Method of soft tissue wound healing of various aetiology
SUBSTANCE: biologically active additive Laviocard+ is prescribed orally 1 capsule 2 times a day with food for 21 days. That is combined with daily wound irrigations with neutral analyte of anhydrohexitol nucleic acid with leaving a sterile gauze bandage impregnated with neutral analyte of anhydrohexitol nucleic acid in the wound until it is clean. That is followed by daily bandaging with Lavitol cosmetic dihydroquercetin powder applied on the wound surface 1-2 mm thick until the wound is healed.
EFFECT: reduced length of wound healing by stimulating the regeneration processes in tissues.
1 ex, 3 tbl
The invention relates to medicine, in particular to surgery, and can be used for the treatment of wounds of the soft tissues of various etiologies.
A comprehensive approach to the treatment of wounds is adequate local treatment of wounds and stimulate regenerative abilities of the organism [Shevchenko UL and others, 2009, 1]. In recent years there has been increased virulence and increasing the resistance of the microflora to the most common antimicrobial agents, the reduction of General and local immunity [Serivece F, 2008, 2].
Among funds with pronounced antimicrobial effect is neutral anolyte ANK [http://agarash/katalog-oborudovaniya/lektrokhimicheski-aktivirovannye-rastvory/anolit,3; http://agarash/katalog-oborudovaniya/lektrokhimicheski-aktivirovannye-rastvory, 4]. Neutral anolyte ANK prepared on the cell type STEL [http://www.bakhir.ru/rus/publications/18-medalphabet-11-2006 .htm, 5] for the instructions for this installation [http://mkolga.ru/catalog/ustanovki-stel.html, 6; technical description and operating instructions installation STEL-10H-120-01, 7]. Known methods of local treatment of wounds neutral anolyte ANK did not involve additional use of antioxidants [Gridin V., 2005, 8; Bachmanov A.E., 2009, 9]. It is now known that the activation of free radical reactions (RAF) lipid peroxidation (LPO) causes a disturbance of the flow of the wound healing process, therefore, the use of different copies of the gene inhibitors of the RAF is the basis of pathogenetic treatment of wounds [Lutsevich O.E. Berlov, 2011, 10]. Among the means, which has strong antioxidant effect, dihydroquercetin (Taxifolin) [http://www.ametis.ru/production/lavitol-dihydroquercetin/application, 11]. Known methods of local application of products containing dihydroquercetin in the form of a gel-balm [No. 2381810, 12], and coatings wound gel "Flamen" [http://www.vitalcrystal.ru/flamena-small.html, 13]. However, these methods have the following differences: 1) do not provide for the application of neutral anolyte ANK in the local treatment of wound healing and simultaneous oral administration of antioxidants; 2) the concentration of dihydroquercetin in the form of powder in the wound higher than in gel and wound coverings; 3) production of gel-balm and wound coverings is technically more difficult and is possible only in the conditions of the pharmaceutical companies, which increases their value.
In addition, there is a method of use of biologically active additives "Lavocat+"containing dihydroquercetin, to stimulate the healing of postoperative wounds in the breast [patent No. 2428198, 14]. This method differs in that it applies solely to stimulate healing of a clean uninfected operative wounds (with overlapped seams) of the breast is the only oral "Lavocat+", does not provide for local effects on the wound neutral anolyte ANK, antioxi the Anta dihydroquercetin.
The objective of the invention is a method of treating, reducing the healing time of wounds.
The essence of the method: a method of treatment of wounds of the soft tissues of various etiologies, allowing to reduce the time of healing by local application of neutral anolyte ANK in the inflammation phase and powder dihydroquercetin "Lavitol cosmetic - phase regeneration in combination with oral administration of biologically active additives "Lavocat+"containing dihydroquercetin, within 21 days.
This object is achieved due to the following: 1) neutral anolyte ANK can effectively suppress wound microflora and clean the wound of necrotic tissue, which reduces the inflammation phase; 2) local application of powder dihydroquercetin "Lavitol beauty" in a phase of regeneration stimulates reparative processes in the wound, reducing the time of the regeneration phase; 3) oral administration of biologically active additives "Lavocat+" contributes to the correction of violations of the processes of lipid peroxidation (LPO) and activation of antioxidant defense (AOD) homeostasis.
The proposed method is as follows. After surgery (incision, drainage, removal of necrotic tissue) in the inflammation phase daily wound cleansing neutral anolyte ANK, leaving the wound is terilee gauze napkins saturated neutral anolyte APK to complete cleansing of the wound, and simultaneously designate biologically active Supplement "Lavocat+" orally 1 capsule 2 times a day during meals for 21 days. After cleansing the wound (regeneration phase) perform daily bandaging powder dihydroquercetin "Lavitol cosmetic that is applied on the wound surface with a layer of 1-2 mm to self-epithelialization of the wound or the imposition of secondary sutures in the wound or pre - and post-autodermoplastiki free split skin graft.
