Antibacterial and necrolytic local lisoamidase pharmaceutical composition

FIELD: medicine.

SUBSTANCE: invention is applied for treatment of purulent wounds and burns, pyoinflammatory dermatopathies, and for acceleration of healing and improvement of wound healing conditions. The composition possesses antibacterial and necrolytic action; it contains an active complex of bacteriolytic and proteolytic enzymes - Lisoamidase, and a base for soft formulation of the composition. The base contains a thermally stable perfluororganic compound emulsion with gas-transport properties and mixed hydrophilic substances specified as follows: proxanol-268, polyethylene oxides, propylene glycol, dimexide, hyaluronic acid or sodium hyaluronate, sorbite, glycerine, aerosil. Besides, the composition can contain at least one desired additive chosen from: anaesthetic (Chinoxycaine, Trimecaine, Pyromecaine, Lidocaine or mixed), a reparative process stimulator (methyluracil, acetamine, ethadene, calcium pantothenate, Solcoseryl or mixed) or mixed. The composition is made in the form of ointment or gel, rectal suppositories or capsules.

EFFECT: extended application, enhanced therapeutic activity and ease of use; lower consumption of the active substance; ensured anaesthetising effect; improved microcirculation in wound tissues, managed inflammatory processes, additional stimulation of reparative processes.

6 cl, 2 tbl, 19 ex

 

The invention relates to medicine and veterinary medicine, namely to pharmacological drugs used in the treatment of wounds and burns, purulent-inflammatory diseases of the skin and the other to accelerate and improve healing.

Known complexes bacteriolytic enzymes that lyse gram-positive microorganisms resistant to antibiotics (patent RU 1549227, C12N 9/00, 1984.10.04; EN 2193063, C12N 9/00, 2000.11.29).

Complex bacteriolytic enzymes (patent RU 1549227), used in medicine under the name isoamylase, and in veterinary medicine - lysomal (patent RU 2064299, A61K 35/74, 1993.12.13), consists of three bacteriolytic enzymes immobilized on the polysaccharide, which increases their stability. The polysaccharide provides long-term (over several years) high activity of its constituent enzymes, and immune-stimulating properties of the drug isoamylase.

On the basis of this complex developed pharmacological agent with antibacterial and necroticism effect produced in the form of dried powder, Packed in 10 ml vials of 50 PE 100 PE with hermetically sealed with rubber stoppers. The kit contains a solvent in ampoules of 5 ml at a rate of 1 vial of 50 PE (monograph FS 42-3329-96 and FS 42-3332-96).

The preparation is applied in liquid form is in phosphate buffer solution with a concentration of 5 PE (LE 50) in 1 ml; 10 PE (LE 100) in 1 ml; 25 PE (LE 250) in 1 ml.

Bacteriolytic enzymes included in the active complex of the specified drug destroys the cells of a wide range of gram-positive pathogens such as staphylococci and streptococci, including those with multiple resistance to antibiotics, the radio micrococci, meningococci, gonococci, gram-positive bacilli. Due to the presence in the complex of proteases and enzymes, possessing at the same time and proteolytic activity, the product cleans the wounds of necrotic masses. Fragments of the destroyed cells possess immune stimulating effects.

Clinical trials of the drug showed that isoamylase in the treatment of purulent wounds of soft tissues accelerates compared with other traditional and non-traditional means in the course of the wound process. Faster decrease the microflora content, faster than normal they, faster rejection of necrotic masses, faster granulation and even the epithelial tissues. The duration of treatment of patients with purulent wounds of soft tissues were reduced in many cases in 2 times. Isoamylase stimulates reparative processes, providing, in addition to necroticism and bacteriolytic action, influence on the course of the 2nd phase of inflammation, not only by reducing phase-1, h is about typical for all enzyme preparations, used to treat in such cases, but also by directly stimulating effect on the cells of granulation tissue, acting directly on the cells of proliferate.

Application of known drug in the form of liquid solutions has a number of disadvantages, namely: the drug is poorly recorded and retained on the wound surface, which leads to increased consumption of active substances in the treatment; requires pre-cultivation in the buffer solution and special measures to prevent rapid drying, that is not convenient in the treatment process. All this reduces the adherence of the patient to treatment. The disadvantages of this drug is that it does not possess local anesthetic action.

Object of the present invention is to provide a pharmaceutical preparation for topical application in the form of soft medicinal forms on the basis of the bacteriolytic complex and proteolytic enzymes.

Technical results that may be obtained by using the present invention: the expansion of the scope, increasing therapeutic activity; improved ease of use; reduction of consumption of the active substance; obtaining an anesthetic effect; improved microcirculation in wound tissues, attenuation of inflammatory processes, updat the additional stimulation of reparative processes.

To solve this problem is proposed pharmaceutical preparation for topical application in the form of soft dosage forms comprising active bacteriolytic complex and proteolytic enzymes, for example lizoamidazy, (hereinafter "active complex") and a framework to provide soft dosage form of the drug, with the following ratio of components (wt.%):

active complex- 0,1-5,0;
base- the rest.

The proposed remedy for topical application in the form of soft medicinal forms additionally contains a special additive that is compatible with the active complex, in the following ratio of components (wt.%):

active complex- 0,1-5,0;
additives target- 0,5-10,0;
base- the rest.

As the target additives may be local anesthetic agent and/or stimulator of reparative processes.

To provide an anesthetic effect in the proposed pharmacological drug can soda is to use local anesthetic substance under the following ratios of components (wt.%):

active complex- 0,1-5,0;
local anesthetic substance- 0,5-5,0;
base- the rest.

