Agent for local treatment of periodontal diseases

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and represents an agent for local treatment of periodontal diseases, on the basis of organosilicone gycerohydrogel Si(C3H7O3)4·6C3H8O3·24H2O, containing therapeutic supplements, differing by the fact that the therapeutic supplements are presented by ketoprofen and methyluracil in the following proportions, wt %: ketoprofen - 0.5 - 1.0; methyluracil - 1.0 - 1.5; organosilicone gycerohydrogel Si(C3H7O3)4·6C3H8O3·24H2O - up to 100.

EFFECT: invention provides creating the effective agent applicable in the integrated therapy for treating the inflammatory periodontal diseases.

6 ex

 

The invention relates to medicine and concerns of local funds in the complex conservative therapy in the treatment of inflammatory periodontal diseases.

Functional disorders of dentition caused by tooth loss from periodontal disease, develop 5 times more frequent than the complications of caries. No tendency to decrease periodontal diseases necessitates the search for new means and methods for effective treatment and prevention.

It is now generally recognized that only a comprehensive tailor made treatment of inflammatory periodontal diseases using therapeutic, surgical, orthodontic, orthopedic and physiotherapy methods gives a good lasting results.

Of great importance in the complex treatment of periodontal disease is conservative therapy. We offer an Arsenal of medication and physical means and methods to achieve the elimination of foci of inflammation, long-term stabilization of periodontal status, restoration of structural and functional properties of the elements of periodontal complex, preventing passage inflammation in deep tissue, increasing local and General factors of protection and, if necessary, to provide preoperative preparation. However, stabilizati the process in all cases is long, therefore, the search of new methods for early diagnosis, treatment and prevention of periodontal disease remains relevant.

It is known tool for local treatment of periodontal disease containing metronidazole, lincomycin, 10%solution of lidocaine hydrochloride, a 0.4%solution of dexamethasone and as a gel base silicone glycerokinase composition Si(C3H7O3)4·6C3H8O3·24H2O (RF patent 2383337, IPC AC 31/04, 2010) (prototype). The tool provides a high therapeutic effect, lack of toxicity and undesirable side effects, positive effects on the body essential element silicon in a biologically active form.

However, the known means used for the treatment of all 3 degrees of periodontitis (light, moderate, heavy) and in the acute stage, therefore, the tool contains an antimicrobial drugs, the presence of which contributes to the violation of the microflora of the oral cavity and subsequent resistance to antibiotics, which is quite invasive method.

Thus, the authors task was to develop a tool for the local treatment of inflammatory periodontal diseases with effective therapeutic effect without the possible negative effects, the use of which implies the t microinvasive treatment methods.

The problem is solved in the proposed tool for local treatment of periodontal disease on the basis of silicone glycerokinase composition Si(C3H7O3)4·6C3H8O3·24H2O, including drug additives. As medicinal supplements the product contains Ketoprofen and methyluracil in the following ratio of components, wt.%:

Ketoprofen- 0,5-1,0
methyluracil- 1,0-1,5
silicone glycerokinase
composition Si(C3H7O3)4·6C3H8O3·24H2O- the rest is up to 100

The offered product is used in the final stage of periodontitis treatment of mild to moderate severity after the General anti-inflammatory and antibacterial therapy using laser curettage of periodontal pockets after which put the proposed tool in the form of applications on the affected areas of the gums.

Currently it is not known tool for local treatment of periodontal diseases on the basis of silicon gli is erogenous composition Si(C 3H7O3)4·4C3H8O3·24H2O, including as medicinal supplements Ketoprofen and methyluracil in the claimed range of the content component.

Used in the proposed tool silicone glycerokinase composition Si(C3H7O3)4·6C3H8O3·24H2O shows high transcutaneous and antitumor activity, wound healing effect, a positive effect on the processes of apitalization, non-toxic (RF patent 2255939, IPC AC 47/30, 2005).

As medicinal supplements in the proposed tool use anti-inflammatory drugs Ketoprofen and plastic surgery.

