TR202017792A2 - A new pharmaceutical composition produced by lyophilization technique containing the active ingredient of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or its sodium salt - Google Patents
A new pharmaceutical composition produced by lyophilization technique containing the active ingredient of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or its sodium salt Download PDFInfo
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- TR202017792A2 TR202017792A2 TR2020/17792A TR202017792A TR202017792A2 TR 202017792 A2 TR202017792 A2 TR 202017792A2 TR 2020/17792 A TR2020/17792 A TR 2020/17792A TR 202017792 A TR202017792 A TR 202017792A TR 202017792 A2 TR202017792 A2 TR 202017792A2
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- pyrazinecarboxamide
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- ZCGNOVWYSGBHAU-UHFFFAOYSA-N favipiravir Chemical compound NC(=O)C1=NC(F)=CNC1=O ZCGNOVWYSGBHAU-UHFFFAOYSA-N 0.000 title claims abstract description 18
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 14
- 159000000000 sodium salts Chemical class 0.000 title claims abstract description 14
- 238000004108 freeze drying Methods 0.000 title claims abstract description 6
- 239000004480 active ingredient Substances 0.000 title abstract description 13
- 238000000034 method Methods 0.000 title abstract description 6
- 230000003612 virological effect Effects 0.000 claims abstract description 6
- 201000010099 disease Diseases 0.000 claims abstract description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 5
- 230000001225 therapeutic effect Effects 0.000 claims abstract description 4
- 229940042126 oral powder Drugs 0.000 claims abstract 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 30
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 24
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 16
- 239000000203 mixture Substances 0.000 claims description 14
- 239000004376 Sucralose Substances 0.000 claims description 12
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 12
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical compound O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 claims description 12
- 235000019408 sucralose Nutrition 0.000 claims description 12
- 239000008176 lyophilized powder Substances 0.000 claims description 8
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 8
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 8
- 239000000243 solution Substances 0.000 claims description 7
- 238000002360 preparation method Methods 0.000 claims description 5
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 4
- 239000007864 aqueous solution Substances 0.000 claims description 4
- PRBFTAJMQYDJMU-UHFFFAOYSA-M sodium (5-fluoro-2-oxo-1H-pyrazine-3-carbonyl)azanide Chemical compound [Na+].FC1=CN=C(C(=N1)C(=O)[NH-])O PRBFTAJMQYDJMU-UHFFFAOYSA-M 0.000 claims description 4
- SZPBAPFUXAADQV-UHFFFAOYSA-N 2-oxo-1h-pyrazine-3-carboxamide Chemical compound NC(=O)C1=NC=CN=C1O SZPBAPFUXAADQV-UHFFFAOYSA-N 0.000 claims description 3
- 238000012371 Aseptic Filling Methods 0.000 claims description 3
- 230000001954 sterilising effect Effects 0.000 claims description 2
- 238000004659 sterilization and disinfection Methods 0.000 claims description 2
- 238000007865 diluting Methods 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 abstract description 4
- 229960005206 pyrazinamide Drugs 0.000 description 6
- IPEHBUMCGVEMRF-UHFFFAOYSA-N pyrazinecarboxamide Chemical compound NC(=O)C1=CN=CC=N1 IPEHBUMCGVEMRF-UHFFFAOYSA-N 0.000 description 5
- 239000007916 tablet composition Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- 229910052708 sodium Inorganic materials 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229950008454 favipiravir Drugs 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 229940127557 pharmaceutical product Drugs 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 108090000626 DNA-directed RNA polymerases Proteins 0.000 description 1
- 102000004163 DNA-directed RNA polymerases Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 108020000999 Viral RNA Proteins 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 241001493065 dsRNA viruses Species 0.000 description 1
- 239000007888 film coating Substances 0.000 description 1
