AR069184A1 - Una composicion farmaceutica que comprende una superestructura (lcz696), de un antagoniste/bloqueante (arb) del recptor angiotensina, e inhibidor de la endopeptidasa neutra (nep). - Google Patents
Una composicion farmaceutica que comprende una superestructura (lcz696), de un antagoniste/bloqueante (arb) del recptor angiotensina, e inhibidor de la endopeptidasa neutra (nep).Info
- Publication number
- AR069184A1 AR069184A1 ARP080104826A ARP080104826A AR069184A1 AR 069184 A1 AR069184 A1 AR 069184A1 AR P080104826 A ARP080104826 A AR P080104826A AR P080104826 A ARP080104826 A AR P080104826A AR 069184 A1 AR069184 A1 AR 069184A1
- Authority
- AR
- Argentina
- Prior art keywords
- methyl
- biphenyl
- dosage form
- oral dosage
- amino
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 102000003729 Neprilysin Human genes 0.000 title 2
- 108090000028 Neprilysin Proteins 0.000 title 2
- 102000008873 Angiotensin II receptor Human genes 0.000 title 1
- 108050000824 Angiotensin II receptor Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 230000000903 blocking effect Effects 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000006186 oral dosage form Substances 0.000 abstract 4
- 239000004072 C09CA03 - Valsartan Substances 0.000 abstract 3
- 239000002253 acid Substances 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 239000007787 solid Substances 0.000 abstract 3
- SJSNUMAYCRRIOM-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 abstract 3
- 229960004699 valsartan Drugs 0.000 abstract 3
- -1 (1S, 3R) -1-biphenyl-4-yl-methyl-3-ethoxy-carbonyl-1-butyl-carbamoyl Chemical group 0.000 abstract 2
- 239000002552 dosage form Substances 0.000 abstract 2
- 125000004494 ethyl ester group Chemical group 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- OVBFMEVBMNZIBR-UHFFFAOYSA-N -2-Methylpentanoic acid Natural products CCCC(C)C(O)=O OVBFMEVBMNZIBR-UHFFFAOYSA-N 0.000 abstract 1
- 238000010521 absorption reaction Methods 0.000 abstract 1
- 238000005056 compaction Methods 0.000 abstract 1
- 238000007907 direct compression Methods 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 abstract 1
- 238000009490 roller compaction Methods 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Las formas de dosificacion oral solidas, en especial tabletas, de una composicion farmacéutica que comprende un complejo supramolecular, se pueden formar a partir de un proceso de compresion directa o de un proceso de compactacion, tal como compactacion con rodillos. Estas formas de dosificacion oral solida proporcionan un perfil de liberacion inmediata que permite tener una rápida libracion del agente terapéutico. Un complejo supramolecular particularmente util es el propionato-(S)-3'-metil-2'-(pentanoil-{2ö-(tetrazol-5-ilato)-bifenil-4'-il-metil}-amino)-butirato]-hemipentahidrato de [3-((1S,3R)-1-bifenil-4-il-metil-3-etoxi-carbonil-1-butil-carbamoílo) de trisodio. Reivindicacion 15: Una forma de dosificacion oral solida, la cual comprende fracciones de: valsartan, o una sal del mismo, y ácido (2R,4S)-5-bifenil-4-il-5-(3-carboxi-propionil-amino)-2-metil-pentanoico, o