Ketoprofen is a racemic mixture of enantiomers, in which the pharmacological activity is associated with the S-enantiomer. White or almost white, fine-grained or granular powder, odourless, non-hygroscopic. Inhibits the activity of COX-1 and COX-2, inhibits the synthesis of PG and LT, which are chemical precursors of inflammatory mediators. And antibradikininova activity stabilizes lysosomal membranes and delaying the release of these enzymes that contribute to tissue destruction in chronic inflammation. Reduces the secretion of cytokines, inhibits the activity of neutrophils. Ketoprofen is used for ku is investing pain syndromes of different origin, including dental, gynecological, neurological, oncological practices, for symptomatic treatment of joint diseases: rheumatoid arthritis, non-specific spondyloarthropathies, osteoarthritis.

In the proposed tool Ketoprofen is used in the form of powder in the range of 0.5÷1.0 wt.%.

Methyluracil enhances the growth and reproduction of cells, improving the flow of regeneration in the damaged tissues, accelerates healing of wounds, ulcers, burns, increases the body's resistance to infections. A characteristic feature of the drug is stimulating effect on the blood (increased formation of leukocytes and erythrocytes in the bone marrow). In addition, methyluracil anti-inflammatory, increases the body's resistance to loss of blood and oxygen deficiency, normalizes the secretion of gastric juice and its acidity. Plastic surgery is used to treat diseases of the blood (leukopenia, agranulocytosis) of different origin, when oppression in connection with the use of drugs, radiation therapy, radiotherapy. Methyluracil finds application in the treatment of weak healing wounds, ulcers, fractures, burns. It is used to stimulate regeneration and normalization of the secretory activity of the mucous membrane of the stomach and intestines when ulcers is authorized diseases, chronic gastritis, ulcerative colitis, and chronic pancreatitis and hepatitis. Used as proof when using drugs oppressive blood.

In the proposed tool methyluracil used in the form of powder in the range of 0.5÷1.0 wt.%.

The proposed tool is a combination of hydrophilic base having a set of positive properties, and anti-inflammatory drugs as the active drug additives. In this case it's not obvious to say that when used as the hydrophilic base silicone glycerokinase will be provided pharmaceutical (physical, physicochemical and chemical) compatible with the specified drugs in the claimed range of their quantitative content in the proposed tool. If this is not obvious pharmacological compatible with achieving the required therapeutic effect of using the proposed products containing hydrophilic base and offer drug additives in the inventive intervals quantitative content.

Thus, the necessary experimental studies showing the possibility of achieving a high therapeutic effect in the specified interval quantitative content of components of the proposed cf is DSTV, due to the pharmaceutical and pharmacological components are compatible.

Research conducted by the authors showed good compatibility Ketoprofen, methyluracil and silicone glycomolecules and reveal the limits of their quantitative content tool that provides a manifestation of the maximum therapeutic effect. Thus, when the content of Ketoprofen less than 0.5 wt.% and methyluracil less than 1.0 wt.% slowing manifestations therapeutic effect. The increase in the content of Ketoprofen more than 1.0 wt.% and methyluracil more than 1.5 wt.% impractical because it increases the probability of physico-chemical incompatibility, and also increases the likelihood of negative side effects.

Thus, the qualitative and quantitative composition of the components of the proposed tool provides pharmaceutical and pharmacological compatibility and, as a consequence, a high therapeutic effect.

In the experiment on animals with experimental model of damage to the periodontium has been shown that the application of the proposed tool has anti-inflammatory activity, as judged on the basis of positive dynamics of leukocyte in the blood picture is already on the third day of application. Optimization of the treatment process suggests the presence of energeti the definition of the effect of all components. Normal levels of bilirubin, urea, transaminases activity indicates no toxic effect.

The proposed tool can be obtained as follows. Take the organosilicon glycerokinase composition Si(C3H7O3)4·6C3H8O3·24H2O representing a transparent or semi-transparent colourless gel, odorless, stable in storage. Add powdered Ketoprofen and plastic surgery at mass ratio of the organosilicon glycerokinase and drug additives, equal 97,5÷98,50:2,5÷1,5.

The mixture was thoroughly stirred at room temperature for 10-15 minutes in the mixer rotor type. Get ready-to-use tool for local use from the white color, soft texture in the following ratio, wt.%: Ketoprofen 0,5÷1,0; methyluracil 1,0÷1,5; silicone glycerokinase - 97,5÷98,5.

