Pharmaceutical composition possessing anti-allergic and anti-inflammatory effect

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a medicinal preparation. As an active component the composition comprises the combination of betamethasone dipropionate and gentamycin sulfate and special additives comprising nipagin, propylene glycol, medicinal vaseline oil, Trilon B, emulsifier agent, buffer substances and water. The pharmaceutical composition is prepared as cream. Invention provides the multidirected therapeutic effect with the useful life of the composition 2 years.

EFFECT: improved and valuable medicinal and pharmaceutical properties of composition.

4 cl, 2 tbl, 3 ex

 

The invention relates to the field of medicine and relates to pharmaceutical agents for the treatment of skin diseases, especially various types of eczema, dermatitis, atopic dermatitis, psoriasis and other

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 treatment-resistant forms of these diseases, as well as complicated by infection. The incidence of allergic is 6-15%, psoriasis - 2-4% of the population that determines the urgency of the problem and socio-economic importance.

Currently there is a trend to increase the number of patients with common chronic dermatosis with a penchant for the dissemination skin rashes, as well as bacterial and fungal infections (Mackillican A.L., Golousenko YOU Experience applying the cream "Triderm" // News of dermatology and venereology. - 1995. No. 1, p.48-49).

Significant place in the treatment of chronic dermatoses belongs rationally selected external therapy. Among the wide range used for this purpose medicines play a special role preparations containing corticosteroids, especially one of the most active in this direction drugs betamethasone.

Betamethasone has expressed protivovospalitel the nutrient and anti-allergic effect and is used in various modifications (betamethasone dipropionate, valerate, disodium phosphate, acetate), preferably dipropionate. Compositions containing as active ingredient betamethasone, are in the form of various dosage forms: tablets, injections, suspensions, creams, ointments, lotions.

Oral administration of betamethasone, like other corticosteroids, with the goal of systemic therapy can cause severe complications (Cushing's syndrome, diabetes, problems with gastrointestinal tract and others) and local application of the drug allows you to avoid these side effects. However, long-term topical application of betamethasone may cause activation of viral, bacterial and fungal infections. One of the ways to reduce the likelihood of side effects, as well as complement and enhance the effects of betamethasone is the creation of medicines, which contain a combination of betamethasone with other active ingredients.

In a number of patents describe the combination of betamethasone with different antibacterial drugs with the purpose of reduction or complete suppression of the side-activation of viral and bacterial infections.

In the United Kingdom patent 2192787, 1988, described the drug to treat excessive granulation containing betamethasone and oxytetracycline or chlortetracycline. The drug may be in the form of fatty cream. In U.S. patent 4013792, 1977, describes an ointment against vospalitelnoe action for the treatment of dermatoses containing betamethasone and neomycin sulphate. In the United Kingdom patent 2049416, 1981, describes a veterinary medicinal product containing one or more hormones of the adrenal cortex (e.g., betamethasone) and one or more hormones, releasing thyrostimulin hormone, and additionally containing antimicrobials: tetracycline, chlortetracycline, oxytetracycline, neomycin, kanamycin, sulfathiazole and many others. The composition is made in the form of ointment that heals eczema, allergic diseases.

More detailed pharmacological studies have shown that one of the most successful combinations of betamethasone is its combination with gentamicin.

In Japanese patent 60156608, 1985, describes an ointment containing 2-10 parts, mostly 3-7 parts of a mixture of alcohol and water at a ratio of 1:1-9:1, 0.1 to 6 parts surfactants, preferably nonionic, 75-97 higher parts of paraffin hydrocarbon, preferably containing 16-40 carbon atoms and 0.02 to 2 parts, preferably of 0.02 to 0.04 parts, pyrosulfite sodium as the base. 1 g ointment contains 0.2 to 5 mg of betamethasone (as ether) and 0.2-5 mg gentamicin sulfate. The amount of water - as much as possible, in order to dissolve as much of the hormone. Further studies have shown that creams containing anti-inflammatory corticosteroid is, have several disadvantages: they are sticky and unpleasant when applied to the skin, have insufficient contact with the skin, because of what steroids not penetrate it.

These drawbacks are eliminated creams. On the Russian market comes the preparation for local application in the form of a cream containing betamethasone valerate (0,122%) and gentamicin sulfate (0.1% in terms of gentamicin) (Schering-Plough Labo N.V., Belgium) under the title "Tselestoderm-In with garamycin". Known as the "Garson" eye ointment, eye and ear drops containing 1 g or 1 ml of betamethasone sodium phosphate 1 mg and gentamicin sulfate 3 mg (Mashkovsky PPM, "Drugs", M, LLC "New Wave", 2004, Vol.2, p.36).

