HRP20161444T1 - Farmaceutski pripravci koji sadrže lokalni anestetik kao što je bupivakain za lokalnu primjenu u usta ili grlo - Google Patents

Farmaceutski pripravci koji sadrže lokalni anestetik kao što je bupivakain za lokalnu primjenu u usta ili grlo Download PDF

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Publication number
HRP20161444T1
HRP20161444T1 HRP20161444TT HRP20161444T HRP20161444T1 HR P20161444 T1 HRP20161444 T1 HR P20161444T1 HR P20161444T T HRP20161444T T HR P20161444TT HR P20161444 T HRP20161444 T HR P20161444T HR P20161444 T1 HRP20161444 T1 HR P20161444T1
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Croatia
Prior art keywords
minutes
sustained
use according
preparation
pharmaceutically active
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HRP20161444TT
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English (en)
Inventor
Ove Andersen
Stine MOGENSEN
Charlotte TRELDAL
Torben Mogensen
Sylvia PULIS
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Moberg Pharma Ab
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Publication of HRP20161444T1 publication Critical patent/HRP20161444T1/hr

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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
    • A61K31/33Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • A61P23/02Local anaesthetics

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Zoology (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (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)

Claims (13)

1. Pripravak s produljenim oslobađanjem koji sadrži kao lokalni anestetik amidni spoj koji ima vrijednost koeficijenta raspodjele oktanol/voda od barem 100, ili njegovu sol, formuliran za lokalnu primjenu u usta ili grlo subjekta u obliku pastile za uporabu za liječenje oralnog mukozitisa kod subjekta koji je podvrgnut liječenju raka.
2. Pripravak s produljenim oslobađanjem prema zahtjevu 1 naznačen time da spoj ima vrijednost koeficijenta raspodjele oktanol/voda od barem 300.
3. Pripravak s produljenim oslobađanjem prema zahtjevu 1 naznačen time da spoj je bupivakain, ropivakain, etidokain ili levobupivakain ili farmaceutski aktivna sol bilo kojeg od tih spojeva, kao što je hidroklorid.
4. Pripravak s produljenim oslobađanjem za uporabu prema zahtjevu 1, naznačen time da spoj je bupivakain ili farmaceutski aktivna sol navedenog spoja, kao što je hidroklorid.
5. Pripravak s produljenim oslobađanjem za uporabu prema bilo kojem od prethodnih zahtjeva, naznačen time da je lokalni anestetik ili njegova farmaceutski aktivna sol prisutan u količini od 0.1 do 75 mg, poželjno 0.1 do 50 mg, na primjer 5 mg, 10 mg, 25 mg ili 50 mg, po oralnom obliku doziranja.
6. Pripravak s produljenim oslobađanjem za uporabu prema bilo kojem od prethodnih zahtjeva naznačen time da je formuliran da osigura produljeno oslobađanje lokalnog anestetika ili njegove farmaceutski aktivne soli kroz vremenski period od barem 20 minuta, na primjer barem 60 minuta, na primjer od oko 70 minuta, kao što je do oko 80 minuta, na primjer do oko 90 minuta, kao što je do oko 100 minuta, na primjer do oko 2 sata, kao što je do oko 3 sata, na primjer do oko 4 sata, kao što je do oko 5 sati, na primjer do oko 6 sati.
7. Pripravak s produljenim oslobađanjem za uporabu prema bilo kojem od prethodnih zahtjeva naznačen time da je vršna koncentracija u krvi kod čovjeka, poslije oralne primjene pripravka na čovjeka i zadržavanja pripravka u usnoj šupljini čovjeka sve do potpunog otapanja pripravka, u prosjeku od 15 do 45 minuta, poželjno 25 do 35 minuta, poželjnije oko 30 minuta, poslije navedenog otapanja.
8. Pripravak s produljenim oslobađanjem za uporabu prema bilo kojem od prethodnih zahtjeva, naznačen time da je pripravak u obliku koji je odabran iz skupine koju čine praškaste pastile, sirupaste pastile i granulirane pastile, pastile sa aplikatorom/lizalice.
9. Pripravak s produljenim oslobađanjem za uporabu prema bilo kojem od prethodnih zahtjeva, naznačen time da lokalni anestetik ili njegova farmaceutski aktivna sol je jedini aktivni sastojak.
10. Pripravak s produljenim oslobađanjem za uporabu prema bilo kojem od zahtjeva 1 do 9, naznačen time da dodatno sadrži drugi aktivni sastojak koji je odabran iz skupine koju čine antimikrobna sredstva kao što su antivirusna sredstva, antimikotička sredstva i antibiotici; protuupalna sredstva, biološka sredstva, kemoterapijska/protutumorska sredstva, pripravci za kašalj i prehladu uključujući ali nije ograničeno na sredstva protiv kašlja, ekspektoranse, dekongestive, spojeve koji otpuštaju fluorid i druge proizvode za zubnu higijenu, sredstva za stimulaciju stvaranja sline, druga anestetička sredstva i antiemetike.
11. Pripravak s produljenim oslobađanjem za uporabu prema bilo kojem od zahtjeva naznačen time da sadrži 0.1- 5% (w/w) lokalnog anestetika ili njegovu farmaceutski aktivnu sol, 70 - 85 % (w/w) punila ili vezivnog sredstva, 0 -10% (w/w) sredstva za poboljšanje klizivosti ili lubrikanta, 0.5 - 5 % (w/w) zaslađivača koji nije na bazi šećera i 5 - 20 % (w/w) arome.
12. Pripravak s produljenim oslobađanjem za uporabu prema bilo kojem od zahtjeva 1 do 10 naznačen time da sadrži 0.01- 5 % (w/w) lokalnog anestetika ili njegovu farmaceutski aktivnu sol, 70 - 95 % (w/w) baze, 3 - 20 % (w/w) arome.
13. Pripravak za uporabu prema bilo kojem od prethodnih zahtjeva, naznačen time da tretman dovodi do smanjenja ozbiljnosti simptoma koji odgovaraju smanjenju vrijednosti kada je mjerena u skladu s VAS vrijenosti od barem 15% unutar 10 minuta od početka tretmana i/ili barem 20% poslije 30 minuta tretmana i/ili barem 30% 1 sat nakon početka tretmana.
HRP20161444TT 2011-04-29 2016-11-02 Farmaceutski pripravci koji sadrže lokalni anestetik kao što je bupivakain za lokalnu primjenu u usta ili grlo HRP20161444T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DKPA201170213 2011-04-29
DKPA201170225 2011-05-06
PCT/EP2012/057864 WO2012146763A1 (en) 2011-04-29 2012-04-27 Pharmaceutical compositions comprising a local anaesthetic such as bupivacaine for local administration to the mouth or throat
EP12719345.6A EP2701681B1 (en) 2011-04-29 2012-04-27 Pharmaceutical compositions comprising a local anaesthetic such as bupivacaine for local administration to the mouth or throat

