A method of treating puppies northern fur seal from uncinaria
(57) Abstract:Usage: in veterinary medicine. The inventive method provides for cutaneous application of levamisole with isopropanol and dimethylsulfoxide at a dose of 3-4 ml per head of animal. table 2. The invention relates to veterinary.Known methods of treatment of helminthes diseases Northern fur seal by disinfection rookeries in the autumn after leaving the seals, as well as using Anthelmintics sulfide group disophenol (Disophenol) and dichlorvos (Dichlorvos). Medications given to animals in the form of tablets, gelatin capsules, through the probe; disophenol subcutaneously in the region of the left armpit. Dose per 1 kg of body weight.There is a way using levamisole (Levamisol) at a dose of 6-8 mg/kg of body weight in the form of a 2% aqueous solution, which is injected once; nilverm (Nilverm) at a dose of 10-12 mg/kg body weight in the form of a 3% aqueous solution, is injected once intramuscularly.The closest method to the present invention is the use of the drug citrin (Citarin-L spot on) Bayer (Germany). The drug is used in cutaneous dose of 3-4 ml per head with the contents of 300-400 mg levamisole skin, in terms of the monsoon climate reduces the effectiveness of the treatment. In addition, when treating spent a large amount Catarina purchased currency.The essence of the proposed method of treatment is to use Catarina with additives, which are used isopropanol and dimethylsulphoxide (DMSO).DMSO increases the penetration of drugs through the skin. Isopropanol easily wets the hair and provides access of the drug to the skin.As a result of a patent search and review of the special literature the authors have not found a description of the treatment of the Northern fur seal citrinum in combination with additives.The authors conducted a series of experiments. Anthelminthic activity Catarina mixed with dimethylsulfoxide and isopropanol against U. lucasi tested in different doses with different content Catarina and acting in it levamisole.Commission experiment was conducted on 45 puppies Northern fur seal, taken from the North-West rookeries, troubled by uncinaria. In the experience were selected puppies after examination of faeces awesomechickin method of Fulleborn, macroscopically for the presence in the data of immature uncinaria eggs in the faeces is not detected, but they contained a lot of blood. The amount of blood detected by visual inspection, identified as follows:
a lot of blood++++< / BR>a lot of blood +++
the average number ++
Selected experience in puppies formed 3 experimental and 2 control groups of 10 animals each. Each group of puppies were kept in separate experimental sites.Research results are reflected in table. 1.I group each puppy printed on the back of a mixture of: citrin 75% DMSO 10% isopropanol 15% at a dose of 4 ml containing 300 mg of levamisole.Group II each puppy printed on the back of a mixture of: citrin 50% DMSO 12.5% isopropanol to 37.5% at a dose of 3 ml (150 mg of levamisole).Group III each puppy printed on the back of a mixture of: citrin 50% DMSO 12.5% isopropanol to 37.5% at a dose of 3 ml (200 mg of levamisole).Group IV control of each pup printed on the back citrin at a dose of 2 ml per head (200 mg of levamisole).V group control is not degelmintizirovano. Anthelmintic applied on the skin handheld device on the surface of the body in the back from a distance of 2.5-3 m Spray was from the body surface at a distance of 5-10 cmAfter deworming in H puppies in the first day began to decline, the amount excreted in the faeces of blood and the release of puppies from uncinaria was faster than when treating citrinum. In the control group, 22 July 2 Palo puppy diagnosed with uncinaria, 8 were alive. As can be seen from the table. 1 (experimental group I) mixture Catarina 75% DMSO 10% isopropanol 15% at a dose of 4 ml containing 300 mg of levamisole showed 100% extensi intensifications. The release of puppies from uncinaria was faster than in the treatment citrinum.When using a mixture of: citrin 50% DMSO 12.5% isopropanol 37,5% extendedrequest was in the II-nd group at the dose of 3 ml of a mixture (150 mg of levamisole) 80% in third group, at a dose of 4 ml (200 mg of levamisole) 90% at 100% intensifications.In group III the effectiveness of the mixture containing 200 mg of levamisole was higher than when applied to the skin 2 ml Catarina with a content of 200 mg of levamisole.These blends have anthelminthic activity on immature uncinaria. From table. 