Pharmaceutical composition for treating dermatoses treated by glucocorticosteroids, and method for preparing it

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, and concerns a pharmaceutical composition for treating skin diseases. The composition contains a combination of methylprednisolone aceponate and glycoceramides and a glycoceramide complex containing cholesterol in the amount of 1-3%, and phospholipids in the amount of 25-34%, and excipients. A method for preparing the composition consists in the fact that methylprednisolone aceponate is introduced into an emulsion base containing the glycoceramide complex in the form of a solution to form a coagulation structure.

EFFECT: new pharmaceutical composition is characterised by a wide spectrum of pharmacological properties, stability, uniform distribution of the active ingredients.

9 cl, 2 tbl

 

The invention relates to the field of medicine and relates to pharmaceutical compositions for the treatment of inflammation and itch curing and can be used for the treatment of skin diseases (including chronic), amenable to therapy with glucocorticosteroids.

Treatment of dermatoses of special importance in connection with the increase in their frequency, including among children, as well as in connection with the increased frequency of severe, often torpid and treatment-resistant forms of these diseases. The incidence of allergic is 6-15%, psoriasis - 2-4% of the world population, which determines the relevance and socio-economic importance of this problem.

Currently there is a trend to increase the number of patients with chronic widespread dermatitis prone to dissemination skin rashes. Attention to this problem due to the fact that to date is not fully elucidated the etiology and many links of the pathogenesis of common chronic dermatosis.

Significant place in the treatment of chronic dermatoses belongs rationally selected external therapy. External therapy could rightly regarded as an extremely important part of a comprehensive treatment of dermatological patients. In the last decades has increased the interest in outer corticosteroid therapy, which is associated with the development and introduction into medical practice of local funds, allowing the directional impact on the region of localization of the pathological process and to minimize the complications that often arise in their oral or parenteral application. In this direction carried out research work on the synthesis of new effective corticosteroids, and the development of new drugs for external therapy, including various corticosteroids.

Most activity have fluorinated synthetic analogues of natural corticosteroids betamethasone fluotsinolon, triamcinolone. However, fluorinated glucocorticoids have a quite marked systemic side effects, especially with prolonged use.

Non-fluorinated glucocorticoids compared with fluorinated generally less effective but safer in the development of systemic side effects during therapy. In this regard, it is important to create drugs comparable potency with fluorinated glucocorticoids, but also provide less significant side effects.

One of these drugs is dehalogenation synthetic glucocorticoid methylprednisolone. Its structural modification - methylprednisolone azep the NAT - combines high therapeutic efficacy comparable to the activity of strong fluorinated glucocorticoids, with minimal systemic side effects. The rapid development of clinical effect and high safety makes methylprednisolone aceponate the drug of choice in the treatment of dermatoses and opens new perspectives in the treatment of skin diseases.

Important by modification of steroids is getting their esters. Steroid esters have low affinity for the receptors, however, the presence in the skin of esterases, which decompose essential communication leads to activation of the steroid at the site of action, i.e. steroid ether can be considered as prodrugs. The optimal combination of high local activity and weak systemic effects have been obtained by including essential side chains in the structure of methylprednisolone [6].

Of methylprednisolone aceponate as fluids, characterized by highly lipophilic, allowing it to easily penetrate the stratum corneum of the skin. Once in the dermis, the drug under the influence of the contained there esterase exposed deesterification education methylprednisolone-17-propionate, which is compared with methylprednisolone by acaponeta and dexamethasone is more active (respectively 2.4 and 1.4 times) associated with steroid intracellular receptor is mi.

The process of bioactively methylprednisolone of aceponate in the skin when inflammation occurs much faster than in normal skin. The penetration of its metabolites from the skin into the blood slightly, the half-life in blood is small, and the binding interacted sufficiently large that determines the practical absence of systemic side effects of the drug.

