Microdispersed histo-equivalent bioplastic material

FIELD: medicine.

SUBSTANCE: what is described is a microdispersed histo-equivalent bioplastic material containing hyaluronic acid, a buffer system, clarithromycin and a proton pump inhibitor. Hyaluronic acid is nanostructured, lyophilised and dispersed to powder with a single particle size falling within the range of 50-100 mcm; the buffer system is Buffer-G with pH 6.8-8.0, while the proton pump inhibitor is the inhibitor H+-K+-Adenosine triphosphatase pantoprazole in the following proportions, wt %: hyaluronic acid - 95, Buffer-G with pH 6.8-8.0- 3, pantoprazole -1, clarithromycin -1; the microdispersed histo-equivalent bioplastic material is placed into capsules melted on exposure to body temperature, e.g. gelatine.

EFFECT: using it for the therapeutic treatment of gastroduodenal ulcers and erosions with the effect of accelerated oral tissue regeneration.

1 tbl

 

The invention relates to medicine and pharmacology, namely to therapy to gastroenterology and may find application in the treatment of gastroduodenal erosions and ulcers.

Currently modern trends in the treatment of gastric ulcer is aimed at developing methods that substitute surgical treatment is the creation of new medicines and technologies for minimally invasive endoscopic technique. Drug treatment of gastric ulcer includes two main pharmaceutical groups: antacids and blockers of gastric secretion.

Antacids neutralize the hydrochloric acid contained in the composition of gastric juice. These drugs contain magnesium, aluminum, calcium, and combinations thereof. Secretomotor inhibit the secretion of hydrochloric acid of gastric juice. Among antiulcer drugs are blockers of H2-histamine receptors, prostaglandins, proton pump inhibitors.

Recently against peptic ulcer disease began to use antibiotics to get rid of its main causes - the bacteria Helicobacter pylori. Second, the Maastricht agreement puts on the first place among the indications for H. pylori eradication therapy for peptic ulcer disease and gastric ulcer disease of the duodenum, regardless of the phase of the disease (exacerbation or REM�Russia), including their complicated shapes (3). Emphasized that eradication therapy in gastroduodenal ulcers and erosions is base in the complex treatment of this pathology.

Drug treatment of peptic ulcer disease has a limitation related to a systemic effect of drugs on the body that is accompanied by the appearance of side effects, so priority is the application of methods and means acting locally on ulcerative process of the gastric mucosa. In this direction the most adequate and promising is the local use of plastic material endoscopic method.

Known bioplastic material, described in method endoscopic bioplastics gastroduodenal ulcers integrated bioplastic material (Patent for invention of the Russian Federation No. 2520599, publ.).

Bioplastic material contains hyaluronic acid, phosphate buffer system, omeprazole and clarithromycin, taken at a certain ratio of components. Perform endoscopic access this material, later in the working channel fibrogastroduodenoscopy administered biopsy forceps with rolled-integrated bioplastic material, cut to the size of the ulcer, stack on ulcerative defect with the help of biopsy forceps, and control is carried out by endoscopic�skim research in 5-7 days.

The disadvantage of this material is the need for a painful procedure endoscopic injection of plastic material into the cavity of the stomach and 12 duodenal ulcer, in addition, the limited size of the input bioplastic material, which does not allow to cover the entire lesion of the mucosa, especially in the case of widespread erosion.

Technical result of the proposed material Microfine gesticulant-bioplastic material is to use it for therapeutic treatment of gastroduodenal ulcers and erosions with the effect of accelerated regeneration of tissue of the mucous membranes of the body.

The task is solved in that in Microfine gesticulant-bioplastic material comprising hyaluronic acid, a buffer system, clarithromycin and a proton pump inhibitor, hialuronowy acid is nanostructured, and lyophilized to a powder dispersed substance with the size of individual particles in the range 50-190 μm as a buffer system Buffer is used-G with a pH of 6.8-8.0, and the proton pump inhibitor is an inhibitor of H+- K+-Afasy pantoprazole in the following ratio of components, wt.%:

hyaluronic acid nanostructured, whether�fileservername and dispersed to a powder substance with the size of the individual
particles in the range of 50-100 µm95
Buffer-G with a pH of 6.8 to 8.03
pantoprazole1
clarithromycin1

and Microfine gesticulant-bioplastic material is placed in a capsule made of a material that is melted by heat of the body, such as gelatin.