The proposed solution is illustrated by the following examples.

Example 1. Take to 98.5 g of silicone glycerokinase composition Si(C3H7O3)4·6C3H8O3·24H2O representing translucent colorless gel, odorless, stable in storage. Add 0.5 g of Ketoprofen powder and 1.0 g of methyluracil. The mixture was thoroughly var who're asked in the rotary type mixer at room temperature for ~15 minutes Get ready to use the ointment of white color in the following ratio, wt.%: Ketoprofen - 0,5; methyluracil - 1,0; silicone glycerokinase - 98,5. Ointment meets the requirements of a pharmaceutical agent for topical use.

Example 2. Take 97.5 g of silicone glycerokinase composition Si(C3H7O3)4·6C3H8O3·24H2O representing translucent colorless gel, odorless, stable in storage. Add 1.0 g of Ketoprofen powder and 1.5 g of methyluracil. The mixture was thoroughly stirred in a rotary type mixer at room temperature for ~15 minutes Get ready to use the ointment of white color in the following ratio, wt.%: Ketoprofen - 1.0; methyluracil - 1,5; silicone glycerokinase - 97,5. Ointment meets the requirements of a pharmaceutical agent for topical use.

The proposed tool was investigated in the Ural State Medical Academy. The composition of the tool corresponds to example 1. In accordance with the purpose of the study, experimental animals were divided into 3 groups (15 rats in each group). Each rat under ether anesthesia was injured on periodontal tissues of the lower jaw using a portable piezoelectric, ultratv the same apparatus Piezon Master. Then the rats of group 1 were left to control rats of the second group immediately after the procedure and daily for the gum was applied 1 gram funds in example 1, the rats of the third group - tool 2 (content, wt.%: Ketoprofen 1,5; methyluracil 2,0; glycerokinase - the rest is up to 100).

To assess inflammatory and reparative processes in tissues used for morphological study. To assess systemic reactions used a set of laboratory tests. It included General clinical blood analysis (analyzer MEK 640), including cell count (WBC), erythrocytes (RBC), platelets (PLT) and the hemoglobin (HGB). The study was performed according to the Protocol recommended by the manufacturer of the device. Leukocyte counts were estimated in the blood smears stained with Rho-manowska-Institute. Biochemical study of blood serum included the determination of the activity of alanine aminotransferase (ALT), asparaginase-times (ACT) a unified method for Reitman-Frankel. The General level of albumin was determined by the unified method with bromcresol green, urea - urease phenol/hypochlorite method. These studies were performed using reagents Biocon (Germany) and semi-automatic biochemical analyzer ROKI (Russia). The leukocyte count was performed standardized what Ecodom the blood smears, stained Pappenheim-practice. The result is expressed in percentage and absolute values. The level of circulating immune complexes in serum (CEC) was determined by the photometric method of selective precipitation of the polyethylene glycol. Laboratory and histological examination of periodontal tissues of the mandible was carried out before the start of the study, after 1 day, 3 days, 7 days and 2 weeks. Laboratory studies on the blood of animals performed at the Department of General pathology of the Central research laboratory of the USMA. Statistical processing was carried out on the basis of the principles of variation statistics. Descriptive statistics included mean, standard error, standard deviation, minimum, maximum, module, median. To assess the validity of differences between groups was used nonparametric test Mann-Whitney. The investigations led to the following conclusions:

In all groups studied animals after injury of the gums in the blood showed a higher content of neutrophils, indicating that an active inflammatory process.

In the second group of studies when applied applications offer tools was a significant decrease inflammation already on the third day after treatment, which indicates pronounced antiaggregatory action. The level is Icewine, bilirubin, ALT and ACT in the second group did not change significantly, indicating the absence of toxicity of the drug.

- Minor short-term increase in ALT activity and ACT in animals of the third treatment group indicates transient and not pronounced cytotoxic effect in the case of high content of anti-inflammatory components.

Data from clinical studies on the use of the proposed tools for the treatment of inflammatory diseases of the oral cavity in patients, volunteers clinic of operative dentistry at the Ural state medical Academy are illustrated by the following examples.

