AR123691A1 - Formulaciones farmacéuticas - Google Patents

Formulaciones farmacéuticas

Info

Publication number
AR123691A1
AR123691A1 ARP210102751A ARP210102751A AR123691A1 AR 123691 A1 AR123691 A1 AR 123691A1 AR P210102751 A ARP210102751 A AR P210102751A AR P210102751 A ARP210102751 A AR P210102751A AR 123691 A1 AR123691 A1 AR 123691A1
Authority
AR
Argentina
Prior art keywords
geometric mean
tablet
cmáx
bexagliflozin
tmáx
Prior art date
Application number
ARP210102751A
Other languages
English (en)
Inventor
Feng Wang
Ankit Shrivastava
Rina Shah
Brian Seed
Vinay Patil
Michael J Hadd
fuxia Dong
Vipan Dhall
Chunfeng Dai
Joseph Ho Chau
- Cai Qiuhua Lun
Original Assignee
Theracos Sub Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Theracos Sub Llc filed Critical Theracos Sub Llc
Publication of AR123691A1 publication Critical patent/AR123691A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0065Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0002Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007Effervescent
    • 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
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1611Inorganic compounds
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/501Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5015Organic compounds, e.g. fats, sugars
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5026Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (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)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

El perfil farmacocinético del inhibidor del SGLT2 bexagliflozina puede mejorarse si este se formula como comprimido de liberación extendida. En comparación con las formas farmacéuticas estándares de liberación inmediata, estos comprimidos pueden permitir una concentración plasmática máxima, Cₘáˣ, más baja y seguir manteniendo concentraciones plasmáticas a niveles terapéuticos durante un periodo deseado. Esto puede usarse, por ejemplo, para administrar dosis más bajas y seguir proporcionando el mismo efecto farmacológico. Reivindicación 1: Un comprimido de liberación extendida caracterizado porque comprende bexagliflozina. Reivindicación 45: Un comprimido, por ejemplo, un comprimido de cualquier reivindicación precedente, caracterizado porque comprende: bexagliflozina; dibehenato de glicerilo; óxido de polietileno; lactosa; poloxámero 188; celulosa microcristalina; dióxido de silicio coloidal; y estearato de magnesio; y opcionalmente tiene un recubrimiento que comprende alcohol polivinílico. Reivindicación 53: Una forma farmacéutica oral sólida caracterizada porque contiene bexagliflozina y que proporciona una primera Cₘáˣ plasmática media geométrica, una primera AUC₀₋ₜ media geométrica y un primer Tₘáˣ mediano en sujetos en ayuno, y proporciona una segunda Cₘáˣ plasmática media geométrica, una segunda AUC₀₋ₜ media geométrica y un segundo Tₘáˣ mediano en sujetos alimentados, donde (I) la relación de la segunda dividida por la primera Cₘáˣ media geométrica está entre 0,8 y 1.8; (II) la relación de la segunda dividida por la primera AUC₀₋ₜ media geométrica está entre 0,8 y 1,8; o (III) la relación del segundo dividido por el primer Tₘáˣ mediano está entre 0,8 y 3,0. Reivindicación 56: Un método para tratar a un sujeto que sufre de diabetes o sus síntomas, caracterizado porque comprende un paso de administrar al sujeto el comprimido de una cualquiera de las reivindicaciones 1 - 46, 51 - 52, ó 55.
ARP210102751A 2020-10-05 2021-10-05 Formulaciones farmacéuticas AR123691A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2020/119816 WO2022073151A1 (en) 2020-10-05 2020-10-05 Pharmaceutical formulations

Publications (1)

Publication Number Publication Date
AR123691A1 true AR123691A1 (es) 2023-01-04

Family

ID=78463953

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP210102751A AR123691A1 (es) 2020-10-05 2021-10-05 Formulaciones farmacéuticas

Country Status (12)

Country Link
US (2) US20220117898A1 (es)
EP (1) EP4225273A1 (es)
JP (1) JP2023544412A (es)
KR (1) KR20230080461A (es)
CN (1) CN116600791A (es)
AR (1) AR123691A1 (es)
AU (1) AU2021357691A1 (es)
CA (1) CA3197660A1 (es)
IL (1) IL301808A (es)
MX (1) MX2023003758A (es)
TW (1) TW202228721A (es)
WO (2) WO2022073151A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023220930A1 (en) * 2022-05-17 2023-11-23 Increvet, Inc. Veterinary pharmaceutical formulations cross-references to related applications
CN115598262B (zh) * 2022-11-24 2023-03-03 则正(济南)生物科技有限公司 一种双氯芬酸钠缓释片体内外相关性评价的方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9149433B2 (en) 2004-11-30 2015-10-06 Basf Corporation Method for formation of micro-prilled polymers
BRPI0917196B8 (pt) 2008-08-22 2021-05-25 Theracos Sub Llc forma cristalina de um composto sendo complexo de (2s,3r,4r,5s,6r)- 2- (4- cloro- 3- (4- (2- ciclopropoxietóxi) benzil)fenil)- 6- (hidroximetil) tetraidro- 2h- piran- 3,4,5- triol, bis(l-prolina)
WO2011153712A1 (en) 2010-06-12 2011-12-15 Theracos, Inc. Crystalline form of benzylbenzene sglt2 inhibitor
CA3023278C (en) * 2016-05-05 2019-04-30 Triastek, Inc. Controlled release dosage form
CN108239055B (zh) * 2016-12-23 2023-07-18 杭州领业医药科技有限公司 一种thr1442 l-天冬氨酸共晶、其制备方法及药物组合物
WO2018167589A1 (en) 2017-03-16 2018-09-20 Inventia Healthcare Private Limited Pharmaceutical composition comprising dapagliflozin
KR102647171B1 (ko) * 2018-02-02 2024-03-15 노보 노르디스크 에이/에스 Glp-1 작용제 및 n-(8-(2-하이드록시벤조일)아미노)카프릴산의 염을 포함하는 고형 조성물
US20190343853A1 (en) * 2018-04-25 2019-11-14 Theracos Sub, Llc Methods of treating hypertension
US20200289457A1 (en) * 2019-03-14 2020-09-17 Increvet, Inc. Compound for the management of feline diabetes

Also Published As

Publication number Publication date
WO2022073151A1 (en) 2022-04-14
US20240139109A1 (en) 2024-05-02
CA3197660A1 (en) 2022-04-14
WO2022076328A1 (en) 2022-04-14
MX2023003758A (es) 2023-05-10
EP4225273A1 (en) 2023-08-16
KR20230080461A (ko) 2023-06-07
IL301808A (en) 2023-05-01
AU2021357691A1 (en) 2023-06-08
US20220117898A1 (en) 2022-04-21
AU2021357691A9 (en) 2024-08-01
JP2023544412A (ja) 2023-10-23
TW202228721A (zh) 2022-08-01
CN116600791A (zh) 2023-08-15

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