Fig. 1 shows a capsule with Microfine gesticulant-bioplastic material, Fig. 2 - nanostructured form of hyaluronic acid.

Capsule with Microfine gesticulant-bioplastic material is a Microfine gesticulant-bioplastic material 1 placed in the capsule 2 from the material that is melted by heat of the body, such as gelatin.

Microdispersion (grinding) gesticulant-bioplastic material can significantly increase the total area of the material per unit volume, its subsequent encapsulation ensures that the natural ways (oral) in the cavity of the stomach and 12 duodenal ulcer. The subsequent release of funds due to the dissolution of sheath� capsules leads to gelation due to contact with gastric juice and enveloping gastroduodenal erosions and ulcers.

Buffer system the Buffer G with a pH of 6.8 to 8.0 provides the neutralization of the excess of hydrochloric acid and protects the underlying mucosa of the stomach from the corrosive effects of gastric juice. Microfine gesticulant-bioplastic material also contains in its structure pantoprazole inhibitor of the enzyme H+- K+-ATPase ("proton pump) in gastric parietal cells of the stomach and thereby blocks the final stage of synthesis of hydrochloric acid. This leads to a decrease in basal and stimulated secretion, regardless of the nature of the stimulus. In addition, the composition of Microfine gesticulant-bioplastic material included resistant to the action of hydrochloric acid bactericidal antibiotic (clarithromycin) against Helicobacter pylori, which is recognized by many researchers as the reason for the development of peptic ulcer disease [Lapina T. L., Ivashkin V. T. Modern approaches to the treatment of gastric ulcer and duodenal ulcer // Russian medical journal. - Vol. 3, No. 1, 2001. - S. 10-15; Lapina T. L. Modern approaches to treatment of acid and H. pylori - associated diseases // prospects of Clinical gastroenterology, Hepatology. 1, 2001. - P. 21-27, Malfertheiner, P., Megraud F., C. O' Morain et al. Current concepts in the management of Helicobacter pylori infection the Maastricht 22000 Consensus Report, // Aliment. Pharmacol. Ther. 2002. - V. 16. - p.167-180]. In connection with the application on the mucosa of�point mechanism of action material, the proposed product should be taken 1 hour before meals (2 times a day) and overnight rate within 7 days.

Shell the inside of the capsule in the conditions of the gastric juice to dissolve with the release of Microfine gesticulant-bioplastic material, the granules of which are also in a humid environment sliming, and envelop the gastric mucosa, thus creating the effect of a depot of the drug for the buffer system and inhibitor of H+- K+-ATPase (pantoprazole) and antibiotic (clarithromycin).

Thus, new therapeutic tools (non-invasive) method of treatment of gastroduodenal erosions and ulcers used Microfine gesticulant-bioplastic material having the following composition, given in the table.

Microfine gesticulant-bioplastic material is prepared as follows.

1. Prescription amount of Buffer G with a pH of 6.8 to 8.0 3%, pantoprazole 1%, clarithromycin 1% is placed in a hydrocolloid hyaluronic acid 95%, which is exposed to the photochemical process of nanostructuring of obtaining cancellous. Is used for this domestic photochemical box (FB-3) ultraviolet radiation (wavelength 270 nm). Hydrocolloid hyaluronic acid in a volume of 100 ml is placed in the cuvette chamber photochemical�wow Boxing, at 20-25°C for 3 hours under atmospheric pressure UV treatment is carried out. The result is a nanostructured hyaluronic acid, sterile (Fig. 2).

2. The obtained spongy substance liofilizirovanny in the chamber freeze drying, such as Freeze drying "NEW Brunswick™" model U101-86. The freezing is carried out at 40°C, within 6-8 hours followed by vacuum dehydration at a temperature shelf - 40°C. the Total time of vacuum dehydration is 9-10 hours of Finished material is removed from the chamber together with the cuvette into jars. Then, the resulting material is subjected to mechanical microdispersion (grinding) mill (ML-2) at room temperature and at atmospheric pressure to obtain a powdery substance with the size of individual particles in the range of 50-100 microns.

3. Microdispersion substance is dosed at 1.0 g in capsules made of a material that is melted under the action of the organism, for example a gelatin capsule dispenser CD-in observance of sterility.

Thus, Microfine gesticulant-bioplastic material becomes ready for use.