Example 3. The patient P. complained of itching and periodic swelling of the gums, bleeding gums when brushing teeth, rapid formation of plaque on the teeth. History: risk factors peaceful. Somatic and infectious diseases denies. Previously, your periodontist not treated. Irregularly conducted professional oral hygiene.

During examination of the oral cavity revealed hyperemia and edema of the mucous membrane of the marginal gingiva and interdental papillae, violation of the tooth-gingival attachment, periodontal pockets 3-4 mm, isolated gingival recession up to 1 mm When the sensing is defined bleeding interdental papillae. Hygiene, Poloshirt unsatisfactory. In the cervical area and approximal tooth surfaces was determined soft plaque. Supra - and subgingival calculus thick consistency light brown color was localized in the cervical area of the front teeth of the lower jaw. Wiig (Universal hygiene index) equal to 1.5 points, PMA (Papillary-marginal-alveolar index, an index of inflammation of the gums) 34%, the index bleeding gums PBI (Index bleeding papilla, Papilla bleeding index) 2.0 points.

Teeth physiological mobility. In the oral cavity fillings in satisfactory condition. The CPU (Index caries-seal-removed tooth) =6.

On the orthopantomogram: atrophy of the bone tissue by mixed type with a predominance of horizontal resorption up to 1/3 of the length of the roots of teeth.

Diagnosis: Chronic generalized periodontitis mild severity.

Treatment:

1. Patient education is the hygiene of the oral cavity with individual selection of methods and means of hygiene.

2. Professional hygiene of the oral cavity (including the removal of supra - and subgingival dental plaque) using ultrasonic devices, followed by coating the teeth with fluoride preparations.

3. Conservative complex antibacterial and anti-inflammatory therapy.

4. Drug treatment of the oral cavity, removal of granulation tissue from clinical pocket is in using diode laser Sirolaser mode gingivectomy. Laser therapy was preceded by application anesthesia (at the request of the patient). In one visit farmed land in the region of 6-8 teeth in the Treatment of periodontal pockets" is a wavelength of 970 nm, the light guide 320 μm, the power 2-2,5 watts, frequency 75-100 Hz in pulse mode for 10-20 seconds on the marginal gingiva around each tooth. After the procedure was produced by repeated drug treatment. The patient is recommended gentle hygiene only on the day of treatment. Visual inspection was performed on the following day, 3 days, 7 days.

The results of the study.

When viewed through 1 day hyperemia and edema of the treated gum significantly decreased, and on the third day was completely absent, also observed no bleeding upon probing, the gums tightly to the tooth tissue. Index assessment of periodontal tissues significantly improved compared with the original data Wiig - 0.8 point, PMA -12%, PBI - 0,64.

After 7 days of complaint was absent. The gums are pale pink color is too close to the tooth tissues.

Example 4. Patient d has complained of itching and periodic swelling of the gums, bleeding gums when brushing teeth, rapid formation of plaque on the teeth. History: risk factors peaceful. Somatic and infectious diseases denies. Previously parodontal the ha is not treated. Irregularly conducted professional oral hygiene.

During examination of the oral cavity revealed hyperemia and edema of the mucous membrane of the marginal gingiva and interdental papillae, violation of the tooth-gingival attachment, periodontal pockets 3-4 mm, isolated gingival recession up to 1 mm When the sounding was determined bleeding interdental papillae. The oral hygiene is poor. In the cervical area and approximal tooth surfaces was determined soft plaque. Supra - and subgingival calculus thick consistency light brown color was localized in the cervical area of the front teeth of the lower jaw. Wiig (Universal hygiene index) is equal to 1.6 points, PMA (Papillary-marginal-alveolar index, an index of inflammation of the gums) 37%, the index bleeding gums PBI (Index bleeding papilla, Papilla bleeding index) score of 2.1.

Teeth physiological mobility. In the oral cavity fillings in satisfactory condition. The CPU (Index caries-seal-removed tooth) =5.

On the orthopantomogram: atrophy of the bone tissue by mixed type with a predominance of horizontal resorption up to 1/3 of the length of the roots of teeth.

Diagnosis: Chronic generalized periodontitis mild severity.

