HRP20191707T1 - Depo formulacija hidrogel kompozita - Google Patents

Depo formulacija hidrogel kompozita Download PDF

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Publication number
HRP20191707T1
HRP20191707T1 HRP20191707T HRP20191707T1 HR P20191707 T1 HRP20191707 T1 HR P20191707T1 HR P20191707 T HRP20191707 T HR P20191707T HR P20191707 T1 HRP20191707 T1 HR P20191707T1
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mass
depot formulation
silica
silica particles
nucleotide
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English (en)
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Lasse Leino
Harry Jalonen
Ari-Pekka Forsback
Mika Jokinen
Panu Noppari
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Delsitech Oy
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    • 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
    • A61K9/0024Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A61K31/708Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
    • 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
    • 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
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M5/00Devices for bringing media into the body in a subcutaneous, intra-vascular or intramuscular way; Accessories therefor, e.g. filling or cleaning devices, arm-rests
    • A61M5/178Syringes
    • A61M5/31Details
    • A61M5/32Needles; Details of needles pertaining to their connection with syringe or hub; Accessories for bringing the needle into, or holding the needle on, the body; Devices for protection of needles
    • A61M5/329Needles; Details of needles pertaining to their connection with syringe or hub; Accessories for bringing the needle into, or holding the needle on, the body; Devices for protection of needles characterised by features of the needle shaft

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Dispersion Chemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Biotechnology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Materials For Medical Uses (AREA)

Claims (15)