Comparative analysis of the results of the application of the method was performed in patients with primary (7) and control groups (7). Patients of the main group was applied the proposed method of treatment, patients of the control group received conventional local treatment (phase of inflammation, and 0.1 - 0.5% chlorhexidine solution; in the regeneration phase - levomicol).
In the main group of 3 women and 4 men; in the control group - 2 female and 5 male. The average age of patients of the main group - 46.3 years, the control group was 45.6 years. In the main group autodermoplasty free split skin graft was performed in 3 patients in the control group, 3 patients. 2 patients of the main group and 3 patients in the control group healed the wounds due to self-epithelialization. Two patients from the main group and one is in the patient control group superimposed secondary seams. The diagnoses of the patients are presented in table 1.
|The diagnosis of patients in the study and control groups|
|Diagnosis||The main group||The control Group|
|Cellulitis of the lower extremities||2||1|
|Necrotic form faces||1||2|
|The soft tissue abscess||1||2|
|The bedsore III senior||1||1|
The results of applying the proposed method was analyzed on the basis of the course of wound process, microbial dissemination of RAS, research performance FLOOR (diene conjugates, malonic dialdehyde) and antioxidant protection - AOD (vitamin E, ceruloplasmin) on the first day and 21-day treatment.
During the wound healing process in patients and control group are reflected in table 2.
|The course of the wound process in the main and control groups|
|Indicators of wound healing||The main group||The control group|
|The time of the cleansing of the wound (days)||3,2±0,2||6,3±0,1|
|The appearance of granulations (days)||4,3±0,6||7,8±0,5|
|Commencement epithelialization (days)||6,3±0,1||9,1±0,4|
|Time epithelization of the wound (days)||17,3±1,2||24,4±2,6|
|Possible scarring of the wound (days)||21,1±1,6||28,3±3,3|
|Timing of preoperative preparation (days)||6,3±1,2||12,1±1,3|
The main group of patients treated by the proposed method, more marked RA is the time of cleansing the wounds of necrotic tissue (3,2±0,2 days) the appearance of granulations (4,3±0.6 days), edge (6,3±0.1 days) and complete epithelialization of the wound (17,3±1.2 days), scarring wounds (21,1±1.6 days) compared with patients in the control group (6,3±0.1 days; 7,8±0.5 days; 9,1±0.4 days; 24,4±2.6 days, and 28.3±3.3 days, respectively).
Timing of preoperative preparation for autodermoplastiki in the main group of patients in the reduction phases of the wound healing process were less (6,3±1.2 days)than in the control group (12,1±1.3 days).
Thus, the main group of patients treated by the proposed method, the time course of the phases of wound healing decreased in 1,5-2 times in comparison with the main group. The duration of preoperative preparation for autodermoplastiki in the main group was 1.9 times less than in the control group.
The study of microbial dissemination of RAS in the 1st and 10th day of treatment patients and control group demonstrated significant antimicrobial effects of neutral anolyte ANK on the wound flora. At the beginning of treatment, patients in both groups was selected microbial flora, which was dominated by Staphylococcus aureus, Klebsiella spp., E. coli, Proteus spp. Microbial colonization at the beginning of treatment was 105-6M.L. on 1 cm2. To 10 days in patients of the main group microflora in the wound was absent or its content decreased to 102-3M.L. on 1 cm2whereas in the control group mi is detailed rate remained and was 10 4-5M.L. on 1 cm2. The obtained data testify to the antimicrobial effectiveness of neutral anolyte ANK.
Indicators GENDER and activity AOD patients and control group are listed in table 3.
|Indicators GENDER and AOD patients and control group|
|Indicators||Days of research||The main group||The control group|
|Diene conjugates (nmol/ml)||1||43,4±2,4||42,1±1,8|
|Malonic dialdehyde (nmol/ml)||1||5,7±1,4||6,0±1,6|
|Vitamin E (µg/ml)||1||41,3±1,6||41,6±1,1|
|Ceruloplasmin (mg/100 ml)||1||22,7±1,2||23,5±1,4|
Indicators GENDER (diene conjugates, malonic dialdehyde) and AOD (vitamin E, ceruloplasmin) in patients and control group in the 1-day treatment had no significant differences. To the 21 days of treatment in patients of the main group showed a significant decrease of LPO products in comparison with the control group. Indicators of diene conjugate is decreased by 30.4% (from 43.4±2.4 nmol/ml to 30.2±1.3 nmol); malondialdehyde - 40.4% (from 5.7±1.4 nmol/ml to 3.4±1.3 nmol/ml), whereas in the control group of diene conjugates - 13.8% (from 42.1±1.8 nmol/ml to 36.3±2.4 nmol/ml); malonic dialdehyde - 11.7% (nmol/ml of 6.0±1,6 to 5.3±1.2 nmol/ml). Patients of the main group content components AOD increased more than in the control group. Patients of the main group content of vitamin E increased by 22.9% (from 41.3±1.6 ĩg/ml to 53.6±2.4 μg/ml) and ceruloplasmin by 20.6% (from 22.7±1.2 mg/100 ml to 28.6±2.0 mg/100 ml), and in the control group vitamin "E" - 5.7% (from 41.6±1.1 µg/ml to 44.1±2,2 µg/ml) and ceruloplasmin - 2.9% (from 23.5±1.4 mg/100 ml to 24.2±1.5 mg/100 ml).
