KR100257228B1 - Cosmetic formulations containing esculoside - Google Patents

Abstract

The present invention relates to compositions comprising only esculosides in the treatment of vasculature associated with peripheral microcirculatory disorders, celluloses associated with the accumulation of excess fat or cosmetic purposes or between adenosine such as phospholine or salvia Milthiohirza diterpene. A composition comprising a combination of phosphodiesterase inhibitors such as clase stimulating substances and / or apigenin-skeletal dimer flavones and esculosides. In order to reduce excess fat accumulation from any source, the abovementioned products are preferably combined with caffeine, theophylline and derivatives thereof.

Description

Cosmetic formulations containing esculosides

The present invention is a composition that is used locally in peripheral vascular disorders associated with peripheral microcirculation disorders, comprising only esculoside or forskolin or Salvia miltiorrhiza diterpenes Adenosine cyclase stimulant and / or a phosphodiesterase inhibitor such as apigenin-skeletal dimer flavone and an esculoside. The present invention also relates to cellulitis associated with excess fat accumulation, either alone or in combination of esculoside with the adenic acid cyclase stimulant and / or the phosphodiesterase inhibitor. It relates to a method for use in treatment for cosmetic purposes. In the latter case, caffeine, theophylline, pentoxifylline can be added to the above-mentioned products.

The present invention also relates to esculoside alone or in combination with esculoside and phosphodiesterase inhibitors such as adenosine cyclase stimulants such as phospholine or salvia Milthiorza diterpene or apigenin-skeleton dimer flavones. To a process for use in preparing the above-mentioned compositions.

Esculoside is a glucosided coumarin extracted from fruit bark and Aculus hippocastanum bark, which has long been used to treat permeability disorders and diseases associated with capillary weakness. ), It is still used for topical or systemic administration and treatment of ophthalmic decongestants.

The technical problem to be achieved by the present invention is to provide a cosmetic composition useful in the treatment for cellulose or cosmetic purposes associated with excess fat accumulation by including esculoside as an active ingredient.

1 is a diagram showing the change of various variables before and after anti-cellulose treatment.

In order to achieve the above technical problem, in the present invention, the active ingredient is composed of a combination of esculoside, adenic acid cyclase stimulant and / or phosphodiesterase inhibitor and / or lipolytic agent, between the adenic acid Claes are selected from the group consisting of phospholine, salvia Milthiohiza diterpene and mixtures thereof, wherein the phosphodiesterase inhibition is apigenin-skeletal dimer flavone and the lipolytic agent is caffeine, theophylline, pentoxifylline Or a mixture thereof.

Preferably, the flavone is selected from the group consisting of ginkgo dimer flavones and amento flavones.

Surprisingly topical administration of esculoside alone or in combination of esculoside and the above-mentioned products results in arterial blood flow at the site of administration (activity on pre-capillary artery that increases muscle cells of the artery and its pulse). It has been found that by increasing the number of capillary vessels perfused, the surface and deep microcirculation are improved. This phenomenon can be measured by noninvasive techniques such as infrared photopulsoplethysmography, laser doppler flowmetry and computerized videocapillaroscopy. The former two techniques can represent the vascular movement of arteries and precapillary arterial arteries, whereas the latter technique can measure capillary and regional vascular structural changes. After the basic data have been recorded, a placebo composition or a composition containing the active or active ingredient is administered to the part of the body to be treated, usually two symmetrical body parts are used to test randomly. Immediately after treatment, the treated area was checked with a video capillary microscopy (Scopemann-Mortex video imaging system, Alpha Instruments, Milan) equipped with a halogen light optical probe at 50 to 400 × magnification, and then capillaries Density (the number of capillaries through the blood per unit surface area), capillary spatial orientation, and shape thereof are evaluated. The device is equipped with a video camera capable of continuously recording biomicroscopic images, so that any change during moving picture can be quantitatively measured. After 20 minutes of treatment with esculoside alone or with the above-mentioned products, cited as the most important compounds, such as esculoside and ginkgo biloba dimer flavones or amentoflavones, the capillary density is at baseline. Rises 200-300% compared to the placebo treated control. The action of esculosides in the 0.5% to 3% concentration range is assessed as described above and lasts for one to three hours.

