RU2209068C1 - "sobi" gel of antiviral activity and transdermal properties for treating hivinfected patients - Google Patents

Abstract

FIELD: medicine, pharmacology. SUBSTANCE: the suggested "SOBI" gel contains silver sulfadiazine, dimethylsulfoxide and alcoholic propolis tincture, and polyethylenoxide gel PEG- 1500 as a foundation at the following ratio of components per 100 ml: silver sulfadiazine 1-1.5 g; dimethylsulfoxide 10-15 ml; 10%-alcoholic propolis tincture prepared on 80%-alcohol 10-15 ml, polyethylenoxide gel PEG-1500 - the rest, moreover, the size of silver sulfadiazine particles does not exceed 5-10 mcm. EFFECT: higher efficiency of therapy. 2 ex, 1 tbl

Description

 The invention relates to pharmacology and medicine and can be used to treat patients infected with HIV (human immunodeficiency virus) at any stage of the disease, including AIDS patients, as well as other viruses, including concomitant ones.

 It is known that drugs based on "silver sulfadiazine" have antiseptic and antiviral activity.

 So the cream "Dermazin" containing 1% "silver sulfadiazine" in a hydrophilic base [1] prevents and suppresses infection on the burned areas of the skin, impregnating necrotic tissue and effusion.

 The disadvantages of the cream are that it is designed to fight infection only on the surface of tissues, i.e. on open wounds, burns, but can not affect the viruses and microorganisms inside the tissues and cells of the sick body.

 Closest to the claimed drug is considered "Silver sulfadiazine to inhibit the AIDS virus during sexual intercourse" [2] - prototype. The drug is intended to neutralize HIV infection on the surface of the mucous membranes of the genital organs. That is, it is known as an antiseptic and cannot be effective in the treatment of patients already infected with HIV and AIDS, when the infection spreads by the circulatory and lymphatic systems to the organs, tissues, cells of the patient.

 The purpose of the proposed solution is to increase the effectiveness of an external therapeutic agent against HIV infection. The practice of treating AIDS patients and HIV-infected people shows that the course of the disease is almost always accompanied by an increase in lymph nodes. They increase several times, are not painful or painless on palpation. This indicates the fact that a large number of viral particles, affected cells and blood leukocytes fighting the infection and, naturally, decay products of both accumulate in the lymph nodes. This process can take a considerable time, if you do not use additional means of combating HIV infection, acting locally, i.e. directly in places where the process of active replication of the virus is observed.

 The task of creating a transdermal drug that is able to penetrate deep into the tissues of a diseased organism and into cells for direct contact with viruses, i.e. with the ability to easily penetrate through the skin and mucous membranes of the patient’s organs with external surface contact.

 The gel composition is disclosed, which contains: the active antiviral component - “Silver sulfadiazine”, dimethyl sulfoxide (hereinafter DMSO) as a carrier of silver ions inside HIV-infected body cells, for direct contact with viruses, PROPOLIS alcohol tincture and a base - polyethylene oxide gel (PEG- 1500). The gel (PEG-1500) is taken ready-made, manufactured according to the technology approved in TU 9154-004-1182-1987-93. The specified gel of polyethylene oxide (PEG-1500) is obtained by radiation crosslinking under the influence of ionizing radiation at a dose of 40 - 420 kGy. The resulting gel contains only 4-6% polyethylene oxide itself, the remaining part is water, and therefore it has good ability to penetrate deep into the tissues of a living organism due to its small molecular weight (i.e. it has relatively small molecular sizes). To increase the penetrating ability in the tissue of the main medicinal component of silver sulfadiazine used in the gel, the silver sulfadiazine powder is pre-treated by grinding it in a special roller mill to obtain particles no larger than 5-10 microns.