So about what atom, patients of the main group, which was applied the proposed method, there has been a significant increase in the content of components AOD on the 21st day of treatment and the reduction of LPO products in comparison with the control group.
When using the proposed method were observed allergic reactions and other side effects in the local application of neutral anolyte APK and powder dihydroquercetin "Lavitol cosmetic, and oral administration of biologically active additives "Lavocat+".
Examples of practical implementation of the proposed method
Patient, 35 years (IB No. 263)
Diagnosis: Infected wound complicated by cellulitis of the left tibia. 4 days ago accidentally cut with a sharp object left ankle and did not pay attention to it. Then came the pain, swelling of the left tibia, inflammation in the wound, fever up to 38.5°C. a State of moderate severity. Skin hot and dry. The temperature of 38.2°C. vesicular Breathing. Heart sounds are clear, rhythmic. Pulse 98, rhythmic. Hell 120/90 mm Hg Abdomen is soft, painless. The liver is not enlarged. Diuresis is not broken.
St.localis. Left lower leg increased in volume due to swelling. On its front surface in 3 is inflammatory infiltrate 12×14 cm thick painful, the skin over it is hyperemic. In Central INFI is trata wound 2×1 cm with abundant purulent discharge, the wound edges sharply infiltrated, the bottom is covered with purulent-necrotic tissue. The General made the cut 8 cm available through the wound and additional drainage cut to 5 cm on the lateral edge of the infiltrate, removed necrotic tissue produced a revision of the wound. Cavity wounds 10×7 cm and is located in the subcutaneous tissue. The wound is washed with 3% R-rum of hydrogen peroxide and neutral anolyte ANK (phase of inflammation). Installed rubber drains and wipes moistened with a neutral anolyte ANK. In further carried out by local treatment: in the inflammation phase - rehabilitation of RAS neutral anolyte ANK and gauze bandages with him daily. At the same time assigned to the biologically active additive "Lavocat+" 1 capsule 2 times a day (a total of 21 days). On the 4th day the wounds were cleansed from purulent-necrotic detachable. Since that time (phase regeneratio) topically applied powder dihydroquercetin "Lavitol beauty", which was applied on the wound surface layer of 1-2 mm daily. On top of the layer of powder was applied to a gauze pad. Additionally, the patient received antibacterial, detoxification, symptomatic therapy. The wound healing process was uneventful. Granulation tissue on the wound surface appeared on day 5, edge epithelialization on day 7. Given the positive dynamics of wound healing, on the 8th the ducks imposed rare secondary sutures on the skin, continuing topically apply powder dihydroquercetin "Lavitol beauty". After 9 days the stitches are removed, healing by second intention.
In dynamics was assessed by lipid peroxidation and AOD on the 1st and 21st day. Decreased LPO products: diene conjugates - 46.1 nmol/ml to 27.3 nmol/ml, malonic dialdehyde - from 24.2 nmol/ml to 7.3 nmol/ml Increased the level of components AOD: Vitamin E - 42,4 μg/ml to 50.7 ág/ml ceruloplasmin - from 21.1 mg/100 ml to 31.4 mg/100 ml
Microbiological study of wounds on 1st day revealed Klebsiella spp.107on 1 cm2; 10-day microflora was absent. Cytologic evaluation of wounds on 1st day and 10-day marked decrease in the number of neutrophils (from 88% to 1.3%), as well as the increase in the number of fibroblasts (from 0% to 23%), epithelial cells (from 0% to 70%), which characterizes the regenerative type cytogram.
Thus, the proposed method that combines the use of neutral anolyte ANK and dihydroquercetin, contributed to the reduction of the flow of wound healing, stimulation of reparative processes in the wound, which helped in the early stages to impose secondary seams and to achieve complete healing of wounds.
Example 2. Patient S., 41 year History No. 5434).
Diagnosis: thermal burn (flame) of the face, neck, trunk, upper and lower extremities AN extent of 20% of the body surface (t). Thermoinsulation injury.
Received within 5 days of receipt of a burn with flame head, torso, upper and lower extremities 20% PT Trauma household (in the fire). With 18.03.12 on 23.03.12 were treated in the trauma ward of CRH, where he received shock therapy. After the stabilization transferred for further treatment to the Department of thermal lesions. A serious condition. Skin pale, warm. Breathing hard, weakened in the lower sections. Wheeze is no BH 20 per minute. Heart sounds rhythmic, muted. Heart rate 90 / min. HELL 130/80 mm Art. RT Tongue wet. The abdomen is soft. Palpation painless.
