Therapeutic composition for treating dermatopathies (versions)

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry, and concerns preparing an agent for treating various dermatopathies: psoriasis, eczema, atopic dermatitis, ulcers incl. trophic and other diseases accompanied by inflammation or skin flaking. According to the first version, the composition contains ethoxylated alcohol, glycerol monostearate, higher fatty alcohols C16-C18 and cocoglycerides, as well as glycerol, olive oil and water. According to the other versions, it contains naphthalan oil or pentoxifylline or urea. All the versions provide a liposomal form of the composition improving healing, soothing and trophic effects.

EFFECT: composition is hypoallergic, easy-to-use.

12 cl, 8 ex

 

The invention relates to pharmaceutical industry and relates to the creation of tools for the treatment of various dermatological diseases: psoriasis, eczema, atopic dermatitis, ulcers, including trophic and other diseases involving inflammation or peeling skin.

To treat these diseases known vitamin: vitamin a 15 drops 3 times a day or intramuscularly for 100000-200000 units through the day. In some cases, prescribe vitamin B1220 injections. Recommended UV exposure in some stages of the disease, Spa treatment using hydrogen sulfide and radon sources. Apply the ointment: salicylic, servedelmarva, astralnova, some creams (Reference practitioner under the editorship of Prof. Aiguablava. - M.: Medicine, 1981, s).

For the treatment of psoriasis are widely used tools in the form of creams, ointments based on herbal components. Thus, in the patent of Russian Federation №2307646 described cream for the treatment of skin diseases, particularly psoriasis, containing celandine, a series of tripartite root sorrel horse, egg white, floral honey, lecithin, petrolatum at a certain ratio of components.

A disadvantage of the known means on the basis of vegetative raw materials is the length and inefficiency of their used what I and dosage forms (ointments, creams stain clothing.

Know the use for the treatment of psoriasis, anti-inflammatory and antihistamine drugs: prednisolone 1 tablet 3 times a day, suprastin, pipolphen 0,025 g 2 times a day. These drugs are cancelled when the transition of the disease in stationary or Contracting stage.

A disadvantage of the known means is ineffective, because the disease is not cured, recidivist persists.

Know the use for the treatment of psoriasis hormonal preparations - ointment sinaflana or sinalar (Yugoslav manufacture), containing in its composition a synthetic analogue of glucocorticoid hormone hydrocortisone in the amount of 0.025% and accessories [Mashkovsky PPM Sinaflana / Drugs. 1977, vol. 1. p.501-502].

The disadvantage of all known hormonal preparations is the occurrence of complications and unwanted side effects. They can cause more severe disease, can cause discomfort, skin atrophy, have unpleasant odors, inconvenient to use, stain the clothes. In addition, the use of these drugs is contraindicated in pregnant women and young people.

The objective of the invention is to provide a safe and effective Allergy-free song, easy to use for the treatment of Shi who will be about the spectrum of dermatological diseases.

The essence of the invention is expressed in the following essential features sufficient to achieve the above provided by the invention a technical result.

According to the invention, the first independent version of the medicinal composition includes a base, which includes alcohol Palmet ethoxylated, monostearate of glycerol, higher fatty alcohols, C16-C18 and cocoglyceride, as well as glycerin and olive oil, in the following ratio of components, g per 1 kg of finished product:

alcohol Palmet ethoxylated 15-25;

the monostearate of glycerol 55-65

higher fatty alcohol C16-C18 10-20

cocoglyceride 5-15

glycerin 50-150

olive oil 40-150

water - the rest.

In addition, the first independent variant is characterized by a number of optional features, namely:

the composition contains liposomal emulsion 5% lecithin.

According to the invention in a second independent variant pharmaceutical composition includes a base, which includes alcohol Palmet ethoxylated, monostearate of glycerol, higher fatty alcohols, C16-C18 and cocoglyceride, as well as glycerine, olive oil and oil naphthalene, in the following ratio of components, g per 1 kg of finished product:

alcohol Palmet ethoxylated 15-25

the monostearate of glycerol 55-65

higher fatty alcohols, C16-C8 10-20

cocoglyceride 5-15

glycerin 50-150

olive oil 40-150

oil naphthalene 10-50

water - the rest.

In addition, a second independent variant is characterized by a number of optional features, namely:

the composition contains liposomal emulsion 5% lecithin.

According to the invention, a third independent variant pharmaceutical composition includes a base, which includes alcohol Palmet ethoxylated, monostearate of glycerol, higher fatty alcohols, C16-C18 and cocoglyceride, as well as glycerine, olive oil and pentoxifylline, in the following ratio of components, g per 1 kg of finished product:

alcohol Palmet ethoxylated 15-25

the monostearate of glycerol 55-65

higher fatty alcohol C16-C18 10-20

cocoglyceride 5-15

glycerin 50-150

olive oil 40-150

pentoxifylline 35-45

water - the rest.