This local anesthetic substance can be, for example, cinoxacin, trimekain, piromekain, lidocaine, benzocaine (benzocaine) and dibucaine or mixtures thereof.

In addition, the proposed pharmacological drug may include a stimulator of reparative processes in the amount (wt.%):

active complex- 0,1-5,0;
stimulator reparative processes- 0,5-5,0;
base- the rest.

This substance, which is a stimulator of reparative processes may be, for example, methyluracil, atsemin, etagen, calcium Pantothenate, solcoseryl, tricresol or their mixture.

The proposed pharmacological preparation containing a local anesthetic substance, may also contain the stimulant of reparative processes in the following ratio of components (wt.%):

active complex- 0,1-5,0;
local anesthetic substance- 0,5-5,0;
stimulator reparative processes- 0,5-5,0;
base- the rest.

In accordance with the invention of soft medicinal forms on the basis of the bacteriolytic complex and proteolytic enzymes, type isoamylase are buttery soft dosage forms (ointments, gels, creams, and also formed of soft medicinal forms - gelatin capsules for rectal application.

In the proposed pharmacological basis of preparation contains a thermally stable emulsion performancesin compounds in the gas transport properties and the mixture hyperosmolar substances in the following ratio of components (wt.%):

emulsion perforamances connections- 5,0-70,0;
the mixture hyperosmolar substances- the rest.

Hyperosmolar substances contained in the mixture, for example, with the following ratio of components (wt.%):

Blend # 1:

proxanol is chosen-268 or polyethyleneoxide-1500- 15,0-50,0;
1,2-propylene glycol- 5,0-50,0;
the polyethylene oxide PEO-400- the rest.

Blend # 2:

proxanol is chosen-268 or polyethyleneoxide-1500- 15,0-40,0;
1,2-propylene glycol- 20,0-50,0;
the polyethylene oxide PEO-400- 5,0-30,0;
phosphate buffer solution or purified water- the rest.

Blend # 3:

proxanol is chosen-268 or polyethyleneoxide-1500- 15,0-40,0;
1,2-propylene glycol- 20,0-50,0;
the polyethylene oxide PEO-400- 10,0-30,0;
dimexide- 0,5-3,0;
phosphate buffer solution or purified water- else is.

Blend # 4:

the polyethylene oxide-1500 or proxanol is chosen-268- 15,0-60,0;
the polyethylene oxide PEO-400- the rest.

Blend # 5:

the polyethylene oxide-1500 or proxanol is chosen-268- 15,0-60,0;
the polyethylene oxide PEO-400- 20,0-80,0;
phosphate buffer solution or purified water- the rest.

Blend # 6:

the polyethylene oxide-1500 or proxanol is chosen-268- 15,0-60,0;
the polyethylene oxide PEO-400- 20,0-80,0;
dimexide-0,5- 3,0;
phosphate buffer solution or purified water- the rest.

Blend # 7:

the polyethylene oxide PEO-1500 or proxanol is chosen-268- 10,0-80,0;
hyaluronic acid or hyaluronate is the sodium of 0.01 to 3.0;
phosphate buffer solution or purified water- the rest.

Blend # 8:

the polyethylene oxide PEO-1500 or proxanol is chosen-268- 10,0-50,0;
the polyethylene oxide PEO-400- 40,0-10,0;
hyaluronic chilota or sodium hyaluronateof 0.01 to 3.0;
phosphate buffer solution or purified water- the rest.

Blend # 9:

the polyethylene oxide PEO-1500 or proxanol is chosen-268- 10,0-50,0;
the polyethylene oxide PEO-400- 5,0-30,0;
1,2-propylene glycol- 10,0-40,0;
hyaluronic acid or sodium hyaluronateof 0.01 to 3.0;
phosphate buffer solution or purified water- the rest.

Blend # 10:

td align="right"> - 5,0-50,0;
proxanol is chosen-268
1,2-propylene glycol- 1,0-20,0;
glycerin- 1,0-10,0;
sorbitol- 2,0-10,0;
phosphate buffer solution or purified water- the rest.

Blend # 11:

1,2-propylene glycol- 1,0-40,0;
glycerin- 1,0-40,0;
phosphate buffer solution or purified water- the rest.

Blend # 12:

glycerol or 1,2-propylene glycol- 10,0-50,0;
Aerosil- 5,0-20,0;
phosphate buffer solution or purified water- the rest.

One of the main tasks of the local treatment of wounds and burns is the problem of suppression of pain. To solve this problem in the proposed drug applied local anesthetic substance, which can be used hinokio is n (a derivative of quinoline), with bacterial and antioxidant activity; lidocaine; trimekain, keeping the activity in an acidic environment, which is characterized by a purulent wound; piromekain; benzocaine; dibucaine. Lidocaine, trimekain and piromekain the most promising part of the proposed drug in a hydrophilic base. For the proposed drug on the basis of fats should be used, for example, benzocaine (benzocaine) and dibucaine.

To provide additional stimulation of repair processes in the wound proposed remedy on the basis of a complex bacterial plankton and proteolytic enzymes contains a substance wound healing actions: methyluracil, atsemin, etagen, calcium Pantothenate, solcoseryl, tricresol or their mixture.

Methyluracil, being a derivative of pyrimidine, has anabolic and anti-catabolic activity. The substance does not have a local irritant, accelerates cell regeneration processes, reducing the healing time of wounds, stimulates cellular and humoral defense factors, anti-inflammatory, stimulates Erythro - and leucopoiesis.