Publications (1)

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HRP20161444T1 true HRP20161444T1 (hr) 2016-12-16

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HRP20161444TT HRP20161444T1 (hr) 2011-04-29 2016-11-02 Farmaceutski pripravci koji sadrže lokalni anestetik kao što je bupivakain za lokalnu primjenu u usta ili grlo
HRP20210487TT HRP20210487T1 (hr) 2011-04-29 2021-03-25 Farmaceutski sastavi koji sadrže lokalni anestetik kao što je bupivakain za lokalnu primjenu u usta ili grlo

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Country Status (15)

Country Link
US (2) US9956211B2 (hr)
EP (3) EP3284459B1 (hr)
CA (2) CA2972211C (hr)
CY (2) CY1118474T1 (hr)
DK (2) DK2701681T3 (hr)
ES (2) ES2605814T3 (hr)
HR (2) HRP20161444T1 (hr)
HU (2) HUE030921T2 (hr)
LT (2) LT2701681T (hr)
PL (2) PL2701681T3 (hr)
PT (2) PT2701681T (hr)
RS (2) RS55372B1 (hr)
SI (2) SI2701681T1 (hr)
SM (1) SMT201700010B (hr)
WO (1) WO2012146763A1 (hr)

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DE102009005865A1 (de) 2009-01-07 2010-07-08 Klosterfrau Berlin Gmbh Dosiereinheit und Zusammensetzung zur Behandlung von entzündlichen Erkrankungen des Mund- und Rachenraums
US20100297265A1 (en) 2009-05-20 2010-11-25 Mckinney Jeffrey A Optimal compositions and methods for treating oral disease and pain
DK2701681T3 (en) * 2011-04-29 2017-01-09 Moberg Pharma Ab PHARMACEUTICAL COMPOSITIONS COMPRISING A LOCAL ANESTHETICS as bupivacaine for local administration to the mouth or throat

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CA2860373C (en) 2017-08-15
US10493068B2 (en) 2019-12-03
HUE030921T2 (en) 2017-06-28
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HRP20210487T1 (hr) 2021-05-14
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CA2972211C (en) 2019-02-05
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