2 shows that the efficiency is given at a dose of 150 mg of active substance of levamisole was 100% after 2 days completely stopped the bleeding with faeces. In order to achieve this efficiency by Catarina without organic solvents the desired dosage of 3-4 ml or 300-400 mg of levamisole, and at a dose of 2 ml (200 mg of levamisole) at 100% intensifications of extensification the ka. When considering puppies commander fishery inspection revealed that mortality was 8.9% Before treatment, the mortality rate is lower than 40% did not fall.Based on the performed experiments, the authors came to the following conclusions.1. Mixture: citrin (Citarin-L spot on) of the company (Bayer) (Germany) 50% DMSO 12.5% isopropanol to 37.5% at a dose of 4 ml (200 mg) of levamisole has a higher anthelminthic efficacy against Uncinaria lucasi (Ancylostomatidae) than pure citrin at a dose of 2 ml containing 200 mg of levamisole at the Northern fur seal when pouring on the skin.2. Using this mixture Catarina with DMSO and isopropanol lower costs Catarina treatment at 50-75%
Based on these findings, the authors believe that the use of citrine with additives increases the effectiveness of treatment puppies Northern fur seal from uncinaria allows you to save the import drug citrin. A METHOD of TREATING PUPPIES NORTHERN fur SEAL FROM UNCINARIA, including the introduction of them anthelmintica, characterized in that as anthelmintica use a solution of levamisole in 1 ml containing 100 mg of active ingredient, and optionally isopropanol and dimethyl sulfoxide in the following ratio of the components is reparat enter cutaneous based 3,0 4,0 ml on the animal's head.
FIELD: organic chemistry, biochemistry.
SUBSTANCE: invention relates to epothilones with modified thiazole substituent, methods for production thereof and pharmaceutical composition capable of cell growth inhibiting containing the same. Claimed compounds have general formula I , wherein P-Q represents double carbon bond or epoxy; R represents H, C1-C6-alkyl; G represents ; R1 represents and ; G1 and G2 represent hydrogen; G3 represents O, S, and NZ1; G4 represents H, optionally substituted C1-C6-alkyl, OZ2, Z2C=O and Z4SO2; G5 represents halogen, N3, CN, NC, heteroaryl containing nitrogen or oxygen, and heterocycle; G6 represents H, C1-C6-alkyl, or OZ5, wherein Z5 represents H, C1-C6-alkyl; G9 represents oxygen; Z1 represents H, optionally substituted C1-C6-alkyl, optionally substituted acyl; Z2 represents optionally substituted C1-C6-alkyl or aryl; Z4 represents optionally substituted aryl.
EFFECT: new epothilones capable of cell growth inhibiting.
19 cl, 39 ex
FIELD: medicine, gastroenterology, pharmacy.
SUBSTANCE: invention relates to a solid composition eliciting with an anti-ulcer activity and to a method for its preparing. Pharmaceutical composition consists of a core containing famotidine as an active component and starch, aerosil, stearic acid salt as accessory inert substances wherein a core is covered by polymeric envelope. Core comprises glucose and stearic acid as an accessory inert substance and magnesium stearate as a stearic acid salt. Polymeric envelope comprises oxypropylmethylcellulose, propylene glycol, castor oil, talc and titanium dioxide taken in the definite ratio of all components in the composition. Method for preparing pharmaceutical composition involves preparing raw, mixing therapeutically effective amount of famotidine with glucose and starch, moistening the mixture with starch paste, granulation, drying wetted granulate, repeated granulation, powdering dry granules, tableting and applying polymeric envelope containing oxypropylmethylcellulose on prepared cores with addition of titanium dioxide, propylene glycol, castor oil and talc. Invention provides enhancement of degradability, solubility and stability in storing.
EFFECT: improved method for preparing, valuable pharmaceutical properties of composition.