Treatment:

1. Patient education is the hygiene of the oral cavity with individual selection of methods and media the TV hygiene.

2. Professional hygiene of the oral cavity (including the removal of supra - and subgingival dental plaque) using ultrasonic devices, followed by coating the teeth with fluoride preparations.

3. Conservative complex antibacterial and anti-inflammatory therapy.

4. Drug treatment of the oral cavity, removal of granulation tissue from clinical pockets with a diode laser Sirolaser mode gingivectomy. Laser therapy was preceded by application anesthesia (at the request of the patient). In one visit farmed land in the region of 6-8 teeth in the Treatment of periodontal pockets" is a wavelength of 970 nm, the light guide 320 μm, the power 2-2,5 watts, frequency 75-100 Hz in pulse mode for 10-20 seconds on the marginal gingiva around each tooth. After the procedure was produced by repeated drug treatment and the application of the composition of example 1 on the gums. The patient is recommended gentle hygiene only on the day of treatment. To put the composition on the gum 2 times a day morning and evening for 3 days. Visual inspection was performed on the following day, 3 days, 7 days.

The results of the study.

When viewed through 1 day hyperemia and edema of the treated gum significantly decreased, and on the third day was completely absent, also not mentioned crovato the news when probing, the gums tightly to the tooth tissue. Index assessment of periodontal tissues significantly improved compared with the original data Wiig - 0.7 points, PMA -10%, PBI - 0,57.

After 7 days of complaint was absent. The gums are pale pink color is too close to the tooth tissues.

Comparison index assessment of periodontal tissues in the absence of application of the proposed tool and in the case of applications with the proposed remedy at the final stage of treatment to talk about improving therapeutic effect in the case of application tools.

Example 5. The patient And. has complained of itching and periodic swelling of the gums, bleeding gums when brushing teeth, rapid formation of plaque on the teeth. Exacerbation of the disease during the autumn-spring period with symptoms of intoxication, the emergence of a single abscesses.

History: risk factors peaceful. Somatic and infectious diseases denies. Previously, your periodontist not treated. Irregularly conducted professional oral hygiene.

During examination of the oral cavity revealed hyperemia and edema of the mucous membrane of the alveolar process, violation of the tooth-gingival attachment, 5-6 mm periodontal pockets, gingival recession up to 1 mm When the sensing is defined bleeding interdental papillae. The oral hygiene is not udovletvoritelnaya. In the cervical area and approximal tooth surfaces was determined soft plaque. Supra - and subgingival calculus thick consistency light brown color was localized in the cervical area of the front teeth of the lower jaw. Wiig (Universal hygiene index) is equal to 2.3 points, PMA (Papillary-marginal-alveolar index, an index of inflammation of the gums) 64%, the index bleeding gums PBI (Index bleeding papillae. Papilla bleeding index) of 3.0 points.

In the mouth stamped-soldered bridges in poor condition. Teeth physiological mobility.

On the orthopantomogram: atrophy of the bone tissue by mixed type with a predominance of horizontal resorption to1/2the length of the roots of teeth.

Diagnosis: Chronic generalized periodontitis of moderate severity.

Treatment:

1. Training the patient to the rules of oral hygiene with individual selection of methods and means of hygiene.

2. Professional hygiene of the oral cavity (including the removal of supra - and subgingival dental plaque) using ultrasonic devices, followed by coating the teeth with fluoride preparations.

3. Conservative complex antibacterial and anti-inflammatory therapy.

4. Drug treatment of the oral cavity, removal of granulation tissue from Klinicheskaya using diode laser Sirolaser mode gingivectomy. Laser therapy was preceded by application anesthesia (at the request of the patient). In one visit farmed land in the region of 6-8 teeth in the Treatment of periodontal pockets" is a wavelength of 970 nm, the light guide 320 μm, the power 2-2,5 watts, frequency 75-100 Hz in pulse mode for 10-20 seconds on the marginal gingiva around each tooth. After the procedure was produced by repeated drug treatment. The patient was recommended gentle hygiene only on the day of treatment. Visual inspection was performed on the following day, 3 days, 7 days.

The results of the study.

When viewed through 1 day hyperemia and edema of the treated gum significantly decreased, and on the third day was completely absent, also observed no bleeding upon probing, the gums tightly to the tooth tissue. Index assessment of periodontal tissues significantly improved compared with the original data Wiig - 0.8 point, PMA -25%, FBI - 0,78.