The atsemin accelerates tissue regeneration and epithelization processes. Used for the treatment of nonhealing wounds and burns.

Atadan stimulates reparative processes in epithelial and hematopoietic tissues, activating m the metabolism of nucleic acids. Indicated for the treatment of thermal and radiation injuries of the skin, the mucous membrane of the rectum, nonhealing granulating wounds, etc.

Calcium Pantothenate is a promising wound healing agent. Is used to treat burns and slowly healing wounds.

Solcoseryl - extract blood of cattle, released from proteins and non-antigenic activity. Substance accelerates the growth of granulation and epithelization of wounds, improves metabolic processes in the tissues.

Traceson - triethanolammonium salt of 2-methylphenoxyacetic acid. Stimulates proliferative-reparative processes, which makes the perspective of its use in surgery to accelerate healing of purulent-necrotic damage and postoperative wounds ("pharmaceutical journal", volume 41, No. 1, 2007, p.3-7).

Aerosil colloidal silica. Fine, micronized powder with a particle size of from 4 to 40 microns (generally 10-30 μm), a density of 2.2 g/cm3has a large specific surface area of 50 to 400 m2/year In water and alcohol in a concentration of 1-3% forms a turbid suspension, with liquids having a refractive index of 1.45, forms a transparent studniarski system (glycerin, liquid paraffin etc). When applied externally, is not irritating to the skin, does not violate skin the currency.

From a microbiological point of view due to the presence of an external polysaccharide membranes and hydrophilic capsules in gram-negative and gram-positive bacteria, which prevent the penetration of microbial cells hydrophobic antibacterial substances, hydrophilic base is preferable, as are the conductors of medicines in the microbial cell.

The hydrophilic base, which can be applied with the bacteriolytic complex and proteolytic enzymes, such as isoamylase in the proposed drug is divided into two groups:

water - soluble bases which, as a rule, contain purified water, hydrophilic non-aqueous solvents include polyethylene oxide, for example PEO-400, 1,2-propylene glycol, glycerin, ethyl cellosolve, dimexide, and water - soluble polymers include polyethylene oxide, for example PEO-1500, proxanol is chosen, for example proxanol is chosen-268;

- vodosnabzhenie basis, which in addition to water-soluble polymers and hydrophilic non-aqueous solvents contain lipophilic substances: higher fatty alcohols, vaseline, vaseline oil, lanolin, waxes (these are the basics, as a rule, are of emulsion type oil/water and require the presence of emulsifier type oil/water).

Basics with hyperosmolar properties play an important role in local therapy of purulent wounds. They provide an outflow of purulent e is sudate from the wound, have anti-inflammatory effect due to absorption of fluid and reduce swelling of the wound, and also protect tissues from overhydration. Often they contribute to the strengthening of action of antibacterial agents.

For substances with high hyperosmolar properties include oxides - water-soluble polymerization products of ethylene oxide, which are physiologically indifferent compounds. In this class of substances are hydrophilic nonaqueous solvents (polyethylene oxide, for example PEO-400; 1,2-propylene glycol; glycerin; ethyl cellosolve; Dimexidum) and polymers (polyethylene oxide, for example PEO-1500, proxanol is chosen-268). They are easy to apply on the wound surface and evenly it is distributed, improving the contact with the juvenile tissues and content wounds, mix well with wound exudate and retain their homogeneity, low toxicity and have no irritant action on the tissues, do not violate their physiological functions.

In the festering wound PEO of different molecular masses behave differently. Thus, molecules PEO-1500 stably retain the primary localization: they remain in the wound cavity and actively associated inflammatory exudate, giving him the armband, with which the liquid evaporates. The released molecules PEO-1500 newly added to the water itself, and the process repeats. the more small molecules PEO-400 have the ability to penetrate deep into the tissue and after 2 hours are defined in the bottom and walls of the wound. Forming complexes with antibacterial substances, PEO-400 holds them in tissue wounds, where localized microbes. The ability of the oxides to provide antimicrobial drug interstitial action fundamentally distinguishes this ointment base from fat frameworks or solutions of antibiotics (antiseptics), antimicrobial action of which is limited only by the surface of the wound, although it was deep microflora determines the intensity and direction of flow of a purulent process.

The main property of PEO is that they have a strong dehydrating (water-absorbing) action on the fabric. Due to its high ability to hydrogenate itself, these polymers actively absorb wound exudate, and with it, and microbial toxins, products of tissue destruction, as well as various biologically active substances of lysosomal enzymes and other mediators of the inflammatory process, thereby interrupting its progressive course. Of fundamental importance is the fact that in the festering wound dehydrating effect of PEO applies not only to the cloth forming the bottom and sides of the wound cavity, but is contained in the wound microbial cells. Dehydration of microbial cells leads to a significant decrease of its biological activity, including resistance to the action of certain drugs is the R funds. Therefore, in the presence of PEO tenfold increases antimicrobial activity of antibiotics.

Is also important that the dissolution of antibiotics, sulfonamides and other substances in PEO increases their dispersion with increasing therapeutic activity, which also contributes to a more rapid release of the fundamentals of antimicrobial substances. PEO is an active conductor of drugs through the skin barrier. Importantly, this penetrating without damage to the cells the ability of PEO increases in conditions of inflammation.

The hydrophilic base on the oxides can dissolve in the secrets of the mucous membranes, to fully release the medicinal substance, not to irritate, have a long shelf-life, high physiological indifference, which facilitates their use in buttery and formed of soft medicinal forms.