In the Russian Federation registered the cream "Belogent" (Belupo, Croatia) and cream "Diprogenta" (Schering-Plough, Belgium). These drugs contain betamethasone dipropionate (0,064%) and gentamicin sulfate (0.1% in terms of gentamicin) on cream base (State register of medicines. 1. - M.: Russian Ministry of health, 2002. - 1300 C.).

However, information about specific excipients in medicines are not available. It is also known that many organisms have developed resistance to antibiotics, which can significantly reduce therapeutic efficacy of the drug.

The objective of this invention is to provide medicines in the form of soft Le is arctonoe form, which comprehensively affects the diseased tissue and exerts multiple therapeutic effect of anti-allergic, anti-inflammatory and antibacterial, without reducing the latter with continued use, meets the requirements of Gosfarmakapei XI edition and has a shelf life of 2 years.

The problem is solved by a pharmaceutical composition with anti-inflammatory and antiallergic effect, comprising as active ingredient a combination of betamethasone dipropionate and gentamicin sulfate and targeted supplements: nipagin, propylene glycol, vaseline oil health, Trilon B, emulsifier, buffer substances and water in the following ratio, wt.%:

Betamethasone dipropionate0,05-0,08
Gentamicin sulfate0,05-0,15
Nipagin0,02-0,30
Propylene glycol10,9-29,60
Vaseline oil health15,0-30,0
Trilon B0,45-0,55
Emulsifier1,0-9,0
Buffer substances0.5 to 1.5
Waterto 100 g

A new pharmaceutical composition is made in the form of soft drugs is army, preferably in the form of cream.

The proposed ratio of the active substance and the target additives found experimentally and is optimal, providing a combined pharmaceutical compositions according to the requirements of Gosfarmakapei XI ed. and the shelf life of not less than 2 years (see table 2).

One of the conditions that determine the quality and safety of medicines for local use, is the effectiveness of antimicrobial preservatives. As the last experimentally selected nipagin, which exhibits antimicrobial activity in a wide range of pH from 3 to 8. Nipagin has a broad spectrum of antimicrobial activity against bacteria and fungi, also in combination with other excipients, for example, propylene glycol, shows a synergistic antimicrobial effect.

The basis of inclusion in the pharmaceutical composition of the hydrophilic solvent is propylene glycol is a good solubility in him nipagina and betamethasone dipropionate, which greatly simplifies the process of obtaining a cream. In addition, the propylene glycol has some preservative action, and in concentrations above 10% it eliminates the inhibitory effect of surfactants on the antimicrobial activity of nipagin. Besides propylenglycol who provides pharmaceutical compositions capacity to absorb exudate, ie has a drying effect.

A study of anti-inflammatory, antiexudative and the drying action of different composition oil phase as the most optimal was chosen as the basis, in which the oil phase is used vaseline oil.

As emulsifiers used a mixture of cetosteatil ether of macrogol 20 and cetosteatil alcohol. The study of rheological properties of pharmaceutical compositions allowed to determine the optimal concentration of emulsifiers and 5-9%, and the ratio of cetosteatil ether of macrogol 20 and cetosteatil alcohol in the range from 1.0 to:from 6.0 to 3.0:about 4.0, preferably from 1.1:5,9 1,5:5,5. The research made it possible to obtain a stable dispersion system, rheological properties which provide the necessary consistency and physical stability of pharmaceutical compositions.

The pH of the pharmaceutical composition should be in the range from 4.5 to 6.0, preferably 5.0 to 5.5. These values are the most favorable pH for the skin, but also to stabilize nipagina during storage in aqueous solutions. In addition, at pH below 4.5 starts the decomposition process of betamethasone propionate. To obtain the desired pH of the cream, and also for the stability of betamethasone dipropionate and nipagina was selected buffer system is mA containing a mixture of sodium disubstituted phosphate and potassium phosphate one-deputizing at a ratio of from 1:1 to 1:39, preferably from 1:4 to 1:13.

It is known that many microorganisms to antibiotics - aminoglycosides may develop resistance. To prevent this phenomenon in cream entered surfactants and hydrophilic non-aqueous solvents (cetyl ether of macrogol 20, propylene glycol), and Trilon B, increasing permeability of the walls of microbial cells and increases the sensitivity of microorganisms to antibiotics.

Specific anti-inflammatory activity proposed composition was studied on a model of acute aseptic dextranomer inflammation of the foot rats, double skin applications (for 30 minutes and at the time of introduction floranova agent) in sexually Mature rats male. As evidenced by the experimental data, two-treatment-and-prophylactic skin application of study drug cause a marked statistically significant anti-inflammatory effect, which is manifested in the reduction of gain swelling of the foot in comparison with untreated control animals, and this effect is virtually indistinguishable from the effect of the standard samples (Belogent" and "Diprogenta").

