WO2014163520A1

WO2014163520A1 - Preparation for treating proctological, urological and gynaecological diseases

Info

Publication number: WO2014163520A1
Application number: PCT/RU2013/000273
Authority: WO
Inventors: Дмитрий Викторович ФРОЛОВ
Original assignee: Общество с ограниченной ответственностью "Гемодан"
Priority date: 2013-04-01
Filing date: 2013-04-01
Publication date: 2014-10-09

Abstract

The invention relates to medicine and concerns a combined preparation for treating diseases of the rectum and female genitalia (erosion, colpitis, condylomas, cysts, endometriosis, myomas, fibroids, polyps of various localisation, lesions resulting from surgical interventions), which can also be used in antineoplastic combination therapy. The technical result achieved by carrying out the claimed invention is to enhance the therapeutic effect of the drug dosage form presented as a suppository comprising effective active substances having anti-inflammatory, anti-microbial, local anaesthetic, wound healing, adaptogenic and anti-tumour properties for treating proctological, urological and gynaecological diseases. Said technical result is achieved in that the combined preparation "Gemodan" for treating proctological, urological and gynaecological diseases in the suppository form comprises diosmin as an active substance, and glycerides of fatty acids as a pharmaceutically acceptable suppository base, and further comprises an oil extract of a medicinal mud from Lake Tambukan and kamellin as bioactive active substances, wherein the total suppository weight is from 1.0 to 3.0 g and the component ratio is, in g: diosmin 0.05-0.2, oil extract of medicinal mud from Lake Tambukan 0.1-0.3, camellin (green tea extract) 0.05-0.2, suppository base - glycerides of fatty acids (the remainder).

Description

DRUG FOR TREATMENT OF PROCTOLOGICAL, UROLOGICAL AND GYNECOLOGICAL DISEASES

Technical field

The invention relates to medicine and relates to a combined preparation for the treatment of diseases of the rectum and female genital area (erosion, colpitis, condylomas, cysts, endometriosis, fibroids, fibromyomas, polyps of various localization, adhesions after surgical interventions), and can also be used in complex therapy neoplasms.

The drug belongs to the new generation of rectal suppositories, which combines a set of innovative technologies that can significantly improve the effectiveness and quality of proctologic services.

State of the art

The French patent FR 6967M, 1969, which first shows the possibility of using diosmin (7 - [[6-0 - (- deoxy-alpha-b-mannopyranosyl) -beta-0-glucopyranosyl] oxy] -5 is known from the prior art. -hydroxy-2- (3-hydroxy-4-methoxyphenyl) -4H-1-benzopyran-4-one) obtained by dehydrogenation of hesperidin (3 ^ 5,7-trihydroxy-4'-methoxyflavonone-7 noglucoside), as well as pharmaceutical a composition containing diosmin as an active substance separately and in combination with hesperidin and citroflavonoids for the treatment of pathologies associated with fragility of capillaries. Known pharmaceutical composition can be performed in various dosage forms: capsules, tablets, granules, suspensions, creams, suppositories. The ratio of diosmin: hesperidin: citroflavonoids in the composition is 1: 1: 0.5 (in May. Parts).

Tablets according to the known invention contain:

Diosmin 100 mg

Hesperidin 100 mg

Citroflavonoids 50 mg

Rice starch 40 mg

Talcum powder rest

Candles according to the known invention contain:

Diosmin 0.100 g Hesperidin 0.100 g

Citroflavonoids 0.050 g

Semi-synthetic glycerides Up to 3 g

The pharmacological effect of diosmin is manifested in increased venous tone, capillary resistance, decreased venous stasis, capillary permeability, and improved microcirculation (Russian Drug Register. Encyclopedia of Medicines. M.: RLS-2002, p.305).

Diosmin - a bioflavonoid, in combination with hesperidin, has a venotonic and angioprotective effect, increases tone and reduces the extensibility of veins, which helps to reduce venous stasis; lowers the permeability of capillaries and increases their resistance; improves microcirculation and lymph drainage. The combination of diosmin with hesperidin provides a fairly high pharmacological effect. However, according to the instructions, hesperidin can cause digestive disorders, manifested as belching, heartburn and a feeling of pressure in the abdomen, as well as symptoms of a neurovegetative disturbance. The use of drugs containing hesperidin, with exacerbation of hemorrhoids does not replace the specific treatment of other anal disorders.

