Method of gastric ulcer prevention

FIELD: medicine; gastroenterology.

SUBSTANCE: 1-1.5 h prior to gastric ulcer modelling carried out by 100% acetoacetic acid applied to mucous membrane within 15-18 seconds, rats are injected with polyoxidonium dosed 0.1-0.2 mg/kg and novocainamide 1-2 min prior to gastric ulcer modelling dosed 0.09-0.12 mg/kg.

EFFECT: effective experimental prevention of peptic ulcer.

3 ex

 

The invention relates to medicine and can be used as a way to prevent stomach ulcers. There is a method of treatment and prophylaxis of peptic ulcer disease, including systemic (diet, restriction of physical and mental stress) and medications (gastrozol and others), taken as the analogue of ([1] - Barracks A.G. and others Gastroenterology. 2002 No. 4, 1-4).

There is a method of treatment and prophylaxis of peptic ulcer, including the introduction of anti-inflammatory drug, adopted for the prototype ([2] - EN No. 2180852).

However, the drug does not provide sufficient prevention of stomach ulcers.

The aim of the invention is to increase the effectiveness of prevention while increasing tolerance of therapy.

The technical result is achieved by the fact that pre-1-1,5 hours to enter polyoxidonium in a dose of 0.1-0.2 mg/kg and 1-2 minutes of entering the procainamide dose 0,09-0,12 mg/kg, followed by modeling of stomach ulcers.

The method is as follows.

Rats of Wistar breed of both sexes weighing 220-250 g at the surgical stage nematalosa anesthesia (40 mg/kg) intramuscularly polyoxidonium in a dose of 0.1-0.2 mg/kg for 1-1 .5 h before modeling ulcers, and for 1-2 min to create a model of intravenous procainamide hydrochloride at a dose of 0.09 and 0.12 mg/kg Model ulcers created by applying a 10% acetoacetic acid on the border of the fundus and the antrum of the stomach at the time of application 15-18 C.

Background the frequency of slow waves EMA fundic Department of the stomach was 8.0-9.7 min, the amplitude of the slow waves - 0,16-0,23 MB. Background the frequency of slow waves EMA antrum was 9.2 and 10.3 min, amplitude - 0,15-0,25 mV. Background the frequency of slow waves EMA duodenal ulcers ranged from 21.3 26.7 in min, the amplitude of the slow waves - 0,17-0,22 MB. The introduction of polyoxidonium not lead to strengthening of the EMA of the stomach and duodenum.

The introduction of procainamide hydrochloride led to the strengthening of the EMA of the stomach and duodenum. Thus, the frequency of slow waves EMA fundic Department of the stomach increased to 12.3-18.7 in min, amplitude - to 0.22-0.26 per MB.

The introduction of procainamide hydrochloride led to increased EMA antrum: the frequency of slow waves increased to 22.9-28.0 in / min, and the amplitude was decreased to 0.14-0.2 mV.

The introduction of procainamide hydrochloride was accompanied by strengthening of EMA duodenum: the frequency of slow waves was increased to 31.5-42,0 min, amplitude up to 0,25-0,30 mV. The increase in the amplitude-frequency characteristics of the electromotive activity testified about the increase in contractile activity of the stomach and duodenum in response to the introduction of procainamide hydrochloride.

Application of acetoacetic acid in the control at the border of the fundic and antral led to a sharp increase in EMA f is Dalnego Department of the stomach: the frequency of slow waves increased to 17,0-18,0 min, the amplitude - to 0.29-0,41 MB.

Antrum in response to chemical irritation reacted by increasing the amplitude and frequency of slow waves EMA: frequency - to 14.0-14.5 V min, amplitude up to 1.1 to 1.2 mV.

EMA duodenum after creating experimental gastric ulcers were characterized by a slight change in the frequency of slow waves EMA - to 28.0-29,5 per minute and an amplitude of up to 0,25-0,28 MB.