- 238000009501 film coating Methods 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 230000001050 lubricating effect Effects 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 229940100688 oral solution Drugs 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 150000003216 pyrazines Chemical group 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 125000000548 ribosyl group Chemical group C1([C@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- 235000011121 sodium hydroxide Nutrition 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000011146 sterile filtration Methods 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- UNXRWKVEANCORM-UHFFFAOYSA-N triphosphoric acid Chemical class OP(O)(=O)OP(O)(=O)OP(O)(O)=O UNXRWKVEANCORM-UHFFFAOYSA-N 0.000 description 1
- WCTAGTRAWPDFQO-UHFFFAOYSA-K trisodium;hydrogen carbonate;carbonate Chemical compound [Na+].[Na+].[Na+].OC([O-])=O.[O-]C([O-])=O WCTAGTRAWPDFQO-UHFFFAOYSA-K 0.000 description 1
Classifications
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- 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
- A61K31/4965—Non-condensed pyrazines
-
- 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
- A61K47/02—Inorganic compounds
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
Abstract
Buluş, viral hastalıkların terapötik tedavisine yönelik olarak, 6-floro-3-hidroksi-2- pirazinkarboksamid etken maddesi veya sodyum tuzunu içeren, liyofilizasyon tekniğiyle üretilen, sulandırılarak kullanıma yönelik liyofilize oral toz formunda yeni bir farmasötik kompozisyon ve üretim yöntemi ile ilgilidir.The invention relates to a new pharmaceutical composition and production method in the form of lyophilized oral powder for reconstituted use, containing the active ingredient or sodium salt of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide, for the therapeutic treatment of viral diseases, produced by the lyophilization technique.
Description
TARIFNAME 6-floro-3-hidroksi-Z-pirazinkarboksamid etken maddesi veya sodyum tuzunu içeren Teknik Alan Bulus, 6-floro-3-hidroksi-2-pirazinkarb0ksamid etken maddesi veya sodyum tuzunu içeren Bulus özellikle, viral hastaliklarin terap'otik tedavisine yönelik olarak, 6-flor0-3-hidr0ksi-2- pirazinkarboksamid etken maddesi veya sodyum tuzunu içeren Iiyofilizasyon teknigiyle üretilen sulandirilarak kullanima yönelik Iiyofilize toz formunda yeni bir farmasötik kompozisyon ve üretim yöntemi ile ilgilidir. DESCRIPTION Containing the active ingredient 6-fluoro-3-hydroxy-Z-pyrazinecarboxamide or its sodium salt Technical Area The invention contains the active ingredient 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or its sodium salt. In particular, the invention is for the therapeutic treatment of viral diseases, including 6-fluoro-3-hydroxy-2- With the lyophilization technique containing the pyrazinecarboxamide active ingredient or sodium salt A new pharmaceutical in the form of lyophilized powder for reconstituted use produced relates to the composition and production method.
Teknigin Bilinen Durumu Günümüzde viral hastaliklarin tedavisi için tablet dozaj formunda kullanilan 6-fl0r0-3- hidroksi-2-pirazinkarboksamid etken maddesi, RNA virüslerine karsi aktiviteye sahip bir pirazinkarboksamid türevidir. Bu etken madde konakçi enzimler tarafindan ribofuranosil trifosfat türevine dönüstürülür ve viral RNA'ya bagimli RNA polimerazi seçici olarak inhibe Formül I veya bunun tuzlarinin yüksek bir içerigine sahip, boyutlandirmasi kolay, film kaplama, paketleme ve nakliyeye dayanikli bir tablet formülasyon açiklanmaktadir. CN105687152B nolu patentte ise hizli salinimli Favipiravir tablet formülasyonu açiklanmaktadir. Burada bir tablet Favipiravir etken maddesi haricinde, mikrokristalin selüloz, çözündürücü; parçalayici, yaglayici ve kayganlastirici ajanlar içermektedir. State of the Art 6-fl0r0-3-, which is currently used in tablet dosage form for the treatment of viral diseases. The active ingredient hydroxy-2-pyrazinecarboxamide is a drug with activity against RNA viruses. It is a pyrazinecarboxamide derivative. This active ingredient is digested by host enzymes ribofuranosyl. It is converted to the triphosphate derivative and selectively inhibits viral RNA-dependent RNA polymerase. Formula I film coating, easy to size, with a high content of salts or A tablet formulation resistant to packaging and transportation is disclosed. CN105687152B An immediate release Favipiravir tablet formulation is described in the patent no. Here is a tablet except Favipiravir active ingredient, microcrystalline cellulose, solubilizer; It contains disintegrating, lubricating and lubricating agents.