St.localis. The wound was located on the back, lower right and upper extremities. They were presented in black with a wet scab. The total area of the Russian Academy of Sciences 20% of the body surface (4500 cm2).
The treatment was conducted in the intensive care unit for 5 days, then in the Department. Received antibacterial, infusion-transfusion, anticoagulant, symptomatic therapy, enteral and parenteral nutrition, rehabilitation of the fibrobronchoscopy. Local treatment consisted of: - step how agressively to debride Slough under General anesthesia, the treatment of wounds neutral anolyte ANK. Over the wounds imposed cloth with a neutral anolyte ANK (phase of inflammation). From receipt of the patient per the Bolsheviks had received the drug " Lavocat+" 1 capsule 2 times a day for 21 days. After cleansing wounds on the 8th day (regeneration phase) to the wounds inflicted powder dihydroquercetin "Lavitol cosmetic layer 1-2 mm daily, on top put a gauze pad. Active granulation appeared on the 17th day. Samostoiatelna epithelialization of wounds of the upper and lower limbs occurred on the 22nd day, the scarring on the 27th day. On the 19th day and 30th day of treatment the patient completed 2 phase autodermoplastiki free split skin graft granulating wounds back 2000 cm2. Over autodermal skin graft was applied powder dihydroquercetin "Lavitol beauty". In the active course of reparative processes achieved good engraftment autodermal flaps and skin restored almost completely. Healing back on the 34th day.
In the dynamics of the estimated indices of lipid peroxidation and AOD on the 1st and 21st day of treatment. Decreased LPO products: diene conjugates with 49.4 nmol/ml to 45.3 nmol/ml; malonic dialdehyde - 6.0 nmol/ml to 5.2 nmol/ml Increased the level of components AOD: vitamin E - from 30.9 to 40.9 μg/ml; ceruloplasmin - from 23.4 mg/100 ml to 24.7 mg/100 ml
Microbiological study of wounds on 1st day revealed Pseudomonas aeruginosa 106on the 21st day - organisms not. Cytologic evaluation of wounds on 1st day and 1st day marked decrease in the number of neutrophils from 92 to 44%, the increase in the number of fibroblasts from 0 to 13%, epithelial cells from 0 to 52%. The patient was discharged in good condition on the 35th day of the place of residence for outpatient treatment.
The example demonstrates that the proposed method of treatment of wounds contributed to the successful treatment of patients with extensive burns, helped to achieve self-epithelialization of wounds on the limbs and full engraftment autodermal flaps on the back with almost full recovery of the skin.
Thus, the proposed method that combines the use of neutral anolyte ANK and dihydroquercetin in powder form "Lavitol cosmetic for topical application and oral administration of biologically active additives "Lavocat +", effective in the treatment of wounds of various etiologies.
The technical result of the present invention is the reduction of the terms of wound healing by reducing the duration of the phases of wound healing and stimulation of regeneration processes.
The proposed method combines well with a variety of surgical methods of exposure to injury, such as necrectomy, secondary seams, autodermoplasty.
1. Shevchenko UL Firmly D.M., Ryabov A.L. and other Modern features of complex treatment of purulent wounds // Bulletin of the National medical-surgical is on Center. N.I. Pirogov. - 2009. No. 2. - P.9-12.
2. Serivece F Purulent wounds of soft tissues. - Perm: GOU VPO PGMA them. AK. E.A. Wagner University, 2008. - 304 S.
3. The anolyte [Electronic resource] - Mode of access: http://agarash/katalog-obomdovaniya/lektrokhimicheski-aktivirovannye-rastvory/anolit the Anolyte, NPO "Ahares", 2010. Found in Internet 09.02.2013.
4. Electrochemically activated solutions [Electronic resource] - access Mode: PIR://agarash/katalog-oborudovaniya/lektrokhimicheski-aktivirovannye-rastvory-Electrochemically activated solutions, LLC NGO Ahares", 2010. Found in Internet 09.02.2013.
5. Installation STEL: history and new horizons [Electronic resource]- Mode of access: http://www.bakhir.ru/rus/publications/18-medalphabet-11-2006. htm - Electrochemical systems and technologies Witold Bahir. Selected articles. Found in Internet 09.02.2013.
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7. The passport. Technical description and operating instructions installation STEL-10H-120-01 mod. - Voronezh, 2010.
8. Gridin V. Application of electroactivated aqueous solutions in the treatment of patients with purulent wounds: author. dis... Kida. the honey. Sciences/ AV Gridin. - Voronezh. 2005.
9. Bachmanov AU Rationalization of complex treatment of purulent-inflammatory processes of the soft tissues on the basis of information technologists who: author. dis... Kida. the honey. Sciences/ A.E. Bachmanov. - Voronezh. 2009.
10. Lutsevich O.E. Berlov, Tamrazov O., Chikunova A. and other Modern view on the pathophysiology and treatment of purulent wounds // Surgery. - 2011. No. 5. - P.72-77.