Thanks nanostructured form of hyaluronic acid Microfine gesticulant-bioplastic material after exiting the capsule in�the outer coat of the stomach and 12 duodenal ulcer due to the interaction with the digestive juice can form on the mucosa of the viscous gel coating, which for 5 hours releases the antibiotic and inhibitor of secretion of hydrochloric acid.

To date in professional medical literature describes Microfine plastic materials in capsules for the treatment of gastroduodenal erosions and ulcers.

As a result of experimental research tools "Microfine gesticulant-bioplastic material" conducted on the basis of Experimental biological clinics (vivarium) go "Orenburg state University". The study was conducted during the spring period, the study included 30 animals (rats Wistar), all work with animals was conducted in strict accordance with the legislation of the Russian Federation, the provisions of the European Convention for the protection of vertebrate animals used for experimental and other scientific purposes", the requirements and recommendations of the "Guidelines for the care and use of laboratory animals". During the experiment the animals were divided into 3 groups (10 animals). The first and second group of animals was formed ulcer of the stomach toxic method with acetylsalicylic acid. The third group is the control.

Subsequently, the first group of animals was given in their feed 2 times 1 hour before the main food intake for 7 days "the Microfine gestae�bivalent-bioplastic material". The second group, treatment was not performed.

As a result of the histological study method, it was found that the tool promotes healing of experimental erosive-ulcerous defects of the mucous of the stomach and 12 duodenal ulcer in average 30% faster than in the control group.

Scientific novelty of the proposed solutions in the "Microfine gesticulant-bioplastic material" is a combination of micro - nanostructured form a sterile hialuronowy acid with an inhibitor of the proton pump (H+- K+-ATPase - "proton pump") - pantoprazole and antibiotic - ranitidine bismuth citrate in the packing of capsules with soluble wrapper for oral administration (for example gelatin). The gelation properties of micro - and nanostructured forms of hyaluronic acid and depot of the drug allow to envelop the mucous membranes (especially in the area of erosive-ulcerous defects of the mucous membrane) with subsequent slow release of therapeutic component (proton pump inhibitor and antibiotics).

The "Microfine gesticulant-bioplastic material" is used 2 times a day (morning and evening) orally 1 hour before meals during the course of treatment recommended by a specialist.

The tool provides a shortening of the healing gust�duodenalnyh erosions and ulcers including long-term healing and not treatable by other means.

Thus, in comparison with the prototype, the proposed Microfine gesticulant-bioplastic material ensures its use for therapeutic treatment of gastroduodenal ulcers and erosions with the effect of accelerated regeneration of tissue of the mucous membranes of the body by oral administration in his stomach. Such use of the drug provides a long-lasting its effect with the effect of accelerated healing of gastroduodenal erosions and ulcers, which ultimately allows the patient to avoid surgical treatment and cut (30-50%) time of stay in the hospital.

Microfine gesticulant-bioplastic material comprising hyaluronic acid, a buffer system, clarithromycin and a proton pump inhibitor, characterized in that hyaluronic acid is nanostructured, and lyophilized to a powder dispersed substance with the size of individual particles in the range of 50-100 μm, as a buffer system Buffer is used-G with a pH of 6.8-8.0, and the proton pump inhibitor is an inhibitor of H+- K+-ATPase pantoprazole in the following ratio of components, wt.%:

hyaluronic acid nanostructured, lyophilise�rowanna and dispersed to a powder substance with a size
individual particles in the range of 50-100 µm95
Buffer-G with a pH of 6.8 to 8.03
pantoprazole1
clarithromycin1

and Microfine gesticulant-bioplastic material is placed in a capsule made of a material that is melted by heat of the body.



