Composition for the treatment of hirsutism

 

(57) Abstract:

The invention relates to medicine, in particular to pharmacology, and can be applied endocrinology and dermatology as a means of treatment of hirsutism. The invention is a composition containing the active substance naftolin, peach butter, emulsifier N 1, sorbic acid and water in the following ratio, wt.%: naftolin 2,38-2,62, oil peach 19,00-21,00, emulsifier N 1 6,65-7,35, sorbic acid 0,19-0,21, water - the rest. The proposed composition effective when applied externally to remove hair from the skin and from the skin of the hands and feet and provides increase of its effectiveness at removing hair.

The proposed composition relates to medicine, in particular to pharmacology, and can be applied in the field of endocrinology and dermatology as a means of treatment of hirsutism.

When hirsutism in women, excessive hair growth on the face.

Increased growth of facial hair in women is often the result of dysfunction of the endocrine glands.

Depilatory tools used for hair removal with cosmetic or therapeutic purposes.

Bolshevist hydrogen sulfide, which causes crumbling and dissolving corticofugal layer of the hair, with the result that they fall away. The action of hydrogen sulfide reinforce the introduction of the caustic alkalis.

Closest to the proposed composition of the essential features is known composition for the treatment of hirsutism, which the authors selected as a prototype.

This composition produces a firm Roussel Zaboritories (UK) and which contains as active substance calcicolous SCu2CO2Ca 3H2O molecular weight 184,2 and water in the following ratio, wt.%:

Calcicolous - 2,5

Water - the Rest

The composition is applied to hair at their base and keep until the end of the process no hair.

Thus calcicolous causes crumbling and destruction cartilage layer of the hair, with the result that they fall away, but after deleting continue to grow, because hair follicles embedded in the skin not exposed to depilatory because calcicolous is not an antagonist of the androgen 1.

The objective of the proposed structure is to increase its effectiveness at removing hair.

Set is the quality of the active substance it contains naftolin and additionally contains oil of peach, emulsifier N 1, sorbic acid, in the following ratio, wt.%:

Neftali - 2,38 - 2,62

Peach oil - 19,00 - 21,00

Emulsifier N 1 - 6,65 - 7,35

Sorbic acid - 0,19 - 0,21

Water - The Rest.

The distinguishing characteristics are that the composition as the active substance contains naftolin and additionally peach butter, emulsifier N 1, sorbic acid, in the following ratio, wt.%:

Neftali - 2,38 - 2,62

Peach oil - 19,00 - 21,00

Emulsifier N 1 - 6,65 - 7,35

Sorbic acid - 0,19 - 0,21

Water - The Rest.

Naftolin

4-nitro-3-triftormetilfullerenov

The structural formula

< / BR>
Brutto - formula C11H11F3N2O3.

Molecular weight 276,22.

Crystalline powder yellow or yellow with a greenish tinge, with a faint aromatic odor. Easily soluble in alcohol, practically insoluble in water. Is peripheral androgen antagonist and prevents the manifestation of the effects of male sex FSH in the skin. Pharmacological properties of naftalina caused by blockade of the interaction of androgens with their cellular receptor is placed trophism of the skin in the composition of the injected oil peach.

Peach oil is a clear light yellow liquid, odorless or with a faint characteristic odor.

The introduction of the surface-active substances (surfactants) emulsifier N 1 provides penetration ability of naftalina at the level of the dermis in the skin and its localization in folicular that eliminates deep resorption of naftalina in tissue and blood.

Emulsifier N 1 - fused mixture of high molecular weight alcohols qaszalataolo fat or synthetic fatty alcohols with sodium salt of sulfonic ethers of such alcohols.

Is a solid mass, practically insoluble in water. Melting point 50-58oC. Broadcasting the number of 3 - 7. The content of high molecular weight alcohols of not less than 92%.

Sorbic acid is used for bacteriostatic ensure ointment.

Sorbic acid - 2,4 hexadienoic acid

CH3-CH=CH-CH-CH-COOH

Brutto - formula C6H8O2< / BR>
White crystalline powder, melting point 134-135oC.

Introduction to the composition of naftalina at a concentration of 2.38-2,62 wt.% established experimentally in vitro and in vivo using 3H-naftalina and pharmacologically recognized Gator N 1 6,65-7,35, acid sorbic 0,19-0,21 is also optimal and installed experimentally on animals radioisotope method and the ability of naftalina to percutaneous absorption of the emitted compositions ointments.

The optimal concentration of the components in the proposed composition is due to the fact that the introduction of naftalina less of 2.38 wt.% reduces the effectiveness of hair removal on the skin, and the introduction of nifida more 2,62 wt.% may result in the application of allergies.

The introduction of the peach butter is less 19,00 wt.% reduces penetration into the skin of the active substance, and more than 21 wt.% to increase maguuma surface and ointment are not fully absorbed into the skin.

With the introduction of the composition of the emulsifier N 1 less of 6.65 wt.%, the composition rapidly exfoliates and its validity period is reduced, and the introduction of more 7,35 wt.% the composition is thick and this makes it difficult to apply to the surface of the skin.

The introduction of the acid sorbic less to 0.19 wt.% leads to mildew, and more of 0.21 wt.% leads to a more acidic environment of the composition, which causes deterioration of the structural stability of the proposed structure.

The proposed composition is prepared as follows:

in the reactor for the cookingoC. Then, while operating the stirrer in the reactor is drained pre-melted emulsifier at a temperature of 75-85oC.

As the mixture is injected solution of sorbic acid in peach oil. Distilled water is injected into the reactor in two stages at a temperature not exceeding 30oC when operating the mixer.

After introduction into the reactor of the water mixture emuleret at least 30 minutes, maintaining the temperature of the mixture is not higher than 55oC. and then pumped the pump pre-prepared concentrate naftalina with a certain dispersion, with the temperature not exceeding 50oC from the reactor for the preparation of the concentrate in the reactor for the preparation of ointments when operating the agitators in both reactors. The resulting mixture emuleret at least one hour at a temperature of 40-45oC. At the end of the emulsification mixture with a pump circulating upwards from 3 to 5 minutes after emulsification, the mixture is cooled to a temperature not exceeding 30oC when operating the mixer.

The resulting ointment is white or light yellow or light yellow with a green tint color, soft texture, high absorbability skin and shelf life of 2 years.

The composition is applied in a thin layer which is manifested in the thinning and light hair, reduction of hair growth, partial loss.

Upon reaching the pronounced effect of the ointment is applied 1 time per day. Treatment courses lasting 6 to 8 months. with a break of 1 month.

Side effects occur rarely in the form of local allergic reactions (redness, burning sensation, rash urticarnaya), which disappear after withdrawal of the drug.

Application of ointment naftalina contraindicated in pregnancy and kidney disease.

The proposed composition is effective in the treatment of hirsutism, which confirmed its biopharmaceutical research conducted by the laboratory of neurohormonal regulation of reproduction Kiev scientific research Institute of endocrinology and metabolism of the substance of the MOH of Ukraine from 10.10.85 g, as well as clinical trials conducted in 8 hospitals of the USSR.

On the basis of clinical trials proposed composition is registered as a medicinal product permitted for medical use (order of the Minister of health and medical industry from 21.04.93 year).

Composition for the treatment of hirsutism, containing the active ingredient and water, characterized in that the active substance it contains neftali the components, wt.%:

Neftali - 2,38 - 2,62

Peach oil - 19,00 - 21,00

Emulsifier N 1 - 6,65 - 7,35

Sorbic acid - 0,19 - 0,21

Water - Ostalnoe

 

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