Modeling of stomach ulcers in advance for 1-1 .5 h the introduction of polyoxidonium in a dose of 0.1-0.2 mg/kg for 1-2 minutes to create the model, the introduction of procainamide hydrochloride in a dose of 0,09-0,12 mg/kg reduced the amplitude-frequency characteristics of the EMA of the stomach and duodenum detected in experimental ulcers.

The method further explain examples of its implementation.

Example 1.

White rat Wistar rats, female weighing 220 g in surgical stage nematalosa anesthesia (40 mg/kg) intramuscularly polyoxidonium in a dose of 0.1 mg/kg 1 hour before modeling ulcers. Then spend a median laparotomy. For 1 min to create a model of intravenous procainamide hydrochloride at a dose of 0.09 mg/kg Model ulcers were created by applying 100% of acetoacetic acid on the border of the fundus and the antrum of the stomach at the time of application 15 C.

Background the frequency of slow waves EMA fundic Department of the stomach was 8.0 min, the amplitude of honey is i.i.d. waves - of 0.16 mV. Background the frequency of slow waves EMA antrum was 9.2 per minute, the amplitude is 0.15 mV. Background the frequency of slow waves EMA duodenum was 21,3 per minute, the amplitude of the slow waves is 0.17 MB.

The introduction of polyoxidonium did not lead to changes in the electric activity of the stomach and duodenum.

The introduction of procainamide hydrochloride led to the strengthening of the EMA of the stomach and duodenum. The frequency of slow waves EMA fundic Department of the stomach increased to 12.3 per minute, the amplitude - to 0.22 mV.

The introduction of procainamide hydrochloride led to increased EMA antrum: the frequency of slow waves increased to 22.9 per minute, and the amplitude was decreased to 0.14 mV.

The introduction of procainamide hydrochloride was accompanied by strengthening of EMA duodenum: the frequency of slow waves was increased to 31.5 min, amplitude to 0.25 mV. The increase in the amplitude-frequency characteristics of the electromotive activity testified about the increase in contractile activity of the stomach and duodenum in response to the introduction of procainamide hydrochloride.

Application of acetoacetic acid in the control at the border of the fundic and antral led to a sharp increase in EMA fundic Department of the stomach: the frequency of slow waves increased to 17.0 min, amplitude - to 0.29 MB.

Antral Department is ludka in response to chemical irritation reacted by increasing the amplitude and frequency of slow waves EMA: frequency - to 14.0 min, amplitude - up to 1.1 MB.

EMA duodenum after creating experimental gastric ulcers was characterized by the change of the frequency of slow waves EMA - to 28.0 per minute and amplitude to 0.25 mV.

Modeling of stomach ulcers in advance for 1 h the introduction of polyoxidonium in a dose of 0.1 mg/kg over 1 min to create the model, the introduction of procainamide hydrochloride in a dose of 0.09 mg/kg reduced the amplitude-frequency characteristics of the EMA of the stomach and duodenum detected in experimental ulcers. Histological examination of the biopsy of the ulcer area identified cicatrization of the ulcer, restoration of function of the secretory apparatus of the stomach and functional state of cardiovascular system of the stomach.

Example 2.

White rat breed Wistar male, weighing 250 g in surgical stage nematalosa anesthesia (40 mg/kg) intramuscularly for 1.5 h before the simulation ulcers impose polyoxidonium in a dose of 0.2 mg/kg Spend a median laparotomy. 2 min to create the model ulcers impose procainamide hydrochloride at a dose of 0.12 mg/kg Model ulcers are created by applying 100% of acetoacetic acid on the border of the fundus and the antrum of the stomach at the time of application 18 C.

Background the frequency of slow waves EMA fundic section of stomach accounted for 9.7 per minute, the amplitude of the slow waves - 0,23 MB. Background the frequency of slow waves e is And antrum represented 10.3 min, the amplitude of 0.25 mV. Background the frequency of slow waves EMA duodenal ulcers accounted for 26.7 per minute, the amplitude of slow waves is 0.22 MB.

The introduction of polyoxidonium not increased the EMA of the stomach and duodenum.

The introduction of procainamide hydrochloride led to the strengthening of the EMA of the stomach and duodenum. The frequency of slow waves EMA fundic Department of the stomach increased to 18.7 per minute, the amplitude - to 0.26 MB.