etil-éster de etil-éster del ácido (2R,4S)-5-bifenil-4-il-5-(3-carboxi-propionil-amino)-2-metil-pentanoico, o una sal de los mismos, suministrar una cantidad terapéuticamente efectiva de ácido libre de valsartan, o una sal farmacéuticamente aceptable del mismo, y un medio portador, en donde la forma de dosificacion oral proporciona una velocidad de absorcion del ácido libre de valsartan con un tmax de 1 a 2.2 horas en seguida de la administracion de una sola dosis de esta forma de dosificacion, y/o proporciona una exposicion de plasma promedio normalizada a la dosis (AUC0-24) de 230 a 400 nanogramosòhora/mililitro/equivalentes en miligramos, en seguida de la administracion de una sola dosis de esta forma de dosificacion.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98566807P | 2007-11-06 | 2007-11-06 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR069184A1 true AR069184A1 (es) | 2010-01-06 |
Family
ID=40451030
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080104826A AR069184A1 (es) | 2007-11-06 | 2008-11-04 | Una composicion farmaceutica que comprende una superestructura (lcz696), de un antagoniste/bloqueante (arb) del recptor angiotensina, e inhibidor de la endopeptidasa neutra (nep). |
Country Status (33)
| Country | Link |
|---|---|
| US (3) | US20100267786A1 (es) |
| EP (4) | EP2295035B1 (es) |
| JP (2) | JP5653218B2 (es) |
| KR (2) | KR101700062B1 (es) |
| CN (2) | CN101848700A (es) |
| AR (1) | AR069184A1 (es) |
| AU (1) | AU2008324878B2 (es) |
| BR (1) | BRPI0823505A2 (es) |
| CA (1) | CA2703598C (es) |
| CL (1) | CL2008003298A1 (es) |
| CY (2) | CY1116280T1 (es) |
| DK (3) | DK2295035T3 (es) |
| EC (1) | ECSP10010160A (es) |
| ES (3) | ES2939163T3 (es) |
| FI (1) | FI3067043T3 (es) |
| GT (1) | GT201000131A (es) |
| HR (3) | HRP20230178T3 (es) |
| HU (2) | HUE028866T2 (es) |
| IL (3) | IL262990B2 (es) |
| JO (1) | JOP20080499B1 (es) |
| MA (1) | MA31797B1 (es) |
| MX (1) | MX2010004930A (es) |
| MY (1) | MY153730A (es) |
| NZ (1) | NZ584686A (es) |
| PE (2) | PE20091390A1 (es) |
| PL (3) | PL2295035T3 (es) |
| PT (3) | PT3067043T (es) |
| RU (1) | RU2493844C3 (es) |
| SG (1) | SG185951A1 (es) |
| SI (3) | SI2217205T1 (es) |
| TN (1) | TN2010000200A1 (es) |
| TW (1) | TWI484982B (es) |
| WO (1) | WO2009061713A1 (es) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2295035T3 (pl) | 2007-11-06 | 2016-11-30 | Podwójne działanie kompozycji farmaceutycznych opartych na superstrukturach antagonisty/blokera receptora angiotensyny (arb) oraz inhibitora obojętnej endopeptydazy (nep) | |
| CN102448928B (zh) | 2009-05-28 | 2014-10-01 | 诺华股份有限公司 | 作为中性溶酶(neprilysin)抑制剂的取代的氨基丁酸衍生物 |
| ES2602902T3 (es) | 2009-05-28 | 2017-02-22 | Novartis Ag | Derivados aminopropiónicos sustituidos como inhibidores de neprilisina |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| KR101864865B1 (ko) * | 2010-08-24 | 2018-06-05 | 노파르티스 아게 | 항응고제 요법을 받고 있는 포유동물에서의 고혈압의 치료 및/또는 심부전의 예방 또는 치료 |
| US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| JP6482462B2 (ja) | 2012-08-24 | 2019-03-13 | ノバルティス アーゲー | 心房拡大又はリモデリングを特徴とする疾患を治療するためのnep阻害剤 |
