FI117122B - Förfarande för framställning av biodegraderbara och biokompatibla mikropartiklar, vilka innehåller en 1,2 -bensazol som aktivt ämne - Google Patents

Förfarande för framställning av biodegraderbara och biokompatibla mikropartiklar, vilka innehåller en 1,2 -bensazol som aktivt ämne Download PDF

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Publication number
FI117122B
FI117122B FI962111A FI962111A FI117122B FI 117122 B FI117122 B FI 117122B FI 962111 A FI962111 A FI 962111A FI 962111 A FI962111 A FI 962111A FI 117122 B FI117122 B FI 117122B
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FI
Finland
Prior art keywords
poly
microparticles
process according
hydrogen
alkyl
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Application number
FI962111A
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English (en)
Finnish (fi)
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FI962111A0 (sv
FI962111A (sv
Inventor
Jean Louis Mesens
Michael E Rickey
Thomas J Atkins
Original Assignee
Janssen Pharmaceutica Nv
Alkermes Inc
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Application filed by Janssen Pharmaceutica Nv, Alkermes Inc filed Critical Janssen Pharmaceutica Nv
Publication of FI962111A0 publication Critical patent/FI962111A0/sv
Publication of FI962111A publication Critical patent/FI962111A/sv
Application granted granted Critical
Publication of FI117122B publication Critical patent/FI117122B/sv

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicinal Preparation (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (10)

1. Förfarande för framställning av biodegr och biokompatibla mikropartiklar, vilka innehäller 5 tivt ämne en 1,2-bensazol med formeln O eller ett farmaceutiskt godtagbart syraad 10 sait därav, där R är väte eller Ci-6-alkyl; R1 och R2 oberoende av varandra är väte, hydroxi, Ci-6-alkoxi eller Ci_6-alkyl; X är 0 eller S;
15 AI k är Ci_4-alkandiyl; ,och R3 är väte eller Ci-6~a-lkyl; Z är -S-, -CH2- eller -CR4=CR5-; där R4 och ^ e roende av varandra är väte eller Ci-6-alkyl;
4 A är en bivalent radikal -CH2-CH2-, -CH2 20 eller CR6=CR7-; där R6 och R7 är väte, halogen, ami Ci-e-alkyl; och ·/«: R8 är väte eller hydroxyl, : och som är kapabla att frisätta nämnda akt »M ;4!*; eller ett sait därav för en förlängd tid, k ä 25 tecknat av att förfarandet omfattar följand # a) ett polymermatrismaterial, som har en vikt pä 100000 - 300000, upplöses i ett organi; » 1 c) den frän steg b) erhällna dispersionen en släckningsvätska; d) mikropartiklarna isoleras; och e) mikropartiklarna torkas. 5 2. Förfarande enligt patentkrav 1, k ä tecknat av att polymermatrismaterialet mikropartikel är poly(glykolsyra), poly-DL-mjölksyr L-mjölksyra, kopolymerer av de föregäende, poly(ai karboxylsyror), kopolyoxalater, polykaprolakton, p 10 onon, poly(ortokarbonater), poly(acetaler), poly(mj kaprolakton), polyortoestrar, poly(glykolsyra-kaprc polyanhydrider, albumin, kasein eller vaxer.
3. Förfarande enligt patentkrav 2, k ä tecknat av att polymermatrismaterialet a^ 15 mikropartikel är en kopolymer av poly(glykolsyra) c DL-mjölksyra.
4. Förfarande enligt patentkrav 3, k ä tecknat av att molförhällandet av laktic glykoliden ligger inom omrädet 85:15-50:50. 20 5. Förfarande enligt nägot av patentkraver kännetecknat av att nämnda mikroparti ···· fattar 1-90 vikt-% av nämnda 1, 2-bensazol. ... : 6. Förfarande enligt nägot av patentkraver kännetecknat av att nämnda mikroparti β·β · 25 nehäller ca 35 - 40 vikt-% av nämnda 1,2-bensazol. • . ·
7. Förfarande enligt nägot av patentkraver Hl kännetecknat av att storleken av nämnd • * · partiklar ligger inom omrädet 1 - 500 pm.
8. Förfarande enligt nägot av patentkraver 30 kännetecknat av att storleken av nämnd 2 oartiklar liacrer inom omrädet 25 - 180 um. 27 1 1
10. Förfarande enligt nagot av patentkrave kännetecknat av att den förlängda per 30 - 60 dagar.
11. Förfarande enligt nagot av patentkraver 5 kännetecknat av att det aktiva ämnet ä ridon. * * · • * 9 9 * 1 • · ♦ · · • 1 · * « * · · • · # »·» «1· * 1 « * · · • a a • · « >«i « • · • Λ m
FI962111A 1993-11-19 1996-05-17 Förfarande för framställning av biodegraderbara och biokompatibla mikropartiklar, vilka innehåller en 1,2 -bensazol som aktivt ämne FI117122B (sv)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US15440393A 1993-11-19 1993-11-19
US15440393 1993-11-19
EP9403754 1994-11-11
PCT/EP1994/003754 WO1995013814A1 (en) 1993-11-19 1994-11-11 Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles

