Combinations of vasoactive agents, their use in pharmaceutical and cosmetic fields and concentration thereof

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to a composition and a combination for treating panniculopathy and problems associated with venous insufficiency of the lower limbs. The composition for treating panniculopathy and problems associated with venous insufficiency of the lower limbs, containing esculoside and at least one compound selected from icarine or its derivatives, or extracts containing it (them), Gingko biloba dimer flavones in a free form or complexed with phospholipids, amentoflavone and at least one compound selected from escin, escin beta sitosterol complexed with phospholipids, sericoside, sericoside complexed with phospholipids, or Centella asiatica extract in a free form or complexed with phospholipids. The use of the combination on the basis of the mentioned ingredients for preparing the composition for treating panniculopathy and problems associated with venous insufficiency of the lower limbs.

EFFECT: above-described composition and combination are effective in reducing panniculopathy and problems associated with venous insufficiency of the lower limbs.

 

The technical field to which the invention relates.

This invention relates to combinations of vasoactive substances that act on venous or arterial level with phosphodiesterase inhibitors, including cGMP phosphodiesterase V.

The prior art inventions

Visnadin is a coumarin, mainly found in the seeds of Ammi visnaga, a plant traditionally used for the treatment of engineerig violations. The connection used in the pharmaceutical industry as coronary dilatator.

It was also shown that the local application of this compound has a strong associationsin effect on precapillary arteries and arterioles and increases the blood flow and tissue perfusion (EP 0418806). Supply of tissue blood includes better nutrition and elimination of waste products of metabolism, with resulting beneficial effects on the treated area. Visnadin also has antitopoisomerase activity.

Escalated, coumarin glucoside present in many plants, such as Aesculus hippocastanum, Fraxinus communis, etc. has associationsin action and inotropes activity and venous and arterial levels.

Icarin and its derivatives, which have an effect on the cGMP phosphodiesterase V, suitable as activators of microcirculation in certain areas.

The AMA is toplivo is belawan, present in small amounts in many plants such as Gingko biloba, Brakeringea zanguebarica and Taxus sp.

Saponins from horse chestnut or Centella asiatica effect on the venous and lymphatic system, where they exert a powerful effect, which facilitates the drainage of lymph.

Description of the invention

The invention relates to pharmaceutical, dietary, cosmetic or nutraceutical composition including:

- visnadin or escalated;

at least one compound selected from Carina or its derivatives or its containing extracts of dimeric flavones Gingko biloba in free form or komplikovanih with phospholipids, and amentoflavone;

at least one compound selected from escin, escin beta-sitosterol, completed with phospholipids, seriesid, seriesid, kompleksowego with phospholipids, or extract of Centella asiatica, in free form or kompleksowego with phospholipids.

The combination of vasoactive substances corresponding to the invention, which operates simultaneously on arterial and venous and lymph drainage, which reduces congestive edema, which is one of the first symptoms of chronic venous insufficiency, with pathological consequences since cellulite and ending with leg ulcers of different etiology. A warning signal is s circulatory insufficiency of the lower extremities include skin temperature is below the normal level a feeling of heaviness in the legs and acrostichoides syndromes with peripheral pain. Have been made various attempts to treat these symptoms, but with little success.

Currently, it has been unexpectedly found that compositions corresponding to the invention contain compounds with different mechanisms of action, prevention of peripheral vascular and tissue degeneration.

The most common disease is cellulite or degenerative panniculopathy.

Prior to the formation of painful fibrous nodules or fat due to degeneration of adipocytes, cellulite is caused by filtration of liquids and protein in perivascular space in the result of venous insufficiency. Due to mechanical compression of the resulting swelling reduces circulation of blood blood flow.

Under these circumstances adipocytes accumulate fats, increase and take away space from other cells. For maximum effect anti-cellulite treatment compositions must begin from this moment. The combination corresponding to the invention facilitates the treatment in pre-pathological stage, to prevent its progression to peripheral damage. Even when the violation has become chronic, the same composition can also CSS is used to apply for the long term treatment to eliminate pain and reduce unwanted fat mass, through stimulation of lipase-induced persistence of cyclic nucleotides in the tissues.

Derivatives of Ikaria, which can be used according to the invention, as an alternative to Carino include 7-hydroxyethylation, 7-ethylaminoethanol, 7-aminoacylation, 7-hydroxyethyl-3-0-remedilean, 7-amino-ethyl-3-remedilean, 8-dihydroequilin and their glucosides in positions 7 and 3, and 7-hydroxyethyl-7-desloratadin.

Compositions corresponding to the invention preferably contain visnadin.