The local application of methylprednisolone aceponate has anti-inflammatory, antiallergic and antiexudative effect, causes antipruritic effect. So, on the model of CROTONALDEHYDE ear oedema in rats anti-inflammatory effect of methylprednisolone aceponate the local application is comparable with the activity of clobetasol propionate, diflucortolone valerate and higher than the activity of betamethasone valerate and hydrocortisone butyrate.

According to the classification adopted in the United States and most European countries, the impact of methylprednisolone aceponate belong to the III class of "strong" topical corticosteroid.

Renowned pharmaceutical composition comprising as active ingredient methylprednisolone aceponate and excipients [Register of medicines Russia: radar encyclopedia of medicine. - M.: "radar-patent", 20046 ñ.38]. The drug has a high anti-inflammatory activity, but negatively affects the% is with reparative proliferation and reduces the skin's barrier function.

The objective of this invention is to provide a new pharmaceutical composition for external use on the basis of methylprednisolone aceponate in the form of soft medicinal forms, as well as the development of a method of obtaining a composition for the treatment of dermatitis.

To solve this problem is proposed pharmaceutical composition comprising as active ingredient methylprednisolone aceponate in therapeutically effective amount, and an excipient, the composition differs in that it additionally contains ceramides or ceramide complex.

A distinctive feature is the introduction song of ceramide (ceramide) or their derivatives in the form of individual compounds or in the form of complexes (compounds) with cholesterol, fatty acids. It is preferable to use picokernel or complex picokernel containing cholesterol in the amount of 1-3% and phospholipids in the number of 25-34%.

The preferred concentration picokernel (or Pickering complex) g/100 g composition:

Of methylprednisolone aceponateof 0.05-0.2
Glycosylamines complex (or glycolamide)0,01-2,0

Ceramide complex is predstavljaet a concentrated and highly purified of glycolamide, similar 4/5 of ceramide on human skin. They included lower cholesterol and phospholipids. The complex, preferably, the product of natural origin. Ceramide complex has a specific biological activity in the upper layers of the epidermis - acts as glycosylamide, as well as the precursors of ceramides.

The investigations conducted have shown the advantage of the claimed combination of methylprednisolone aceponate with glycosylamide or complex picokernel, in particular:

- on the model of linear wounds in rats found that the introduction picokernel in composition, containing methylprednisolone aceponate (MPA), contributes to significantly increasing the strength of the wound scar. As the data enabling picokernel or complex picokernel in the composition of the soft dosage forms containing MPA, reparative activity increases dramatically compared to the control pathology, indicating the presence of high wound healing activity proposed combination (table 1). The influence of concentration picokernel strength of the wound scar and it is shown that reparative activity in this model, the maximum at a concentration of picokernel or complex based picokernel of 0.25-0.5%.

- on the model plane wounds in rats shows that h is about the proposed combination eliminated the side effects of glucocorticosteroid on reparative proliferation and barrier function of the skin, resulting in a new composition has a positive effect on the healing process, thereby reducing the area of RAS and epithelialization (table 2), as well as preventing the development of infectious processes and the death of animals.

Table 1
Reparative activity on the model of linear incised wounds in rats formulations with different concentration of the complex on the basis of picokernel
Conditions of experienceIndicators of tensiometry, gReparative activity, %
Control, pathology371,7±45,2-
MPA + 0% picokernel435,8±47,617,2
IPA + 0.1% of picokernel505,0±33,9*35,9
MPA + 0,25% picokernel590,0±38,7*58,7
MPA + 0,5% picokernelof 600.0±54,8*61,4
MPA + 0,75% picokernel 560, 0m±40,3*50,7
MPA + 1,0% picokernel546,7±32,3*47,1

Table 2
Comparison of reparative properties
Indicators reparative actionCream (MPA + complex picokernel)Cream (MPA)
The area of the Russian Academy of SciencesDecreased 26.8 timesDecreased to 1.01 times
The rate of wound healing25,80,01
The death of animals (%)033,3

Also the results of the study of the structure of the linear cut wounds in rats confirm the rationality of the combination of methylprednisolone aceponate and picokernel or complex picokernel.