After 7 days of complaint was absent. During examination of the oral cavity were present etiological factor of periodontal inflammation in orthopedic structures requiring replacement, violations of marginal fit of restorations. In other cases, the gums are pale pink color is too close to the tooth tissues.

Example 6. Patient N. He complained of itching and periodic PR is puhana gums, bleeding gums when brushing teeth, rapid formation of plaque on the teeth. Exacerbation of the disease during the autumn-spring period with symptoms of General intoxication.

History: risk factors peaceful. Somatic and infectious diseases denies. Previously, your periodontist not treated. Irregularly conducted professional oral hygiene.

During examination of the oral cavity revealed hyperemia and edema of the mucous membrane of the alveolar process, violation of the tooth-gingival attachment, 5-6 mm periodontal pockets, gingival recession up to 1 mm When the sensing is defined bleeding interdental papillae. The oral hygiene is poor. In the cervical area and approximal tooth surfaces was determined soft plaque. Supra - and subgingival calculus thick consistency light brown color was localized in the cervical area of the front teeth of the lower jaw. Wiig (Universal hygiene index) is equal to 2.4 points, PMA (Papillary-marginal-alveolar index, an index of inflammation of the gums) 58%, the index bleeding gums PBI (Index bleeding papilla Papilla bleeding index) of 3.0 points.

In the oral cavity fillings in poor condition. Teeth physiological mobility.

On the orthopantomogram: atrophy of the bone tissue by mixed type with a predominance of horizontal resolution is bcii to 1/2the length of the tooth roots. Diagnosis: Chronic generalized periodontitis of moderate severity.

Treatment:

1. Training the patient to the rules of oral hygiene with individual selection of methods and means of hygiene.

2. Professional hygiene of the oral cavity (including the removal of supra - and subgingival dental plaque) using ultrasonic devices, followed by coating the teeth with fluoride preparations.

3. Conservative complex antibacterial and anti-inflammatory therapy.

4. Drug treatment of the oral cavity, removal of granulation tissue from clinical pockets with a diode laser Sirolaser mode gingivectomy. Laser therapy was preceded by application anesthesia (at the request of the patient). In one visit farmed land in the region of 6-8 teeth in the Treatment of periodontal pockets" is a wavelength of 970 nm, the light guide 320 μm, the power 2-2,5 watts, frequency 75-100 Hz in pulse mode for 10-20 seconds on the marginal gingiva around each tooth. After the procedure produced the applique means to example 1. The patient was recommended gentle hygiene only on the day of treatment. To put the composition on the gum 2 times a day morning and evening for 3 days. Visual inspection was performed on the following day, 3 days, 7 days.

Raza is Tata research.

When viewed through 1 day hyperemia and edema of the treated gum significantly decreased, and on the third day was completely absent, also observed no bleeding upon probing, the gums tightly to the tooth tissue. Index assessment of periodontal tissues significantly improved compared with the original data Wiig - 0.7 points, PMA - 20%, FBI - 0,58.

After 7 days of complaint was absent. During examination of the oral cavity were present etiological factor of periodontal inflammation in violation of marginal fit of restorations. In other cases, the gums are pale pink color is too close to the tooth tissues.

Comparison index assessment of periodontal tissues in the absence of application of the proposed tool and in the case of applications with the proposed remedy at the final stage of treatment to talk about improving therapeutic effect in the case of application tools.

Thus, the authors propose a new tool for the treatment of inflammatory periodontal disease (mild or moderate severity, which can be effectively used at the final stage of treatment after the laser curettage of periodontal pockets.

Tool for local treatment of periodontal diseases on the basis of silicone glycerokinase composition Si(C3H7O3) 4·6C3H8O3·24H2O, including drug additives, characterized in that as medicinal supplements contains Ketoprofen and methyluracil in the following ratio, wt.%:

Ketoprofen0,5÷1,0
methyluracil1,0÷1,5
silicone glycerokinase
composition Si(C3H7O3)4·6C3H8O3·24H2Othe rest is up to 100



 

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1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a formulation for delivery of amphotericin B and other drugs, wherein the formulation contains an active ingredient, one or more esters of glycerol and fatty acids and one or more esters of fatty acids containing polyoxyethylene oxide, wherein the ratio of esters of glycerol and fatty acids and esters of fatty acids containing polyoxyethylene oxide makes from approximately 20:80 to approximately 80:20 vol/vol.

