CN109310627B - 福奈妥匹坦的生理平衡注射制剂 - Google Patents

福奈妥匹坦的生理平衡注射制剂 Download PDF

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Publication number
CN109310627B
CN109310627B CN201780034681.5A CN201780034681A CN109310627B CN 109310627 B CN109310627 B CN 109310627B CN 201780034681 A CN201780034681 A CN 201780034681A CN 109310627 B CN109310627 B CN 109310627B
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injectable formulation
formulation
fornetupitant
liquid
lyophilized
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Chinese (zh)
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CN109310627A (zh
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阿莱西奥·温特维尼
罗伯特·凯尼拉
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Helsinn Healthcare SA
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Helsinn Healthcare SA
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/473Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183Amino acids, e.g. glycine, EDTA or aspartame
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201780034681.5A 2016-06-06 2017-06-01 福奈妥匹坦的生理平衡注射制剂 Active CN109310627B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662345942P 2016-06-06 2016-06-06
US62/345,942 2016-06-06
PCT/EP2017/063268 WO2017211663A1 (en) 2016-06-06 2017-06-01 Physiologically balanced injectable formulations of fosnetupitant

Publications (2)

Publication Number Publication Date
CN109310627A CN109310627A (zh) 2019-02-05
CN109310627B true CN109310627B (zh) 2021-12-14

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CN201780034681.5A Active CN109310627B (zh) 2016-06-06 2017-06-01 福奈妥匹坦的生理平衡注射制剂

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US (4) US10624911B2 (enExample)
EP (2) EP3626231A1 (enExample)
JP (2) JP6936817B2 (enExample)
KR (1) KR102459416B1 (enExample)
CN (1) CN109310627B (enExample)
AR (1) AR108676A1 (enExample)
AU (1) AU2017276588B2 (enExample)
BR (1) BR112018074655B1 (enExample)
CA (1) CA3025837C (enExample)
CL (1) CL2018003338A1 (enExample)
CO (1) CO2018011686A2 (enExample)
CY (1) CY1122755T1 (enExample)
DK (1) DK3435980T3 (enExample)
EA (1) EA036605B1 (enExample)
EC (1) ECSP19000169A (enExample)
ES (1) ES2771226T3 (enExample)
HR (1) HRP20200196T1 (enExample)
IL (1) IL263126B (enExample)
JO (1) JOP20170137B1 (enExample)
LT (1) LT3435980T (enExample)
MA (1) MA44513B1 (enExample)
MD (1) MD3435980T2 (enExample)
MX (1) MX376118B (enExample)
MY (1) MY194081A (enExample)
PE (1) PE20190347A1 (enExample)
PH (1) PH12018502524B1 (enExample)
PL (1) PL3435980T3 (enExample)
PT (1) PT3435980T (enExample)
RS (1) RS59852B1 (enExample)
SG (1) SG11201809708PA (enExample)
SI (1) SI3435980T1 (enExample)
TW (1) TWI725191B (enExample)
UA (1) UA122285C2 (enExample)
UY (1) UY37273A (enExample)
WO (1) WO2017211663A1 (enExample)
ZA (1) ZA201807932B (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11654154B2 (en) 2019-01-29 2023-05-23 Navinta Iii Inc Process for preparing injectable Fosaprepitant Dimeglumine compositions having improved storage stability
US12097197B2 (en) 2021-12-21 2024-09-24 Slayback Pharma Llc Stable liquid compositions of netupitant and palonosetron
JP7783403B2 (ja) * 2022-03-23 2025-12-09 大鵬薬品工業株式会社 ホスネツピタント又はその医薬上許容される塩の安定化製剤およびその製造方法
WO2025036703A1 (en) * 2023-08-13 2025-02-20 Helsinn Healthcare Sa Fosnetupitant for administration via intravenous bolus
WO2025056094A1 (zh) * 2023-09-15 2025-03-20 广州帝奇医药技术有限公司 一种冻干制剂和注射液及其制备方法
CN119185243A (zh) * 2024-11-28 2024-12-27 山东齐都药业有限公司 福奈妥匹坦帕洛诺司琼口服掩味颗粒剂及其制备方法与应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004067005A1 (en) * 2003-01-30 2004-08-12 Helsinn Healthcare Sa Liquid pharmaceutical formulations of palonosetron
US8426450B1 (en) * 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect

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IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
ES2164758T3 (es) 1993-12-29 2002-03-01 Merck Sharp & Dohme Derivados de morfolina sustituidos y su uso como agentes terapeuticos.
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
US20060167072A1 (en) * 2004-01-30 2006-07-27 Helsinn Healthcare Sa Liquid pharmaceutical formulations of palonosetron
US20100048607A1 (en) * 2008-08-25 2010-02-25 Chandrashekhar Kocherlakota Formulations comprising palonosetron
EP2866797B1 (en) * 2012-07-06 2020-04-29 Pharmathen S.A. Stable injectable pharmaceutical composition of neurokinin 1 receptor antagonist and process for preparation thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004067005A1 (en) * 2003-01-30 2004-08-12 Helsinn Healthcare Sa Liquid pharmaceutical formulations of palonosetron
US8426450B1 (en) * 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
"Efficacy and safety of NEPA, an oral combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting following highly emetogenic chemotherapy: a randomized dose-ranging pivotal study";P. J. Hesketh1等;《Annals of Oncology》;20140307;第25卷;第1340–1346页 *
"In vitro and in vivo pharmacological characterization of Pronetupitant,a prodrug of the neurokinin 1 receptor antagonist Netupitant";Chiara Ruzza等;《Peptides》;20150403;第69卷;第26-32页 *
"Phase 3 Safety Study of Intravenous NEPA, a Novel Fixed Antiemetic Combination of Fosnetupitant and Palonosetron in Patients Receiving Highly Emetogenic Chemotherapy";L. Schwartzberg等;《Annals of Oncology》;20181231;第29卷(第7期);第1535-1540页 *
"世界新药之窗";无;《中国新药杂志》;20141231;第23卷(第22期);第2581-2582页 *
"新型化疗止吐药神经激肽-1受体拮抗剂的研究进展";孙秀波等;《中国新药杂志》;20051231;第24卷(第7期);第765-770页 *

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CY1122755T1 (el) 2021-03-12
WO2017211663A1 (en) 2017-12-14
MA44513B1 (fr) 2020-02-28
ECSP19000169A (es) 2019-01-31
EP3435980A1 (en) 2019-02-06
SG11201809708PA (en) 2018-11-29
JP2021183639A (ja) 2021-12-02
EA036605B1 (ru) 2020-11-27
KR20190015276A (ko) 2019-02-13
PH12018502524B1 (en) 2022-04-27
JP2019521102A (ja) 2019-07-25
AR108676A1 (es) 2018-09-12
MD3435980T2 (ro) 2020-03-31
US12208109B2 (en) 2025-01-28
KR102459416B1 (ko) 2022-10-27
UA122285C2 (uk) 2020-10-12
BR112018074655B1 (pt) 2024-02-15
ZA201807932B (en) 2019-08-28
TWI725191B (zh) 2021-04-21
PE20190347A1 (es) 2019-03-07
TW201801727A (zh) 2018-01-16
LT3435980T (lt) 2020-02-25
ES2771226T3 (es) 2020-07-06
US20250235473A1 (en) 2025-07-24
EP3626231A1 (en) 2020-03-25
NZ747865A (en) 2024-05-31
CA3025837C (en) 2024-02-13
US10624911B2 (en) 2020-04-21
US20200206249A1 (en) 2020-07-02
JP6936817B2 (ja) 2021-09-22
EP3435980B1 (en) 2019-11-13
SI3435980T1 (sl) 2020-03-31
CN109310627A (zh) 2019-02-05
PL3435980T3 (pl) 2020-05-18
HRP20200196T1 (hr) 2020-05-01
MX2018015036A (es) 2019-04-11
RS59852B1 (sr) 2020-02-28
PH12018502524A1 (en) 2019-10-14
CO2018011686A2 (es) 2019-02-08
MY194081A (en) 2022-11-11
BR112018074655A2 (pt) 2019-03-06
US20230172953A1 (en) 2023-06-08
DK3435980T3 (da) 2020-02-24
IL263126A (en) 2018-12-31
US11529362B2 (en) 2022-12-20
EA201892837A1 (ru) 2019-06-28
AU2017276588B2 (en) 2022-06-02
CL2018003338A1 (es) 2019-02-22
AU2017276588A1 (en) 2018-11-22
US20170348335A1 (en) 2017-12-07
PT3435980T (pt) 2020-02-21
JOP20170137B1 (ar) 2021-08-17
UY37273A (es) 2018-01-31
JP7223084B2 (ja) 2023-02-15
MX376118B (es) 2025-03-07
IL263126B (en) 2021-04-29
CA3025837A1 (en) 2017-12-14

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