Important biomedical requirement ointment soft medicinal forms, is the ability to moisten the wound surface and to spread it, due to the surfactant properties of solvents, polymers, surface-active substances (surfactants) and the framework in General. The most pronounced surface activity are alcohols and ethyl cellosolve, which is unsuitable for inclusion in the basis is found in high concentrations. From glycols preferably the use of 1,2-propylene glycol and PEO-400 compared with glycerol, with a weak surface-active properties.

In the State register of medicines registered 5 polyethylene oxides (PEO) with different molecular weight PEO-400; PEO-1000; PEO-1500; PEO-2000 and PEO-4000.

When mixed solvent PEO-400 polymer PEO-1500 latter acts as a thickener, which, depending on the number in the total mass is the desired consistency created the dosage form. In addition, PEO-1500 is an osmotically active substance, absorbing purulent exudate due to the binding of water molecules with hydroxyl and ether groups. This basis is recommended for topical dosage forms used in the local treatment of wounds in the 1st phase of wound healing.

Proxanol is chosen-268 - oxides block copolymers of propylene and ethylene. Proxanol is chosen-268 as osmotically active substance provides a more uniform nature of the absorption and has a longer period of osmotic action. The total mass of absorbed water solutions proxanol is chosen-268 24 hours significantly exceeds that in the case of the use of PEO-1500. This is due to the higher mass of proxanol is chosen-268 (8.7 times greater than that of PEO-1500).

The kinetics of water absorption solvents and poly the apostrophes depends on their molecular weight, the concentration and molecular structure. So PEO-400 absorbs more water than the 1,2-glycol, and has a longer period of osmotic action. Sorption activity of 1,2-propylene glycol is maintained for 4-6 hours. This is due both to lower its molecular weight compared to the PEO-400, and a lower hydrophilic-lipophilic balance (products HLB), which for propylene glycol is 9,38.

The amount of hydrophilic-lipophilic balance (products HLB) greater than greater hydrophilicity has substance. Therefore, the above products HLB and molecular weight, the stronger and longer will be apparent osmotic effect of a substance at a given concentration. The products HLB values for some substances: 1,2-propylene glycol - 9,375; glycerol - 11,275; ethyl cellosolve to 8.3; PEO-400 - 12,49; PEO-1500 - 20,74.

1,2-propylene glycol, PEO-400, PEO-1500, proxanol is chosen-268 can be preservatives in developing soft medicinal forms.

Violation of microcirculatory is one of the main factors in the pathogenesis of the inflammatory process. It includes not only the blood flow through the arterioles, capillaries and venules, but also the transcapillary exchange, providing the necessary for living tissue homeostasis. Disorders microcirculation divided into intravascular changes, disorders of the vascular and extravascular changes. Treatment with the ECHR drugs used to improve the processes of microcirculation in the tissues of the wound, to a considerable extent can be implemented at the expense of their antihistamine, anti-inflammatory and dehydrating steps.

The use of hyperosmolar framework, compatible with the complex bacterial plankton and proteolytic enzymes, improves microcirculation in the tissues of the wound due to its dehydrating action. When applied the basis consisting of hyperosmolar substances, has an indirect anti-inflammatory effect due to the absorption of fluid and reduce swelling of the wound.

Dimexide - 30%solution of dimethyl sulfoxide (DMSO) is used as an anti-inflammatory drug for external use, inactivating hydroxyl radicals and improves the course of metabolic processes in inflammation. Also has local anesthetic, analgesic and antimicrobial effects, has a moderate fibrinolytic activity. Penetrates the skin, mucous membranes, membrane microbial cells increases their sensitivity to antibiotics) and other biological membranes without damaging them and can hold a variety of medicines in the depth of the wound. Negative characteristics of Dimexidum should include the fact that it dries quickly.

Hyaluronic acid is a polysaccharide from the family of the glucose is Mogliano - has the ability to bind to 1000 times more water than it weighs itself. Hyaluronic acid has the highest water absorption compared to other moisturizing agents such as glycerin and sorbitol. This absorbed water is retained within the gel and does not evaporate even at lower relative humidity of the surrounding air. Due to its high hydrophilicity, hyaluronic acid forms with water a high-viscosity gel that moisturizes the skin and mucous membranes. Hyaluronic acid is non-toxic. In the composition of the gels of hyaluronic acid has antimicrobial, wound healing and anti-inflammatory, promotes regeneration of the epithelium, prevents the formation of granulation tissue, adhesions, scarring, normalize circulation, does not cause clinical complications.

Hyaluronic acid has a positive effect on the course of local inflammatory processes, binds microflora, as well as the products of its decay and life, has a pronounced anti-inflammatory action and local anesthetic effect. At the same time, hyaluronic acid performs and mechanical protection of the Russian Academy of Sciences, as it forms thin film that prevents the penetration into the wound environmental factors - disease-causing agents. Gels based on hyaluronic acid is used to treat the local and General inflammatory processes, thermal and chemical burns, trophic ulcers, chronic venous insufficiency, radiation skin lesions, cracks, abrasions, and also for the treatment of nonhealing wounds of different etiology (patent RU №2195262).

Sodium hyaluronate is the sodium salt of hyaluronic acid is soluble in water to form a viscous colorless gel with a pH of 6.0 -7,5 (0.1%solution). In its activity of sodium hyaluronate is a complete analogue of hyaluronic acid, promotes tissue regeneration without the formation of scars, has the ability to stimulate cell migration and proliferation. Used in concentrations ranging from 0.01 to 0.5%.