On models dextranomer and aerosoling inflammation of the foot rats established that the claimed combination exhibits anti-inflammatory activity comparable to the activity of the drug comparisons (prototype)

Thus, the introduction picokernel (or complex based picokernel) in the form of pharmaceutical compositions containing MPA, expands the range of its pharmacological properties; along with anti-inflammatory action of the drug is also healing activity, it can be used to normalize the skin barrier during curing, accompanied by the erosion and violation of the integrity of the skin.

Preferably as excipients composition comprises a hydrophobic component, a hydrophilic component, emulsifier and preservative.

The preferred ratio of ingredients of the composition is, g/100 g composition:

Of methylprednisolone aceponateof 0.05-0.2
Glycolamide (or complex picokernel)0,01-2,0
Hydrophobic component11,0-52,0
The hydrophilic component30,0-82,8
Emulsifier4,5-16,5
Preservative0,05-1,5

As the hydrophobic component (hydrophobic phase) use the form of liquid oil with different spreading coefficient in the range from 1600 mm 2/10 min to 250 mm2/10 min, for example, dicaprylyl carbonate, isopropylmyristate, isopropyl, octyldodecanol, hexidecimal, squalane, silicone (cyclomethicone, Dimethicone different viscosities), vegetable oil, castor oil, palm oil, and semisolid lanolin and its derivatives, Shea butter) and solid fatty acids and lipids, phospholipids, cholesterol.

To provide softening and moisturizing action required combination of emlenton (oils) with strong, medium and weak spreading. The combination of the combination of essential oils will provide a good distribution on the surface of the skin, fast and easy absorption, the creation of a uniform protective oil film.

At the present time in the world practice in the pharmaceutical and cosmetic products is used quite a large number of emollients (emlenton), which is not oxidized during storage of the drug and, therefore, does not require the introduction of additional antioxidants. The combination of these substances is carried out on the basis that they have different spreading coefficient, and to provide softening and moisturizing action necessary combination of emollients with strong, medium and weak spreading. The concentration of each emlenton with different spreading, preferably, should be the same DL the achievements of cascade spreading effect when applying the cream. In addition, preferably the inclusion of silicone oil, for example dimetikona, in a concentration of from 0.5 to 10.5 g/100 g of the composition, which improves absorption and helps to eliminate a greasy feeling after application.

The total content of the hydrophobic phase may range from 11.0 to 52,0, the preferred content of component hydrophobic phase from of 18.0 to 27.0 g/100 g of composition.

As the hydrophilic phase (hydrophilic component) using hydrophilic nonaqueous solvent, a buffering agent, disodium edetate (Trilon B), and water.

The preferred ratio is, g/100 g composition:

Hydrophilic nonaqueous solvent1,0-10,0
Buffer substances0,1-2,0
Disodium edetate0,01-0,5
Water17,5-81,7

Hydrophilic nonaqueous solvent used for dissolution of methylprednisolone aceponate, in addition, can have a moisturizing effect on the skin. As hydrophilic nonaqueous solvent can be used propylene glycol, glycerin, sorbitol, hexyleneglycol, PEO-400.

Disodium ADETEF in RA the framework of the present invention performs the function of the complexing agents, binding metal ions and reduce the likelihood of microbiological her dirt cream. Disodium ADETEF may be excluded from the composition in the case of the introduction of high concentrations of preservative.

As the buffer can be used inorganic buffering agent, preferably a salt of phosphoric acid (potassium and sodium phosphates).

As the emulsifier composition preferably contains a combination of emulsifiers of the 1st and 2nd kind, number, g/100 g of the composition

Emulsifier4,5-16,5

Emulsifiers can be substances difiles nature based on ethoxylated alcohols, fatty alcohols, esters mnogotomnogo alcohol and a fatty acid, a derivative of glucose.