| TR201808541T4 (tr) | 2013-02-14 | 2018-07-23 | Novartis Ag | Nep (nötr endopeptidaz) inhibitörleri olarak ikame edilmiş bisfenil butanoik fosfonik asit türevleri. |
| EP2956445A1 (en) | 2013-02-14 | 2015-12-23 | Novartis AG | Substituted bisphenyl butanoic acid derivatives as nep inhibitors with improved in vivo efficacy |
| EP3038653A1 (en) * | 2013-08-26 | 2016-07-06 | Novartis AG | New use |
| HUE064634T2 (hu) | 2013-08-26 | 2024-04-28 | Novartis Ag | Kardiovaszkuláris betegségek kezelése |
| CN106795099B (zh) * | 2014-04-10 | 2019-11-26 | 南京奥昭生物科技有限公司 | 用于治疗高血压和心血管疾病的前药和组合物 |
| CN105461647B (zh) * | 2014-09-28 | 2018-06-29 | 四川海思科制药有限公司 | 缬沙坦沙库比曲三钠盐复合物的固态形式及其制备方法和用途 |
| SI3229799T1 (sl) | 2014-12-08 | 2019-03-29 | Crystal Pharmatech Co., Ltd. | Kristalinične oblike trinatrijevega supramolekularnega kompleksa, ki obsega valsartan in AHU-377, ter njihovi postopki |
| CN104473938B (zh) * | 2014-12-30 | 2017-06-09 | 北京瑞都医药科技有限公司 | 一种治疗慢性心衰药物及其制备方法 |
| CN104826115A (zh) * | 2015-04-19 | 2015-08-12 | 浙江巨泰药业有限公司 | 一种抗心衰药物组合物及其制备方法 |
| JP6576469B2 (ja) | 2015-05-11 | 2019-09-18 | ノバルティス アーゲー | 心不全の治療のためのサクビトリル−バルサルタンの用量計画 |
| JP2018516267A (ja) | 2015-05-29 | 2018-06-21 | ノバルティス アーゲー | 代謝性疾患を治療するためのサクビトリルおよびバルサルタン |
| CN106309388A (zh) * | 2015-06-30 | 2017-01-11 | 深圳信立泰药业股份有限公司 | 一种用于心衰治疗的药物组合物及其制备方法 |
| WO2017006254A1 (en) | 2015-07-08 | 2017-01-12 | Novartis Ag | Drug combination comprising an angiotensin ii receptor antagonist, a neutral endopeptidase inhibitor and a mineralcorticoid receptor antagonist |
| CN106176723A (zh) * | 2015-07-11 | 2016-12-07 | 凌莉 | 一种固体药物组合物及其制备方法 |
| CN106176724A (zh) * | 2015-07-11 | 2016-12-07 | 凌莉 | 一种稳定的固体药物组合物及其制备方法 |
| CN105997994A (zh) * | 2015-07-11 | 2016-10-12 | 凌莉 | 一种固体口服型制剂及其制备方法 |
| CN106176725A (zh) * | 2015-07-11 | 2016-12-07 | 凌莉 | 一种提高稳定性的药物组合物及其制备方法和用途 |
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| CN105997993B (zh) * | 2015-07-11 | 2018-03-30 | 麦丽芳 | 一种用于心血管疾病治疗的固体口服型制剂及其制备方法 |
| WO2017012600A1 (en) | 2015-07-20 | 2017-01-26 | Zentiva, K.S. | A pharmaceutical composition containing valsartan and sacubitril and methods for preparation and stabilization thereof |
| CN106397248A (zh) * | 2015-08-03 | 2017-02-15 | 深圳信立泰药业股份有限公司 | 一种lcz696结晶粉末及其制备方法 |
| EP3355880A1 (en) | 2015-08-28 | 2018-08-08 | Novartis AG | New use |
| WO2017037596A1 (en) * | 2015-08-28 | 2017-03-09 | Dr. Reddy's Laboratories Limited | Amorphous solid dispersion of lcz-696 |
| US20180303799A1 (en) * | 2015-10-16 | 2018-10-25 | Shenzhen Salubris Pharmaceuticals Co., Ltd | An Oral Preparation for the Treatment of Cardiovascular Disease and Its Preparation Method |
| CN105669581B (zh) * | 2015-11-09 | 2017-03-22 | 成都苑东生物制药股份有限公司 | 一种血管紧张受体拮抗剂和中性内肽酶抑制剂复合物 |
| WO2017085573A1 (en) * | 2015-11-20 | 2017-05-26 | Lupin Limited | Amorphous sacubitril-valsartan complex and process for preparation thereof |
| CN105330609B (zh) * | 2015-12-07 | 2017-12-22 | 南京正大天晴制药有限公司 | 一种制备lcz696的方法 |
| CN105935358B (zh) * | 2015-12-18 | 2019-06-07 | 重庆两江药物研发中心有限公司 | 一种沙库比曲缬沙坦缓释剂及其制备方法 |
| CN105929031B (zh) * | 2015-12-18 | 2018-08-21 | 重庆两江药物研发中心有限公司 | 一种血管紧张素受体拮抗剂和nep抑制剂的复合物中杂质的分离方法 |