Compositions corresponding to the invention usually have the following intervals concentrations by weight:

- visnadin or escalated: 0.05 to 2%;

- dimers of amentoflavone or Gingko biloba in free form or komplektovanie with phospholipids: 0,1-1%;

- icarin or its derivatives or extracts containing it: 0,1-1%;

at least one compound selected from the number of escin, escin beta-sitosterol, kompleksowego with phospholipids, seriesid, seriesid, kompleksowego with phospholipids or extract of Centella asiatica, in free form or kompleksowego with phospholipids: 0,5%-2%.

These compounds can be introduced in the most common pharmaceutical and cosmetic compositions, such as oil-in-water and water-in-oil emulsion, portable respectively fillers, surfacename and solubilization.

To the ome, for treatment of large areas of skin products can be produced in the form of a cream, jelly and gel.

The following examples illustrate the invention in detail.

Example 1 - gel composition

Visnadin0.25 g
7-hydroxyethyl-7-desloratadin0.35 g
Amentoflavone0.25 g
Escin1,00 g
Lecithin20,00 g
Cholesterol0.50 g
Ethanol8.00 g
Equivalent0.01 g
Imidazolinone0,30 g
The hypromellose2,00 g
Waterqs to 100 g

Example 2 - gel composition

Esculated1,00 g
0.35 g
Amentoflavone0.25 g
Escin1,00 g
Lecithin20,00 g
Cholesterol0.50 g
Ethanol8.00 g
Equivalent0.01 g
Imidazolinone0,30 g
The hypromellose2,00 g
Waterqs to 100 g

Example 3 gel composition

Visnadin0.25 g
7-hydroxyethyl-7-despotically0.35 g
The dimers Gingko biloba, komplektovanie with phospholipids0.25 g
Escin beta-sitosterol, komplikovany with phospholipids1,00 g
LecithinCholesterol0.50 g
Ethanol8.00 g
Equivalent0.01 g
Imidazolinone0,30 g
The hypromellose2,00 g
Waterqs to 100 g

Example 4 gel composition

Esculated0.25 g
7-hydroxyethyl-7-despotically0.35 g
Amentoflavone0.25 g
Seriesid1,00 g
Lecithin20,00 g
Cholesterol0.50 g
Ethanol8.00 g
Equivalent0.01 g
Imidazolinone0,30 g
The hypromellose2,00 g
Waterqs to 100 g

Example 5 - gel composition

Visnadin0.3 g
Amentoflavone0.4 g
Extract of Centella asiatica1.0 g
Lecithin20,00 g
Cholesterol0.50 g
Ethanol8.00 g
Equivalent0.01 g
Imidazolinone0,30 g
The hypromellose2,00 g
Waterqs to 100 g

1. Composition for the treatment of panniculopathy and problems associated with venous insufficiency of the lower extremities, including:
- escalated;
at least one compound selected from Carina or its derivatives, or containing it(them) extras the mswb, dimeric flavones Gingko biloba in free form or komplikovanih with phospholipids, amentoflavone;
at least one compound selected from escin, escin beta-sitosterol, kompleksowego with phospholipids, seriesid, seriesid, kompleksowego with phospholipids, or extract of Centella asiatica in free form or kompleksowego with phospholipids.

2. The composition according to claim 1, having the following intervals concentrations by weight:
- esculated: 0.05 to 2%;
- icarin or containing extracts, dimeric flavones Gingko biloba in free form or komplektovanie with phospholipids, amentoflavone: 0,1-1%;
- escin, escin beta-sitosterol, komplikovany with phospholipids, seriesid, seriesid, komplikovany with phospholipids, or extract of Centella asiatica in free form or komplikovany with phospholipids: 0,5-2%.

3. The composition according to claim 1, in which the derivatives of Ocarina include 7-hydroxyethylation, 7-ethylaminoethanol, 7-aminoacylation, 7-hydroxyethyl-3-0-remedilean, 7-amino-ethyl-3-remedilean, 8-dihydroequilin and its glucosides in positions 7 and 3, and 7-hydroxyethyl-7-desloratadin.

4. Composition according to any one of claims 1 to 3 in the form of creams, gel, lotions, jelly.

5. The composition according to claim 1, containing escalated, icarin, amentoflavone, escin.

6. The composition according to claim 1, containing escalated, dimeric flavones Gingko biloba, komplektovanie with the phospholipids is, of escin beta-sitosterol, komplikovany with phospholipids.

7. Applying a combination of:
- escalated;
- Ocarina or containing extracts of dimeric flavones Gingko biloba in free form or komplikovanih with phospholipids, amentoflavone;
at least one compound selected from escin, escin beta-sitosterol, kompleksowego with phospholipids, seriesid, seriesid, kompleksowego with phospholipids, or extract of Centella asiatica in free form or kompleksowego with phospholipids, to obtain a composition for the treatment of panniculopathy and problems associated with venous insufficiency of the lower extremities.



 

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