1. Depo formulacija koja sadrži biorazgradiv silika hidrogel kompozit uključujući nukleotidni ili nukleozidni analog inhibitor reverzne transkriptaze, gdje se silika hidrogel kompozit može dobiti miješanjem a) čestica silike koje sadrže navedeni nukleotidni ili nukleozidni analog inhibitor reverzne transkriptaze i koje imaju maksimalni promjer od ≤ 1 000 µm, kao takvih ili kao suspenzije, sa b) silika solom gdje i) navedeni silika sol ima sadržaj čvrste materije od ≤ 5 mas-%, ii) navedeni silika hidrogel kompozit sadrži do 85 mas-% navedenih silika čestica, i iii) navedeni hidrogel kompozit ne teče i strukturno je stabilan kada se čuva u mirovanju i pseudoplastično teče kada je smicanje primijenjeno ubrizgavanjem.
2. Depo formulacija iz patentnog zahtjeva 1, naznačena time da silika hidrogel kompozit ne teče i strukturno je stabilan hidrogel na 37°C nakon što je smicanje primijenjeno ubrizgavanjem.
3. Depo formulacija iz patentnog zahtjeva 1 ili 2 naznačena time da silika sol ima sadržaj čvrste materije od ≤ 3 mas-%, poželjno ≤ 2 mas-% i najpoželjnije ≤ 1 mas-%.
4. Depo formulacija iz bilo kojeg od prethodnih patentnih zahtjeva naznačena time da silika čestice sadrže od 0.1 do 70 mas-%, poželjno od 0.3 do 50 mas-%, i najpoželjnije od 1 do 15 mas-% inkorporiranog nukleotidnog ili nukleozidnog analoga inhibitora reverzne transkriptaze.
5. Depo formulacija iz bilo kojeg od prethodnih patentnih zahtjeva naznačena time da su silika čestice mikročestice koje imaju promjer između 0.5 µm i 300 µm, poželjno 0.5 µm i 100 µm, poželjnije 0.5 µm i 30 µm i najpoželjnije 0.5 µm i 20 µm.
6. Depo formulacija iz patentnog zahtjeva 5 naznačena time da volumenska frakcija silika čestica koje imaju promjer < 1 µm je < 3 %, poželjno < 2 %, i najpoželjnije < 1 zapreminskog-%.
7. Depo formulacija iz bilo kojeg od prethodnih patentnih zahtjeva naznačena time da hidrogel kompozit sadrži od do 80 mas-%, poželjno 10 do 80 mas-%, najpoželjnije 20 do 60 mas-% silika čestica.
8. Depo formulacija iz bilo kojeg od prethodnih patentnih zahtjeva naznačena time da sadržaj čvrste materije kompozita je od 10 mas-% do 75 mas-%, poželjno od 15 mas-% do 60 mas-% i najpoželjnije od 25 mas-% do 55 mas-%.
9. Depo formulacija iz bilo kojeg od prethodnih patentnih zahtjeva naznačena time da - složeni modul izmjeren pod malim kutom oscilatornog smicanja u linearnom viskoelastičnom regionu je < 2400 kPa, poželjno < 1200 kPa i najpoželjnije < 600 kPa, i/ili - faktor gubitka, tj. viskozni modul/elastični modul, je < 1, poželjno < 0.8 i najpoželjnije < 0.6, i/ili - viskozitet je 10-50 Pas izmjerena stopom smicanja od 10-50 s-1, viskozitet je 0.4-1.5 Pas izmjerena stopom smicanja od 200-210 s-1, i 0.1-0.4 Pas izmjerena stopom smicanja od 600-610 s-1.
10. Depo formulacija iz bilo kojeg od prethodnih patentnih zahtjeva naznačena time da su silika čestice dobivene procesom odabranim od sušenje raspršivanjem, jednostruka emulzija, dvostruka emulzija, polimerizacija, fazno razdvajanje koacervacijom i metode ekstakcije rastvarača, poželjno sušenje raspršivanjem, najpoželjnije sušenje raspršivanjem sa neprekidnim odvajanjem čestica pomoću ciklonskog separatora.
11. Depo formulacija u skladu sa patentnim zahtjevom 10 naznačena time da nukleotidni ili nukleozidni analog inhibitor reverzne transkriptaze, sadržan u česticama silike, je inkorporiran u česticama silike koristeći kontinuirani proces unutar cijevnog reaktora gdje se navedeni nukleotidni ili nukleozidni analog inhibitor reverzne transkriptaze i silika sol kontinuirano dopremaju kao odvojeni tokovi unutar i kombiniraju u navedenom reaktoru, zatim se kontinuirano odvode iz navedenog cijevnog reaktora i u proces kontinuiranog sušenja raspršivanjem sa neprekidnim odvajanjem čestica pomoću ciklonskog separatora.
12. Depo formulacija u skladu sa bilo kojim od prethodnih patentnih zahtjeva naznačena time da nukleotidni ili nukleozidni analog inhibitor reverzne transkriptaze je odabran od grupe koja se sastoji od - dideoksinukleozida, i/ili - zidovudina, didanozina, zalcitabina, stavudina, lamivudin abakavira, emtricitabina, entekavira, tenofovira, adefovira, apricitabina, elvucitabina, amdoksovira i racivira, poželjno entekavira.
13. Depo formulacija u skladu sa bilo kojim od prethodnih patentnih zahtjeva naznačena time da nukleotidni ili nukleozidni analog inhibitor reverzne transkriptaze je analog deoksiguanozina, poželjno odabran iz grupe koja se sastoji od hidroksimetil(metilenciklopentil)purina i pirimidina.
14. Depo formulacija u skladu sa bilo kojim od prethodnih patentnih zahtjeva naznačena time da je odabrana iz grupe koja se sastoji od formulacija koje se mogu ubrizgati i implantabilnih formulacija, poželjno koje se mogu ubrizgati.
15. Depo formulacija u skladu sa bilo kojim od prethodnih patentnih zahtjeva za primjenu u liječenju kroničnih virusnih infekcija i prevenciji kronične virusne reinfekcije poželjno odabrane od grupe infekcija koja se sastoji od hepatitisa B i HIV infekcija, i najpoželjnije grupe koja se sastoji od infekcija hepatitisom B.
HRP20191707 2015-10-22 2019-09-20 Depo formulacija hidrogel kompozita HRP20191707T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FI20155750 2015-10-22
PCT/FI2016/050745 WO2017068245A1 (en) 2015-10-22 2016-10-21 Hydrogel composite depot formulation
EP16794670.6A EP3365020B1 (en) 2015-10-22 2016-10-21 Hydrogel composite depot formulation