Mevcut tablet formülasyonlarinda etken madde yaninda birçok yardimci madde içerir. Existing tablet formulations contain many excipients besides the active ingredient.
Bununla beraber tablet formülasyonlar düsük çözünme orani sorununa sahiptir. Bu yüzden etken maddenin insan vücudu tarafindan emilimi ve tedavinin basarisi büyük ölçüde olumsuz olarak etkilenir. However, tablet formulations have the problem of low dissolution rate. This Therefore, the absorption of the active substance by the human body and the success of the treatment are great. substantially negatively affected.
Bu sebeple, 6-flor0-3-hidroksi-2-pirazinkarb0ksamid etken maddesinin oral yoldan uygulanmasina izin verirken, çözünme, salinim ve emilim sorunlarini ortan kaldiran, diger farmasötik formlarin çoklu içeriklerinin gösterdigi yan etkileri göstermeyen, kullanima hazir gelistirilmis formülasyona ihtiyaç duyulmaktadir. For this reason, oral administration of the active ingredient of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide other, which eliminates dissolution, release and absorption problems while allowing ready-to-use, which does not show the side effects of multiple ingredients of pharmaceutical forms improved formulation is needed.
Sonuç olarak yukarida anlatilan olumsuzluklardan dolayi ve mevcut çözümlerin konu hakkindaki yetersizligi nedeniyle ilgili teknik alanda bir gelistirme yapilmasi gerekli kilinmistir. As a result, due to the above-mentioned negativities and existing solutions It is necessary to make an improvement in the relevant technical field due to the inadequacy of the is locked.
Bulusun Kisa Açiklamasi Mevcut bulus, yukarida bahsedilen gereksinimleri karsilayan, tüm dezavantajlari ortadan kaldiran ve ilave bazi avantajlar getiren 6-floro-3-hidroksi-2-pirazinkarboksamid etken maddesi veya farmasötik olarak kabul edilebilir sodyum tuzunu içeren yeni bir farmasötik kompozisyon ile ilgilidir. Brief Description of the Invention The present invention satisfies the above-mentioned requirements, eliminates all disadvantages. 6-fluoro-3-hydroxy-2-pyrazinecarboxamide agent, which removes the a new pharmaceutical product containing the substance or a pharmaceutically acceptable sodium salt It's about composition.
Bulusun öncelikli amaci, yüksek safliktaki Iiyofilize toz formülasyonu ile herhangi bir yan etkiye yol açmaksizin viral hastaliklarda etkili bir tedavi sunmaktir. The primary object of the invention is to use the high purity lyophilized powder formulation with no side effects. To provide an effective treatment in viral diseases without causing any effect.
Bulusun bir amaci, yüksek bir çözünürlük sergileyen, stabil olan, bitmis üründen sulandirilarak kullanima yönelik, kullanim kolayligi ve güvenilirlik saglayan yeni bir farmasötik kompozisyon sunmaktir. It is an object of the invention to produce a stable, finished product that exhibits a high solubility. It is a new product for reconstituted use, providing ease of use and reliability. is to present a pharmaceutical composition.
Bulusun bir diger amaci, etken madde yaninda tercih edilen yardimci maddeleri spesifik oranlarda kullanarak sunulan Iiyofilize toz dozaj formu ile, etkin çözünürlük ve stabilite yaninda, sulandirilarak kullanima uygun tat saglayan yeni bir farmasötik kompozisyon sunmaktir. Another aim of the invention is to specify the preferred excipients besides the active substance. Effective solubility and stability with the lyophilized powder dosage form offered using the In addition, a new pharmaceutical composition is diluted to provide a taste suitable for use. is to present.