In addition, independent third variant is characterized by a number of optional features, namely:

the composition contains oil naphthalene - 10-50;

the composition contains liposomal emulsion 5% lecithin.

According to the invention of a fourth independent variant pharmaceutical composition includes a base, which includes alcohol Palmet ethoxylated, monostearate of glycerol, higher fatty alcohols, C16-C18 and cocoglyceride, as well as glycerin, olive oil, and urine is inu, in the following ratio of components, g per 1 kg of finished product:

alcohol Palmet ethoxylated 15-25

the monostearate of glycerol 55-65

versie fatty alcohol C16-C18 10-20

cocoglyceride 5-15

glycerin 50-150

olive oil 40-150

urea 80-120

water - the rest.

In addition, the fourth independent variant is characterized by a number of optional features, namely:

the composition comprises pentoxifylline 35-45

the composition comprises oil naphthalene 10-50

the composition comprises pentoxifylline 35-45 and oil naphthalene 10-50;

the composition contains liposomal emulsion 5% lecithin;

BAS 80-150.

The applicant has not identified the sources containing information on technical solutions, the combination of features which coincide with the set of distinctive features of the claimed invention.

General technical result achieved when using all variants of the claimed invention, is its anti-inflammatory effect.

The first variant of the claimed invention is additionally characterized by hypoallergenic and easy to use.

The second variant of the claimed invention is additionally characterized by the fact that this variant of the claimed composition due to natural preservative (oil naphthalene) provides slow fission glue is OK, has an exfoliating effect, which together with other components provides a resolving action.

The third variant of the claimed invention is additionally characterized by the fact that this variant of the claimed compositions by pentoxifylline in combination with other components this option provides the suppression of cell proliferation in the acute phase of disease, has a resolving and healing effect ulcers, has a universal effect on the skin, on lymphocytes.

The fourth variant of the claimed invention is additionally characterized by the fact that this variant of the claimed compositions by urea provides the neutralization of IgE in the skin, has an exfoliating effect and moisturizes the skin.

Liposomal form of the claimed compositions in all its variants enhances healing, soothing and trophic effects.

The claimed compositions are prepared as follows. The Foundation placed in a beaker and heated to the point of melting. The remaining components of the compositions, taken in respective variants quantities, add water by weight and mixed in a continuous mode, while in the preparation of liposomal compositions in the form of exercise effects on the prepared solution by ultrasound, resulting in vkluchennosti with BAS (oil, pentoxifylline, urea) in liposomes and stabilization of membranes of liposomes. Then thus obtained liposomal solution is mixed with the molten base.

The effectiveness of the claimed compositions is illustrated by the following examples.

Example 1.

Hypoallergenic cream for option 1.

Patient K., 43 years. Hurts widespread atopic dermatitis since childhood. The present aggravation of the strongest area of skin is 70%. From the anamnesis it was found that previously regularly used corticosteroid (CS) creams and ointments, such as sinople, tselestoderm, Elokim, etc. In real time from outside the COP was getting worse and worse.

Used hypoallergenic cream with urea 2 times a day to areas within 2.5 months. Remission was 3 years (see N5). Remission was maintained through the use, for the prevention and skin care, hypoallergenic cream 2-3 times a day to areas on the skin, exposed to weather, frost, etc. (hands, face). The patient really liked this cream because of the rapid absorption, lack of irritating odors, good cushioning effect, colorless, respectively, not soiling their clothes.

Example 2.

Hypoallergenic cream with Naftalan for option 2.

Patient P., 53. Hurts focal neurodermatitis internal over the spine of the thighs and genitals, accompanied by pronounced lichenification more than 18 years. Applies to good effect hypoallergenic cream with naphthalene 2 times a day to areas 2.5 months., 2 times a year, in the period of seasonal exacerbations of the disease.

Example 3.

Hypoallergenic cream with pentoxifylline for option 3.

Patient M., 19 years. Hurts hemorrhagic vasculitis 1.5 years. As it turned out from the external history of the COP and General therapy was ineffective. Used hypoallergenic cream with pentoxifylline 2 times a day to areas 2.5 months. until complete resolution of the rash. Remission was 1 year.

Example 4.

Hypoallergenic cream with pentoxifylline and naphthalene on pvariant 3.

Patient K., 43 years. Hurts krupnoblyashechny the parapsoriasis within 3 years. According to the prescription of a dermatologist regularly used COP external agents. Without much effect. Used hypoallergenic cream with pentoxifylline and naphthalene 2 times a day to areas within 2.5 months. Remission was 2 years old.