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula

,

possessing properties of binding with delta opioid receptors. In formula I R1 is selected from the group, consisting of phenyl, pyridinyl and thiazolyl, with R1 being optionally substituted with one or two substituents, independently selected from the group, consisting of C1-4alkoxy, fluorine atom, chlorine atom, bromine atom and cyanogroup; in addition, R1 is optionally substituted with di(C1-4alkyl)aminocarbonyl; Y represents O, S, H3, vinyl, ethinyl or S(O); R2 represents a substituent, selected from the group, consisting of hydrogen, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, fluorine atom, chlorine atom, bromine atom and hydroxy; Ra represents hydrogen or methyl; R3 is selected from the group, consisting of pyrrolidin-2-ylmethyl; pyrrolidin-3-ylmethyl; piperidin-2-ylmethyl, piperidin-3-ylmethyl, piperidin-4-ylmethyl, piperidin-2-ylethyl, piperidin-3-ylethyl, piperidin-4-ylethyl, pyridine-4-yl-(C1-2)alkyl, azetidin-3-ylmethyl; morpholin-2-ylmethyl, morpholin-3-ylmethyl, imidazolylmethyl, thiazolylmethyl, (amino)-C3-6cycloalkyl, 3-hydroxy-2-aminopropyl, 8-azabicyclo[3.2.1]octanyl, 1-azabicyclo[2.2.2]octanyl, guanidinylethyl, 4-(imidazol-1-yl)phenylmethyl, 2-(methylamino)ethyl, 2-diethylaminoethyl, 4-diethylaminobut-2-yl, piperidin-3-yl, piperidin-4-yl and pyrrolidin-3-yl; with piperidin-3-yl being optionally substituted on a carbon atom with phenyl; with pyrrolidin-2-yl in pyrrolidin-2-yl-methyl, pyrrolidin-3-yl, piperidin-3-yl and piperidin-4-yl being optionally substituted on a nitrogen atom with methyl, phenylmethyl, phenethyl or methylcarbonyl.

EFFECT: compounds can be used in the treatment of pain, induced by diseases or conditions, such as osteoarthritis, rheumatoid arthritis, migraine, burn, fibromyalgia, cystitis, rhinitis, neuropathic pain, idiopathic neuralgia, toothache, etc.

24 cl, 3 tbl, 19 ex

FIELD: medicine.

SUBSTANCE: method involves the fasting oral administration of placenta hydrolysate 2ml in water 200 ml at a temperature of 37°C in the morning. After that, the patient is laid down on his/her back and exposed to infrared laser light generated by the laser scanning physiotherapeutic simulator SLSF-03.2 IK. An initial end face output power is 2 mW at a power flow density of 50 mW/cm2 on a projection of an ulcer defect on frame No. 57 or No. 59 with laser light modulation at a frequency of 12-15 a second for 3 minutes per one field. That is followed by exposing a projection of a bend of the elbow on frame No. 30 or No. 40 for 10 minutes per a field. Further, the patient stays in the same position to perform transcranial electric stimulation generated by the Doctor TES-03 apparatus. A gel forehead electrode (+) is applied in the middle of the forehead skin until adhered to the skin uniformly. Two gel postaural electrodes are applied on bony mastoid processes (-) until adhered to the skin uniformly. The electrodes are fixed with a headband. The exposure has a current intensity of 1.5 mA in the form of a bipolar pulsing frequency of 77.5 Hz for 20 minutes. The therapeutic course makes 10 daily procedures.

EFFECT: method provides reducing pain and dyspeptic syndromes, asthenovegetative syndrome, accelerating ulcerous process healing in the mucous membrane, achieving a stable remission, normalising the functional state of the adjacent organs, namely the liver, pancreas, reducing a desire to smoke up to a complete smoking cessation completely for the whole period of treatment.

4 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula I, possessing ability of binding with delta-opioid receptors. In formula R1 is selected from the group, consisting of i) phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxyl, di(C1-4alkyl), aminocarbonyl, chlorine and fluorine, in such a way that only one di(C1-4alkyl)aminocarbonyl is present; ii) naphthyl; iii) pyridinyl, optionally substituted with one substituent, selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxy, fluorine, chlorine and cyano; iv) pyrimidin-5-yl; v) furanyl; vi) thienyl; vii) 5-oxo-4,5-dihydro-[1,2,4]oxodiazol-3-yl; and viii) di(C1-2alkyl)aminocarbonyl; Y represents ethyl, vinyl or bond; or Y represents O, when R1 represents optionally substituted phenyl, where substituent represents C1-4alcoxy; R2 represents phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, fluorine, chlorine and cyano, trifluoromethoxy and hydroxy; or R2 represents phenyl, substituted with one aminocarbonyl, di(C1-4alkyl)aminocarbonyl, C1-4alcoxycarbonyl or carboxysubstituent; R3 is selected from the group, consisting of i) 3-aminocyclohexyl; ii) 4-aminocyclohexyl; iii) piperidin-3-yl; iv) piperidin-4-yl; v) pyrrolodin-2-yl-methyl, in which pyrrolodin-2-yl is optionally substituted by 3-rd or 4-th position with one or two fluorine-substituents; vi) azetidin-3-yl; vii) 2-(N-methylamino)ethyl; viii) 3-hydroxy-2-aminopropyl; ix) piperidin-3-yl-methyl; x) 1-azabicyclo[2.2.2]octan-3-yl; and xi) 8-azabicyclo[3.2.1]octan-3-yl; or R3 together with Ra and nitrogen atom, which they both are bound to, form piperazinyl, optionally substituted with 4-C1-4alkyl; Ra represents hydrogen, 2-(N-methylamino)ethyl or C1-2alkyl, optionally substituted with azetidin-3-yl.

