Pharmaceutical composition for treating herpes viral infections

 

(57) Abstract:

The invention relates to the field of pharmaceutical industry and relates to pharmaceutical compositions for the treatment of herpes virus infection. The invention consists in that in the composition as Antiherpes virus effect tools use composition containing glycyrrhizinic acid, epiderm, mefenamico acid, proteolytic enzymes, the filler in the form of a mixture of vaseline, lanolin, and ethyl alcohol and purified water in a predetermined ratio. The invention allows to completely arrest the infectious process at the stage of latent signs of the disease, reduces the period of treatment to 1-2 days and prolongs remission of up to one year or more. 2 C.p. f-crystals.

The invention relates to medicine, namely to pharmacology, and can be used for the treatment of herpes viral infections.

Herpes is an infectious disease caused by one of several related viruses, including viruses type 1 and 2 herpes simplex (HSV) and the virus stays zoster (VZV). This infection can occur in utero, respiratory and sexually transmitted infections involving in pathological process any organ and system of the body, you are the Central nervous system: there encephalitis, meningoencephalitis. One-third of the patients dies, another third becomes disabled. In recent times there are serious grounds to believe that herpes causes and some types of cancer. Herpetic disease is quite widespread among the population (according to the who, about 35% of the world's population is infected them) and deaths among viral diseases is on the second place after influenza (excluding AIDS).

The herpes simplex virus type (HSV-1) usually causes bubbles “cold” on the lips, around the nostrils and the mouth. Herpes simplex type II (HSV-2) is the main cause of genital herpes (genital herpes). The virus stays zoster (VZV) is responsible for the development of varicella and herpes zoster.

For the treatment of herpes developed many drugs as symptomatic of the nature and causal actions aimed directly to the virus is the causative agent of disease.

Drugs symptomatic actions are aimed at relief of pain (pain relievers), the removal of the inflammatory process (anti-inflammatory drugs), increased ry) of the organism.

Action etiotropic drugs directly pathogen, namely pathogen simple or herpes zoster.

Analysis of the level of the known technical solutions shows that the severity of diseases caused by viruses types 1 and 2 herpes simplex virus and virus stays zoster, their wide distribution and a large percentage of deaths caused occurrence in medical practice, a sufficiently large number of different layout and applicable beginning Antiherpes virus effect means that, without impacting significantly on the frequency of new outbreaks of diseases are able for some time to stop herpes process. The latter largely determines the relevance of the task to search for new, more effective means of protection against herpes virus lesions of the body.

For the treatment of herpes simplex use, for example, garlic extract, which is taken orally daily for 1-3 weeks, every week, reducing the dose, or use the application of garlic extract on the affected area (U.S. patent No. 4795636, op. 03.01.1989).

Known drug Proceesed (Registration certificate №R. 02.01/02777), tosa L. and Calamagrostis epigeios L., which are able to suppress nonspecific enzyme DNA polymerase in cells infected with herpes simplex viruses 1-St and 2-nd type, herpes zoster and AIDS. This leads to decreased capacity or complete blocking replication of viral DNA and, consequently, inhibits the multiplication of viruses. The drug used for the treatment, prophylaxis and prevention of viral infections caused by herpes simplex virus 1-St and 2-nd type.

The drug is inside the drops, put on a bit of sugar (or food starch). For the treatment of infections herpes simplex, including initial and recurrent genital herpes, and herpes of the lips, the drug is applied in the form of lotions on the affected area of the skin or mucous membranes 3-5 times a day. For the preparation of lotions with Protelecom® 1.5 ml (36-38 drops), diluted in 10 ml saline. Soaked in saline gauze is applied on the affected area of the skin up to 3 times per day. For the preparation of vaginal tampons with Protelecom® 3 ml (72-75 drops), diluted in 20 ml of physiological solution.

Treatment continued until the disappearance of the skin lesions or mucous membranes. Maximum Kursk-therapeutic drug current top of which is a synthetic analogue of one of the most commonly occurring nucleosides in DNA triplets - acyclovir (9-[(2-hydroxyethoxy)methyl]guanine), created in the 70-ies and released into practice under the name Zovirax (UK).