Example 5.

Hypoallergenic cream with urea for option 4.

Patient K., 43 years. Hurts widespread atopic dermatitis since childhood. The present aggravation of the strongest area of skin is 70%. From the anamnesis it was found that previously regularly used corticosteroid (CS) creams and ointments, such as sinople, Celeste is derm, Elokim, etc. In real time from external COP only gets worse. Used hypoallergenic cream with urea 2 times a day to areas within 2.5 months. Remission was 3 years old.

Example 6.

Hypoallergenic cream with urea and Naftalan version 4.

Patient S., 63. Sore dry eczema of the legs within 3 years. Remission for the last 2 years were observed. After applying the CC creams and ointments, such as sinople, tselestoderm, Elokim, etc. there has been a significant deterioration. Appeared severe exudation, distribution of lesions, secondary infection. Used hypoallergenic cream with urea and naphthalene 2 times a day to areas within 2.5 months. Remission was 3 years old.

Example 7.

Hypoallergenic cream with pentoxifylline and urea for option 4.

Patient F., age 16, psoriasis suffers from birth. From the anamnesis it is known that the process usually wore common, with lesions of the scalp, face, limbs and buttocks. In this case, the patient was observed allergic reactions to Biseptol, folic acid, Amit, fish oil, ointment ibuprofen tablets Nurofen and naproxen at a dose of 1000 mg/day. In addition, it was noted the development of eritrodermii after intravenous administration of a solution gemodeza, the development of nasal bleeding after application of immunodeficiency, the Ala per os. The solution of calcium gluconate, vitamins B6, B12 transferred patients are also bad.

Long-term treatment showed that such external means, as sinopean and flutsinar, belosalic and diprosalic, jaxson, skin cap spray, serenitienow and tar ointments are ineffective. The use of "Hungarian" schema with calcium gluconate without positive dynamics.

The positive effect from the lesions on the skin was observed only from applying the cream elokom.

The last relapse post-influenza, manifested by profuse eruption of papules on the face, torso and limbs, and pain in the ankle joint and joints of the foot, swelling and redness of the skin. In this regard, in the clinic at the place of residence of the patient was assigned inside Nurofen and outward in the region of the involved joints ointment ibuprofen, which led to a sharp increase in pain in the joints, shortness of movement in them, the rapid growth of papules on the periphery and their merger. Within a few days almost all of the skin has been affected.

About widespread psoriasis, lesions of the scalp, face and psoriatic arthritis undifferentiated form, the average degree of activity, the patient was recommended inpatient treatment. In connection with psychopathic features p is doing (birth trauma history, convulsive syndrome) patient refused hospitalization.

In connection with the data on long-term use of corticosteroid ointments for external therapy, as well as in connection with the cultural selection of multiple colonies of yeast cells from lesions on the skin use cream elokom became problematic and impractical.

It was decided to assign the patient inside naproxen 0.25×3 times a day and externally hypoallergenic cream with pentoxifylline and urea, putting on plaques in the morning and evening.

After 1 month the patient lesions were completely resolved. Remission was 2.5 months. Given the severe allergic background and psychopathic behavior of our patient, we got a great result without the use of strong corticosteroids and cytostatics, using domestic external means, not containing corticosteroid.

It should be noted that such patients are increasingly common in our medical practice, and effective hypoallergenic domestic preparations for the treatment of psoriasis almost none. Foreign drugs are expensive and often dangerous for the health of patients with psoriasis. In this regard, hypoallergenic cream with pentoxifylline and urea different for the better. It costs 5 times lower than used in psoriasis foreign exterior, in addition to the state funds. Example 8.

Hypoallergenic cream with pentoxifylline, urea and Naftalan version 4.

Patient N., 28 years. Suffering from psoriasis for 6 years. Present seasonal exacerbation of the strongest. Arrived to me on outpatient reception in the doldrums, with common exudative psoriasis, with a clear trend towards the development of eritrodermii, with sticky underwear to saturated with exudate and blood plaques. Previously used CC creams and ointments, such as diprosalic, akriderm Ledger, Elokim. Currently from outside the COP only gets worse.

For the external treatment of the patient was used hypoallergenic cream with pentoxifylline, urea and naphthalene. Leather N. got rid of rash on 95% within 1.5 months only to rescue plaques on the elbows. Remission was 1.5 years.