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12. RF patent №2381810. The Chuprikov VI, Nagovitsyn S.N. Gel-balm with healing actions. Publ. 20.02.2010.
13. Cover wound gel FLAMEN [Electronic resource] -Mode of access: http://www.vitalcrystal.ru/flamena-small.html -Coating wound gel FLAMINA, "Crystal life", 2010-2012. Found in Internet 09.02.2013.
14. RF patent №2428198. Satyr N.A., dorovskikh, VA, Yanova V.V. method of promoting the healing of postoperative wounds in the breast. Publ. 10.09.2011.
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16. Lavocat+ [Electronic resource] - Mode of access: http://www.ametis.ru/production/laviocard - Lavocat+, "Ametis", 2003-2013. Found in Internet 09.02.2013.
A method of treating wounds of the soft tissues of various etiologies, including the appointment of biologically active additives "Lavocat+" orally 1 capsule 2 times a day during meals for 21 days and provedeniyasvobodnogo washing wounds neutral anolyte ANK, leaving the wound with sterile gauze napkins saturated neutral anolyte ANK, to cleanse the wound, and then perform the daily dressing with the powder of dihydroquercetin "Lavitol cosmetic that is applied on the wound surface with a layer of 1-2 mm to wound healing.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to quinazolinone compounds of formula (I) and its pharmaceutically acceptable salts, wherein n is equal to 0 to 3, and R1 is defined as stated in the patent claim. The above compounds are prolyl hydroxylase inhibitors and can be used in pharmaceutical compositions and methods of treating pathological conditions, disorders and conditions mediated by prolyl hydroxylase activity.
EFFECT: compounds can be administered into the patient for treating, eg anaemia, vascular diseases, metabolic disorders, as well as for wound healing.
22 cl, 2 tbl, 211 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a new compound of formula [I] or to its pharmaceutically acceptable salt, wherein A represents optionally substituted alkyl, wherein the substitute represents identical or different 1-3 groups specified in aryl optionally substituted by 1-3 groups specified in alkyl, halogen, alkoxy and alkanoyl; cycloalkyl optionally substituted by 1-3 groups specified in alkyl and halogen; hydroxy; alkoxy; halogen; an amino group and oxo; an optionally substituted carbocyclic group specified in a mono- and bicyclic group, wherein an aromatic ring and cycloalkyl are condensed; optionally substituted aryl, an optionally substituted completely saturated 5- or 6-merous monocyclic heterocyclic group each of which contains 1 heteroatom specified in nitrogen and oxygen, wherein the substitute of optionally substituted aryl, the optionally substituted carbocyclic group and the optionally substituted heterocyclic group for A represents identical or different 1-3 groups specified in alkyl, optionally substituted hydroxy, alkoxy, cycloalkyl or halogen; cycloalkyl optionally substituted by alkyl or alkoxy; alkoxy optionally substituted by halogen; halogen; hydroxy; oxo; heterocycle; alkyl sulphonyl; and mono- or dialkylcarbamoyl, optionally substituted amino, wherein the substitute represents identical or different 1 or 2 alkyl or aryl, or optionally substituted carbamoyl, wherein the substitute represents identical or different 1 or 2 alkyls optionally substituted by aryl, X represents optionally substituted methylene or -O-, wherein the substitute of optionally substituted methylene for X represents alkoxy or hydroxy, Q represents N or C-R4, L1 represents a single bond, methylene, -CH=CH-, -O-, -CO-, -NR11-, -NR11CO-, -CONR11- or -CH2NR11-, L2 represents a single bond, -CR6R7- or a bivalent 5- or 6-merous completely saturated monocyclic heterocyclic group each of which contains 1 heteroatom specified in nitrogen and oxygen, R1 and R2 are identical or different, and each represents hydrogen, alkyl or halogen, R3 and R4 are identical or different, and each represents hydrogen, alkyl, alkoxy, cyano or halogen, R1 and R3 are optionally bond thereby forming 5- or 6-merous cycloalkane, or a 5- or 6-merous aliphatic heterocycle containing oxygen atom, R5 represents a carboxyl group, an alkoxycarbonyl group or a bioisosteric group of the carboxyl group, R6 and R7 are identical or different, and each represents hydrogen or alkyl, or R6 and R7 are bond thereby forming cycloalkane, R8 represents hydroxy, alkanoylamino or alkyl sulphonylamino, R9 and R10 represent hydrogen or halogen, and R11 represents hydrogen or alkyl. Besides, the invention refers to specific compounds of formula [I], a drug based on the compound of formula [I], using the compound of formula [I], a method of treating based on using the compound of formula [I], and an intermediate compound of formula [II].
EFFECT: there are prepared new compounds possessing the agonist activity on thyroid hormone β receptor.
18 cl, 36 tbl, 344 ex
SUBSTANCE: invention relates to a stable liquid pharmaceutical composition, which includes 3-(2,2,2-trimethylhydrazinium)propionate-2-ethyl-6-methyl-3-hydroxypyridine disuccinate in amount of 0.1-50 wt %, auxiliary substances in amount of 0.01-50 wt % and water.