EFFECT: formulation is applicable for preparing the drug with improved bioavailability for infectious diseases.

13 cl, 21 dwg, 8 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel medication for treatment of purulent-inflammatory processes of skin and mucous membranes of different etiology. Medication is made in form of gel and contains the following ingredients with the following ratio of components in g per 100 g: biocomplex of metronidazole with zinc 0.5-2.0, biocomplex of furacilinum with copper 0.1-0.2, trimecaine 3.0-5.0, vitamins (vitamin A, vitamin E, vitamin PP, vitamin C or their mixture) 0.1-1.0, dimexide 10.0, hydrogel of methylsiliconic acid 1.0-5.0, hydrophilic base 3.0-7.0, water 82.3-69.8.

EFFECT: extension of assortment of wound-healing medications.

2 tbl, 1 ex

Drug carrier // 2476204

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to pharmacology and concerns a circulating drug carrier. The carrier contains polyethylene glycol modified phospholipid presented by general formula or its pharmaceutically acceptable salt: wherein X represents as follows or ; and n represents an integer 30 to 150 wherein R1 represents a residue of saturated unbranched fatty acid having 17 to 22 carbon atoms, and 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoyl glycerol. Polyethylene glycol modified phospholipid is found in the amount of 30 wt % - 50 wt % of total weight of lipids in the carrier. What is also presented is a pharmaceutical composition containing the carrier described above and a drug.

EFFECT: group of inventions prolongs a circulation time and respectively improves the efficacy of the drug.

6 cl, 19 dwg, 5 tbl, 49 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are offered: light-stable pharmaceutical composition containing vitamin B12, butanol and butaphosphane, its use for preparing a drug; use of butanol and butaphosphane for preparing the drug; use of butanol and butaphosphane for light-stabilising vitamin B12 in the pharmaceutical composition and use of butanol and butaphosphane for preparing the pharmaceutical composition of vitamin B12 with improved light-stability of vitamin B12.

EFFECT: what is shown is improved light-stability of the composition as related to the n-butanol free composition after 3-hour light exposure.

7 cl, 1 dwg, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: stable fat emulsion contains prostaglandin as an active ingredient and phospholipids containing phosphatidylcholine and phosphatidyl glycerol in mass ratio 85:15 to 99.7:0.3. The fat emulsion under the invention and its active ingredient (prostaglandin) possess physical and chemical stability thereby increasing shelf life to approximately two years, and/or extended range of storage temperature to 10°C as compared with a commercially available fat prostaglandin emulsion.

EFFECT: fat emulsion under the invention enables satisfactory effectiveness even in the introduction of a low amount.

25 cl, 10 tbl, 12 ex

FIELD: medicine.

SUBSTANCE: invention refers to fine stable emulsions of perfluoroorganic compounds (PFOC) which may be used as a base for preparing blood substitutes with gas transport function, as well as radiopaque contrast agents and mediums for organ preservation. The emulsion contains PFOC in the amount of 8÷80.0 wt %, an emulsifying and stabilising additive in the amount of 0.25÷8.0 wt % and a physiologically acceptable solution - the rest. The emulsifying and stabilising additive of the emulsion is presented by a non-ionic surfactant presenting mixed block copolymers of ethylene oxide and/or propylene oxide and/or polyalkylene glycol esters of tocopherol with polyglycidyl esters of fluorinated alcohols in relation 2:1 to 0.5:1, or the anionic surfactant presenting a monoester salt of dicarboxylic acid with aliphatic and/or pxyalkylated aliphatic and/or perfluorinated alcohols, or mixed said non-ionic and anionic surfactants in relation 39:1 to 1:39.

EFFECT: emulsion under the invention is aggregation- and sedimentation-stable; average particle size is no more than 200 nm; it is stored for a long period of time at room and high temperature with no substantial change in emulsion particle size.