3 cl, 1 ex
FIELD: organic chemistry, biochemistry, medicine, pharmacy.
SUBSTANCE: invention relates to methods for treatment of diseases or syndromes associated with metabolism of fatty acids and glucose and to new compounds and their pharmaceutically acceptable salts. Invention relates to applying new compounds and pharmaceutical compositions for treatment of cardiovascular diseases, diabetes mellitus, cancer diseases, acidosis and obesity by inhibition of activity of enzyme malonyl-CoA-decarboxylase. Indicated compounds correspond to formulae (I) and (II) wherein Y, C, R1, R2, R6 and R7 have values given in the invention claim.
EFFECT: valuable medicinal and biochemical properties of azoles.
27 cl, 8 tbl
FIELD: medicine, therapy, gastroenterology.
SUBSTANCE: method involves preliminary assay of the disorder type in gallbladder motor contraction and bile-excretion ways followed by prescribing thermal low-mineralized hydrocarbonate-sodium-sulfate-calcium-magnesium mineral water in the dose by 200-300 ml, 3 times per a day, 1 h before eating, tubages № 3 with mineral water, bathes and shower with mineral water every day for 10-14 days. In the hypotonic type of motor activity method involves mineral water at temperature 25-30°C, and in the hypertonic type - at temperature 38-40°C. Method provides accelerating in scars formation of ulcers and epithelization of erosions in gastroduodenal system, to prevent frequent exacerbations and to reduce activity of Chelicobacter-induced inflammation.
EFFECT: improved therapy method.
4 tbl, 2 ex
FIELD: medicine, endocrinology.
SUBSTANCE: invention relates to treatment of diabetes mellitus in mammals. Invention proposes applying inhibitors of enzyme dipeptidyl peptidase IV as an active component in manufacturing a medicinal agent, and in a method for treatment of diabetes mellitus. Invention provides enhancing the functional activity of insulin-producing cells in animal and differentiation of epithelial cells of the pancreas.
EFFECT: improved method for insulin producing and diabetes treatment.
20 cl, 5 dwg, 2 tbl, 2 ex
FIELD: medicine, pharmacy.
SUBSTANCE: invention relates to lyophilized composition comprising epotilone in the effective amount and mannitol or cyclodextrin. The second variant of the lyophilized composition involves epotilone and hydroxypropyl-beta-cyclodextrin. The preferable content of epotilone in the lyophilized composition is from 0.1% to 1.5%, and cyclodextrin - from 90% to 99% as measured for the total mass of solid components. Epotilone-containing lyophilized compositions can be used fro preparing an anti-tumor medicinal agent useful for parenteral administration and the lyophilized composition can be reduced preferably before administration directly. Epotilone-containing lyophilized compositions show improved indices of epotilone solubility and can retain stability for 24-36 months at temperature from 2°C to 30°C being without change of the solubility index.
EFFECT: improved and valuable properties of composition.
10 cl, 4 tbl, 14 ex
FIELD: organic chemistry, chemical technology, medicine, pharmacy.
SUBSTANCE: invention describes bicyclic N-acylated imidazo-3-amines or imidazo-5-amines salts of the general formula (I): wherein R1 means tert.-butyl, 1,1,3,3-tetramethylbutyl, (C4-C8)-cycloalkyl, phenyl disubstituted with (C1-C4)-alkyl, -CH2Ra wherein Ra means the group -CO(OR') wherein R' means (C1-C8)-alkyl; R2 means hydrogen atom, the group -CORb wherein Rb means (C1-C8)-alkyl or (C3-C8)-cycloalkyl; R3 means (C1-C8)-alkyl, (C3-C8)-cycloalkyl, phenyl, pyridyl, furfuryl or thiophenyl; A means tri-linked fragment of ring of the formula: wherein R6 and R7 mean hydrogen atom or tetra-linked fragment of ring of the following formulae: wherein R4' means hydrogen atom or benzyloxy-group; R5' means hydrogen atom; R6' means hydrogen atom, (C1-C8)-alkyl or nitro- (NO2)-group; R7' means hydrogen atom, (C1-C8)-alkyl, or R6' and R7' mean in common the following fragment of ring: -CRi=CRj-CH=CH- wherein Ri and Rj mean hydrogen atom; R5'' means hydrogen, chlorine atom or (C1-C8)-alkyl; R6'' means hydrogen atom; R7''n means hydrogen atom, amino- (NH2)-group or (C1-C8)-alkyl; R4''', R6''' and R7''' mean hydrogen atom; R8 means (C1-C8)-alkyl or (C3-C8)-cycloalkyl; X means anion of inorganic or organic acid, or their acid-additive compounds. Also, invention relates to a method for their preparing and a pharmaceutical composition based on thereof. These new compounds show affinity to opiate μ-receptor and can be used, in particular, as analgesic agents.