EFFECT: invention enables to obtain stable pharmaceutical compositions for injection, peroral and local application, having marked antihypoxic, antioxidant and adaptogenic action.
32 cl, 1 dwg, 14 tbl, 60 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to novel compounds of formula III or to its pharmaceutically acceptable salts, in which: R1 and R2 are independently selected from group, consisting of: (a) H, (b) (C2-C6)alkyl, (c) C1-C6 alkyl, interrupted by one or more groups -O-, (d) (C0-C3)alkyl-(C3-C7)cycloalkyl and (e) (CH2)nQ, where n=1-2 and where Q stands for aromatic ring system, which has from 5 to 6 ring atoms C, and Q can be independently substituted with groups up to 3 in number, selected from halogen, on condition that R1 and R2 simultaneously do not stand for H, and each alkyl of R1 and R2 can be independently substituted with one or more groups, selected from group, consisting of halogen, hydroxy, cyano, CF3 or C1-C4 alkyl, or R1 and R2 together with carbon, to which they are attached, form 3-7-member cycloalkyl or 6-member heterocycloalkyl ring, including one oxygen atom and which in case of necessity carries C1-C4 alkyl substituent, or R1 and R2 together with carbon, to which they are connected, form 3-7-member cycloalkyl ring, substituted with R20 and R21, and R20 and R21 together with carbon or carbons, to which they are connected, form 3-7-member cycloalkyl ring; R6 stands for C1-C6 alkyl; each R7 independently stands for C1-C6 alkyl; Y stands for -O-; R4 is selected from group, consisting of: (a) (C0-C3)alkyl-(C3-C7)cycloalkyl, (b) trifluoroethyl, and (c) trifluoropropyl; Z stands for phenyl or bicyclic ring system, which has 9 ring atoms, independently selected from C, N, O and S, on condition that not more than 3 ring atoms in any single ring differs from C, and said ring system can carry to 3 substituents, independently selected from group, consisting of R6, CF3 and SR6; and R5 is selected from group, consisting of NO2, NH2, F, Cl, Br, CN, SR6, S(O)2N(R7)2 and (C1-C4)alkyl, and each alkyl can be independently substituted with one or more halogens or CF3. Invention also relates to pharmaceutical composition for treatment of neurodegenerative disorder or improvement of cognitive function, containing therapeutically effective quantity of said compound; as well as to method of treatment of neurodegenerative disorder, for instance Alzheimer's disease, or improvement of cognitive function.
EFFECT: compounds act as modulators of gamma-secretase.
31 cl, 14 tbl, 3147 ex, 1 dwg
SUBSTANCE: rats are being cooled at temperature -15°C for 3 hours a day throughout 4 weeks. The cooling session is preceded by daily oral administration of the preparation molluskam 10 mg/kg of body weight.
EFFECT: method provides the tissue-protective effect on the prostate, higher adaptive capability of the prostate in the extremely low temperature environment.
4 dwg, 2 tbl,1 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to a method for modulation of biological functions associated with the ageing process in a senior or senile pet partner specified in a small/medium dog, big dog and a cat, involving feeding a pet partner with an effective amount of a composition containing at least one omega-3 polyunsaturated fatty acid and various combinations of amino acids, minerals and antioxidants in amounts effective for an increase of activity, vitality, protection of cartilages, muscle mass maintenance, better digestion and quality of skin and hair at a dry basis. Besides, feeding the animal with the following composition enables inducing favourable changes of gene expression in the animal associated with several biological cascades corresponding to higher quality of life in the above animal.
EFFECT: invention enables providing higher quality of life in the senior animals.
10 cl, 20 tbl, 5 ex
SUBSTANCE: group of inventions refers to medicine, namely to cardiac surgery, and concerns creating cardiovascular homografts (CVHG) applied as vascular biological prostheses in cardiovascular surgeries. There are presented versions of a homograft representing a great vessel section or right and left ventricular outflow tracks taken from a dead body. The homograft is also characterised by min. 30-minute preparation in a medium containing gentamycin, diflucan and pH stabiliser. At a stage of preparation the homograft is processed with a medium of pH 7.0-7.4 representing a DMEM/F12 solution and containing gentamycin, diflucan, cephalosporin and metrogyl. Further, the homograft is kept in a medium containing the DMEM/F12 solution, gentamycin, diflucan and a phosphate buffer. There are also presented methods for producing the CVHG versions, as well as the media for the homograft treatment at the various stages of producing, keeping and handling.
EFFECT: creating the CVHG of more rigid structures resistant to damaging factors of the treatment, handling and storage media that improves their body functions.
16 cl, 10 ex, 9 tbl, 10 dwg
SUBSTANCE: correcting the neurotoxic action of administering the preparation dapsone is ensured by using alpha tocopherol acetate as a correcting agent. Alpha tocopherol acetate is administered per os in a combination with dapsone to non-linear male and female white rats in a dose of 5 mg/kg once a day for 21 day.