The introduction of procainamide hydrochloride led to increased EMA antrum: the frequency of slow waves increased to 28.0 per minute, and the amplitude was decreased to 0.2 mV.

The introduction of procainamide hydrochloride was accompanied by strengthening of EMA duodenum: the frequency of slow waves was increased to 42.0 per minute, amplitude up to 0.30 mV. The increase in the amplitude-frequency characteristics of the electromotive activity testified about the increase in contractile activity of the stomach and duodenum in response to the introduction of procainamide hydrochloride.

Application of acetoacetic acid in the control at the border of the fundic and antral led to a sharp increase in EMA fundic Department of the stomach (in comparison with the baseline indicators EMA): the frequency of slow waves increased to 18.0 min, amplitude - to 0.41 MB.

Antrum in response to chemical irritation reacted increase amplit the water and frequency of slow waves EMAT (compared with background indicators EMA): frequency - up to 14.5 min, amplitude - up to 1.2 mV.

EMA duodenum after creating experimental gastric ulcers were characterized by a slight change in the frequency of slow waves EMA - to 29.5 per minute and amplitude to 0.28 MB.

Morphological study of gastric ulcers in rats in the control executed on the 10th day of the simulation ulcers. An ulcer is a defect in mucosal destruction of the epithelial layer, muscularis mucosea; made by granulation tissue. Identify areas of cellular detritus.

Vessels expanded, crownpointe. Find single hemorrhage. In a separate visual fields marked accumulation of cells of the lymphoid series with the formation of infiltrates. Isolated neutrophils.

Modeling of stomach ulcers in advance for 1.5 h the introduction of polyoxidonium in a dose of 0.2 mg/kg over 2 min to create the model, the introduction of procainamide hydrochloride in a dose of 0.12 mg/kg reduced the amplitude-frequency characteristics of the EMA of the stomach and duodenum detected in experimental ulcers.

Morphological study of gastric ulcers in rats in conditions of pretreatment with polyoxidonium and procainamide hydrochloride is made on the 10th day of the simulation ulcers. Sores drug is not detected. Gastric epithelium single layer with a plot of scarring. The smooth muscle cells of the muscular layer of normal structure. Since the courts have not extended, single, enhanced blood supply is not.

The preventive effect of prior administration of drugs was confirmed morphologically.

Example 3.

White rat Wistar rats female weighing 240 g in surgical stage nematalosa anesthesia (40 mg/kg) intramuscularly polyoxidonium in a dose of 0.15 mg/kg for 1 hour and 15 minutes before modeling ulcers, and for 1.5 min to create model enter procainamide dose of 0.1 mg/kg. Model ulcers were created by applying 100% of acetoacetic acid on the border of the fundus and the antrum of the stomach at the time of application 16 C.

Background the frequency of slow waves EMA fundic Department of the stomach was 8.8 min, the amplitude of the slow waves - 0.2 mV. Background the frequency of slow waves EMA antrum was 9.7 min, amplitude - of 0.18 mV. Background the frequency of slow waves EMA duodenal ulcers accounted for 24.5 per minute, the amplitude of the slow waves - 0,19 MB. The introduction of polyoxidonium not lead to strengthening of the EMA of the stomach and duodenum.

The introduction of procainamide hydrochloride led to the strengthening of the EMA of the stomach and duodenum. Thus, the frequency of slow waves EMA fundic Department of the stomach increased to 16.4 per minute, amplitude - 0.24 mV. The introduction of procainamide hydrochloride led to increased EMA antrum: the frequency of slow waves increased to 24.6 min, and the magnitude of the number is decreased - of 0.16 mV. The introduction of procainamide hydrochloride was accompanied by strengthening of EMA duodenum: the frequency of slow waves was increased to 37.5 min, amplitude - to 0.27 mV. The increase in the amplitude-frequency characteristics of the electromotive activity testified about the increase in contractile activity of the stomach and duodenum in response to the introduction of procainamide hydrochloride.