The preferred amount of emulsifiers is, g/100 g composition:

Emulsifiers5,5-13,0

As preservative preferably use preservatives on the basis of Phenoxyethanol in a total concentration of from 0.05 g to 1.5 g per 100 g of the composition. You can also use preservatives from among: methyl-, ethyl - and propylparabens and mixtures thereof; phenethyl alcohol, sorbic acid, diazolidinyl the wine, imidazolidinedione.

From the data obtained it follows that in the test samples of the drug content Euxyl PE 9010 1.0 g/100 g of the composition was observed rapid killing of bacteria and fungi. In the original seeding logarithm reduce the number of viable cells P.aeruginosa was 2,72, with subsequent sowing of viable cells were not detected. Viable cells of the test organisms S. aureus, C. albicans and A. niger are already in the original and subsequent sowing were not detected.

The proposed pharmaceutical composition is in the form of soft medicinal forms, preferably in the form of a cream, and is a complex dispersed system, which is simultaneously emulsion (water/oil) and the solution (with respect to the active ingredient).

The introduction of the rationally selected combinations of emulsifiers in combination with other optional ingredients in the stated ratio is achieved creamy consistency of the dosage form, the stability of the emulsion during storage and good extrusion finished dosage forms of packaging (tubes), which is very important for ease of use for patients.

The selected composition ensures a homogeneous distribution and a sufficiently small particle size of the dispersed phase of the emulsion is less than 25 microns, and a creamy consistency and structural viscosity, is the quiet provide the physical stability of the emulsion during storage and proper extrusion of the cream from the tube.

The claimed composition is stable during storage.

the pH of the water extract from the composition of the claimed composition lies in the range of 4.0 to 5.5, which reduces the possibility of undesirable side reactions at the application and at the same time prevents the degradation of the active ingredient during manufacture and during storage.

The choice of ingredients and their ratio significantly affects the way of obtaining the drug.

According to the proposed method type methylprednisolone aceponate in the form of a solution in an emulsion base of the dosage form, which also includes the complex picokernel. In a preferred variant of the method base is prepared in a single reactor without the use of auxiliary tanks for heating water and oil phases. More preferably of methylprednisolone aceponate in the form of a solution in a nonaqueous solvent, and optionally included in the composition buffer substances and sodium edetate they are at the stage of preparation of bases in aqueous solution. The solution of the active substance is injected into the liquid until the beginning of the formation of coagulation structure.

The use of the claimed method of obtaining protivotarannogo tools enables efficient homogenization of the composition (almost without destruction of the emulsion) and a decrease in the action of destructive factors on the active ingredient in the manufacturing process.

A typical example.

Charged to the reactor water clean, and if necessary, buffer substances, and Trilon B, add ceramides LS (complex picokernel), a hydrophobic component and emulsifier (glyceryl the monostearate, macrogol 40 stearate, cetosteatil alcohol). Heat the mass to 70°C and carry out the shutter speed to a complete melting of all components. Include high-speed homogenizer and intensive mixing, are the liquid emulsion and cool it to a temperature of 60°C. Dissolve when heated to 60°C methylprednisolone aceponate in propylene glycol, load the resulting solution simultaneously with the preservative in the base of the cream and spend homogenization. Cool the resulting cream to room temperature with slow stirring under vacuum. Get the cream white color, which is Packed in tubes. Specific examples of carrying out the invention is presented in table 3.

The resulting composition on the basis of methylprednisolone aceponate of examples 1, 2, 3, 4 meet regulatory requirements for microbiological purity and uniformity, and has a shelf life of over 2 years.