It is known that performancesee emulsion with gas transport properties, type perftoran was used in the complex treatment of wounds and wound infection (Krylov, D., and other Methods infusion of perftoran in treatment of wounds and wound infection. Problems of intensive therapy in the clinic. Abstracts of scientific conference. December 12-13, 1985): B. I., 1985 - p.12-13). In addition, it is known that perfluorocarbon compounds are promising anti-inflammatory drugs for the treatment of skin diseases and can be used in dermatology and medical cosmetology (Umerov JG, Filipov E.A. Perfluorocarbon compound is a promising anti-inflammatory drugs for treatment the skin diseases. IX all-Union Congress of dermatovenereologists. Alma-ATA, September 23-27, 1991, Abstracts. - M., 1991. - str).

Performancesee emulsion with gas transport properties have wound-healing effect, which is associated with their effect on the gas exchange of surrounding tissue as the wound lesion is accompanied with progressive tissue hypoxia and increasing acidosis (patent RU №2033163, A61K 33/16, 1995.04.20).

Known performancesee emulsion with gas transport properties (for example, patent RU No. 2088217, A61K 9/10, 1993.05.07)that can be stored at room temperature for at least 1 year.

The above analysis of the known properties of hyperosmolar agents allowed to pick up the above basis with hyperosmolar properties for the proposed pharmacological preparation containing the bacteriolytic complex and proteolytic enzymes.

Using these bases for soft medicinal forms, as well as the bacteriolytic complex and proteolytic enzymes, mestnoanesteziruyuschee substances and stimulates reparative processes proposed composition of hydrophilic ointments, hydrophilic creams, hydrophilic gels, which can also be used for the manufacture of gelatin or other capsules for rectal application.

Type dosage forms offer pharmacological what about the drug depends on the molecular weight used hyperosmolar substances, their ratio in the mixture, and the quantitative ratio of hyperosmolar basis with other components of the pharmaceutical preparation. Based on these quantitative ratios, dosage form proposed pharmacological drug may be an ointment, gel or cream.

Most preferred for external use is an ointment form, as it is well recorded and retained on the wound surface, longer has therapeutic activity, cheaper to manufacture, convenient in use, which increases the motivation of the patient to treatment.

Hydrophilic ointments are hyperosmolar, resulting in the application can absorb a significant amount of exudate.

Hydrophilic creams prepared on the basis of emulsions of the water/oil or water/oil/water, stabilized with suitable emulsifiers. It also includes colloidal disperse system consisting of a dispersed in water or mixed water-glycol solvents, higher fatty alcohols or acids, stable hydrophilic surfactant. Creams are a two - or multiphase dispersed system, a dispersive medium which when installed the storage temperature, as a rule, has a Newtonian type currents and low values of rheological parameters.

Gidrofiljnihe (hydrogels) prepared on bases, consisting of water, hydrophilic or mixed non-aqueous solvent (glycerol, 1,2-propylene glycol, polyethylene oxide PEO-400) and the hydrophilic gelling (carbomer, derivatives of cellulose, tragakant, sodium hyaluronate, hyaluronic acid and others). Gels are one-, two - or multiphase dispersed liquid dispersive medium, the rheological properties due to the presence of geleobrazovanie in relatively small concentrations. In this dosage form, geleobrazovanie additionally can act as stabilizers of disperse systems: suspensions or emulsions.

Gelatin capsules for rectal use of technology, biopharmaceutical and economic point of view. Gelatinous sheath protects the medicinal substance from the effects of environmental factors and has advantages over the suppositories, as it can capsulitis substances in the form of ointment, liniment, cream, gel, emulsion, suspension and other drug Release is faster and easier than suppositories, as under the influence of a slightly alkaline environment (pH 7.3 to 7.6) content rectal gelatin membranes swell, and in this state, even weak peristalsis of the rectal wall is sufficient to rupture and release the contents. Colchesterstarting substance in the capsule, providing the desired therapeutic effect, is a double dose suppositories.

Thus, the production of rectal means in the gelatin shell saves costly biologically active ingredients and to reduce the cost of drugs. Rectal gelatin capsules with the proposed pharmacological drug meet all the requirements of an ideal suppositories and can be used in medicine for the treatment of proctologic diseases.

The bacteriolytic complex and proteolytic enzymes, type isoamylase, offer pharmacological drug analyzes gram-positive microorganisms, including antibiotic-resistant, and also due to its proteolytic activity cleanses the wounds of necrotic masses, providing the immunostimulatory effects. In addition, isoamylase stimulates reparative processes due to the stimulating effect on the cells of granulation tissue.

The application of the proposed local anesthetic drug substances, as monocomponent, and in the form of a mixture of components, significantly suppresses pain syndrome in the treatment of wounds and burns. In this application of local anesthetic substances with antibacterial and antioxidant activity, such as cinoxacin, enhances therapeutic effect of redlounge pharmacological tools.

To provide additional stimulation of repair processes in the wound in the proposed pharmacological tool applied in the form of monocomponent, and a mixture of components with different mechanism and spectrum of activity, a substance that stimulates reparative processes in the wound.