Application of acetoacetic acid in the control at the border of the fundic and antral led to a sharp increase in EMA fundic Department of the stomach (compared to background EMA): the frequency of slow waves increased to 17.7 min, amplitude - to 0.38 MB.

Antrum in response to chemical irritation reacted by increasing the amplitude and frequency of slow waves EMAT (compared to background EMA): frequency - to 14.2 min, amplitude - up to 1.15 MB.

EMA duodenum after creating experimental gastric ulcers were characterized by a slight change in the frequency of slow waves EMAT (compared to background EMA) - to 29.0 per minute and amplitude of up to 0.27 MB.

Modeling of stomach ulcers in advance for 1 hour 15 minutes introduction of polyoxidonium in a dose of 0.15 mg/kg and 1.5 min to create the model, the introduction of procainamide hydrochloride in a dose of 0.1 mg/kg reduced the amplitude-frequency characteristics of the EMA of the stomach and duodenum, the first is mined in experimental ulcers.

Morphological study of gastric ulcers in rats in the control executed on the 10th day of the simulation ulcers. An ulcer is a defect in the mucous membrane with purulent overlays. The vessels of the capillary type, extended crownpointe. Observed phenomenon of stasis, a single hemorrhage. In a separate visual fields marked accumulation of cells of the lymphoid series with the formation of infiltrates. Neutrophils are not detected.

Morphological study of gastric ulcers in rats in conditions of pretreatment with polyoxidonium and procainamide hydrochloride is made on the 10th day of the simulation ulcers. Gastric epithelium single layer. Sores drug is not detected. Smooth muscle cells of the muscular layer of normal structure. Vessels unit, located in the connective tissue.

Thus, the introduction of procainamide hydrochloride had a self-stimulating effect on the background EMA of the stomach and duodenum. However, experimental gastric ulcer preliminary introduction polyoxidonium and procainamide hydrochloride significantly reduced pain motility" of the stomach as in the antegrade and retrograde directions and motility of the duodenum. Therefore, pre-treatment with these drugs has a preventive effect on experimental gastric ulcer, confirmed the morphological study the deposits.

The way to prevent stomach ulcers, including the introduction of medicinal substances, characterized in that the pre-1-1,5 hours to enter polyoxidonium in a dose of 0.1-0.2 mg/kg and 1-2 minutes of entering the procainamide dose 0,09-0,12 mg/kg, followed by modeling of stomach ulcers.



 