11 cl, 24 tbl, 23 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to application of therapeutic amount of docosahexaenoic acid (DHA), eicosapentaenoic acid (EPA) or EPA, formed from DHA, included into glyceride, where said DHA, EPA or EPA formed from DHA, included into glyceride, is formed enzymatically, and said DHA, EPA or EPA formed from DHA is in percent ratio by weight from 40 to 100% with respect to total weight of fatty acids, or where said DHA, EPA or EPA formed from DHA is included into sn-2 position of glyceride, for preparation of product, suitable for treatment of processes, into which accompanying oxidative damage is included. In particular, it is intended for treatment of processes, associated with neurodegenerative, eye, ischemic and inflammatory pathology, atherosclerosis, with oxidative damage of cells and with physical exercise.

EFFECT: claimed is method of diet therapy of oxidative damage of cells associated with ageing, physical exercise, hypoglycemia during or after physical exercise, in which efficient amount of said acids is introduced to said subject, also claimed is non-therapeutic application of said acids as cell antioxidant, anti-ageing agent, fitness enhancer, for support of glucose level in flood in individuals during physical exercise.

29 cl, 33 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to transporting filler for introduction of biologically active compounds, which contains one or more C1-C4 alcohols, water and combination of one or more diphosphate derivatives of electronic transfer agents and one or more monophosphate derivatives of electronic transfer agents. C1-C4 alcohols are present in amount from 0.5 to 50% by weight. Preferably C1-C4 alcohol represents ethanol. Transporting filler can have the shape of vesicles.

EFFECT: transporting filler in accordance with invention increases bioavailability of biologically active compounds, in particular, pharmaceutical preparations, including cosmetic ones.

33 cl, 4 dwg, 1 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, medicine and pharmacology, particularly to invention refers to, and can be used in development of antimycotic preparations of amphotericin B exhibiting low nephro- and hepatotoxicity. For the purpose of providing higher therapeutic efficacy, lower toxicity of a pharmaceutical composition, improved stability of amphotericin B as an ingredient, it contains oxidised dextrane produced by dextrane oxidation by potassium permanganate in an acid medium. It also contains a liposome-forming agent representing phosphatidylcholine. The ingredients of the pharmaceutical composition are related as follows: amphotericin B: oxidised dextrane: a liposome-forming agent: a pharmaceutically acceptable solvent as 0.0005:1-10:0.1-1.0:solvent up to 100 wt % respectively.

EFFECT: composition shows high efficacy.

2 cl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of the following general formula [1a], wherein R1 represents (1) a hydrogen atom, (2) C1-C6alkyl group, (3) C2-C6alkenyl group, (4) C2-C6alkynyl group, (5) C1-C6alkoxygroup, (6) hydroxyC1-C6alkyl group, (7) C1-C6alkoxy(C1-C6)alkyl group, (8) -CONR11R12, wherein R11 and R12 are identical or different, and each represents a hydrogen atom or C1-C6alkyl group, (9) phenyl group or (10) a five-member heteroaryl group which contains at least one heteroatom specified in a group consisting of a nitrogen atom and oxygen atom, and which may be substituted by C1-C6alkyl group; R2 represents (1) a halogen atom, (2) C1-C6alkyl group, (3) hydroxy group or (4) C1-C6alkoxy group; p is equal to 0, 1, 2 or 3; X represents a carbon atom or nitrogen atom; m1 is equal to 0, 1 or 2; m2 is equal to 0 or 1; the spiro ring AB may be substituted by 1-5 identical or different, specified in a group consisting of (1) hydroxy group, (2) C1-C6alkyl group, (3) C1-C6alkoxygroup and (4) oxo group; n1 is equal to 0, 1, 2, 3 or 4; n2 is equal to 1, 2, 3 or 4; n3 is equal to 0, 1 or 2, provided n2+n3 is equal to 2, 3 or 4; and a bond presented by the symbol means a single bond or a double bond, provided the three adjoining carbon atoms forms no allene bond presented by formula: C=C=C, or a pharmaceutically acceptable salt thereof.

EFFECT: invention refers to a pharmaceutical composition possessing GPR40 agonist activity, to a GPR40 agonist drugs; to a hypoglycemic agent stimulating insulin secretion on the basis of the above compounds.

45 cl, 42 tbl, 120 ex

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