EFFECT: compounds can be used in treatment of pain in the range from medium to strong, caused by diseases or conditions, such as osteoarthritis, migraine, burn, fibromyalgia, cystitis, rhenite, neuropathic pain, idiopathic neuralgia, toothache, etc.

21 cl, 4 tbl, 26 ex

FIELD: medicine.

SUBSTANCE: invention is intended for endoscopic haemostasis in case of gastroduodenal bleedings of non-varicose aetiology, peptic ulcer, erosive injuries of upper organs of gastrointestinal tract (GIT). Endoscopic injections of medications in area of ulcer defect are performed. 0.2% solution of noradrenalin in quantity 1 ml per injection is introduced paravasally in 3 points around source of bleeding, as well as in submucous layer on defect edges, with the total volume of introduced solution 7-8 ml.

EFFECT: method makes it possible to obtain more stable endoscopic haemostasis, reduce bleeding recurrences and postoperative complications.

1 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine and is intended for the treatment of patients with the perforation of gastric and duodenal ulcer. A laparotomy is performed, operative aid concerning the ulcer perforation is realised, during the operation an exudate is sampled from the abdominal cavity, pH of the exudate is determined. If Ph of the said material is 6.6 and lower, a conclusion about the presence in it of anaerobic flora is made and serves the basis for the administration of an antibacterial preparation, influencing the anaerobic flora, into the scheme of initial antibacterial therapy.

EFFECT: method makes it possible to administer specific antibacterial therapy without waiting for culture results.

1 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to gastroenterology, and deals with the treatment of gastritis, stomach and duodenal ulcer. For this purpose a water solution of high-dispersive cluster silver with the concentration of 0.05-0.5 mg/ml is introduced inside in a dose of 30-50 ml 1-2 times per day for 10-30 days, or is applied on an injury focus in the process of endoscopic examination. In the latter case the solution of high-dispersive cluster silver with the concentration of 0.5-1.0 mg/ml is applied in a dose of 3-10 ml depending on the size of the injury focus.

EFFECT: method ensures the effective treatment of the said gastrointestinal diseases due to the increase of the specific antimicrobial and anti-inflammatory activity of nanosilver in the combination with its higher stability to inactivating factors of the stomach medium.

3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a novel crystalline form of N-[-2[[(2,3-difluorophenyl)methyl]thio]-6-{[(1R,2S)-2,3-dihydroxy-1-methylpropyl]oxy}-4-pyrimidinyl]-1-azatidine-sulphonamide, which has an X-ray powder diffractogram, measured with the application of a wavelength of X-rays of 1.5418 E and containing, at least, one crystalline peak with a value 2-theta (in degrees) 21.0, 28.8 and/or 29.1; or containing, at least, 2 crystalline peaks with a value 2-theta (in degrees) 21.0, 28.8 and/or 29.1; or containing, at least, 3 crystalline peaks with a value 2-theta (in degrees) 21.0, 28.8 and/or 29.1. The said crystalline form can contain additional crystalline peaks with a value 2-theta (in degrees), selected from 12.9 and 18.0, obtained under the said conditions.

EFFECT: crystalline form has the X-ray powder diffractogram, measured with the application of a wavelength of X-rays of 1,5418 E, with the crystalline peaks with a value 2-theta (in degrees) 12,9, 13,1, 18,0, 21,0, 22,5, 25,1, 25,3, 28,8, 29,1 and 30,4, and has melting point (beginning) 152,7°C.