Yukaridaki amaçlari yerine getirmek için bulus, sulandirilarak kullanima yönelik liyofilize toz formunda farmasötik bir kompozisyon olup, etken madde olarak 6-fl0ro-3-hidroksi-2- pirazinkarboksamid veya farmasbtik olarak kabul edilebilir sodyum tuzu ile yardimci madde olarak sodyum hidroksit, sodyum bikarbonat, sodyum karbonat, süklaroz arasindan seçilen birey veya kombinsasyonlar içermektedir. To fulfill the above purposes, the invention is reconstituted and lyophilized for use. It is a pharmaceutical composition in powder form and as active ingredient 6-fluoro-3-hydroxy-2- Supplement with pyrazinecarboxamide or its pharmaceutically acceptable sodium salt as substances sodium hydroxide, sodium bicarbonate, sodium carbonate, suclarose contains individuals or combinations selected from among
Yukaridaki amaçlari yerine getirmek için bulus, sulandirilarak kullanima yönelik Iiyofilize toz formunda farmasötik kompozisyon hazirlama yöntemi olup, 6-floro-3-hidroksi-2- pirazinkarboksamid veya farmasötik olarak kabul edilebilir sodyum tuzunun, sodyum hidroksit, sodyum bikarbonat veya sodyum karbonat kullanilarak, tercihen sükraloz ilave edilerek homojenize sulu çözeltisinin hazirlanmasi ve hazirlanan çözeltiye sterilizasyon, aseptik dolum, Iiyofilizasyon uygulanmasi islemlerini içermektedir. To fulfill the above purposes, the invention is reconstituted for use in Lyophilized It is a method of preparing pharmaceutical composition in powder form, 6-fluoro-3-hydroxy-2- pyrazinecarboxamide or its pharmaceutically acceptable sodium salt, sodium adding sucralose, preferably using hydroxide, sodium bicarbonate or sodium carbonate preparation of the homogenized aqueous solution and sterilization into the prepared solution, It includes aseptic filling, lyophilization application processes.
Bulusun yapisal ve karakteristik 'Özellikleri ve tüm avantajlari asagida verilen detayli açiklama sayesinde daha net olarak anlasilacaktir ve bu nedenle degerlendirmenin de bu detayli açiklama göz önüne alinarak yapilmasi gerekmektedir. The structural and characteristic features of the invention and all its advantages are detailed below. will be more clearly understood by the explanation and therefore this should be made taking into account the detailed explanation.
Bulusun Detayli Açiklamasi Bu detayli açiklamada bulus konusu farmasötik kompozisyon ve üretim yöntemi sadece konunun daha iyi anlasilmasina yönelik olarak ve hiçbir sinirlayici etki olusturmayacak sekilde açiklanmaktadir. 6-fl0r0-3-hidr0ksi-2-pirazinkarboksamid viral vakalarda terapötik kullanim için onaylanmis modifiye edilmis bir pirazin analogudur. Detailed Description of the Invention In this detailed description, the inventive pharmaceutical composition and method of manufacture are only for a better understanding of the subject and will not have any limiting effect is explained in the following. 6-fluoro-3-hydroxy-2-pyrazinecarboxamide approved for therapeutic use in viral conditions It is a modified pyrazine analog.
Bulus konusu farmas'otik kompozisyonda etken madde olarak 6-floro-3-hidroksi-2- pirazinkarboksamid veya farmas'otik olarak kabul edilebilir sodyum tuzu, yardimci maddeler olarak s'ükraloz, sodyum hidroksit, sodyum bikarbonat veya sodyum karbonat kullanilmaktadir. Sulandirilarak kullanima uygun olarak hazirlanarak uygulanacak olan içilebilirlik saglayan tatlandirici olarak tercih edilmektedir. Sodyum hidroksit, sodyum bikarbonat veya sodyum karbonat ise hazirlanacak çözeltide, çözeltinin pHiini ayarlayarak 6-roro-B-hidroksi-2-pirazinkarboksamidin çözünürlügüne katkida bulunmaktadir. As an active ingredient in the pharmaceutical composition of the invention, 6-fluoro-3-hydroxy-2- pyrazinecarboxamide or pharmaceutically acceptable sodium salt, adjuvant sucralose, sodium hydroxide, sodium bicarbonate or sodium carbonate as substances is used. Diluted and prepared in accordance with use, to be applied It is preferred as a sweetener that provides drinkability. sodium hydroxide, sodium bicarbonate or sodium carbonate, in the solution to be prepared, by adjusting the pH of the solution. It contributes to the solubility of 6-roro-B-hydroxy-2-pyrazinecarboxamide.
