlorination and processing the mixture with an aqueous solution of sodium bicarbonate, taken in a molar excess to the mixture, followed by removal of unbound water.

The known method does not provide the possibility of obtaining sodium salt chlororesorcinol acid out of the mixture with other components of the above adduct.

The invention consists in the application of the sodium salt chlororesorcinol acid as a drug with immunomodulatory, anti-inflammatory and anticancer properties.

The invention consists in that in a method of producing a medicinal product sodium salt chlororesorcinol acid comprising bubbling resocialise acid chloride with subsequent exposure to aqueous sodium bicarbonate solution, obtained after ozonation chlororesorcinol acid is added is to obtain a dark residue, after decanting mixed with an aqueous solution of sodium bicarbonate, and the resulting composition is cooled to a temperature of (4-10)oC and get the target product in the form of loose then as a precipitate of white or slightly yellowish crystalline powder.

When heated add distilled water in the ratio, wt.%: harrisoniana acid (0,002-0,2); water - the rest.

Studies have shown that drug - sodium salt chlororesorcinol acid has anabolic activity, stimulates cellular and humoral defense factors of the body, has anti-inflammatory and antitumor activity.

This is confirmed by instrumental and laboratory examinations of patients by conducting a blood test to check immunological indicators (patients) leukocyte and lymphocyte systems.

This medicine can be taken orally in the form of powder or tablets during or after a meal, and its application in a wide range of doses (from 20 mg to 2 g) does not cause allergic reactions and other side effects, and its effectiveness in the treatment with stenny the drug was obtained as follows.

First, the interaction of molten at (100-120)oC cresol mixture (C7H8About) and glacial acetic acid (C2H4O3) get kresoximmethyl acid (C9H10ABOUT3), from which, after ozonation for 30 to 50 min of gaseous chlorine (CL2and cooling the reaction mixture, get chlororesorcinol acid (l9H9O3in the form of a crystalline powder, which is washed from acetic acid and dried. This powder with boiling distilled water and incubated until the precipitate of dark color, but not more than (20-40) min at a temperature (80-100)oC, and then hold the decantation followed by treatment of this sludge with sodium bicarbonate solution (Panso3in the water, getting as appropriate sediment target product - sodium salt chlororesorcinol acid (ClC9H8O3Na) in the form of a white or slightly yellowish powder, which is washed with distilled water, then dried in a drying Cabinet and pack up.

It should be stated that heated to boiling distilled water add to balance, wt.%: powder - (0,002-0,2); water - the rest.

For himin8ABOUT3CL Na. Calculated, %: 48,34; N 3,50; Cl 15,85; Na At 10.64.

Chemical identity sodium salt chlororesorcinol acid was proved by thin-layer chromatography on plates Culefol UV-254 the presence of one of the spots on the chromatogram in the system butanol:ethanol:25% aqueous ammonia at a ratio of 1:1:1 Rf=0,60.

The manifestation of the chromatograms was performed by annealing these records over a gas burner, and iodine.

The possibility of applying the proposed drug product is confirmed by examples.

Example 1.

Patient A., aged 35.

Diagnosis: Hodgkin's Disease. Several courses of chemotherapy. A serious condition.

Turning: in the neck left a dense formation h cm, painful spanne with adjacent tissues. On the radiograph in the mediastinum tumor formation 5x5 see Paroxysmal coughing and choking.

Blood count: leukocytes to 30 thousand, erythrocytes - 2.5 million, platelet - 19 thousand units.

The treatment drug - sodium salt chlororesorcinol acid: 300 mg 2 times a day during meals in the course of a month.

Abrupt is vedennogo treatment: the tumor on his neck almost disappeared (palpation of this area painless), on the radiograph, the tumor also not detected. Blood count: leukocytes - 5.5 thousand, erythrocytes - 6.5 million, platelets 350 thousand units.

Example 2.

Patient C., 52.

Diagnosis: carcinoma (3-4) the extent of the lung with metastasis to the liver and brain.

When a state of extreme gravity.

The treatment drug - sodium salt chlororesorcinol acid within 2 months.

The first 7 days 450 mg 3 times a day during meals, then within 3 weeks 300 mg also 3 times a day, later in the month 200 mg 2 times after eating.

On the fifth day after the start of treatment, marked improvement in General condition, abolished the use of painkillers.

In the process of further treatment showed positive dynamics. After 2 months the patient returned to normal on ultrasound primary tumor and metastases are not detected.

Example 3.

Patient T., 28 years.

Diagnosis: AIDS with a lesion of the skin of the lower part of the trunk and legs. Profuse diarrhea.

Prior to treatment the year the patient was treated with injections of complex drugs: leykomaks and zidovudine.

Example 4.

Patient S., 49.

Diagnosis: viral infection, astheno-vegetative syndrome, prolonged diarrhea.

Ill for 3 months, severe depletion, previous treatment by known means gave no effect.

The treatment of drug - sodium salt chlororesorcinol acid mg times a day for 10 days.

According to the survey patient: two weeks after start of treatment in this medication symptoms of diarrhea removed, the normalized state.

Example 5.

Patient K., aged 60.

Diagnosis: atropunicea fever due to cytotoxic chemotherapy for chronic leukemia.

The treatment of drug - sodium salt chlororesorcinol acid mg times on the x2">

After a month of treatment the patient's condition is normalized, the results of the blood tests, the number of neutrophils (%): stab - 6,0 (when - 5,3), segmented - 79,0 (when - 47,6).

During the course of chemotherapy, the patient is recommended during treatment, prophylactic administration of a specified drug (50-100) mg (1-2) times daily.

1. Drug with immunomodulatory, anti-inflammatory and antitumor properties, characterized in that it contains sodium salt chlororesorcinol acid.

2. The method of obtaining the medicinal product sodium salt chlororesorcinol acid comprising bubbling resocialise acid chloride with subsequent exposure to an aqueous solution of sodium bicarbonate, characterized in that after ozonation chlororesorcinol acid is added at a temperature of (80-100)oWith distilled water, stirring, maintained at this temperature until a dark precipitate, which, after decantation is mixed with an aqueous solution of sodium bicarbonate, and the resulting composition is cooled to a temperature of (4-10)oWith and receive target CLASS="ptx2">

3. The method according to p. 2, characterized in that the heated distilled water is added in the ratio, wt.%: harrisoniana acid of 0.002 to 0.2, the water - the rest.

 

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