| CN106905253B (zh) * | 2015-12-23 | 2020-01-03 | 正大天晴药业集团股份有限公司 | 一种超分子复合物的结晶 |
| WO2017134600A1 (en) | 2016-02-03 | 2017-08-10 | Novartis Ag | New use of a combination of sacubitril and valsartan |
| HK1256865A1 (zh) | 2016-02-03 | 2019-10-04 | Novartis Ag | 有机化合物的盖伦制剂 |
| CN105748420B (zh) * | 2016-03-04 | 2018-11-06 | 山东省药学科学院 | 一种治疗心力衰竭的lcz696缓释骨架片的制备方法 |
| CN105902506A (zh) * | 2016-06-12 | 2016-08-31 | 佛山市腾瑞医药科技有限公司 | 一种沙卡布曲缬沙坦制剂及其应用 |
| WO2018069937A1 (en) | 2016-10-13 | 2018-04-19 | Mylan Laboratories Limited | Solid dispersions of trisodium sacubitril valsartan and process for the preparation thereof |
| EP3600255B1 (en) * | 2017-03-31 | 2021-07-07 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Stable hot-melt extrudate containing valsartan and sacubitril |
| WO2018178295A1 (en) | 2017-03-31 | 2018-10-04 | Alfred E. Tiefenbacher (Gmbh & Co. Kg) | Stable hot-melt extrudate containing valsartan and sacubitril |
| WO2018211479A1 (en) * | 2017-05-19 | 2018-11-22 | Lupin Limited | Stabilized compositions of angiotensin ii inhibitors and neutral endopeptidase inhibitors and process for preparation thereof |
| US11382866B2 (en) | 2017-07-06 | 2022-07-12 | Mankind Pharma Ltd. | Fixed dose pharmaceutical composition of valsartan and sacubitril |
| EA202090398A1 (ru) | 2017-07-28 | 2020-05-15 | Синтон Б.В. | Фармацевтическая композиция, включающая сакубитрил и валсартан |
| US20200276129A1 (en) | 2017-10-13 | 2020-09-03 | Alfred E. Tiefenbacher (Gmbh & Co. Kg) | Tablet containing valsartan and sacubitril |
| WO2019180735A1 (en) * | 2018-03-19 | 2019-09-26 | Natco Pharma Limited | Stable pharmaceutical compositions comprising sacubitril-valsartan complex |
| US11877576B2 (en) | 2018-06-22 | 2024-01-23 | Ideaz, Llc | Diphenyl tablets and methods of preparing the same |
| CA3110152A1 (en) | 2018-08-23 | 2020-02-27 | Novartis Ag | New pharmaceutical use for the treatment of heart failure |
| WO2020039394A1 (en) | 2018-08-24 | 2020-02-27 | Novartis Ag | New drug combinations |
| EP3766484B1 (en) | 2019-07-19 | 2021-08-25 | Zentiva, K.S. | Solid pharmaceutical dosage form comprising valsartan and sacubitril |
| KR102545274B1 (ko) | 2020-02-26 | 2023-06-20 | 에리슨제약(주) | 사쿠비트릴 및 발사르탄을 포함하는 심부전 치료용 서방성 제제, 및 이를 포함하는 다중방출 복합제제와 이의 제조방법 |
| KR20210120560A (ko) | 2020-03-27 | 2021-10-07 | 주식회사 유영제약 | 고함량의 주성분을 포함하는 정제 및 그 제조방법 |
| KR20210138510A (ko) | 2020-05-12 | 2021-11-19 | 에리슨제약(주) | 사쿠비트릴, 발사르탄 및 네비보롤을 포함하는 심부전 및 허혈성 심질환의 예방 또는 치료용 약제학적 조성물 및 이를 포함하는 약제학적 복합제제 |
| KR20220091767A (ko) | 2020-12-24 | 2022-07-01 | 주식회사 보령 | 사쿠비트릴 발사르탄 하이브리드 화합물 또는 그 약제학적으로 허용되는 염을 유효성분으로 포함하는 약제학적 조성물 |
| KR102486815B1 (ko) | 2021-01-20 | 2023-01-10 | 주식회사 대웅제약 | Nep 저해제 및 arb를 포함하는 약학 조성물 및 이의 제조 방법 |
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| PL2295035T3 (pl) | 2007-11-06 | 2016-11-30 | Podwójne działanie kompozycji farmaceutycznych opartych na superstrukturach antagonisty/blokera receptora angiotensyny (arb) oraz inhibitora obojętnej endopeptydazy (nep) |
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2008
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