Table 3
ComponentsExamples g/100 g of the composition
1234
Of methylprednisolone aceponate0,10,20,150,05
Complex picokernel0,52,01,00,01
Hydrophobic component24,99,030,6552,0
The hydrophilic component64,582,851,635,54
Emulsifier9,04,516,5to 12.0
Preservative1,01,50,10,4

1. Pharmaceutical composition in the form of soft medicinal forms for the treatment of skin diseases, which includes methylprednisolone aceponate in therapeutically effective amounts and vspomogate the further substances, characterized in that it further includes glycosylamide or complex picokernel containing cholesterol in the amount of 1-3% and phospholipids in the number of 25-34% in the following ratio, g/100 g composition:

Of methylprednisolone aceponateof 0.05-0.2
Glycosylamide or complex picokernel0,01-2,0

2. The pharmaceutical composition according to claim 1, characterized in that it contains as excipients hydrophobic component, a hydrophilic component, emulsifier and preservative.

3. The pharmaceutical composition according to claim 2, characterized in that it contains as a hydrophobic component, a combination of octyldodecanol, exercisesthat and dimeticone.

4. The pharmaceutical composition according to claim 3, characterized in that it contains as a hydrophilic component, a combination of non-aqueous solvent and water.

5. The pharmaceutical composition according to claim 4, characterized in that it additionally contains a buffer substance and sodium edetate.

6. The pharmaceutical composition according to claim 5, characterized in that it contains as a non-aqueous solvent is propylene glycol and as a buffer substance is a combination of potassium phosphate and one-deputizing sodium phosphate dunamase the nogo 12-water.

7. The pharmaceutical composition according to claim 6, characterized in that it contains as complex based picokernel ceramides LS.

8. A method of obtaining a pharmaceutical composition for the treatment of skin diseases according to any one of claims 1 to 7, whereby methylprednisolone aceponate injected into the emulsion base containing complex picokernel in the form of a solution.

9. The method of claim 8, whereby methylprednisolone aceponate injected prior to the formation of coagulation structure.



 

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FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new compounds of formula (I) or to its stereoisomers, or to a pharmaceutically acceptable salt, wherein Ra represents H or (C1-C6)alkyl; Rb is specified in an optionally substituted group consisting of -(CH2)n-aryl, -CH(CH3)-aryl, -(CH2)n-arylaryl, -(CH2)n-arylheteroaryl, -(CH2)n-(C3-C8) cycloalkyl, -(CH2)n-heteroaryl, -(CH2)n-heterocyclyl and -(C3-C8) cycloalkylaryl; or Ra and Rb taken together with a nitrogen atom form 2,3-dihydro-1H-isoindolyl, decahydroisoquinolinyl, optionally substituted piperidinyl or optionally substituted pyrrolidinyl; Y is specified in an an optionally substituted group consisting of 5,6,7,8-tetrahydro[1,6]naphthyridinyl, -NH-(CH2)n-heterocyclyl, wherein NH is attached to carbonyl, and -heterocyclylaryl, wherein heterocyclyl is attached to carbonyl; and n is equal to 0, 1 or 2; wherein each heterocyclyl represents an independent non-aromatic ring system containing 3 to 12 ring atoms, and at least one ring atom specified in a group consisting of nitrogen, oxygen and sulphur; wherein each heteroaryl represents an independent non-aromatic ring system containing 3 to 12 ring atoms and at least one ring atom specified in a group consisting of nitrogen, oxygen and sulphur; and wherein the optional substitutes are independently specified in a group consisting of C1-C6-alkyl, C1-C6-alkoxy, halogen, CN, CF3, OCF3, NH2, NH(CH3), N(CH3)2, hydroxy, cyclohexyl, phenyl, pyrrolidinyl, -C(O)-piperidinyl, -N(H)-C(O)-C1-C6-alkyl and N(H)-S(O)2-C1-C6-alkyl. The invention also describes a pharmaceutical composition having chemokine receptor antagonist activity and a method of treating such diseases, such as rheumatoid arthritis, psoriasis, lupus, etc.

EFFECT: there are prepared and described new chemical compounds that can be used as chemokine receptor antagonists and, as such, may be used in treating certain pathological conditions and diseases, particularly inflammatory pathological conditions and diseases and proliferative disorders and conditions, eg rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.