Also known derivatives of acyclovir - valacyclovir (VALTREX), famciclovir (FAMVIR) (WO 9725989), which is used for patients with herpes viral infections with disorders of intestinal absorption: the elderly, cancer patients, HIV-infected (Matias C. I., Shevchuk Century B., Tolkunova T. L., L. Vasilenko, "Etiopathogenetic therapy of severe forms of herpes infection". Institute of epidemiology and infectious diseases named after. L. C. clinic, whose Academy of medical Sciences of Ukraine (Kiev)).

As a rule, ointments and creams with the use of these compounds is prepared on the basis of paraffin or propylene glycol, with a content of active substance of at least 5 wt.%.

Known composition, which as the beginning of the current intended for the suppression and destruction of the virus, includes urea, hyaluronic acid or its salt (U.S. patent No. 5550112). To enhance therapeutic and consumer properties of the composition it is injected additives: antisepticise in the composition, containing as active substance Riboflavin, supplements containing carotenoids, flavonoids, acetyl COA, vitamins a, E, C, B6, B9, and lysozyme, glutathione and others (U.S. patent No. 6020333).

Known antiviral drug HERPIGEN company Sananavita Enterprises produced in the form of ointments, containing as active substance 0.1 g of glycyrrhizic acid and a filler. The ointment is applied three times daily to the affected areas, usually within weeks. For faster recovery possible application for 6-8 hours daily.

Closest to the claimed is the drug Epigenes (EPIGEN) company Cheminova Internacional S. A., Spain, which includes 0.1 wt.% glycyrrhizic acid, a set of organic acids with preservative, emollient and antiseptic action, emulsion wax as filler, as well as odorant and purified water. The medication comes in the form of a cream, ointment or spray. The ointment is applied in a thin layer without rubbing on the affected skin and mucous 3-5 times a day for at least 3 days.

An object of the invention is to expand the Arsenal of domestic remedies, used for Antiherpes virus effect of therapy with whom agrees pharmaceutical composition for treating herpes viral infections, containing glycyrrhizinic acid, a filler in the form of a mixture of vaseline and lanolin in the ratio of 1:6, purified water and optionally water-glycerol complex (2,3-DIXIPAY)-orthotitanate hydrochloride, mefenamico acid (Acidum mephenamicum), proteolytic enzymes and ethyl alcohol in the following ratio, wt.%:

Epiderm 40,0-80,0

Glycyrrhizin acid of 0.1-1.0

Vaseline yellow health of 10.0 to 50.0

Anhydrous lanolin is 1.0-10.0

Mefenamovaya acid 0,4-1,0

Ethyl alcohol 3,0-10,0

Proteolytic enzymes from 0.01 to 0.40

Purified water Rest

The composition of the pharmaceutical composition is selected eksperimentalno based on the maximum efficiency of its actions and acceleration of reparative effects in the treatment of herpes viral infections.

Used in the claimed composition glycyrrhizin acid is a triterpene glycoside, molecular formula C42H62O16molecular weight 822,94 (M. D. Mashkovsky. "Medicinal product", M, Medicine, 1978, S. 325). It has antiviral, anti-inflammatory action.

Water-glycerol complex (2,3-DIXIPAY)-orait a translucent, a gelatinous mass, pale yellow, soluble in water, glycerin and alcohol.

Mefenamovaya acid crystalline powder grayish-white color. Practically insoluble in water, very soluble in alcohol, has anti-inflammatory, analgesic and cough activity (M. D. Mashkovsky. "Drugs", so 1, m, Medicine, 1994, S. 219). The introduction of acid in the inventive composition are carried out either directly, or use alcohol solution.

Proteolytic enzymes included in the composition, such as lydasum, Pancreatin, lipase and others, increase the degree of reparative mechanisms and restore the integrity of damaged skin and mucous coats.

As a filler, a mixture of vaseline yellow medical (FS 42-2456-57) and anhydrous lanolin (FS 373, ed. the tenth) in the ratio 1:6 that improve consumer properties of the composition, and provides for easy application and even distribution of the composition on the surface of the skin.