EFFECT: using the method enables providing more effective correction of the neurotoxic side actions of dapsone with no side effects.
SUBSTANCE: allogenic multipotent mesenchymal stromal cells in the number of 6 million cells/kg are introduced intravenously in a dose of 3.0 Gy into rats suffered from radiation exposure. Additionally, haemopoietic stem cells recovered from umbilical blood in the number of 300 thousand cells/kg are introduced. The cells are transplanted in such a manner 60 min after radiation exposure.
EFFECT: higher mitosis count that leads to a substantial cryptal epithelium increase.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to the field of biochemistry, in particular to clostridial neurotoxins with a modified persistence. Claimed is a polypeptide, containing HC-domain, the first and, at least, one additional LC-domain with amino acid sequences, at least, 90% identical to the respective sequences of a neurotoxic component of botulotoxin of a serotype A, B, C1, D, E, F or G. Also claimed are nucleic acid, an expression vector and a host cell, intended for the expression of the said polypeptide. Also claimed are a method of obtaining and application of the said polypeptide, including as a component of a pharmaceutical composition, for treatment of a condition, associated with hyperactive cholinergic innervations of a muscle or a exocrine gland, and for cosmetic procedures, associated with wrinkles.
EFFECT: invention makes it possible to controllably vary a period of activity of clostridial neurotoxins.
12 cl, 1 tbl, 4 ex
SUBSTANCE: inorganic clay, represented by sodium-calcium, and/or calcium and/or ferrous forms of montmorillonite, is modified with a water solution of silver nitrate with a concentration 0.16-9.9 wt % in a weight ratio clay:water solution of silver nitrate 1:5. Modification is carried out with mixing from 3 to 7 hours at a temperature in the interval from 10°C to the temperature of boiling. The obtained material is washed with distilled water to pH ≈6-5, until excess of silver nitrate is removed, stood at room temperature and decanted. The material is dried at a temperature of 20-160°C.
EFFECT: obtaining an efficient antibacterial material for traditional and veterinary medicine.
2 tbl, 5 ex
FIELD: veterinary medicine.
SUBSTANCE: agent for prevention of mastitis in dairy cows in the dry period, characterised in that it contains as ingredients the polymer PVP/VA, silicone, polyhexamethylene biguanide, ethyl alcohol, glycerol - as emollient component, gelation agents - triethanolamine and carbopol and purified water in the following ratio of ingredients, %: polymer PVP/VA 9-10; silicone 5-6; ethyl alcohol 35-40; polyhexamethylene biguanide 0.008-0.01; glycerol 5; gelation agents - triethanolamine and carbopol 0.1; purified water - the rest.
EFFECT: method enables to minimise or eliminate the use of chemotherapeutic agents, antibiotics and their derivatives, sulphonamides, nitrofurans and eliminate the side effect of the agent on animal body, as well as to reduce the number of visits of the veterinarian during the dry period of cows, to improve the preventive efficacy.
1 tbl, 3 ex
SUBSTANCE: invention refers to the veterinary science, particularly to substances used in treating purulent-necrotic involvements of bovine's distal extremities, including digital dermatitis. A preparation for treating bovine digital dermatitis in the form of an ointment consists of an excipient, containing an ointment base, and an active ingredient - zinc oxide and copper sulphate in the following proportions, wt %: zinc oxide 9-11, copper sulphate 35-45, the ointment base - the rest.
EFFECT: invention provides higher clinical effectiveness with cost cutting for the ointment preparation.
SUBSTANCE: invention refers to medicine, namely to otorhinolaryngology, and may be used for the preoperative preparation of the patients suffering a perforated nasal septum. Intranasal silicone splints are placed 10 days before the operation. The splint is incised from one side within a perforation border. A 30° endoscope is used to assist a 7-day daily nasal perforation rinsing with chlorhexidine. A suction unit is used to evacuate mucosal secretion; synthomycin ointment is introduced through the incision in the silicone splint to the perforation region. The nasal cavity is irrigated daily with antiseptic and vasoconstrictive preparations. On the 7th day, the intranasal splints are removed.
EFFECT: method enables relieving the mucosal inflammation within the perforation, promotes the prolonged drug retention in the introduction place, ensures avoiding an overlay of a secondary infection, improves the functional state of ciliated epithelium.
SUBSTANCE: invention refers to medicine, namely to surgical dentistry and maxillofacial surgery, and is applicable in maxillary sinusotomy with fistula repair. A mucous membrane is incised to a bone under an intubation narcosis after a two-fold preparation of a surgical area. A D-shaped flap is cut out within an alveolar socket of an extracted tooth to be extended along a mucobuccal fold of an upper jaw on one side to a second incisor, and on the other side - to a third molar. The flap together with the periosteum is separated and retracted upwards with exposing a canine fossa and the alveolar socket of the extracted tooth. A hole is created within the canine fossa. Pathologically changed tissues or all sinus mucosa is scooped with a bone curette through the created hole. The alveolar socket of the extracted tooth is inspected. After the cavity has been scooped, an artificial hole is created towards a nasal cavity through an inferior nasal meatus. The sinus cavity is packed with a iodoform cotton swab; an end of the cotton swab is laid thoroughly on a sinus bottom, namely within the defect; the end of the cotton swab is brought out into a nose. A mucoperiosteal flap is mobilised within the alveolar socket of the extracted tooth, laid on the alveolar socket; the wound is closed completely. In the postoperative period, the cotton swab is removed from the sinus on the 9-10th day. The sutures are removed on the 10-11th day.