Tabl0.1: Bulusun tercih edilen bir örneginin içerigi Içerik Agirlikça tercih edilen Agirlikça miktar kullanilabilir miktar 6-floro-3-hidroksi-2-pirazinkarboksamid 86,0 Min. Table0.1: Contents of a preferred example of the invention Content By Weight Preferred By Weight quantity available quantity 6-fluoro-3-hydroxy-2-pyrazinecarboxamide 86.0 Min.
Sükraloz 1,0 Maks. Sucralose 1.0 Max.
Sodyum Hidroksit k.m k.m Sodyum Bikarbonat Sodyum Karbonat k.m.: kâfi miktarda Tablo.2: Bulusun tercih edilen diger bir Örneginin Içerik Agirlikça tercih edilen Agirlikça miktar kullanilabilir miktar pirazinkarboksamid S'L'ikraloz 0,4 Maks. 1,0 Bulus, en temel halinde sulandirilarak kullanima yönelik Iiyofilize toz formunda farmasötik kompozisyon olup, etken madde olarak 6-flor0-3-hidroksi-2-pirazinkarb0ksamid veya farmasötik olarak kabul edilebilir sodyum tuzu ile yardimci madde olarak sodyum hidroksit, sodyum bikarbonat, sodyum karbonat, s'L'iklaroz arasindan seçilen birey veya kombinsasyonlar içermektedir. Sodium Hydroxide k.m k.m Sodium bicarbonate Sodium Carbonate k.m.: enough amount Table.2: Another Preferred Example of the Invention Content By Weight Preferred By Weight quantity available quantity pyrazinecarboxamide S'L'icralose 0.4 Max. 1.0 In its most basic form, the invention is a pharmaceutical product in the form of lyophilized powder for reconstituted use. The composition is 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or pharmaceutically acceptable sodium salt with sodium as excipient individual selected from hydroxide, sodium bicarbonate, sodium carbonate, s'L'iclarose, or contains combinations.
Bulusun bir uygulamasina göre farmasötik kompozisyon, agirlikça minimum %86 oraninda 6-floro-3-hidroksi-2-pirazinkarboksamid içermektedir. According to one embodiment of the invention, the pharmaceutical composition contains a minimum of 86% by weight. It contains 6-fluoro-3-hydroxy-2-pyrazinecarboxamide at the rate of.
Bulusun bir uygulamasina göre farmasötik kompozisyon, agirlikça minimum %99,6 oraninda 6-fl0ro-3-hidroksi-2-pirazinkarb0ksamid sodyum tuzunu içermektedir. According to one embodiment of the invention, the pharmaceutical composition contains a minimum of 99.6% by weight. It contains 6-fluoro-3-hydroxy-2-pyrazinecarboxamide sodium salt in the ratio.
Bulusun bir uygulamasina göre farmasötik kompozisyon, kâfi miktarda sodyum hidroksit, sodyum bikarbonat, sodyum karbonat arasindan seçilen birey veya kombinsasyonlar içermektedir. According to one embodiment of the invention, the pharmaceutical composition consists of a sufficient amount of sodium hydroxide, individual or combinations selected from sodium bicarbonate, sodium carbonate contains.
Bulusun bir uygulamasina göre farmasötik kompozisyon ayrica tercihen agirlikça maksimum %1 oraninda sükraloz içermektedir. According to one embodiment of the invention, the pharmaceutical composition is further preferably by weight. It contains a maximum of 1% sucralose.
Bulusun tercih edilen bir örnegi; agirlikça %86 oraninda 6-floro-3-hidr0ksi-2- pirazinkarboksamid; agirlikça %1 oraninda sükraloz ve kafi miktarda sodyum hidroksit, sodyum bikarbonat veya sodyum karbonat içermektedir. A preferred example of the invention is; 86% by weight of 6-fluoro-3-hydroxy-2- pyrazinecarboxamide; 1% by weight of sucralose and sufficient amount of sodium hydroxide, Contains sodium bicarbonate or sodium carbonate.
