HUP0302631A2 - Stavudint tartalmazó elnyújtott hatóanyag-kibocsátású szemcsék - Google Patents

Stavudint tartalmazó elnyújtott hatóanyag-kibocsátású szemcsék

Info

Publication number
HUP0302631A2
HUP0302631A2 HU0302631A HUP0302631A HUP0302631A2 HU P0302631 A2 HUP0302631 A2 HU P0302631A2 HU 0302631 A HU0302631 A HU 0302631A HU P0302631 A HUP0302631 A HU P0302631A HU P0302631 A2 HUP0302631 A2 HU P0302631A2
Authority
HU
Hungary
Prior art keywords
stavudine
granules
coating
extruded
spheronized
Prior art date
Application number
HU0302631A
Other languages
English (en)
Inventor
Rober Abramowitz
Nemichand B. Jain
Denise M. O'donoghue
Original Assignee
Bristol-Myers Squibb Co.
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 Bristol-Myers Squibb Co. filed Critical Bristol-Myers Squibb Co.
Publication of HUP0302631A2 publication Critical patent/HUP0302631A2/hu

Links

Classifications

    • 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
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7068—Compounds 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
    • A61K31/7072—Compounds 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
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7076—Compounds 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
    • 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
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules 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
    • A61K9/5073—Microcapsules 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 having two or more different coatings optionally including drug-containing subcoatings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Biophysics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

A találmány tárgyát stavudint tartalmazó olyan elnyújtotthatóanyagkibocsátású, extrudált-szferonizált, záróbevonattal ésmódosított hatóanyagkibocsátású bevonattal ellátott szemcsék képezik,amelyek a stavudin hatásos vérszintjét körülbelül 24 órán átbiztosítják. A stavudinnak az extrúziós-szferonizációs eljáráshozszükséges korlátozott mennyiségű víz hatására létrejöhetőhidrolíziséből származó bomlása megakadályozására a szemcsék astavudin jelenlévő tömegére vonatkoztatott körülbelül 0,5 és 3,0tömeg% közötti mennyiségű magnézium-sztearátot, továbbá egyszferonizáló ágenst, előnyösen mikrokristályos cellulózt, egyhígítószert, előnyösen laktózt tartalmaznak. Az estrudált-szferonizáltszemcsék záróbevonata egy filmképző anyagot, előnyösen(hidroxipropil)-metil-cellulózt és egy tapadásgátló anyagot, előnyösentalkumot tartalmaznak. A módosított hatóanyagkibocsátású bevonat egypolimer záróanyagot, előnyösen etil-cellulózt és egy lágyítószert,előnyösen desztillált acetilezett monoglicerideket tartalmaz. Az így,kettős bevonattal ellátott szemcséket keményzselatin kapszulákbatöltik, amelyekbe tölthetnek még a retrovírusos fertőzések kezelésérealkalmas egyéb terápiás szereket tartalmazó hasonló szemcséket is. Ó
HU0302631A 2000-03-30 2001-03-29 Stavudint tartalmazó elnyújtott hatóanyag-kibocsátású szemcsék HUP0302631A2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US19358800P 2000-03-30 2000-03-30
PCT/US2001/010078 WO2001074329A2 (en) 2000-03-30 2001-03-29 Sustained release beadlets containing stavudine

Publications (1)

Publication Number Publication Date
HUP0302631A2 true HUP0302631A2 (hu) 2003-11-28

Family

ID=22714247

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0302631A HUP0302631A2 (hu) 2000-03-30 2001-03-29 Stavudint tartalmazó elnyújtott hatóanyag-kibocsátású szemcsék

Country Status (26)

Country Link
US (1) US7135465B2 (hu)
EP (1) EP1267879A2 (hu)
JP (1) JP2003528905A (hu)
KR (1) KR20030011805A (hu)
CN (1) CN1187052C (hu)
AR (1) AR027748A1 (hu)
AU (1) AU2001249591A1 (hu)
BG (1) BG107157A (hu)
BR (1) BR0109602A (hu)
CA (1) CA2404687A1 (hu)
CZ (1) CZ20023003A3 (hu)
EE (1) EE200200564A (hu)
GE (1) GEP20043285B (hu)
HU (1) HUP0302631A2 (hu)
IL (1) IL151475A0 (hu)
LT (1) LT5045B (hu)
LV (1) LV12939B (hu)
MX (1) MXPA02009534A (hu)
NO (1) NO20024645L (hu)
NZ (1) NZ522250A (hu)
PE (1) PE20011179A1 (hu)
PL (1) PL366089A1 (hu)
RU (1) RU2239435C2 (hu)
SK (1) SK12822002A3 (hu)
WO (1) WO2001074329A2 (hu)
ZA (1) ZA200207760B (hu)

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Also Published As

Publication number Publication date
NO20024645D0 (no) 2002-09-27
EP1267879A2 (en) 2003-01-02
EE200200564A (et) 2004-06-15
WO2001074329A2 (en) 2001-10-11
NO20024645L (no) 2002-09-27
SK12822002A3 (sk) 2003-02-04
CN1187052C (zh) 2005-02-02
PE20011179A1 (es) 2001-12-06
MXPA02009534A (es) 2003-05-14
ZA200207760B (en) 2004-01-30
LT2002099A (en) 2003-04-25
LV12939B (en) 2003-04-20
RU2239435C2 (ru) 2004-11-10
AR027748A1 (es) 2003-04-09
AU2001249591A1 (en) 2001-10-15
KR20030011805A (ko) 2003-02-11
RU2002126540A (ru) 2004-03-27
PL366089A1 (en) 2005-01-24
BR0109602A (pt) 2004-06-29
GEP20043285B (en) 2004-07-26
LT5045B (lt) 2003-08-25
NZ522250A (en) 2004-09-24
CN1420774A (zh) 2003-05-28
WO2001074329A3 (en) 2002-05-10
CA2404687A1 (en) 2001-10-11
CZ20023003A3 (cs) 2002-11-13
US7135465B2 (en) 2006-11-14
US20020002147A1 (en) 2002-01-03
IL151475A0 (en) 2003-04-10
JP2003528905A (ja) 2003-09-30
BG107157A (en) 2003-06-30

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