EFFECT: method enables reducing an incidence of recurrent oroantral communications in the postoperative period ensured by a compact packing of the sinus, and the antiseptic and regeneration effect of iodoform on the maxillary sinus.
SUBSTANCE: invention relates to veterinary science, namely to obstetrics and gynaecology. A preparation for treating and preventing sub-clinical, clinical, acute and chronic mastitis in farm and domestic animals contains an active substance that is - triphenyl-(3,5-di-tert-butyl-4-hydroxybenzyl)phosphonium bromide and a pharmaceutically acceptable carrier that is Vaseline in ratio 1:2000.
EFFECT: invention provides the higher antimicrobial effectiveness and the lower toxicity of the ointment with the lower concentration of the active substance.
3 tbl, 5 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to an antiseptic drug with haemostatic action for wound cleaning. The drug contains ingredients in the following ratio, wt %: an antimicrobial substance - 0.01-3, an active complex - 1-25, glycerol - 2-35 and water - up to 100. The antimicrobial substance is specified in a group consisting of cetyl pyridinium or cetyl methyl ammonium halogenide, chlorhexidine, miramistin and other quaternary bases applicable in medical practice to treat burns and to clean open wounds, and the active complex is presented by a haemostatic preparation in the form of a mixed-ligand chelated complex of zinc, ethylene diamine tetraacetic acid and ε - aminocapronic acid. The invention also refers to a method for preparing the antiseptic drug with haemostatic action. The method consists in the fact the active complex is prepared in a water-glycerol mixture while stirring by dissolving ε - aminocapronic acid, then zinc oxide, adding powdered ethylene diamine tetraacetic acid and after dissolved completely, adding a liquid solution of the antimicrobial substance in the water-glycerol mixture.
EFFECT: preparing the antiseptic drug with haemostatic action for wound cleaning.
2 cl, 9 ex
SUBSTANCE: invention refers to pharmaceutical industry and represents a preparation possessing the anti-inflammatory action, stimulating the mucosa regeneration, and containing magnesium-chloride mineral bischofit brine 1.27±0.01 g/ml with normalised specific gravity, slastiline, menthol, thymol, and a stabilising agent differing by the fact that it contains magnesium-chloride mineral bischofit brine free from technogenic impurities, with the ingredients in the preparation are taken in specific proportions, g.
EFFECT: reducing acute daily oral toxicity in 1,7-1,9 times.
SUBSTANCE: invention refers to derivatives of oxazolopyrimidine in any of their stereoisomeric forms, or in the form of a mixture of stereoisomeric forms specified in Claim 1.
EFFECT: oxazolopyrimidine derivatives having agonistic activity in relation to Edg-1 receptor.
5 tbl, 319 ex
SUBSTANCE: invention relates to medicine, namely to general surgery, and can be applied in prevention of purulent-inflammatory complications of anterior abdominal wall wounds in case of strangulated ventral hernias. For this purpose, 10% solution of colloidal nanosilver is introduced into operation wound after elimination of strangulation, with preliminary injections on perimetre of hernial orifice edges in dose 0.1 ml of solution per 1 cm2 of aponeurosis. After that, after fixation of synthetic implant, injections are made along the line of sutures on periphery in dose 0.1 ml per 1 cm2 of suture. After that, subcutaneous adipose cellular tissue is infiltrated with solution of colloidal nanosilver in dose 0.1 ml of solution per 1 cm2 of wound.
EFFECT: method ensures considerable reduction of risk of development of purulent-inflammatory complications in patients with said pathology, as well as acceleration of processes of tissue reparation due to application of biologically active colloidal solution of nanosilver, producing selective impact only on pathogenic microorganisms, on all layers of anterior abdominal wall and zone of synthetic implant fixation.
5 cl, 1 ex
SUBSTANCE: invention concerns a stabilised antimicrobial gel compound containing hydrogen peroxide (H2O2) and other additives. As the additives, the compound contains the thickener cellulose ester, the stabiliser dipotassium hydrogenphosphate (K2HPO4) and disodium salt ethylenediamine-N,N,N1,N1-tetraacetic acid (Na2EDTA), glycerol and water in certain proportions.
EFFECT: preparing the antimicrobial compound with stabilised hydrogen peroxide with no toxic components used, applicable as skin antiseptics, eg for hand cleaning.
2 cl, 21 tbl, 12 ex