6 cl, 3 dwg, 2 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to oral pharmaceutical composition in the form of a granulate produced without spheronisation. The composition contains 92-98 wt % of mesalazine or its pharmaceutically acceptable salt, 2-8 wt % of polyvinylpyrrolidone and an ethylcellulose coating, wherein the above coating weight relates to the above mesalazine weight as 0.3-1.5% and the ethylcellulose coating weight makes 0.11-0.15 mg/cm2. The granulate is packed in a sachet, a capsule or a blister. What is also described is a method for preparing a pharmaceutical composition.

EFFECT: ethylcellulose-coated mesalazine granulate combines a high drug load and a desired mesalazine release profile, namely, 5-25% of released mesalazine 15 min later, 30-70% of released mesalazine 90 min later and 75-100% of released mesalazine 240 min later.

10 cl, 1 ex

FIELD: medicine.

SUBSTANCE: invention refers to a method for Helicobacter pylori eradication of a gastroduodenal zone by a silver nitrate monotherapy consisting in administering an electrolyte solution of silver ions in the concentration of 300 mcg/l in a daily volume of 960 ml, for the first three days - in an amount of 120 ml every 3 h, 160 ml - every 4 hours and for the following three days - every 6 hours in an amount of 240 ml.

EFFECT: achieving the stable eradication of the vegetative and coccal forms of Helicobacter pylori, reducing the length of treatment by the early recovery of the involved gastric and duodenal mucosa.

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics and medicine and concerns a pharmaceutical composition for treating gastrointestinal disorders and conditions containing: (a) peptide of 14 amino acids, which activates a guanylate cyclase C (GC-C) receptor, (b) an agent specified in: a proton-pump inhibitor, an H2 receptor agonist, an opioid receptor antagonist, an opioid receptor agonist, and (c) a pharmaceutically acceptable carrier.

EFFECT: invention provides reducing inflammation, pain, and improves the patient's gastrointestinal motility.

3 cl, 6 ex, 10 dwg

FIELD: medicine.

SUBSTANCE: claimed invention relates to capsule for application with inhalator of dry powder, which contains composition in form of dry powder for pulmonary introduction, which contains mechanosynthesised microparticles, consisting of antibiotic and magnesium stearate.

EFFECT: invention relates to method of obtaining claimed capsule and its application in treatment of bacterial infection, associated with certain lungs diseases.

10 cl, 4 ex, 3 tbl, 1 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to a pharmaceutical composition, namely to a method of manufacturing a solid, coated pharmaceutical composition by the method of applying a coating by melt.

EFFECT: method is adapted to the provision of the solid, coated pharmaceutical composition, possessing fast release, by means of covering by melt.

6 ex, 8 tbl, 13 cl

FIELD: medicine.

SUBSTANCE: invention represents an oral anti-enteroviral and immunostimulant agent in the form of capsules containing interferon and additives, differing by the fact that a therapeutic substance is human recombinant interferon alpha-2b immobilised on polyethylene glycol, having a molecular weight of 1.5 kD by a physical method of binding by an accelerated electron flow in a dose of 1.5 Mrad. The ingredients in the agent are taken in a certain ratio.

EFFECT: extending the range of anti-enteroviral agents possessing immunostimulant properties.

6 ex, 10 tbl

FIELD: medicine.

SUBSTANCE: presented egg-shaped vaginal suppositories contains the following mass ratio in 1 capsule (egg-shaped vaginal suppository): sulphadimine 0.05 g; metronidazole 0.01 g, potato starch 0.02 g, glucose 0.04 g, 5% polyvinyl alcohol 0.07 g, 15% oily extract of propolis 1.0 g; gelatine 0.2 g; dimethicone 0.04 g; glycerol 0.4 g; purified water 0.37 g.

EFFECT: using the invention increases the therapeutic effect and bioavailability of the capsules, increases the prolonged action time, provides the control release of the active substances.

3 cl, 1 dwg, 1 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention concerns a simplified capsular form of clofazimine, containing clofazimine, bee wax, soya bean lecithin, butylhydroxy toluene, soya bean oil, gelatine, glycerol, sorbitol, methylparabene, propylparabene, titanium dioxide, brown chocolate and purified water with preserving high efficacy.

EFFECT: simplifying the form.

