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
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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
- A61K31/21—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)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (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 (34)
Country | Link |
---|---|
US (3) | US20100267786A1 (es) |
EP (4) | EP2295035B1 (es) |
JP (2) | JP5653218B2 (es) |
KR (2) | KR101589317B1 (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) | DK3067043T3 (es) |
EC (1) | ECSP10010160A (es) |
ES (3) | ES2536514T3 (es) |
FI (1) | FI3067043T3 (es) |
GT (1) | GT201000131A (es) |
HK (3) | HK1143529A1 (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) | PE20141072A1 (es) |
PL (3) | PL3067043T3 (es) |
PT (3) | PT2217205E (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) |
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ES2536514T3 (es) | 2007-11-06 | 2015-05-26 | Novartis Ag | Composiciones farmacéuticas de doble acción basadas en superestructuras de antagonista/bloqueador de receptores de angiotensina (ARB) y receptor de endopeptidasa neutra (NEP) |
MX2011012627A (es) | 2009-05-28 | 2011-12-14 | Novartis Ag | Derivados aminobutiricos sustituidos como inhibidores de nepralisina. |
EP2594557B1 (en) | 2009-05-28 | 2016-08-10 | Novartis AG | Substituted aminopropionic derivatives as neprilysin inhibitors |
JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
CA2807830C (en) * | 2010-08-24 | 2018-04-03 | Novartis Ag | Treatment of hypertension and/or prevention or treatment of heart failure in a mammal receiving anti-coagulant therapy |
US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
MA37850A1 (fr) | 2012-08-24 | 2018-07-31 | Novartis Ag | Inhibiteurs de nep pour le traitement de maladies caractérisées par un agrandissement atrial ou une remodélisation atriale |
EA026989B1 (ru) | 2013-02-14 | 2017-06-30 | Новартис Аг | Производные замещенной бисфенилбутановой кислоты в качестве ингибиторов nep с улучшенной in vivo эффективностью |
CN105073762B (zh) | 2013-02-14 | 2017-03-08 | 诺华股份有限公司 | 作为nep(中性内肽酶)抑制剂的取代的联苯丁酰膦酸衍生物 |
US20160206597A1 (en) * | 2013-08-26 | 2016-07-21 | Toni Lynne Bransford | New Use |
WO2015028941A1 (en) | 2013-08-26 | 2015-03-05 | Novartis Ag | New use |
WO2015154673A1 (en) * | 2014-04-10 | 2015-10-15 | Zhaoyin Wang | Novel prodrugs and combinations for treatment of hypertension and cardiovascular diseases |
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 |
MX2017007426A (es) | 2014-12-08 | 2018-04-20 | Crystal Pharmatech Co Ltd | Formas cristalinas de complejo supramolecular trisodico que comprende valsartan y ahu-377 y metodos de las mismas. |
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 |
HRP20230480T1 (hr) | 2015-05-11 | 2023-07-21 | Novartis Ag | Režim doziranja sakubitrila i valsartana za liječenje zatajenja srca |
US20180140579A1 (en) | 2015-05-29 | 2018-05-24 | Novartis Ag | Sacubitril and valsartan for treating metabolic disease |
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 |
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 |
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 |
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 |
CN106074421A (zh) * | 2015-07-11 | 2016-11-09 | 凌莉 | 一种提高稳定性的药物组合物 |
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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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 |
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 |
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 |
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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 |
WO2018178295A1 (en) | 2017-03-31 | 2018-10-04 | Alfred E. Tiefenbacher (Gmbh & Co. Kg) | Stable hot-melt extrudate containing valsartan and sacubitril |
ES2890573T3 (es) * | 2017-03-31 | 2022-01-20 | Tiefenbacher Alfred E Gmbh & Co Kg | Producto extruido de fusión en caliente estable que contiene valsartán y sacubitrilo |
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 |
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US20210177803A1 (en) | 2018-08-23 | 2021-06-17 | 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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AR057882A1 (es) * | 2005-11-09 | 2007-12-26 | Novartis Ag | Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra |
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