Experimental study of the anti-allergic action C the show was conducted on the model DNCB-dermatitis in Guinea pigs. Morphological studies showed that the drug has expressed specific antiallergic, antipruritic and anti-inflammatory effect, virtually indistinguishable from the standard samples.

The pharmaceutical composition on the basis of betamethasone dipropionate and gentamicin sulfate meets all regulatory requirements and has a shelf life of at least 2 years (see table 2).

The inventive tool can be obtained by the known methods used for the preparation of soft medicinal forms.

The following examples illustrate the invention.

A typical example. In reactor No. 1 pre-dissolve otusanya of betamethasone dipropionate and nipagin in parts of propylene glycol at a temperature of 60-65°and With stirring. In reactor No. 2 under stirring and at room temperature is dissolved in parts of water gentamicin sulfate. In reactor No. 3 is placed pre-otusanya sodium disubstituted phosphate and potassium phosphate one-deputizing and dissolve them at room temperature and the stirring of the water. In reactor No. 4 load the remaining water, pre-otusanya Trilon B, propylene glycol, cetosteatil alcohol, cetosteatil ether of macrogol 20 and vaseline oil health. The mass in the reactor is heated to 70-75°with stirring, emuleret and Hledat to 55-60° S, after which the emulsion is injected solution from the reactor No. 1. With constant stirring the mass in the reactor No. 4 is cooled to a temperature of 35-40°and then injected sequentially solutions from reactors No. 2 and No. 3. With constant stirring the mass in the reactor No. 4 is cooled to room temperature and cream Packed in tubes.

Specific examples of carrying out the invention is presented in table 1.

The resulting cream on the basis of betamethasone dipropionate and gentamicin sulfate meets all regulatory requirements and has a shelf life of at least 2 years (see table 2).

1,30
Table 1
IngredientsContent, wt.%
Examples
123
Betamethasone dipropionate0,0640,020,18
Gentamicin sulfate0,100,250,02
Nipagin0,200,020,30
Propylene glycol21,710,929,6
Vaseline oil health20,015,030,0
Cetosteatil ether macrogol 201,003,00
Cetosteatil alcohol5,706,004,00
Trilon B0,500,11,0
Sodium phosphate disubstituted0,100,020,50
Potassium phosphate one-deputizing0,900,500,99
Water100100100

Table 2
Name

quality score
The actual indicators
Standards of quality requirementsExample 1Example 2Example 3
DescriptionCream white or almost whiteCream whiteCream whiteCream white
pHFrom 4.5 to 6.05,05,1a 4.9
UniformityThe cream should be homogeneousUniformUniformUniform
Microbiological purityOn GF XI and var. No. 3
Quantitative1 g of the drug:
definitionthe content of betamethasone dipropionate
from 0,180 to 0,220 mg-0,207-
from 0,576 to 0.704 mg0,640--
from 1,620 to 1,980 mg--1,790
the content of gentamicin sulfate
from 0,180 to 0,220 mg--0,198
from 0.900 for up to 1,350 mg1,100--
from 2,250 to 2,750 mg-2,525-
Shelf life2 years2 years2 years2 years

1. Pharmaceutical composition with anti-inflammatory and antiallergic action, which includes the activities of the respective substances the combination of betamethasone dipropionate and gentamicin sulfate and targeted supplements, characterized in that as the target additives it contains nipagin, propylene glycol, vaseline oil health, Trilon B, emulsifier, in which it contains a mixture of cetosteatil ether of macrogol 20 and cetosteatil alcohol at a ratio of from 1:6 to 3:4, buffer substances which it contains a mixture of sodium disubstituted phosphate and potassium phosphate one-deputizing at a ratio of from 1:1 to 1:39, and water in the following ratio, wt.%:

Betamethasone dipropionate0,05-0,08
Gentamicin sulfate0,05-0,15
Nipagin0,02-0,30
Propylene glycol10,9-29,60
Vaseline oil health15,0-30,0
The trylon B0,45-0,55
Emulsifier1,0-9,0
Buffer substances0.5 to 1.5
Water100

2. The pharmaceutical composition according to claim 1, characterized in that the ratio of cetosteatil ether of macrogol 20 and cetosteatil alcohol is from 1.1:5,9 1,5:5,5.

3. The pharmaceutical composition according to claim 1, characterized in that the ratio of sodium disubstituted phosphate and potassium phosphate odnosnie the th is from 1:4 to 1:13.

4. The pharmaceutical composition according to 1, characterized in that it is made mainly in the form of cream.



 

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