RU2333751C1 - Antiviral medicine - Google Patents

Abstract

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.

Description

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

The known complex of individual drugs of the day for 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 are administered as an oil solution intramuscularly in parallel with interferon (ed. Certificate. USSR No. 1530189, 1988).

A few synthetic antiviral agents - midintan, metisazon find limited prophylactic use, and such as iodoxyuridine, oxolin are used topically for viral skin diseases, and the toxicity of the former is very high (Pharmacology, M .: Medicine, 1981, p. 399-401).

Known drugs have a long latent period of action, which creates a risk of infection of the body before the peak of the protective effect of interferon develops and, in addition, known antiviral drugs have a certain toxicity.

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

To solve this problem, an antiviral agent is proposed in the form of a suppository containing fullerene-polyhydropolyaminocaproic acid and excipients dimethyl sulfoxide, as well as anhydrous or vegetable oil lanolin selected from the group of olive, peach, pumpkin seeds, and a base selected from the group of W brand Witepsol -35 or H-15, cocoa butter, solid fat in the following ingredients per 1 candle weighing 2 g:

fullerene polyhydropolyaminocaproic acid 5-20 mg dimethyl sulfoxide 50-200 mg anhydrous lanolin or vegetable oil 20-100 mg the basis rest

Fullerenepolyhydropolyaminocaproic acid is a powder of dark brown, almost black, odorless color. The compound is insoluble neither in water nor in chloroform, but soluble in dimethyl sulfoxide (about 100 mg / ml), so that it becomes soluble in both water and chloroform.

Most chemical reactions with fullerenes are not selective, which complicates the synthesis of individual compounds. Therefore, both positional isomers and compounds differing in the number of attached amino acids are present in the product.

A derivative of fullerene and aminocaproic acid with the number of attached groups of at least 2, of the general formula:

C ₆₀ H _n [NH (CH ₂ ) ₅ C (O) O ^- ] _n ,

where C ₆₀ is the fullerene core,

[NH (CH ₂ ) ₅ C (O) O ^- ] - aminocaproic anion

Fullerenetetrahydrotetraaminocaproic acid

The content of the active substance is fullerenpolyhydropolyaminocaproic acid in 1 suppository 5 mg, 10 mg and 20 mg. Vegetable oils used in suppositories to introduce the active substance into a suppository base help to evenly distribute the substance in the suppository.

Suppositories are prepared as follows.

A portion of fullerene polyhydropolyaminocaproic acid 0.2 g is added portionwise to a solution of DMSO 3 g with constant stirring. The dissolution is carried out at room temperature or by heating to 40 ° C for 30 minutes until complete dissolution of fullerene polyhydropolyaminocaproic acid. Then add 0.8 g of peach oil, the mixture is stirred for 30 minutes.

A portion of Vitepsol 36 g is melted at 60 ° C, cooled to 35-36 ° C, a mixture of the substance in DMSO with peach oil is added, the temperature of which is also 35-36 ° C, with constant stirring for 2 hours, until the suppository mass becomes even Brown color.

Suppositories are molded in 0.2 g, placed in a refrigerator at 2-5 ° C. The hardening time of suppositories is about 40 minutes. Exit - 17 suppositories. Melting point - 35 ° C.

Keep suppositories in a dark place and out of the reach of children at a temperature of no higher than 25 ° C, shelf life 2 years.

Dosage and administration

The drug is active against HSV, as well as with simple herpes of the skin and mucous membranes in patients with impaired immune systems, with genital herpes (primary and recurrent), with herpes zoster and chicken pox.

Suppositories are used rectally for 1-2 suppositories per day for at least 10 days to 1 month.

With a daily intake for a month, the patient will receive a total of 300 mg of the active substance - in the treatment of HIV infections and in case of severe herpes virus infections, accompanied by disorders of the immune system.

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

It is assumed that since the drug does not penetrate 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, non-steroidal anti-inflammatory drugs.

Do not use in conjunction with drugs that affect leukopoiesis; exclude myelosuppressive drugs, thiazide diuretics, estrogen and ethanol, which suppress platelet production. Suppositories were tested at the Institute of Virology. D.I. Ivanovo RAMA and Clinical Infectious Diseases Hospital No. 2 (Nizhny Novgorod).

In vitro and clinical trials have shown:

The use of the drug in the treatment of patients with herpes virus infections with low immune status leads to an increase in the duration of remission. The drug is able to prevent the formation of lesions, if applied when the first symptoms of herpes simplex relapse appear. The drug helps to eliminate pain, reduces the number of rashes, accelerates their disappearance.

During treatment, renal function was regularly monitored, the content of blood cells was determined, and biochemical and hematological blood tests were performed at least once a month. In case of deterioration of hematological parameters, the doses were specified or treatment was stopped. In case of skin rashes, the drug was stopped for up to 1 month.

Claims (1)

An antiviral agent, characterized in that it is in the form of a suppository and contains the active substance fullerene-polyhydropolyaminocaproic acid and excipients dimethyl sulfoxide, as well as anhydrous or vegetable oil lanolin selected from the group of olive, peach, pumpkin seeds and a base selected from the group of witepsol brand W-35 or H-15, cocoa butter, solid fat in the following ingredients per 1 candle weighing 2 g: fullerene polyhydropolyaminocaproic acid 5-20 mg dimethyl sulfoxide 50-200 mg anhydrous lanolin or vegetable oil 20-100 mg the basis rest.