The use of hydrophilic base, consisting of a mixture of polietilenoksidov and proxanol is chosen in the proposed pharmacological drug ensures quick delivery of active substances to microbial cells and the cells of the tissue that enhances therapeutic activity of the proposed drug. In addition, the de-hydration of the hydrophilic base cells of gram-positive microorganisms reduces their resistance to the damaging effects of complex bacterial plankton and proteolytic enzymes. It also enhances therapeutic activity of the proposed drug. The use of hyperosmolar basics additionally improves microcirculation in the tissues of the wound due to its dehydrating action, and also provides additional anti-inflammatory effect due to absorption of fluid and reduce swelling of the wound.

Hyperosmolarity Foundation provides outflow of purulent exudate from the wound and protects the tissue from overhydration. It is easy to apply on the wound surface, well it is charged evenly it is aspidella, improving contact with the juvenile tissues and the contents of the wounds, it penetrates beneath the scab, mixes well with wound exudate, while maintaining its homogeneity, low-toxic and does not intrude on the fabric, does not violate their physiological functions. The dissolution of the active substances in polietilenoksidnoy basis improves their dispersibility and the ability to more rapid release of the framework, thereby increasing therapeutic activity of the proposed drug. This basis is the conductor of the active substances through the skin barrier, with such penetrating without cell damage ability is enhanced in conditions of inflammation.

Hydrophilic is based on the oxides can dissolve in the secrets of the mucous membranes, completely releasing the drug substance is not irritating when this mucous has a long shelf-life and high physiological indifference.

The implementation of the present invention is illustrated by the following examples, but is not limited to them.

Example 1.

100 g of ointment contains:

isoamylase- 1,0;

emulsion performancesin connections:

PERFLUORO [1-( methylcyclohexyl)piperidine] - 25,0;
the stabilizer lecithin-standard- 2,5;
purified water- 22,5;

hydrophilic components:

1,2-propylene glycol- 20,0;
proxanol is chosen-268- 20,0;
the polyethylene oxide PEO-400- 9,0.

Example 2. The ointment.

100 g of ointment contains:

isoamylase- 2,0;
trimekain- 2,0;
atadan- 4,0;
emulsion performancesin connections- 42,0;

blend # 2:

proxanol is chosen-268- 25,0;
1,2-propylene glycol- 10,0;
the polyethylene oxide PEO-400- 5,0;
phosphate buffer solution (0.01 M, pH 8.0- 10,0.

Example 3. The ointment.

100 g of ointment contains:

isoamylase- 4,0;
cinoxacin- 1,0;
methyluracil- 3,0;
the atsemin- 1,0;
emulsion performancesin connections- 45,0;

blend # 3:

proxanol is chosen-268- 21,0;
1,2-propylene glycol- 11,0;
the polyethylene oxide PEO-400- 6,0;
dimexide- 1,6;
phosphate buffer solution (0.01 M), pH 8.0- 6,4.

Example 4.

100 g of ointment contains:

isoamylase- 2,5;
methyluracil- 4,0;

emulsion performancesin connections:

PERFLUORO [1-(4 methylcyclohexyl)piperidine]- 6,0;CIS/Tran-perpendicular- 24,0;the stabilizer of a phospholipid Lipoid E80- 3,0;purified water- 27,0;

hydrophilic components:

proxanol is chosen-268- 20,0;
the polyethylene oxide PEO-400- 13,5.

Example 5. The ointment.

100 g of ointment contains:

isoamylase- 4,0;
piromekain- 2,0;
emulsion performancesin connections- 50,0;

blend # 5

proxanol is chosen- 26,0;
the polyethylene oxide PEO-400- 8,0;
phosphate buffer solution (0.01 M), pH 8.0- 10,0.

Example 6. The ointment.

In 100 g of m is zi contains, g:

isoamylase- 4,0;
trimekain- 3,0;
emulsion performancesin connections- 45,0;

blend # 6:

proxanol is chosen 268- 25,0;
the polyethylene oxide PEO-400- 10,0;
dimexide- 2,0;
phosphate buffer solution (0.01 M), pH 8.0- 11,0.

Example 7. The gel.

100 g of gel contains:

isoamylase- 2,5;
emulsion performancesin connections- 30,0;

blend # 7:

the polyethylene oxide- 30,0;
sodium hyaluronate- 0,5;
purified water- 37,0.

Example 8. The gel.

100 g of the El contains, g:

isoamylase- 4,0;
emulsion performancesin connections- 20,0;

blend # 8:

proxanol is chosen-268- 30,0;
the polyethylene oxide EC-400- 15,0;
sodium hyaluronate- 0,3;
phosphate buffer solution (0.01 M), pH 8.0- 30,7.

Example 9. The gel.

100 g of gel contains:

isoamylase- 2,0;
trimekain- 4,0;
methyluracil- 2,0;
emulsion performancesin connections- 25,0;

blend # 9:

proxanol is chosen-268- 30,0;
the polyethylene oxide PEO-400- 7,0;
1,2-ol is palinpinon to 12.0;
sodium hyaluronate- 0,5;
purified water- 17,5.

Example 10. The gel.

100 g of gel contains:

isoamylase- 2,0;
emulsion performancesin connections- 50,0;

blend # 10:

proxanol is chosen-268- 23,0;
1,2-propylene glycol- 9,0;
glycerin- 4,0;
sorbitol- 2,0;
phosphate buffer solution (0.01 M), pH 8.0- 10,0.

Example 11. The gel.

100 g of gel contains:

isoamylase- 2,0;

emulsion performancesin connections

blend # 11:

1,2-propylene glycol- 15,0;
glycerin- 10,0;
phosphate buffer solution (0.01 M), pH 8.0- 13,0.

Example 12.

