HRP20220180T1 - Liposomska otopina kapi za oči i njihova uporaba za liječenje sindroma suhog oka - Google Patents

Liposomska otopina kapi za oči i njihova uporaba za liječenje sindroma suhog oka Download PDF

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HRP20220180T1
HRP20220180T1 HRP20220180TT HRP20220180T HRP20220180T1 HR P20220180 T1 HRP20220180 T1 HR P20220180T1 HR P20220180T T HRP20220180T T HR P20220180TT HR P20220180 T HRP20220180 T HR P20220180T HR P20220180 T1 HRP20220180 T1 HR P20220180T1
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Croatia
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vitamin
solution
liposomes
eye
eye drop
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HRP20220180TT
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English (en)
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Rolf Lambert
Giovanni Cavallo
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Dr. Rolf Lambert Pharma-Consulting Gmbh
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Publication of HRP20220180T1 publication Critical patent/HRP20220180T1/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
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
    • A61K31/232Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
    • 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
    • A61K31/352Heterocyclic 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 condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355Tocopherols, e.g. vitamin E
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/683Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • 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
    • A61K31/7135Compounds containing heavy metals
    • A61K31/714Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12
    • 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
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728Hyaluronic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/55Linaceae (Flax family), e.g. Linum
    • 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
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/127Liposomes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/04Artificial tears; Irrigation solutions
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Engineering & Computer Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Dispersion Chemistry (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medical Preparation Storing Or Oral Administration Devices (AREA)
  • Medicines Containing Plant Substances (AREA)

Claims (10)

1. Otopina kapi za oči za uporabu u liječenju sindroma suhog oka, naznačena time, da sadrži liposomsku strukturu s ne-hidrogeniranim fosfolipidima koji sadrže laneno ulje, vitamin A palmitat, vitamin E TPGS, i u vodenoj fazi, vitamin B12 i piknogenole.
2. Otopina kapi za oči prema patentnom zahtjevu 1, naznačena time, da liposomska otopina kapi za oči nadalje sadrži sustav koji čini 2-amino-2(hidroksimetil)-propan-1,3-diol, koji djeluje kao sredstvo za tvorbu soli piknogenola, topive u gaziranoj vodi, i puferski regulator pH.
3. Otopina kapi za oči prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time, da se sterilizira filtracijom kroz 0,2 μm, budući da sterilizacija parom koja se postiže izlaganjem navedene otopine zasićenoj pari pri visokim temperaturama od 121°C tijekom 15 minuta na 1x105 Pa (1 Atm), uništava sve liposomske komponente.
4. Otopina kapi za oči prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time, da liposomske kapi za oči predstavljaju zaštitu protiv UVA UVB zraka (UVA 315-400 nm – UVB 315-280), gdje je ovo svojstvo povezano primarno s liposomima (plus Vitamin E TPGS) i sekundarno s vitaminom B12 i piknogenolima u vodenoj fazi.
5. Otopina kapi za oči prema bilo kojem od patentnih zahtjeva 2-4, naznačena time, da ima slijedeći sastav: Sastojci % težina/težina Fosfolipid S80 0,250/0,750 Laneno ulje 0,025/0,075 Vitamin A palmitat 0,005/0,015 Vitamin E TPGS unutar liposoma 0,0125/0,0375 Piknogenol 0,0085/0,0255 Tris (2-amino-2(hidroksimetil)propan-1,3-diol 0,3-0,2/0,4-0,3 Vitamin B12 0,00175/0,00525 Sol hijaluronske kiseline (1,5-1,7 MDa) izvan liposoma 0,0750/0,225 Borna kiselina 0,775 Natrij tetraborat dekahidrat 0,0600 Natrij klorid 0,2-0,15 Destilirana voda 100 Sterilizacija filtracijom kroz 0,2 μm (0,2 mikrona) Da pH 7,1-7,4 Osmolalnost mMOs/kg 275-290
6. Otopina za oči prema patentnom zahtjevu 5, naznačena time, da ima slijedeći sastav: Sastojci % težina/težina Fosfolipid S80 0,500 Laneno ulje 0,050 Vitamin A palmitat 0,010 Piknogenol 0,017 Tris (2-amino-2(hidroksimetil)propan-1,3-diol 0,3-0,2 Vitamin B12 0,0035 Sol hijaluronske kiseline (1,5-1,7 MDa) izvan liposoma 0,150 Vitamin E TPGS unutar liposoma 0,025 Borna kiselina 0,775 Natrij tetraborat dekahidrat 0,060 Natrij klorid 0,2-0,15 Destilirana voda 100 Sterilizacija filtracijom kroz 0,2 μm (0,2 mikrona) Da pH 7,1-7,4 Osmolalnost mMOs/kg 275-290
7. Postupak za pripravu otopine za oči za uporabu u liječenju sindroma suhog oka, naznačen time, da obuhvaća slijedeće korake: Prvi korak: Priprava liposoma koji nose lipofilne supstance: - otope se svi lipofilni sastojci, ne-hidrogenirani fosfolipidi, laneno ulje, vitamin A palmitata plus vitamin E TPGS u otapalu, često etanolu, - otapalo se uklanja pod vakuumom kako bi se dobio suhi prah, - prah se disperzira u boratnom puferu i miješa mehaničkim mikserom, dobije se otopina velikih liposoma, koja se može definirati kao pro liposomi; - otopina ovakvih velikih liposoma se tada istiskuje pod visokim tlakom, između 600/1000 bar; - postupak istiskivanja pod visokim tlakom se ponavlja nekoliko puta ,između 4 i 7, kako bi se dobili liposomi veličine manje od 200 nm; Drugi korak: Priprava vodene otopine koja sadrži hidrofilne supstance - u destiliranoj se vodi otope piknogenoli, Tris, vitamin B12, hijaluronska kiselina i boratni pufer; gdje je koncentracija lipofilnih supstanci u prvom koraku i koncentracija hidrofilnih supstanci u drugom koraku takva da dopušta, kad se doda svaka u omjeru 1:1, da se dobije otopina željene koncentracije; - dobije se bistra i crveno obojena otopina; Treći korak: Priprava finalnih sterilnih kapi za oči: Količina „X“ liposomske otopine, pripravljena u prvom koraku, doda se istoj količini „X“ vodene obojene otopine, pripravljene u drugom koraku, dobivši količinu „2X“ finalne standardne otopine kapi za oči formule prema patentnom zahtjevu 5, i finalna se standardna otopina kapi za oči sterilizira filtracijom kroz 0,2 μm (0,2 mikron) filter.
8. Otopina kapi za oči prema bilo kojem od patentnih zahtjeva 4 i 5 za uporabu u liječenju sindroma suhog oka, naznačena time, da se koristi kao zaštita protiv UVA/UVB zraka.
9. Otopina kapi za oči prema bilo kojem od prethodnih patentnih zahtjeva 1-6 za uporabu u liječenju sindroma suhog oka, naznačena time, da je namjera smanjenje negativnog učinka sindroma suhog oka.
10. Otopina kapi za oči dobivene postupkom prema patentnom zahtjevu 7 za uporabu u liječenju sindroma suhog oka, naznačena time, da je se koristi kao zaštita protiv UVA/UVB zraka.
HRP20220180TT 2018-12-28 2018-12-28 Liposomska otopina kapi za oči i njihova uporaba za liječenje sindroma suhog oka HRP20220180T1 (hr)