As mentioned above, skin microangiology can be evaluated by videocapillaroscopy to determine spatial orientation and its stratification, as well as the number of perfused capillaries.

As part of the present invention, a composition comprising only esculoside and compounds having esculoside and adenic acid cyclase stimulating activity or antiphosphodiesterase activity and also optionally caffeine, theophylline, pentoxifylline and the like When a combination of other lipolytic agents is administered to a site with chronic venous insufficiency, such as cellulose, or where a cosmetic excess of fat is required to force a diet, local microcirculation may be re-elected due to esculoside. It has been surprisingly found that the symptoms of the disease are significantly alleviated due to the lipolytic effects of other components. Dosing takes several days to several months, usually three months, depending on the severity of the pathology or non-interesting.

As long as the vascular system is involved, esculoside alone or in combination with esculoside and antiphosphodiesterase or adenic acid cyclase stimulants, cold-induced vasospasm, especially at the finger and toe microcirculation levels. In addition, it can be used for chronic venous insufficiency, Raynaud's disease and terminal blue-blue disease. At the site treated with the active ingredient, more blood flow also acts effectively on premature aging of the skin, in particular facial and neck skin, subcutaneous fat histopathology such as cellulose, and stretch spots (skin atrophy); Also works effectively on skin that is not as smooth as scalp and is useful for treating primary and secondary alopecia.

In the field of cosmetics, the main use of the desired product of the present invention is related to skin aging and cellulose, which affects many people in industrialized countries.

As an example for the uses described above, the thigh site for three months divided into two groups of 20 patients suffering from chronic venous insufficiency (Phase 1) divided into two groups twice a day for three months From to ankle.

Before long-term treatment, patients underwent acute testing by video microscopy measurements of skin microcirculation increases to assess their responsiveness. The capillary density of the placebo-treated group was measured 20 minutes after treatment, which was 8.6 ± 2.2% when calculated by the Student's test at p <0.01, whereas it was 18.6 ± 3.1% in the group treated with esculoside.

The observed symptoms and their extent are shown in the following table, with a rating of 0-4.

For thigh cellulose caused by chronic venous insufficiency, 1.5% esculoside, 0.3% Salvia Milthiorhiza extract (which contains 15% tansinone A2) for 20 groups of subjects, Treatment was performed for 3 months from the thigh site to the ankle with a composition comprising 0.4% ginkgovillava dimer flavone (made according to Indena patent EP 0360556) and 0.2% theophylline. As can be seen from the data described in FIG. 1, the variables observed in these subjects changed dramatically.

In another test, a composition comprising 1.5% esculoside, 0.3% Salvia Miltiohiza extract and 1% pentoxifylline for 20 groups of 20 subjects with fibrosclerosis fatty disease at the femoral site with excess fat accumulation Treated for 2 months. The main control parameter was to remove excess fat deposits so thigh diameters were measured; The diameter was surprisingly reduced by 2.6 ± 0.2 cm.

In addition, numerous tests have been carried out for the treatment of the above mentioned pathologies and cosmetic purposes by varying the composition and component proportions or the nature of the components. In addition to the active ingredients mentioned above, the compositions according to the invention comprise conventional carriers, additives, preservatives and the like, which are known in the pharmaceutical art, as described in the following non-limiting examples.

Example I-Gel Containing Esculoside, Salvia Milthirhiza Extract and Ginkgovillava Dimerflavones.

Per 100 g of gel:

Salvia Miltiohiza Extract 0.30g

Escool Seed 1.50g

Ginkgo Biloba Dimer Flavones 0.50g

Hydrogenated Castor Oil 40 (OE)

(Cremopher RH40-BASF) 1.00 g

Propylene Glycol 1.50g

Preservative 0.10g

Hydroxyethyl cellulose

(Nitrosol 250 HHX-Achelon) 3.00 g

Adjust to 100 g using an appropriate amount of purified water.