100 g of gel contains:

isoamylase- 2,5;
methyluracil- 4,0;
Aerosil- 10,0;

emulsion performancesin connections:

PERFLUORO[1-(4 methylcyclohexyl)piperidine]- 20,0;
the stabilizer proxanol is chosen-268- 2,0;
purified water- 18,0;

hydrophilic components:

1,2-propylene glycol- 26,0;
phosphate buffer solution (0,01M), pH 8.0- 17,5.

Example 13. The capsule.

Ointment of example 2 is filled 500 piece gelatin capsules No. 00, the volume of 0.95 ml Raspadaemost received capsules less than 20 min, which meets the requirements of the global Fund XI (stopsley, str).

Example 14.

100 g of the El contains, g:

isoamylase- 0,1;
the atsemin- 1,0;

emulsion performancesin connections:

PERFLUORO [1-(4 methylcyclohexyl)piperidine]- 10,0;
the stabilizer of a phospholipid Lipoid E80- 1,6;
purified water- 8,4;

hydrophilic components

gel polyethylene oxide-1500- 78,9.

Example 15.

100 g of ointment contains:

isoamylase- 1,0;
lidocaine- 1,0;

performancesee emulsion:

PERFLUORO[1-(4 methylcyclohexyl) piperidin]- 25,0;
the stabilizer lecithin-standard- 2,5;
purified water - 22,5;

hydrophilic base:

1,2-propylene glycol- 20,0;
proxanol is chosen-268- 20,0;
the polyethylene oxide PEO-400to 8.0.

Example 16.

In 100 g of ointment contains, g;

isoamylase- 0,2;

performancesee emulsion:

PERFLUORO[1-(4 methylcyclohexyl) piperidine]- 25,0;
the stabilizer lecithin-standard- 2,5;
purified water- 22,5;

hydrophilic base:

1,2-propylene glycolto 20.0
proxanol is chosen-268- 20,8;
the polyethylene oxide PEO-400- 9,0.

Example 17.

The possibility of using the proposed composition for the treatment of inflammatory lesions shown on the next model. The first, second and third experimental groups of animals, each of which consisted of 10 animals outbred rats weighing 260-340 g, caused the formation of cellulitis by introducing the order of 108microbial tel culture of Staphylococcus aureus, and 0.25 ml of 25%aqueous solution of magnesium sulfate. Phlegmon animals have evolved over 5-7 days, then under the mask anesthesia in aseptic conditions, the abscess was opened and the treatment of inflammatory lesions was carried out according to the following scheme.

Each animal in the first group on the surface of the wound after opening phlegmon within 5 days 1 time per day was applied about 0.3 ml of 1%ointment with isoamylase (0.003 g) and anesthetic lidocaine (1%) on a hydrophilic base (oxides) with performancesee emulsion: PERFLUORO[1-(4 methylcyclohexyl) piperidin] - 25%; stabilizer lecithin-standard - 2,5%; purified water at 22.5%. (15.)

Each animal in the second group on the surface of the wound after opening phlegmon within 5 days 1 time per day was applied about 0.3 ml of 1%ointment with isoamylase (0.003 g) ointment in Example 15, but without special additives (without lidocaine).

When this ointment in the first and the second group was put on a sterile cloth, which was fixed on the wound.

For each animal from the third group of the wound after opening phlegmon within 5 su is OK 3 times a day was campanulales 0.5 ml of 1%solution lizoamidazy (0.005 g) in 0.01 M sodium phosphate buffer solution, which were drenched with sterile cloth. The wound on top covered with a dry sterile cloth and plastic film in order to reduce drying headbands and transition of the drug beyond.

Under the action of the composition with isoamylase in first, second and third group character separated in the first 1-3 days serous-purulent and serous-hemorrhagic, to the third day, mostly serous. On the third day observed regression of the inflammatory process, disappeared hypermia, the swelling of tissues. Granulation appeared in all groups mainly in 3-4 days. Epithelization was started in the first group at 4-5 days, reaching a maximum at 7-8 day, the second and the third group was started at 6-8 day, reaching a maximum at 8-12 day.

Thus, the presence of the emulsion performancesin compounds in the juvenile isoamylase accelerated epithelization of the tissue.

In addition, the pharmaceutical composition used in the first group, had a strong anesthetic effects as anxiety, lethargy, loss of appetite in the first group, animals were significantly less pronounced, especially during the 3-5 days after opening phlegmon than in the second and third group.

Example 18.

The first, second and third experimental groups of animals, each of which consisted of 10 animals outbred rats weighing 260-340 g, who reported the formation of cellulitis by introducing about 10 microbial bodies of the daily culture of Staphylococcus aureus, and 0.25 ml of 25%aqueous solution of magnesium sulfate. Phlegmon animals have evolved over 5-7 days, then under the mask anesthesia in aseptic conditions, the abscess was opened, and was treating inflammatory lesions according to the following scheme.

Each animal in the first group on the surface of the wound after opening phlegmon within 8 days 2 times a day put about 0.3 ml of 0.2%ointment with isoamylase (0,0006 g) according to Example 16.

For each animal from the second group of the wound after opening phlegmon within 8 days, 4 times a day was temporaroly 0,2%solution lizoamidazy (0,0006 g) in 0.01 M sodium phosphate buffer solution. The wound from the top was covered with sterile towels and plastic wrap to reduce drying headbands and transition of the drug beyond.

For each animal from the third group of the wound after opening phlegmon within 8 days 2 times a day were treated with 1%solution dioksidina. After treatment, the wound was deposited about 0.3 ml ointment Vishnevskogo.

