RU2017123772A - Фармацевтическая композиция на основе N-бензил-N-метил-1-фенилпирроло [1,2-a] пиразин-3-карбоксамида - Google Patents
Фармацевтическая композиция на основе N-бензил-N-метил-1-фенилпирроло [1,2-a] пиразин-3-карбоксамида Download PDFInfo
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- RU2017123772A RU2017123772A RU2017123772A RU2017123772A RU2017123772A RU 2017123772 A RU2017123772 A RU 2017123772A RU 2017123772 A RU2017123772 A RU 2017123772A RU 2017123772 A RU2017123772 A RU 2017123772A RU 2017123772 A RU2017123772 A RU 2017123772A
- Authority
- RU
- Russia
- Prior art keywords
- pharmaceutical composition
- phenylpyrrolo
- pyrazine
- benzyl
- methyl
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims 5
- QFYYHTVZHIEVCW-UHFFFAOYSA-N N-benzyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide Chemical compound C(C1=CC=CC=C1)N(C(=O)C=1N=C(C=2N(C=1)C=CC=2)C1=CC=CC=C1)C QFYYHTVZHIEVCW-UHFFFAOYSA-N 0.000 title claims 3
- 239000011230 binding agent Substances 0.000 claims 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- 239000007884 disintegrant Substances 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 1
- 235000019441 ethanol Nutrition 0.000 claims 1
- 239000000945 filler Substances 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 1
- 239000008213 purified water Substances 0.000 claims 1
- 238000005096 rolling process Methods 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000000377 silicon dioxide Substances 0.000 claims 1
- 235000012239 silicon dioxide Nutrition 0.000 claims 1
- 229940079832 sodium starch glycolate Drugs 0.000 claims 1
- 239000008109 sodium starch glycolate Substances 0.000 claims 1
- 229920003109 sodium starch glycolate Polymers 0.000 claims 1
- 239000007909 solid dosage form Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/58—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Claims (5)
1. Фармацевтическая композиция для получения твердой лекарственной формы, содержащая N-бензил-N-метил-1-фенилпирроло[1,2-a]пиразин-3-карбоксамид и фармацевтически приемлемые вспомогательные вещества из следующих групп в указанных количествах, г (мас. %):
2. Фармацевтическая композиция по п. 1, содержащая N-бензил-N-метил-1-фенилпирроло[1,2-а]пиразин-3-карбоксамид в количестве 0,00005-0,005 г (0,06-6,25%).
3. Фармацевтическая композиция по п. 1, содержащая в качестве наполнителя лактозу или микрокристаллическую целлюлозу, наиболее предпочтительно микрокристаллическую целлюлозу с размером частиц 101; в качестве связующего - поливинилпирролидон, наиболее предпочтительно поливинилпирролидон с молекулярной массой 28000-34000; в качестве дезинтегрирующего вещества - поперечносшитый поливинилпирролидон (кросповидон), натрия крахмала гликолят или кроскармелозу натрия; в качестве скользящего вещества - диоксид кремния коллоидный или стеариновая кислота и ее соли, предпочтительно магния стеарат. В качестве растворителя для приготовления раствора связующего предпочтительно использование воды очищенной или спирта этилового.
4. Фармацевтическая композиция по п. 1, предназначенная для формования таблеток или заполнения капсул.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU2017123772A RU2689396C2 (ru) | 2017-07-06 | 2017-07-06 | Фармацевтическая композиция на основе N-бензил-N-метил-1-фенилпирроло [1,2-a] пиразин-3-карбоксамида |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU2017123772A RU2689396C2 (ru) | 2017-07-06 | 2017-07-06 | Фармацевтическая композиция на основе N-бензил-N-метил-1-фенилпирроло [1,2-a] пиразин-3-карбоксамида |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2017123772A3 RU2017123772A3 (ru) | 2019-01-09 |
| RU2017123772A true RU2017123772A (ru) | 2019-01-09 |
| RU2689396C2 RU2689396C2 (ru) | 2019-05-28 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017123772A RU2689396C2 (ru) | 2017-07-06 | 2017-07-06 | Фармацевтическая композиция на основе N-бензил-N-метил-1-фенилпирроло [1,2-a] пиразин-3-карбоксамида |
Country Status (1)
| Country | Link |
|---|---|
| RU (1) | RU2689396C2 (ru) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2572076C2 (ru) * | 2014-03-26 | 2015-12-27 | Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт фармакологии имени В.В. Закусова" | 1-арилпирроло[1,2-a]пиразин-3-карбоксамиды с нейропсихотропной активностью |
| RU2573823C2 (ru) * | 2014-03-26 | 2016-01-27 | Федеральное государственное бюджетное научное учреждение "Научно-исследовательский институт фармакологии имени В.В. Закусова" | Замещенные дипептиды с нейропсихотропной активностью |
-
2017
- 2017-07-06 RU RU2017123772A patent/RU2689396C2/ru active
Also Published As
| Publication number | Publication date |
|---|---|
| RU2017123772A3 (ru) | 2019-01-09 |
| RU2689396C2 (ru) | 2019-05-28 |
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