Example II-Alcohol Fluid Gel Containing Salvia Miltiohiza Extract and Caffeine.

Per 100 g of gel:

Salvia Miltiohiza Extract 0.25g

Escool Seed 1.50g

0.50 g caffeine

Hydrogenated Pizza Horse Oil 40 (OE)

(Chromopher RH40-BASF) 5.00 g

Propylene Glycol 3.00g

Carbomer 940

Carbopol 980-Good Rich 1.00g

Ethanol 45.00g

Phosphatidylcholine (phospholipone 90-nater only) 0.70 g

Glyceryl 6 (OE) Caprylate / Kyprinate

(Softgen 767) 15.00g

Preservative 0.40g

0.05 g butylhydroxytoluene

0.20 g of α- (tocopherol)

0.30 g of ascorbic acid

Dimethicone Copolyol

(SF 1188-General Electric) 2.00 g

10% triethanolamine solution `5.00 g

Use purified water to adjust to 100g

Example III-Cream containing E. coloside, Salvia Miltiohiza extract and Cola Nut Extract titrated with caffeine alkaloids.

Per 100 g of cream:

Salvia Miltiohiza Extract 0.25g

Escoloside 1.50g

Cola Nut Dry Extract

(14% Total Alkaloids) 0.50g

Hydrogenated Pharma Oil 40 (OE)

(Cremopher RH40-BASF) 2.00 g

Propylene Glycol 2.00g

Carbomer 934

(Carbopol 934 P-Goodrich) 0.50 g

Acrylate / Alkyl C _10-30- acrylate _crosspolymer

(Carbopol 1382-Goodrich) 0.50 g

Ethanol 15.0 g

Preservative 0.40g

Cetyl Palmitate (Cutina CP-Helkel) 8.00 g

Polyisoprene (Centesupen-Baby) 5.00g

2.00 g of plysorbate 80 (twin 80-ICI American)

0.20 g of α-tocopherol

Ascorbyl Palmitate 0.10g

5.0 g hydrogenated lanolin (lanoselina-esperis)

Dimethicone 350cps (Tegisiloxane 350-Tego) 0.50 g

2.40 g of 10% sodium hydroxide solution

Use purified water to adjust to 100g

Example IV-Losshon containing Eskoloside and Theophylline.

Per 100ml lotion:

Esculoside 1.00g

Theophylline 0.50 g

Butylhydroxytoluene 0.10g

Adjust 50ml of ethyl alcohol to the appropriate amount.

Example V-Emulsified Gelling Emulsion

Per 100 g of gelling emulsion:

Esculoside 1.00g

Isopropyl myristate 5.00g

Preservative 0.40g

0.10 g of spices

Polyacrylamide, C _13-14 isoparaffin and lauryl alcohol 7 (OE)

(Sepigel 305-Sepic) 3.00 g

Use purified water to adjust to 100g.

At the site treated with the active ingredient of the cosmetic composition according to the invention, more blood flow also acts effectively on premature aging of the skin, in particular facial and neck skin, subcutaneous fat histopathology such as cellulose and stretch spots (skin atrophy). . In addition, more blood supply also works effectively on skin that is not as smooth as the scalp and is useful in treating primary and secondary alopecia.

Claims (2)

a) eskuloxide; b) an adenic acid cyclase stimulant selected from the group consisting of phoscholine, salvia milthiohirza diterpene and mixtures thereof; c) phosphodiesterase inhibitors that are apigenin-skeletal dimer flavones; And / or d) a cosmetic composition comprising a lipophilic agent selected from the group consisting of caffeine, theophylline, pentoxifylline or mixtures thereof. The cosmetic composition of claim 1 wherein the flavone is selected from the group consisting of ginkgo dimer flavones and amento flavones.