EFFECT: improved preparing method, valuable medicinal properties of compounds and pharmaceutical compositions.
12 cl, 2 dwg, 32 ex
FIELD: organic chemistry, biochemistry, medicine, pharmacy.
SUBSTANCE: invention proposes compounds of the general formula (1): wherein X is chosen from sulfur atom and methylene group; X1 is chosen from sulfur atom and methylene group; X2 is chosen from oxygen (O), sulfur (S) atoms and methylene group; X3 means -NR5 or carbonyl group; R1 means hydrogen atom or nitrile group; R and R3 are chosen independently from hydrogen atom (H) and (C1-C6)-alkyl; R4 means R4A when X3 means -NR5 and R4B when X3 means carbonyl group; R4A is chosen from -R6R7NC(=O), -R6R7NC(=S), -R8(CH2)qC(=O), -R8(CH2)qC(=S), -R8(CH2)qSO2 and -R8(CH2)qOC(=O); R4B means -R6R7N; R5 means hydrogen atom (H); R6 and R7 are chosen independently from -R8(CH2)q, or they form in common -(CH2)2-Z1-(CH2)2- or -CHR9-X2-CH2-CHR10-; R8 is chosen from hydrogen atom (H), (C1-C4)-alkyl, cycloalkyl group condensed with benzene ring, acyl, dialkylcarbamoyl, dialkylamino-group, N-alkylpiperidyl, optionally substituted aryl, optionally substituted α-alkylbenzyl, optionally substituted aroyl, optionally substituted arylsulfonyl and optionally substituted heteroaryl representing monocyclic 5- and 6-membered ring aromatic group with one or two heteroatoms chosen from nitrogen, oxygen and sulfur atoms, and derivatives of abovementioned rings condensed with benzene; R9 and R10 are chosen independently from hydrogen atom (H), hydroxymethyl and cyanomethyl groups; Z1 is chosen from -(CH2)r-, -O-, and -N((CH2)q)R8)-; Z2 means optionally the substituted ortho-phenylene group; m = 1-3; n = 0-4; p = 2-5; q = 0-3, and r = 1 or 3. Proposed compounds are inhibitors of dipeptidyl-peptidase IV and can be used in preparing pharmaceutical compositions designated for treatment of different diseases, among them, diabetes mellitus of type 2.
EFFECT: valuable medicinal and biochemical properties of compounds and pharmaceutical composition.
22 cl, 8 tbl, 453 ex
SUBSTANCE: method involves using dipeptidyl peptidase IV (DP IV or CD 26) or DP IV-like enzyme for producing drug for treating stress or anxiety cases. Inhibitors are usable in combination with neuropeptides Y. The inhibitors are transported in physiologically compatible carriers. The inhibitors are also produced as prodrugs.
EFFECT: enhanced effectiveness of treatment.
6 cl, 11 dwg, 2 tbl
FIELD: organic chemistry.
SUBSTANCE: invention relates to new polymorphous crystalline forms of 5-[4-[2-[N-methyl-N-(2-pyridyl)-amino]-ethoxy]-benzyl]-thiazolidine-2,4-dione maleate of formula and stereomers thereof.
EFFECT: polymorphous crystalline forms of high stability.
12 cl, 1 tbl, 13 dwg, 5 ex