When this ointment in the first and the third group was put on a sterile cloth, which was fixed on the wound.

Under the influence of pharmaceutical compositions with isoamylase in the first and second group of 4-5 days the animals were wound cleansing from purulent-necrotic masses were observed re the Congress of the inflammatory process, disappeared hypermia, the swelling of tissues. Granulation appeared in the first and second groups mainly through 6 days. Epithelization was started in the first group on the 6-7th day, reaching a maximum at 9-10 day, while the second began at 8-10 days, reaching a maximum at 12-14 day.

In the third group of granulation appeared to 8-10 days from the start of treatment. Inflammation has died down slowly. Epithelization was reached on average after 20 to 26 days.

Example 19.

Pharmaceutical composition in the form of ointments from the above examples 1 and 2 was laid on storage at a temperature of +8°C in hermetically sealed cans of dark glass with a volume of 50 ml. Sample to determine bacteriolytic specific activity ointment with isoamylase were taken 1 time per month for 1 year.

The results of the bacteriolytic activity of ointments depending on the time of storage are given in tables 1 and 2.

Table 2
Change bacteriolytic activity ointment (Example 2) during storage
Cycle (month)
1234 56789101112
Activity (U/mg)272727272727272726262625
Activity (%)10010010010010010010010096,396,396,392,6

Bacteriolytic activity lizoamidazy in the proposed composition under storage at a temperature of +4÷+8°C (in a sealed bowl) is reduced by less than 10% within 1 year.

Thus, it is shown that the use of the ointment form lizoamidazy hydrophilic on the basis of confirmed its advantage compared the structure with liquid form in the form of a solution, because I used a smaller amount of the active substance in the same therapeutic effect, the wound is less processed, provided a more convenient and faster to apply the drug to the wound.

In addition, the use of the ointment form lizoamidazy confirmed its advantage compared with the traditional form of treatment of purulent-inflammatory diseases (because the treatment time is significantly reduced), and also compared with liquid form in the form of a solution lizoamidazy, as it used a smaller amount of the active substance in the same therapeutic effect, provided a more convenient and faster to apply the drug to the wound.

On the basis of the proposed solutions can be created a number of new drugs in the form of soft medicinal forms such as ointment and formed containing the bacteriolytic complex and proteolytic enzymes of the type isoamylase.

The proposed drug analyzes gram-positive microorganisms, including antibiotic resistant, has a high therapeutic activity, improves usability, reduces the consumption of the active substance, gives anaesthetic effect, additionally stimulates reparative processes in the wound, improves microcirculation.

In the proposed drug as the e component framework used thermostable performancesee emulsion, enhancing the wound-healing effect of the proposed drug.

A search of patent documents did not reveal identical and similar technical solutions.

The above set of features offered pharmacological drug (the drug, its dosage form and proportion of components) was not previously known, which indicates the novelty of the proposed solution. The set of essential features of the claimed pharmaceutical preparation for external use on the basis of the bacteriolytic complex and proteolytic enzymes should not be explicitly studied the prior art, has significant differences from the one considered analogues. Still similar decisions have been proposed, although the drug isoamylase known since 1989 (VFS 42-1916-89 on isoamylase, introduced in September 1989). Therefore, the applicant believes that the inventive pharmaceutical preparation for topical application on the basis of the bacteriolytic complex and proteolytic enzymes involves an inventive step.

The inventive pharmaceutical composition may be recommended in the treatment of wounds and burns, inflammatory skin diseases, mastitis and endometritis, proctologic diseases and other

The proposed pharmaceutical composition d is I a local application on the basis of the bacteriolytic complex and proteolytic enzymes can be used for industrial mass production of buttery soft forms, such as ointments, creams, gels, liniments, as well as for industrial production generated soft dosage forms: capsules for rectal application.

1. Pharmaceutical composition for topical application having antibacterial and necroticism action, containing the active bacteriolytic complex and proteolytic enzymes - lipoamide, characterized in that it further comprises a base, providing a soft dosage form composition comprising a thermally stable emulsion performancesin compounds in the gas transport properties and a mixture of hydrophilic substances in the following ratio, wt.%:

isoamylase0,1-5,0
emulsion performancesin connections5,0-70,0
a mixture of hydrophilic substancesrest

2. The pharmaceutical composition according to claim 1, characterized in that it further comprises at least one of the following special additives from the series: anesthetic, stimulant reparative processes or their mixture in the following ratio, wt.%:

isoamylase 0,1-5,0
target additive0.5 to 10.0
baserest

3. The pharmaceutical composition according to claim 2, characterized in that as an anesthetic it contains a substance selected from the group: cinoxacin, trimekain, piromekain, lidocaine, or their mixture.

4. The pharmaceutical composition according to claim 2, characterized in that as a stimulator of reparative processes it contains a substance selected from the group: methyluracil, atsemin, etagen, calcium Pantothenate, solcoseryl, or their mixture.

5. The pharmaceutical composition according to claim 1, characterized in that it is made in the form of soft medicinal forms - ointment or gel or formed of soft medicinal forms of suppositories or capsules for rectal application.

6. The pharmaceutical composition according to claim 2, characterized in that a mixture of hydrophilic substances it contains substances selected from the range: proxanol is chosen-268, polyethylene oxides, propylene glycol, dimexide, hyaluronic acid or sodium hyaluronate, sorbitol, glycerin, Aerosil.



 

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3 ex

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