4 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention represents an encapsulated liposomal antiviral agent based on human interferon alpha-2b for vaginal application, characterised by the fact that each capsule is made in the form of a hollow coating, which encloses a powder excipient and liposomes distributed in the excipient, and sodium alginate, a water-soluble polymer gel former; the excipient consists of lactose, sodium chloride, 12-aqueous disodium hydrogen phosphate and sodium dihydrogen phosphate, whereas each of the liposomes represents a hollow coating containing lecithin, cholesterol and alpha-tocopherol, and a nucleus inside the coating and containing recombinant human interferon alpha-2; the ingredients of the agents are taken in a certain ratio, mg.

EFFECT: maintaining the storage activity of recombinant human interferon alpha-2 and prolonged action in vaginal application.

2 cl, 3 dwg, 6 tbl, 6 ex

Abt-263 capsule // 2550956

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutics, in particular, described is a capsule, containing a capsule envelope, which includes an encapsulated liquid solution of N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)3-(morpholin-4-yl)-1-(phenylsulphanyl)methyl)propyl)-amino)-3-((trifluoromethyl)sulphonyl)benzenesulphonamide (ABT-263) or its bis-hydrochloride salts in a non-ethanol carrier. As filling agents used are: a phospholipid, a solubilising agent for the phospholipid, selected from glycols, glycolides, glycerides and their mixtures, a surface-active substance of a non-phospholipid type and a sulphur-containing antioxidant in an amount, effective for the reduction of oxidising ABT-263 degradation in storage. The sulphur-containing antioxidant is selected from sulphites, bisulphites, metabisulphites and thiosulphites and their mixtures. A method of the capsule obtaining is also described. The capsule is used for treating a disease, characterised by the overexpression of one or several anti-apoptotic proteins of the Bcl-2 family, for instance, cancer.

EFFECT: invention provides a long storage term for the said capsule.

33 cl, 3 dwg, 20 tbl, 14 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry, namely to a formulation of a cough medical composition. The formulation of the cough medical composition contains an active substance presented by thermopsis herb powder or a dry extract of thermopsis and sodium hydrocarbonate, as well as an excipient, a granulating agent and a lubricant taken in certain relations (versions).

EFFECT: composition of the cough medical composition possesses improved pharmaceutical (appearance, taste) and technological characteristics (hardness, disintegration).

11 cl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a storage-stable pharmaceutical composition and a pharmaceutical formulation containing at least one active pharmaceutical ingredient presenting a nitrocatechol derivative, 2,5-dichlor-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4,6-dimethylpyridine 1-oxide, at least one excipients and at least one binding agent, wherein at least one excipient is other than a phosphate derivative, wherein at least one binding ingredient is other than a polyvinylpyrrolidone compound, and wherein the above active pharmaceutical ingredient is present in the granulated form.

EFFECT: compositions and/or formulations according to the invention are stable for a long period of time and show a high stability if stored in the high temperature and moisture environment.

26 cl, 8 tbl, 4 ex

FIELD: medicine.

SUBSTANCE: therapeutic agent contains anastrozole, poly(lactic-co-glycolic acid), polyvinyl alcohol and D-mannitol. The therapeutic agent represents sub-micron particles and can be presented in the form of capsules, granules, powder, as well as a suspension for injections.

EFFECT: using the developed therapeutic agent enables achieving the therapeutic effect with lower therapeutic doses and making the antitumour therapy more comfortable for the patient.

2 cl, 1 tbl, 2 dwg, 3 ex

FIELD: medicine.

SUBSTANCE: invention aims at treating drug-induced dry eye syndrome (DI-DES). Treating DI-DES implies taking the past medical history, measuring tear production and eye xerosis values reduced and increased respectively in relation to the norm. Unpreserved ocular hypotensive medications are prescribed in the patient. Unpreserved artificial tears are also applied. The lachrymal fluid is analysed by a multicytokine technique. If the analysis shows increased concentrations of proinflammatory cytokines - interleukin-6, interleukin-8, interleukin-12, Th-1 - interleukin-2, interferon-gamma, and Th-2 - interleukin-4, by min 30% in relation to the patient's age norm, a chronic immune ocular inflammation is detected. That requires transpalpebral Blepharogel-1 phonophoresis and 1% hydrocortisone ointment phonophoresis on the sub-mastoidal region from both sides; the therapeutic course is 8-10 daily procedures.

EFFECT: optimal conditions for diagnosing and reasoned differentiated therapy of DI-DES that enables prescribing the pathogenetically reasoned therapy in due time and increasing the efficacy of the therapeutic exposure.

1 tbl, 2 ex

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