 This particle size corresponds to the pore size of the skin, hair tubules, lymphatic vessels, blood capillaries, which contributes to the free penetration of particles into the depths of tissues, in particular the lymph nodes. In the tissues of the affected organism, "silver sulfadiazine" moderately dissociates. Silver ions are released uniformly and rather slowly and therefore do not bind quickly and widely with chlorine ions, proteins and other components of body fluids. The presence of a sulfamide component in the "silver sulfadiazine" suppresses concomitant bacterial infection in the lymph nodes. DMSO contained in the gel has a special function, i.e. specifically solvates silver ions and carries out transmembrane transfer of silver ions into viral particles, as well as affected cells, which contributes to their further inactivation by competent cells of the immune system. In addition, the processing of silver sulfadiazine powder in a special roller mill changes the physicochemical properties of the particles, and probably increases their internal energy intensity, which makes them more active.

 The presence of propolis in the gel increases the effectiveness of the gel as a medicine due to the unique properties of propolis, which is a natural biocomponent with anesthetic, antitoxic, antiviral, fungicidal, antioxidant, antitumor properties that increase the immunological resistance of the patient. It also serves as a perfume, softening and damping the smell of organic matter (DMSO), due to the large content in its structure of natural essential oils.

 EXAMPLE 1

 The inventive gel is prepared by mixing to a volume of 100 ml: 1 gram of "silver sulfadiazine" with a particle size of not more than 5-10 microns, 10 ml of DMSO and 10 ml of 10% alcohol tincture of propolis prepared in 80% ethyl alcohol. Up to 100 ml gel of polyethylene oxide (PEG-1500) is added and all components are thoroughly mixed until a homogeneous consistency is obtained. A uniform gel with a pleasant odor is obtained, which is important for the patient, white in color, leaving no residue on the skin of the body and clothing. The resulting drug is packaged in a glass container and stored in a dark, cool place for no more than 6 months.

 EXAMPLE 2

Subject to the conditions of example 1 for the preparation of the gel take the components in the following quantities:
"Sulfadiazine silver" - 1.5 g
DMSO - 15 ml
Alcohol 10% tincture of propolis, cooked in 80% ethanol - 15 ml
Polyethylene Oxide Gel (PEG 1500) - Else.

 The effectiveness of the gel was tested in the Novosibirsk Regional AIDS Center (Novosibirsk Region, Koltsovo) for HIV-infected patients simultaneously with the course of treatment with microclysters with preparations containing silver. Gel treatment was carried out in case of patients with enlarged, painless or several painful lymph nodes in the neck, armpits, and groin. This circumstance indicated the presence of active replication of the HIV virus in the lymph nodes. The gel was applied 2 times a day directly to the area of the enlarged lymph nodes with a layer of 1-2 mm, followed by rubbing it into the skin with light movements of the fingers. The course of treatment of HIV-infected patients during treatment with drugs containing silver, with parallel rubbing of the inventive gel into the skin in the area of the location of the enlarged lymph nodes, was more effective and gave a good therapeutic result in a shorter treatment time. The terms of treatment were reduced by 15-20%.

 The table below shows the results of clinical trials conducted in the Novosibirsk Regional AIDS Center (Koltsovo, Novosibirsk Region) with the participation of five patients from different regions of the Russian Federation. The treatment results were evaluated by us according to the physiological state of patients at the end of the planned course of treatment lasting 20 days. During the course of treatment, we recorded the dynamics of changes in the state over time (sizes in diameter, consistency) of the lymph nodes of patients.

Sources of information
1. Cream "Dermazin". Abstract by Lek Pharmaceutical and Chemical Company dd

 2. Patent EP 287204 CL, A 61 K 31/635. Publication 10.19.88 g. - prototype.

Claims (1)

A gel with antiviral activity and transdermal properties for the treatment of HIV-infected patients, containing silver sulfadiazine and a base, characterized in that it additionally contains dimethyl sulfoxide and propolis alcohol tincture, and PEG-1500 polyethylene oxide gel as a base, with the following ratio of components per 100 ml volume:
Silver sulfadiazine, g - 1 - 1.5
Dimethyl sulfoxide, ml - 10 - 15
10% alcohol tincture of propolis, prepared with 80% alcohol, ml - 10 - 15
PEG-1500 Polyethylene Oxide Gel - Else
moreover, the particle size of silver sulfadiazine does not exceed 5-10 microns.

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