Antiviral medicine

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns chemical pharmaceutical industry, particularly medicine for treatment of virus diseases, including HIV infection (AIDS and HIV-related diseases). The antiviral medicine is a suppository containing fullerene-polyhydropolyaminocaproic acid and auxiliary substances of dimethylsulfoxide, water-free lanolin or vegetable oil selected out of olive, peach, bumpkin seed oil, and base selected out of W-35 or H-15 vitepsol, cacao butter, solid fat, in the following amount per one 2 g suppository: fullerene-polyhydropolyaminocaproic acid 5-20 mg, diemthylsulfoxide 50-200 mg, water-free lanolin or vegetable oil 20-100 mg, the rest being the base.

EFFECT: obtaining antiviral medicine for treatment of virus diseases, including HIV infection.

 

The invention relates to pharmaceutical industry and relates to the creation of tools for the treatment of viral diseases, including HIV infection (AIDS and HIV associated diseases).

Famous complex of separate preparations of the day the treatment of viral infections, consisting of interferon, which is administered rectally in the form of an aqueous solution, and vitamins E and C, which is administered in the form of oil solution intramuscularly in parallel with interferon (ed. mon. The USSR №1530189, 1988).

Small synthetic antiviral agents - Medinan, methisazone find a limited prophylactic use, such as iodoxuridine, oksolina are applied topically in viral diseases of the skin, and the toxicity of the first very high (Pharmacology, M.: Medicine, 1981, s-401).

Known drugs have long latency period, which creates the risk of exposure of the organism to the development of the maximum protective effect of interferon and, in addition, a known antiviral have a certain toxicity.

The present invention is the creation of facilities possessing antiviral activity, especially effective in the treatment of HIV infection.

To solve the problem proposed antiviral agent, executed in the form of a suppository containing fullerene-polig topolinonote.png acid and excipients dimethyl sulfoxide, and anhydrous lanolin or vegetable oil selected from the group of olive, peach, pumpkin seeds, and a base selected from the group of witepsol W-35 or H-15, cocoa butter, tallow in the following ingredients in 1 candle by weight of 2 g:

fullerenepolyhydropolyaminocaproic acid5-20 mg
the sulfoxide50-200 mg
lanolin anhydrous or
vegetable oil20-100 mg
baserest

Fullerenepolyhydropolyaminocaproic acid is a powder dark brown, almost black, color with no odor. The connection is not soluble either in water or chloroform, but soluble in dimethyl sulfoxide (100 mg/ml), so it is soluble in water and in chloroform.

Most chemical reactions with the fullerenes are not selective, which complicates the synthesis of individual compounds. Therefore, in the product are present as position isomers, and compounds that differ in the number of attached amino acids.

Derivative of fullerene and aminocaproic acid with the number of connected groups of at least 2, the General formula:

With60Hn[NH(CH2) 5C(O)O-]n,

where C60- fullerene core,

[NH(CH2)5C(O)O-] - aminocapronic anion

Fullerenepolyhydropolyaminocaproic acid

The content of active substance - fullerenepolyhydropolyaminocaproic acid in 1 suppositories 5 mg, 10 mg and 20 mg of Vegetable oil used in candles for the introduction of the active substance in suppozitornyj basis, help the uniform distribution of the substance in suppositories.

Suppositories prepared as follows.

A portion fullerenepolyhydropolyaminocaproic acid 0.2 g portions contribute to the DMSO solution of 3 g with constant stirring. The dissolution is carried out at room temperature or when heated to 40°C for 30 min to dissolve fullerenepolyhydropolyaminocaproic acid. Next, add 0.8 g of peach oil, the mixture is stirred for 30 minutes

A portion of Witepsol 36 g melted at 60°C, cooled to 35-36°add the mixture of substances in DMSO with peach oil, the temperature of which also 35-36°C, With constant stirring for 2 hours until suppozitornyj the mixture will become smooth brown color.

Suppositories molded 0.2 g, placed in the refrigerator at 2-5°C. the hardening Time of suppositories for about 40 minutes Yield -17 suppositories. The melting point is 35°C.

Store suppositories in the dark and inaccessible to children at temperature not above 25°With shelf life of 2 years.

The method of application and doses

The drug is active against HSV, and in case of simple herpes of the skin and mucous membranes in patients with impaired immune systems with genital herpes (primary and recurrent), shingles and chickenpox.

Suppositories rectally by suppository 1-2 per day rate not less than 10 days to 1 month.

Daily admission within one month the patient will receive a total of 300 mg of the active substance in the treatment of HIV infections, and in case of serious herpes viral infections involving disorders of the immune system.

In other cases, a course of about 100 mg of active substance, i.e. of 20 mg per day for 5 days or 10 mg per day for 10 days.

It is assumed that because the tool does not penetrate into the cell, there is no danger of its interaction with other antiviral drugs, but it is necessary to exclude drugs that cause drug sensitization: antibiotics, nonsteroidal anti-inflammatory agents.

Not be used in conjunction with drugs that affect leucopoiesis; exclude myelodepression drugs, tiazidove diuretics, estrogen and ethanol, under which engaged in the production of platelets. Suppositories were tested in the Institute of Virology. Dijanoveckog FRAME and clinical infectious diseases hospital No. 2 (Nizhny Novgorod).

Tests in vitro and clinical trials have shown:

The use of the drug in the treatment of patients with herpes viral infections, low immune status leads to an increase in the duration of remission. The drug is able to prevent the formation of lesions when applied at the first symptoms of recurrent herpes simplex. The drug helps to eliminate pain, reduce the number of lesions, accelerate their disappearance.

During treatment was regularly controlled renal function, determined the content of the formed elements of the blood, also conducted biochemical and hematological blood tests at least once per month. In case of deterioration of the hematological parameters were specified dose or stop treatment. In the case of skin rash the drug was suspended up to 1 month.

Antiviral agent, characterized in that it is made in the form of a suppository and contains the active substance fullerene-polyhydroxyalkanoate acid and excipients dimethyl sulfoxide, and anhydrous lanolin or vegetable oil selected from the group of olive, peach, pumpkin seeds and a base selected from the group of vitepsk the W-35 or H-15, cocoa butter, hard fat in the following ingredients in 1 candle by weight of 2 g:

fullerenepolyhydropolyaminocaproic acid5-20 mg
the sulfoxide50-200 mg
lanolin anhydrous or
vegetable oil20-100 mg
basethe rest of it.



 

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