Disclosure of invention

The problem to which the present invention is directed, is to expand the raw material base for the production of a dosage form in the form of a suppository containing diosmin and biologically active active substances.

The technical result achieved by the implementation of the claimed invention is to increase the therapeutic effect of the dosage form in the form of a suppository containing active active ingredients having anti-inflammatory, antimicrobial, local analgesic, wound healing, adaptogenic and antitumor properties for the treatment of proctological, urological and gynecological diseases. The combined preparation completely restores the normal state of the tissues of the anorectal region and is highly effective in the absence of side effects and complications. The drug "Hemodan" provides a complex effect on all organs of the anorectal region, due to the complex of constituent active substances, normalization of tissue microcirculation occurs, and, as a result, improvement of venous outflow and achievement of a stable therapeutic effect. Stabilization of local metabolism allows you to create a favorable background for eliminating the disease, and the natural origin of the components - to treat the underlying disease and eliminate the associated pathology.

The specified technical result is achieved by the fact that the combined preparation “Hemodan” for the treatment of proctological, urological and gynecological diseases in the form of suppositories contains diosmin and a pharmaceutically acceptable base of the suppository of fatty acid glycerides as an active ingredient, and additionally contains biologically active active ingredients an oil extract of the healing mud of the lake Tambucan, camelline with a total mass of suppository from 1.0 to 3.0 g and the following ratio of components, in g:

Diosmin 0.05 - 0.2

Mud oil extract Tambucan 0.1 - 0.3 Camellin (Green tea extract) 0.05 - 0.2 Suppository base:

Fatty acid glycerides (rest)

Moreover, the resulting suppositories have the following physicochemical characteristics:

Color - Light Yellow.

The suppository form is torpedo-shaped with a smooth waxy surface.

Melting point - not higher than 35 ° С

Full deformation time - no more than 15 minutes.

Experimentally, the compositions of the claimed preparation were selected and it was found that high results in compatibility with the suppository base and in the therapeutic effect were achieved when using fatty acid glycerides as the base. In one embodiment, suppositories contain solid fat as a suppository base as glyceride. In another embodiment, suppositories contain cocoa butter or witepsol as a suppository base. At concentrations of active substances: diosmin below 0.05 g, oil extract of the therapeutic mud of Lake Tambukan below 0.1 g and camellin below 0.05 g, the therapeutic activity of the composition decreases. At concentrations of the active substances of diosmin above 0.2 g, there is no oil extract of the therapeutic mud of Lake Tambukan above 0.3 g and camelline above 0.2 g increased therapeutic effect, and may lead to an overdose of active substances.

Introduction to the combined preparation "Hemodan" for the treatment of proctological, urological and gynecological diseases of diosmin helps to increase the tone of the veins, reduces venous congestion and the volume of venous stasis. In addition, its content in the specified dose has a vasoconstrictive effect on the veins and is dose-dependent in nature, thereby increasing the resistance of capillaries, decreasing their permeability, and improving microcirculation of tissues. Diosmin has an angioprotective effect, resulting in increased vascular resistance, systolic and diastolic pressure with orthostatic hypertension in the postoperative period, and improved lymphatic drainage of blood vessels.

The use of the oil extract of the therapeutic mud of Lake Tambukan in the Hemodan combined preparation, which has immunomodulating, antioxidant, anti-inflammatory, antibacterial action, in turn, actively stimulates the regenerative processes in the tissues. The therapeutic effect of the mud is due to the organic substances of the healing mud, macro and microelements contained in the extract.

The introduction of the active natural antioxidant Camellin (extract of green tea) into the suppository prevents the damage to cellular structures by free radicals and has an anti-inflammatory and antioxidant effect. The substance Camellin is made from a dry extract of green tea, obtained from the leaves of Chinese Tea (Camellia sinensis), the Theaceae family, in appearance it is a finely divided powder from greenish brown to dark brown in color with a faint specific smell. Camellin contains in its composition natural polyphenolic compounds having a basic structure of C6-C3-C6 in an amount of at least 75%. The main substances are flavan-3-ol derivatives represented by epicatechin, catechin gallate, epicatechin gallate, gallocatechin gallate and flavanon-3-ol derivatives, quercetin, dihydroquercetin.