Preparation of the inventive compositions provide a standard method of preparation of ointments and creams by mixing all members of cut directly mefenamico acid, enzymes, alcohol and water, and then the resulting mixture is introduced into the filler is a mixture of vaseline with lanolin and mix thoroughly to obtain a homogeneous mass.

The composition may further contain fragrance, which can use any suitable for this purpose alcoholic extracts or essential oils, such as eucalyptus, peppermint, and so on, Their number is selected empirically, traditional ways, but, as a rule, their content in the composition does not exceed 0.01 to 1.00 wt.%.

To give a composition with anti-allergic properties in its composition optionally enter any suitable for this purpose antiallergic drugs, such as diphenhydramine, pipolphen, suprastin, etc. in the amount of 0.02 to 0.05 wt.%.

As studies have shown, the use of the claimed composition allows you to completely arrest the initial stage of infection, to strengthen anti-herpes and reparative effects of the composition. This result is achieved due to the immunomodulatory effect arising from the application of this composition to the damaged surface of the skin or mucous membrane, enhancing the actions of the local cell specification the Oia.

Methods of surface and deep biopsy and indirect membrane immunofluorescence (MIF) ("Immunological methods", M, Medicine, 1987, S. 136) showed that the inventive composition has a stimulating effect on immunocompetent cells possessing antiviral activity of NK-cells (CD-16), T-cytological lymphocytes (CD-8), monocytes and macrophages (CD-23), as evidenced by comparison of their content before treatment and after 12 hours after application of the composition, namely before treatment the contents of the SD-16, SD-8 and SD-23 were respectively 1,9±0,14; 1,5±0,24 and 0.4±0,43, and 12 hours respectively 3,8±0,26; 5,8±0,3 and 4,6±0,26.

Strengthening of reparative processes in the lesion indicates an increased number of fibroblasts and Poliplast. So, before applying the composition fibroblasts were not found, and within 12 hours after application, their number amounted to 3,4±0.3 to. The same applies to polylactam that were not found before treatment and after 12 hours after application of the composition of their number amounted to 6,7±0,8.

It is known that glycyrrhizin acid, penetrating through the skin and the mucous membranes of the skin, acts on the herpes virus, located in the intercellular space (Century. In which notizie enhances the antiviral effect of the drug due to the inactivation of viruses not only in the intercellular fluid, but directly in the target cell, leading to more rapid relief of herpes virus infection and thus preventing further spread of herpes viruses, as evidenced by the increasing term remission of up to one year or more.

The inventive composition allows you to quickly remove the pain that accompanies herpes infection completely arrest the infectious process at the stage of latent symptoms (tingling, numbness), with a simultaneous increase in term remission of up to one year and more, and also reduce the duration of treatment clinical stage of the disease to 1-2 days.

The action of the inventive pharmaceutical composition has been tested in the clinic for skin and venereal diseases, VGA (Vladivostok state medical University).

The study included 22 patients with various forms of herpes simplex (11 genital herpes, 10 - labial herpes and 1 - herpes), including 16 women, 6 men aged from 18 to 36 years. 10 the observed patients progress has been recurrent in nature (no more than 3 relapses per year) and in 12 lesions developed for the first time. The clinical examination of patients with localized lesions in about the bubbles, filled with bright content, without signs of inflammation at the periphery of the lesion. In 5 of the 11 were observed erythema, swelling in the lesion, accompanied intensivnym burning and itching. In 6 of 10 patients with localized lesions in the area of the red portion of the lip process are grouped in small vesicles with serous content, and the remaining 4 - erosions, with serous-hemorrhagic crusts mucosa is edematous, hyperemic. In a patient with zoster was observed vesicles with serous content in the lumbar region, burning and itching. The control group consisted of 5 patients with genital herpes and 5-labialis who received outdoor therapy cream EPIGENOME.

In the group of observed patients was used for the external treatment of the claimed composition containing 45 g epiderma, 0.1 g of glycyrrhizic acid, 0.5 g mefenamovoy acid, dissolved in 10 ml of 50% ethanol, 0.02 g lidz, 9,38 g of purified water. These components were thoroughly mixed and then added to pre-prepared filler consisting of 30 g of vaseline and 5 g of lanolin. All are thoroughly mixed until a homogeneous creamy mass of light yellow color.