Publications (3)

Publication Number Publication Date
FI962111A0 FI962111A0 (sv) 1996-05-17
FI962111A FI962111A (sv) 1996-05-17
FI117122B true FI117122B (sv) 2006-06-30

Family

ID=22551225

Family Applications (1)

Application Number Title Priority Date Filing Date
FI962111A FI117122B (sv) 1993-11-19 1996-05-17 Förfarande för framställning av biodegraderbara och biokompatibla mikropartiklar, vilka innehåller en 1,2 -bensazol som aktivt ämne

Country Status (30)

Country Link
US (11) US5688801A (sv)
EP (1) EP0729357B1 (sv)
JP (1) JP3645906B2 (sv)
KR (1) KR100354270B1 (sv)
CN (1) CN1074923C (sv)
AT (1) ATE288270T1 (sv)
AU (1) AU694147B2 (sv)
BG (1) BG63246B1 (sv)
CL (1) CL2004001182A1 (sv)
CZ (1) CZ293764B6 (sv)
DE (1) DE69434258T2 (sv)
DK (1) DK0729357T3 (sv)
ES (1) ES2236700T3 (sv)
FI (1) FI117122B (sv)
HK (1) HK1010694A1 (sv)
HU (1) HU219487B (sv)
IL (1) IL111647A (sv)
MX (1) MX9408969A (sv)
MY (1) MY113298A (sv)
NO (1) NO309226B1 (sv)
NZ (1) NZ276088A (sv)
PL (1) PL314481A1 (sv)
PT (1) PT729357E (sv)
RO (1) RO119224B1 (sv)
RU (1) RU2178695C2 (sv)
SG (1) SG47445A1 (sv)
SI (1) SI0729357T1 (sv)
SK (1) SK282231B6 (sv)
WO (1) WO1995013814A1 (sv)
ZA (1) ZA949191B (sv)

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US20020098233A1 (en) 2002-07-25
AU694147B2 (en) 1998-07-16
US6368632B1 (en) 2002-04-09
BG100632A (bg) 1997-03-31
NO309226B1 (no) 2001-01-02
HU219487B (hu) 2001-04-28
IL111647A (en) 1999-12-22
JPH09505286A (ja) 1997-05-27
US6803055B2 (en) 2004-10-12
HK1010694A1 (en) 1999-06-25
IL111647A0 (en) 1995-01-24
CL2004001182A1 (es) 2005-06-03
US20050025828A1 (en) 2005-02-03
PT729357E (pt) 2005-06-30
NZ276088A (en) 1999-07-29
ES2236700T3 (es) 2005-07-16
DE69434258D1 (de) 2005-03-10

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