The claimed compositions in all variants are Hypo-allergenic, safe, easy to use and effective means for the treatment of various skin diseases at different stages of their development. All components of the claimed compositions are prepared using commercially available preparations, namely that 38.107119-85 Alcohols of synthetic primary higher fatty ethoxylated (alcohol Palmet ethoxylated), THE 9154-008-00333813-03 (glycerol monostearate), THE 38.107119-85 (higher fatty alcohol C16-C18 ethoxylated who), THE 38.107119-85 (kocoglu-potassium), GOST 6824-96 (glycerine distilled), THE 9146-008-58837688-2005 (soy lecithin), TU 6-09-2117-87 (urea (non-sterile) brand OP-3 highly pure 3-3).

1. Medicinal composition for treating skin diseases includes a base, which includes alcohol Palmet ethoxylated, monostearate of glycerol, higher fatty alcohols, C16-C18 and cocoglyceride, as well as glycerine, olive oil and water in the following ratio of components in g per kg of finished product:

alcohol Palmet ethoxylated15-25
the glycerol monostearate55-65
higher fatty alcohol C16-C1810-20
cocoglyceride5-15
glycerin50-150
olive oil40-150
waterrest

2. The composition according to claim 1, characterized in that it contains liposomal emulsion 5% lecithin.

3. Medicinal composition for treating skin diseases includes a base, which includes alcohol Pallet of amoxillian the th, the monostearate of glycerol, higher fatty alcohols, C16-C18 and cocoglyceride, as well as glycerin, olive oil, crude naphthalene, and water in the following ratio of components in g per kg of finished product:

alcohol Palmet ethoxylated15-25
the glycerol monostearate55-65
higher fatty alcohol C16-C1810-20
cocoglyceride5-15
glycerin50-150
olive oil40-150
oil naphthalene10-50
waterrest

4. The composition according to claim 3, characterized in that it contains liposomal emulsion 5% lecithin.

5. Medicinal composition for treating skin diseases includes a base, which includes alcohol Palmet ethoxylated, monostearate of glycerol, higher fatty alcohols, C16-C18 and cocoglyceride, as well as glycerine, olive oil and water pentoxifylline in the following ratio of components in g per kg of the finished product

alcohol Palmet ethoxylated15-25
the glycerol monostearate55-65
higher fatty alcohol C16-C1810-20
cocoglyceride5-15
glycerin50-150
olive oil40-150
pentoxifylline35-45
waterrest

6. The composition according to claim 5, characterized in that it contains oil naphthalene - 10-50.

7. Composition according to any one of pp.5 and 6, characterized in that it contains liposomal emulsion 5% lecithin.

8. Medicinal composition for treating skin diseases includes a base, which includes alcohol Palmet ethoxylated, monostearate of glycerol, higher fatty alcohols, C16-C18 and cocoglyceride, as well as glycerin, olive oil, urea and water in the following ratio of components in g per kg of finished product:

alcohol Palmet ethoxylated 15-25
the glycerol monostearate55-65
higher fatty alcohol C16-C1810-20
cocoglyceride5-15
glycerin50-150
olive oil40-150
urea80-120
waterrest

9. The composition according to claim 8, characterized in that it contains pentoxifylline - 30-50.

10. The composition according to claim 8, characterized in that it contains oil naphthalene - 10-50.

11. The composition according to claim 8, characterized in that it contains pentoxifylline - 30-50 and oil naphthalene - 10-50.

12. Composition according to any one of p-11, characterized in that the composition contains liposomal emulsion 5% lecithin.



 

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6 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new benzimidazole derivatives of general formula (I) or to its pharmacologically acceptable salts wherein R1 represents a C6-aryl group which can be substituted by 1-3 groups optionally specified in a group of substitutes (a), or a heterocyclic group which represents pyridyl, dihydrobenzofuranyl, 1,3-benzodioxolyl, tetrahydropyranyl, tetrahydrofuranyl which can be substituted by 1-3 groups optionally specified in a group of substitutes (a), R2 represents a C1-C6 alkyl group, R3 represents a C6-aryl group which can be substituted by 1-2 groups optionally specified in a group of substitutes (a), Q represents a group represented by formula =CH-, or a nitrogen atom and a group of substitutes (a) represents a group consisting of a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a carboxyl group, a C2-C7 alkylcarbonyl group, a C2-C7 alkoxycarbonyl group, a C1-C6 alkoxy group, a C1-C6 halogenated alkoxy group, an amino group, a 4-morpholinyl group and a di-C1-C6 alkyl)amino group. Also, the invention refers to a pharmaceutical composition based on a compound of formula (I), to a PPARγ activator/modulator based on the compound of formula (I), to using the compound of formula (I), to a method of reducing blood glucose, to a method of activating PPARγ, a method of treating and/or preventing said pathological conditions.

EFFECT: there are produced new benzimidazole derivatives showing PPARγ modulatory activity.

41 cl, 2 dwg, 6 tbl, 76 ex

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