Identification and quantification of the sum of polyphenols are based on redox reactions provided by phenolic groups. Antioxidant properties are due to the presence of a large number of phenolic groups in the structure of green tea catechins, which are “traps” of free radicals (Zenkov N.K., Kandalintseva N.V., Lankin V. 3., Menitsikova E. B., Prosenko A. E. Phenolic bioantioxidants - Novosibirsk, 2003). According to the pharmacological action, the polyphenols of the substance Camellin are powerful natural antioxidants with a wide spectrum of biological activity.

Diosmin 0.1

Tambucan Lake Mud Oil Extract 0.25 Camellin (Green Tea Extract) 0.1 Suppository Base:

Solid fat (rest)

The basis for suppositories, solid fat is melted at a temperature of 60-65 ° C, mixed, cooled to a temperature of 35-36 ° C.

Active pharmaceutical substances (APS): diosmin, camellin, oil extract of tambucan mud, loaded into a prepared base, homogenized to obtain a homogeneous mass.

The resulting suppository mass is packaged in a cell package from a film of polyvinyl chloride (type EP-73). The temperature of the suppository mass is 37-38 ° C. The average mass of the suppository is 2.0 g.

The resulting suppositories have the following physico-chemical characteristics:

Color - Light Yellow.

The suppository form is torpedo-shaped with a smooth waxy surface.

Melting point - 32.1 ° С not higher than 37 ° С.

They are used mainly at night for 1-2 suppositories. The course of treatment is 10-14 days.

Example 2

Composition per 1 candle weighing 2.55 g:

Diosmin 0.15 g

Oil extract of therapeutic mud of Tambukan lake 0.25 g

Camellin (Green Tea Extract) 0, 15 g Suppository base:

Cocoa Butter (rest) The basis for suppositories cocoa butter is melted at a temperature of 60-65 ° C, mixed, cooled to a temperature of 35-36 ° C.

The resulting suppository mass is packaged in a cell package from a film of polyvinyl chloride (type EP-73). The temperature of the suppository mass is 37-38 ° C. The average weight of the suppository is 2.55 g.

Color - Light yellow to light brown.

The suppository form is torpedo-shaped with a smooth waxy surface.

Melting point - 32.1 ° С not higher than 37 ° С.

They are used mainly at night for 1-2 suppositories. The course of treatment is 10-14 days. Example 3

Composition per 1 candle weighing 2.0 g:

Diosmin 0.15 g

Oil extract of therapeutic mud of Tambukan lake 0.25 g

Camellin (Green Tea Extract) 0.15 g

Suppository base:

Vitepsol (rest)

The basis for Vitepsol suppositories is melted at a temperature of 60-65 ° C, mixed, cooled to a temperature of 35-36 ° C.

Color - Light Yellow.

The suppository form is torpedo-shaped with a smooth waxy surface.

Melting point - 32.1 ° С not higher than 37 ° С. They are used mainly at night for 1-2 suppositories. The course of treatment is 10-14 days.

The combined preparation "Hemodan" for the treatment of proctological, urological and gynecological diseases in the form of suppositories is a highly effective therapeutic agent used in patients with anorectal pathology, as well as the treatment of diseases of the female genital area. An advantage of the claimed invention is a complex effect on all organs of the anorectal region, due to the active complex of constituent substances, the venous outflow is improved, a stable therapeutic effect is achieved, in addition, local exposure to tissues reduces the need for enteral and parenteral administration of the necessary drugs. Candles do not cause side effects, convenient to use.

Claims

CLAIM

1. The combined preparation "Hemodan" for the treatment of proctological, urological and gynecological diseases, containing as an active substance diosmin and a pharmaceutically acceptable suppository base of fatty acid glycerides, characterized in that it additionally contains biologically active active substances, extract of therapeutic mud of Lake Tambukan, Camellin with a total the mass of the suppository from 1.0 to 3.0 g and the following ratio of components, in g:

Diosmin 0.05 - 0.2

Oil extract of the therapeutic mud of Lake Tambukan 0.1 - 0.3 Camellin (Green Tea Extract) 0.05 - 0.2 Suppository base:

Fatty acid glycerides (rest)

2. The combined preparation "Hemodan" for the treatment of proctological, urological and gynecological diseases according to claim 1, characterized in that solid fat or cocoa butter, or vitepsol, is used as fatty acid glycerides.