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HRP20191707T1 true HRP20191707T1 (hr) 2019-12-13

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US (1) US10172792B2 (hr)
EP (1) EP3365020B1 (hr)
JP (1) JP6905520B2 (hr)
KR (1) KR102228986B1 (hr)
CN (1) CN108367076B (hr)
AU (1) AU2016342470B2 (hr)
BR (1) BR112018006784B1 (hr)
CA (1) CA3001752C (hr)
DK (1) DK3365020T3 (hr)
ES (1) ES2748032T3 (hr)
HR (1) HRP20191707T1 (hr)
HU (1) HUE046419T2 (hr)
LT (1) LT3365020T (hr)
MX (1) MX2018004797A (hr)
PL (1) PL3365020T3 (hr)
PT (1) PT3365020T (hr)
WO (1) WO2017068245A1 (hr)
ZA (1) ZA201802040B (hr)

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JP2023532778A (ja) 2020-07-07 2023-07-31 デルシテック オサケユイチア シリカハイドロゲルコンポジットおよびその使用
CA3214619A1 (en) * 2021-04-07 2022-10-13 Martin P. Redmon Silica-based formulations of therapeutic oliogpeptides and peptidomimetics
WO2024047230A1 (en) 2022-09-01 2024-03-07 Optifye Therapeutics Ag Ophthalmic compositions

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JP4322315B2 (ja) 1996-05-29 2009-08-26 デルシテク オサケ ユキチュア 生物学的適用のための溶解性酸化物
CN101541939A (zh) * 2006-11-22 2009-09-23 阿普尔顿纸张公司 含有益剂的递送颗粒
CN101444503B (zh) * 2008-12-31 2011-02-02 江苏大学 一种水飞蓟宾高效长效制剂及其制法
US8974709B2 (en) * 2010-06-25 2015-03-10 Colabs Intl Corp Ceramic encapsulation with controlled layering by use of prehydrolyzed functionalized silanes
US9579283B2 (en) * 2011-04-28 2017-02-28 Stc.Unm Porous nanoparticle-supported lipid bilayers (protocells) for targeted delivery and methods of using same
KR101594820B1 (ko) 2011-06-16 2016-02-17 건일제약 주식회사 엔테카비르를 함유하는 미립구 및 이의 제조방법
ITTO20111242A1 (it) * 2011-12-30 2013-07-01 Miso S R L Composizioni per il trattamento di patologie delle mucose
DK3013317T3 (da) 2013-06-24 2020-02-17 Delsitech Oy Silicahydrogelkomposit
JP2016527308A (ja) 2013-08-06 2016-09-08 ドン クック ファーマシューティカル カンパニー リミテッド エンテカビル微小球及びこれを含む非経口投与用医薬組成物

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JP6905520B2 (ja) 2021-07-21
CA3001752A1 (en) 2017-04-27
AU2016342470B2 (en) 2019-03-21
ES2748032T3 (es) 2020-03-12
AU2016342470A1 (en) 2018-04-12
US10172792B2 (en) 2019-01-08
WO2017068245A1 (en) 2017-04-27
PT3365020T (pt) 2019-10-24
US20180311150A1 (en) 2018-11-01
PL3365020T3 (pl) 2020-03-31
EP3365020A1 (en) 2018-08-29
HUE046419T2 (hu) 2020-02-28
EP3365020B1 (en) 2019-07-17
BR112018006784B1 (pt) 2023-10-03
DK3365020T3 (da) 2019-10-07
MX2018004797A (es) 2018-09-06
KR102228986B1 (ko) 2021-03-18
CA3001752C (en) 2021-10-05
BR112018006784A2 (pt) 2018-10-16
CN108367076A (zh) 2018-08-03
LT3365020T (lt) 2019-10-25
ZA201802040B (en) 2019-07-31
CN108367076B (zh) 2021-08-31
JP2018531270A (ja) 2018-10-25
KR20180071253A (ko) 2018-06-27

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