Applications Claiming Priority (1)

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EP18425109.8A EP3673896B9 (en) 2018-12-28 2018-12-28 Liposomial eye drops solution and uses thereof for the treatment of dry eye syndrome

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EP (1) EP3673896B9 (hr)
JP (1) JP7280638B2 (hr)
KR (1) KR102493604B1 (hr)
CN (1) CN112804990B (hr)
AU (1) AU2019412448B2 (hr)
CA (1) CA3124727C (hr)
DK (1) DK3673896T3 (hr)
ES (1) ES2910121T3 (hr)
HR (1) HRP20220180T1 (hr)
IL (1) IL284454B2 (hr)
PH (1) PH12021551094A1 (hr)
PL (1) PL3673896T3 (hr)
PT (1) PT3673896T (hr)
SG (1) SG11202105666WA (hr)
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CN111671722A (zh) * 2020-07-30 2020-09-18 成都大学 一种滴眼液及其制备方法

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PT3673896T (pt) 2022-02-03
CN112804990B (zh) 2024-05-24
SG11202105666WA (en) 2021-07-29
KR102493604B1 (ko) 2023-01-31
CA3124727A1 (en) 2020-07-02
EP3673896B9 (en) 2022-05-18
EP3673896B1 (en) 2022-01-12
AU2019412448B2 (en) 2023-04-20
US20220304970A1 (en) 2022-09-29
AU2019412448A1 (en) 2021-08-12
CN112804990A (zh) 2021-05-14
CA3124727C (en) 2023-10-31
EP3673896A1 (en) 2020-07-01
JP7280638B2 (ja) 2023-05-24
PH12021551094A1 (en) 2021-11-22
IL284454A (en) 2021-08-31
PL3673896T3 (pl) 2022-06-27
KR20210110653A (ko) 2021-09-08
DK3673896T3 (da) 2022-02-07
WO2020135940A1 (en) 2020-07-02
JP2022514809A (ja) 2022-02-16
IL284454B1 (en) 2024-04-01
ZA202104891B (en) 2022-07-27
ES2910121T3 (es) 2022-05-11
IL284454B2 (en) 2024-08-01

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