Bulusun tercih edilen diger bir örnegi; agirlikça %99,6 oraninda 6-fl0ro-3-hidroksi-2- pirazinkarboksamid sodyum tuzu; agirlikça %0,4 oraninda sükraloz içermektedir. Another preferred example of the invention is; 99.6% by weight of 6-fluoro-3-hydroxy-2- pyrazinecarboxamide sodium salt; It contains 0.4% sucralose by weight.
Bulus konusu oral çözelti hazirlamaya yönelik liyofilize toz formunda farmasötik kompozisyon `üretim yöntemi; oda sicakliginda Tablo 1'de verilen hammaddelerin belirtilen miktarlarda karistirilarak sulu çözelti hazirlanmasi ile baslar. 6-fl0ro-3-hidroksi-2- pirazinkarboksamid veya farmasötik olarak kabul edilebilir sodyum tuzu ile sodyum hidroksit, sodyum bikarbonat ve/veya sodyum karbonat kullanilarak tercihen sükraloz ilave edilerek homojenize sulu çözeltisi hazirlanir. Hazirlanan Çözeltiye steril filtrasyon uygulanir. Sterilize edilen çözeltinin aseptik dolumu yapilir ve Iiyofilizasyon uygulanarak, 6-fl0r0-3-hidroksi-2-pirazinkarboksamid etken maddesi içeren liyofilize toz formundaki son hidroksi-2-pirazinkarboksamid dozajlarinda veya bunun esdeger miktarlarda sodyum tuzu içeren dozlarda liyofilize toz olarak ambalajlanarak, sulandirilarak sulandirilarak kullanima yönelik jenerik bir beseri ilaç olarak piyasaya sunulmaktadir. Pharmaceutical in the form of lyophilized powder for the preparation of oral solution of the invention composition`s production method; of the raw materials given in Table 1 at room temperature. It starts with the preparation of an aqueous solution by mixing in amounts. 6-fluoro-3-hydroxy-2- sodium with pyrazinecarboxamide or its pharmaceutically acceptable sodium salt Sucralose is added preferably using hydroxide, sodium bicarbonate and/or sodium carbonate. homogenized aqueous solution is prepared. Sterile filtration into the Prepared Solution is applied. Aseptic filling of the sterilized solution is made and by applying lyophilization, The final product in the form of lyophilized powder containing the active ingredient 6-fl0r0-3-hydroxy-2-pyrazinecarboxamide sodium salt in dosages of hydroxy-2-pyrazinecarboxamide or equivalent amounts Packaged as lyophilized powder in doses containing It is marketed as a generic medicine for human use.
Claims (3)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TR2020/17792A TR202017792A2 (en) | 2020-11-06 | 2020-11-06 | A new pharmaceutical composition produced by lyophilization technique containing the active ingredient of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or its sodium salt |
| PCT/TR2021/050149 WO2022098324A1 (en) | 2020-11-06 | 2021-02-17 | A new pharmaceutical composition produced by lyophylisation method containing 6-fluoro-3-hydroxy-2-pyrazinecarboxamide active ingredient or its sodium salt |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| TR2020/17792A TR202017792A2 (en) | 2020-11-06 | 2020-11-06 | A new pharmaceutical composition produced by lyophilization technique containing the active ingredient of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or its sodium salt |
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| TR202017792A2 true TR202017792A2 (en) | 2021-01-21 |
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| TR2020/17792A TR202017792A2 (en) | 2020-11-06 | 2020-11-06 | A new pharmaceutical composition produced by lyophilization technique containing the active ingredient of 6-fluoro-3-hydroxy-2-pyrazinecarboxamide or its sodium salt |
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| WO (1) | WO2022098324A1 (en) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY161429A (en) * | 2010-09-30 | 2017-04-14 | Toyama Chemical Co Ltd | Sodium salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide |
| BR112020009101A2 (en) * | 2017-12-28 | 2020-10-20 | Fujifilm Toyama Chemical Co., Ltd. | method for producing frozen formulation |
| CN111228226B (en) * | 2020-03-06 | 2021-12-28 | 瑞阳制药有限公司 | Freeze-dried preparation of pyrrosia faberi for injection and preparation method thereof |
-
2020
- 2020-11-06 TR TR2020/17792A patent/TR202017792A2/en unknown
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