23 cl, 59 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, biotechnology, as well as to pharmaceutical, food and cosmetic industries, and concerns an agent made of sea urchin viscera being waste after edible gonads have been separated. The agent with anti-inflammatory and immunotropic activity is characterised by the fact that it represents an alcoholic extract prepared of sea urchin viscera after gonad separation, containing 10-15% of peptides, 35-45% of amino acids, 4-8% of phospholipids, trace substances, and has the following characteristics: molecular weight of the peptide fractions as determined by polyacrylamide gel electrophoresis is 19-15 kDa, 6-3,5 kDa and less than 3.5 kDa. The agent is prepared by separating gonads from sea urchins, taking the viscera, extraction in ethanol in ratio 1:1-3 at temperature 0 to plus 10°C for 2 h to 10 days, separation of a liquid portion to produce a water-alcohol extract, alcohol distillation, and drying.

EFFECT: invention provides preparing the safe agent with the evident therapeutic effect.

3 cl, 7 ex, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is an antimicrobial, anti-inflammatory and analgesic agent of a benzamidine derivative of empirical formula (C13H11N3O2), namely N-4-nitrophenylbenzamidine (I) as an active substance. It is shown that N-4-nitrophenylbenzamidine is low-toxic; it possess antimicrobial (on Gram-positive and Gram-negative bacteria), anti-inflammatory and analgesic activity.

EFFECT: these properties make it possible to suggest that N-4-nitrophenylbenzamidine may be used in medicine, as an ingredient of the drug preparation for specified application.

2 tbl, 5 ex

FIELD: chemistry.

SUBSTANCE: invention discloses a product of modification of sulphanilic acid, and specifically n-(1,5-dihydro-3-methyl-8-R1-8-R2-9-hydroxy-[1,3]dioxepino[5,6-c]pyridinyl-6-azo)phenylsulphonic acid and salt forms thereof of general formula I: , where R1, R2 are selected from a group comprising: a hydrogen atom, methyl, a linear or branched alkyl or R1 and R2 together form a spirocycloalkyl group. Compounds of formula (I) have antibacterial activity, are more efficient with respect to both gram-negative bacteria Proteus vulgaris, Pseudomonas aeroginosa and gram-positive bacteria Staphylococcus aureus, and can be used in medicine and veterinary.

EFFECT: improved properties.

1 cl, 1 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to novel pyridyloxy derivatives or its pharmaceutically acceptable ester or a pharmaceutically acceptable salt of the mentioned derivatice or ester of general formula (I), wherein R represents a pyridyl group substituted by 1-3 groups independently specified in a group of substitutes A; the group of substitutes A represents a group comprising halogen atom, C1-C6 alkyl group and C1-C6 alkoxy group, and Me represents a methyl group. Also, the invention refers to specific compounds of formula (I), to a pharmaceutical composition and a receptor-γ activator/modulator on the basis of a compound of formula (I), to a method of treating and/or preventing a disease.

EFFECT: there are prepared novel pyridyloxy derivatives effective in treating the disease mediated by peroxisome proliferator activated receptor-γ (PPAR) γ.

37 cl, 2 tbl, 21 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to combinations of peptides in each case with the same sequence length (SEQL) which can be prepared in a stable reproducible quality and quantity of a mixture (A) containing a number of x amino acid with protected acid groups or a number of z peptides with the acid groups protected by the protective groups and the activated amino groups, with the amino acids in the mixture (A) found in a specific molar ratio, and a mixture (B), containing a number of y amino acids with the amino groups protected by the protective groups, with a molar ratio of the amino acids of the mixture (B) being the same as the molar ratio of the amino acids of the mixture (A), and the number x=y, and x is a figure from 11 to 18.

EFFECT: new combinations of the peptides are presented.

13 cl, 2 dwg, 1 ex

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