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14 cl

FIELD: organic chemistry, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel derivatives of aniline of the general formula (I): and their pharmaceutically acceptable salts and isomeric forms possessing properties of phosphodiesterase-4 inhibitors. Compounds can be used, fore example, for enhancing cognitive ability. In compounds of the general formula (I) R1 means linear or branched (C1-C4)-alkyl that can be unsubstituted or substituted with one or more halogen atoms; R2 means linear or branched (C1-C4)-alkyl that can be unsubstituted or substituted with one or more substitutes of the following order: halogen atom, (C1-C4)-alkoxy or their combinations, (C3-C10)-cycloalkyl, (C4-C16)-cycloalkylalkyl wherein alkyl fragment comprises from 1 to 4 carbon atoms, (C7-C11)-arylalkyl wherein aryl fragment comprises 6 carbon atoms, and alkyl fragment that can be linear or branched and comprises from 1 to 5 carbon atoms and wherein radical arylalkyl can be unsubstituted or substituted in aryl fragment with one or more substitutes of the following order: halogen atom, alkoxy group comprising from 1 to 4 carbon atoms or their combinations, and in alkyl fragment one group -CH2CH2- is optionally replaced for group -CH=CH-, and one group -CH2- is optionally replaced for -O- for -NH-, partially unsaturated carbocyclic group comprising from 5 to 9 carbon atoms that can comprise condensed benzene ring, heterocyclic group that can be saturated, partially saturated or unsaturated and comprises from 5 to 6 carbon atoms in cycle including one atom chosen from oxygen (O), or heterocyclylalkyl group wherein heterocyclic fragment can be saturated, partially saturated or unsaturated and comprises from 5 to 6 carbon atoms in cycle including 1-2 atoms chosen from nitrogen (N) or sulfur (S) atoms, and alkyl fragment that can be linear or branched comprises from 1 to 5 carbon atoms; R3 means partially unsaturated carbocyclylalkyl group wherein carbocyclic fragment comprises from 5 to 6 carbon atoms, and linear or branched alkyl fragment comprises from 1 to 5 carbon atoms, (C7-C11)-arylalkyl wherein aryl fragment comprises 6 carbon atoms, and linear or branched alkyl fragment comprises from 1 to 5 carbon atoms and wherein arylalkyl radical can be linear or substituted in aryl fragment with one or more substitutes of the following group: trifluoromethyl, (C1-C4)-alkyl, (C1-C4)-alkoxy or their combinations, heterocyclylalkyl group wherein heterocyclic fragment can be aromatic, partially or completely saturated and comprises from 5 to 10 atoms in cycle including 1-2 atoms chosen from N, O or S, and linear or branched alkyl fragment comprises from 1 to 5 carbon atoms and wherein heterocyclylalkyl group can be linear or substituted in heterocyclic fragment with one or more substitutes of the following order: halogen atom, (C1-C4)-alkyl, (C1-C4)-alkoxy or their combinations; R4 means (C6-C12)-aryl that can be linear or substituted with one or more substitutes of the following order: halogen atom, (C1-C4)-alkyl, (C2-C4)-alkenyl, hydroxy, (C1-C4)-alkoxy, (C2-C4)-alkoxyalkoxy, nitro, trifluoromethyl, -OCF3, amino group, aminoalkyl, aminoalkoxy, hydroxy-(C1-C4)-alkyl, hydroxamic acid, tetrazol-5-yl, 2-(heterocyclyl)-tetrazol-5-yl, carboxy, alkoxycarbonyl, cyano, acyl, alkylsulfonyl, phenoxy, trialkyloxy, R5-L or their combinations, or heteroaryl comprising from 5 to 10 atoms in cycle including 1-2 atoms chosen from N wherein heteroaryl can be linear or substituted with one or more substitutes of the following order: (C1-C4)-alkyl, (C1-C4)-alkoxy, carboxy, alkoxycarbonyl or their combinations; R5 means hydrogen atom, (C1-C8)-alkyl, (C3-C10)-cycloalkyl, C6-aryl, heterocyclic group that can be saturated, partially saturated or unsaturated and comprises from 5 to 10 atoms in cycle from which at least atom means N or O, and wherein heterocyclic group can be linear or substituted with one or more (C1-C4)-alkyls, or group heterocyclylalkyl, and others. Also, invention relates to intermediates compounds and to a method for enhancing the cognitive ability.

EFFECT: valuable biological and biochemical property of compounds.

49 cl, 8 sch, 26 ex

FIELD: organic chemistry, chemical technology, medicine.

SUBSTANCE: invention relates to 1,4,5,6-tetrahydro-6-oxo-5-(2-piperazinoethyl)-4-phenyl-3-(4-chlorophenyl)pyrrolo[3.4]pyrazole dihydrochloride of the formula (I): . This compound is synthesized by interaction of 1-(2-piperazinoethyl)-5-phenyl-4-(4-chlorobenzoyl)-3-hydroxy-3-pyrrolin-2-one dihydrochloride with hydrazine hydrate. Synthesized compound can be used in medicine as agent decreasing arterial blood pressure and blood coagulation. Invention provides synthesis of a novel compound not described early that possesses hypotensive and anti-coagulant effect simultaneously.

EFFECT: valuable medicinal properties of compound.

3 tbl, 1 ex

FIELD: medicine; veterinary science.

SUBSTANCE: composition for animals' infectious diseases prevention contains Dorogov's antiseptic stimulator of the second fraction (DAS-F2), succinct acid, ascorbic acid, novocaine, sodium chlorides, calcium chloride or calcium gluconate, distilled water taken in specified ratio.

EFFECT: improved therapeutic efficiency of infectious acute course symptom complex treatment of farm animals.

2 ex

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