Prepago syndrome, 1-2 hours significantly reduced erythema, swelling. After 12 hours there is drying of the skin rash that is seen as clinical resolution of the disease. In the control group, lesions were resolved on a 4-6 day. Side effect in the form of meningeal phenomena, defeat conjuctiva eye after application of the claimed composition in the observed patients was not found.

Thus, the inventive pharmaceutical composition can be widely used in medical practice. It allows you to completely arrest the infectious process at the stage of latent signs of the disease, increases the period of remission of up to one year or more, reduces the period of treatment clinical stage of the disease to 1-2 days and may serve as a prophylactic treatment of herpes viral infections.

1. Pharmaceutical composition for treating herpes viral infections, containing glycyrrhizinic acid, a filler, and water purified, characterized in that the composition additionally contains a water-glycerol complex (2,3-DIXIPAY)-ortho-titanate hydrochloride, (epiderm) mefenamico acid (Acidum mephenamicum), protolytic enzymes and ethyl alcohol, and the filler is a mixture of

Glycyrrhizin acid of 0.1-1.0

Vaseline yellow medical 10,0-50

Anhydrous lanolin is 1.0-10.0

Mefenamovaya acid 0,4-1,0

Ethyl alcohol 3-10

Protolytic enzymes 0,01-0,4

Purified water Rest

2. The pharmaceutical composition under item 1, characterized in that it further contains an anti-allergic substance diphenhydramine or pipolphen or suprastin in the amount of 0.02 to 0.05 wt.%.

3. The pharmaceutical composition according to any one of paragraphs.1 and 2, characterized in that it further comprises an odorant in the form of alcoholic extracts or essential oils of eucalyptus and/or peppermint in an amount of 0.01 to 1.00 wt.%.



 

Same patents:

The invention relates to medicine, namely to the development of new combinations Antiherpes virus effect of actions

The invention relates to new biologically active phosphonate derivative of acyclovir

The invention relates to 4-hydroxy-3-chinainternational and hydrazides of General formula (I), where a represents a-CH2- or-NH-, a R1, R2, R3and R4such as defined in the claims

The invention relates to new 6-(3-acetylphenyl)aminouracil formula I, which stimulates the immune system and antiviral properties and can be used in the treatment of viral diseases caused by chlamydia, as well as diseases caused by immunodeficiency, in particular malignant tumors, and also in veterinary medicine

The invention relates to pharmacology and medicine and relates to investigation of new anti-virus tools

The invention relates to the field of medicine and for new dosage forms of demoliton

The invention relates to the field of medicine and pharmacology and applies to new effectors of interferon against viruses genital herpes and human papilloma
The invention relates to medicine, namely to skin diseases, and can be used to treat herpesvirus infections
The invention relates to the field of veterinary medicine and relates to means for the treatment of infected wounds, abscesses, phlegmon, burns, mastitis, arthritis, bruises, hemorrhoids, vaginitis, endometritis, cervical erosion and fungal skin diseases of man and animals

The invention relates to the field of pharmaceutical industry and relates to means for treating diseases of the joints

The invention relates to medicine, more specifically to the treatment of wounds

The invention relates to the pharmaceutical industry and relates to a drug for treatment and prevention of pathological lesions of blood vessels and tissues
Drug // 2238730
The invention relates to medicine, namely to medicines broad-spectrum

The invention relates to medicine, specifically to non-steroidal anti-inflammatory drug Ketoprofen
The invention relates to the field of pharmaceutical industry and relates to anti-inflammatory, regenerative and anti-microbial action
The invention relates to the field of pharmaceutical industry and relates to nasal ointment for the prevention of inhalant allergic reactions
The invention relates to the field of medicine and cosmetology
The invention relates to medicine, namely to create medications in the form of ointments based on vegetable raw materials
Drug // 2238730
The invention relates to medicine, namely to medicines broad-spectrum
Up!