DE69929959T2 - Zubereitungen enthaltend mikropartikel von wasserunlöslichen substanzen, sowie verfahren zu deren herstellung - Google Patents
Zubereitungen enthaltend mikropartikel von wasserunlöslichen substanzen, sowie verfahren zu deren herstellung Download PDFInfo
- Publication number
- DE69929959T2 DE69929959T2 DE69929959T DE69929959T DE69929959T2 DE 69929959 T2 DE69929959 T2 DE 69929959T2 DE 69929959 T DE69929959 T DE 69929959T DE 69929959 T DE69929959 T DE 69929959T DE 69929959 T2 DE69929959 T2 DE 69929959T2
- Authority
- DE
- Germany
- Prior art keywords
- phospholipid
- block copolymer
- particles
- weight
- charged
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Lifetime
Links
- 238000000034 method Methods 0.000 title claims abstract description 23
- 239000011859 microparticle Substances 0.000 title description 12
- 239000000126 substance Substances 0.000 title description 7
- 238000004519 manufacturing process Methods 0.000 title description 5
- 238000002360 preparation method Methods 0.000 title description 3
- 239000002245 particle Substances 0.000 claims abstract description 64
- 150000003904 phospholipids Chemical class 0.000 claims abstract description 50
- 239000000203 mixture Substances 0.000 claims abstract description 39
- 239000003607 modifier Substances 0.000 claims abstract description 37
- 239000003814 drug Substances 0.000 claims abstract description 34
- 229940079593 drug Drugs 0.000 claims abstract description 33
- 229920001400 block copolymer Polymers 0.000 claims abstract description 29
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 11
- 230000015572 biosynthetic process Effects 0.000 claims abstract description 10
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims description 5
- GOOHAUXETOMSMM-UHFFFAOYSA-N Propylene oxide Chemical compound CC1CO1 GOOHAUXETOMSMM-UHFFFAOYSA-N 0.000 claims description 5
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 claims description 4
- PORPENFLTBBHSG-MGBGTMOVSA-N 1,2-dihexadecanoyl-sn-glycerol-3-phosphate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=O)OC(=O)CCCCCCCCCCCCCCC PORPENFLTBBHSG-MGBGTMOVSA-N 0.000 claims description 3
- TZCPCKNHXULUIY-RGULYWFUSA-N 1,2-distearoyl-sn-glycero-3-phosphoserine Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@H](N)C(O)=O)OC(=O)CCCCCCCCCCCCCCCCC TZCPCKNHXULUIY-RGULYWFUSA-N 0.000 claims description 3
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 claims description 3
- ZWZWYGMENQVNFU-UHFFFAOYSA-N Glycerophosphorylserin Natural products OC(=O)C(N)COP(O)(=O)OCC(O)CO ZWZWYGMENQVNFU-UHFFFAOYSA-N 0.000 claims description 3
- 239000002775 capsule Substances 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 150000003839 salts Chemical group 0.000 claims description 3
- 230000000087 stabilizing effect Effects 0.000 claims description 3
- 239000000725 suspension Substances 0.000 claims description 3
- 239000008187 granular material Substances 0.000 claims description 2
- JZNWSCPGTDBMEW-UHFFFAOYSA-N Glycerophosphorylethanolamin Natural products NCCOP(O)(=O)OCC(O)CO JZNWSCPGTDBMEW-UHFFFAOYSA-N 0.000 claims 2
- 150000008104 phosphatidylethanolamines Chemical class 0.000 claims 2
- QLNOOKSBAYIHQI-SKZICHJRSA-M sodium;2,3-dihydroxypropyl [(2r)-2,3-di(tetradecanoyloxy)propyl] phosphate Chemical compound [Na+].CCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC(O)CO)OC(=O)CCCCCCCCCCCCC QLNOOKSBAYIHQI-SKZICHJRSA-M 0.000 claims 2
- 238000001361 intraarterial administration Methods 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 238000007912 intraperitoneal administration Methods 0.000 claims 1
- 230000002601 intratumoral effect Effects 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 239000008176 lyophilized powder Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 abstract description 9
- 230000012010 growth Effects 0.000 abstract description 9
- 230000006641 stabilisation Effects 0.000 abstract description 9
- 238000011105 stabilization Methods 0.000 abstract description 9
- 230000002776 aggregation Effects 0.000 abstract description 7
- 238000004220 aggregation Methods 0.000 abstract description 7
- 238000005189 flocculation Methods 0.000 abstract description 2
- 230000016615 flocculation Effects 0.000 abstract description 2
- 238000009472 formulation Methods 0.000 description 18
- 239000003381 stabilizer Substances 0.000 description 7
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 description 6
- 229930105110 Cyclosporin A Natural products 0.000 description 6
- 108010036949 Cyclosporine Proteins 0.000 description 6
- 229960001265 ciclosporin Drugs 0.000 description 6
- 229930182912 cyclosporin Natural products 0.000 description 6
- 238000010951 particle size reduction Methods 0.000 description 6
- 238000012545 processing Methods 0.000 description 6
- 239000004480 active ingredient Substances 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 238000003860 storage Methods 0.000 description 5
- 239000004094 surface-active agent Substances 0.000 description 5
- AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 description 4
- 230000005070 ripening Effects 0.000 description 4
- RUDATBOHQWOJDD-UHFFFAOYSA-N (3beta,5beta,7alpha)-3,7-Dihydroxycholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)CC2 RUDATBOHQWOJDD-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- ATBOMIWRCZXYSZ-XZBBILGWSA-N [1-[2,3-dihydroxypropoxy(hydroxy)phosphoryl]oxy-3-hexadecanoyloxypropan-2-yl] (9e,12e)-octadeca-9,12-dienoate Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(COP(O)(=O)OCC(O)CO)OC(=O)CCCCCCC\C=C\C\C=C\CCCCC ATBOMIWRCZXYSZ-XZBBILGWSA-N 0.000 description 3
- 238000005299 abrasion Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- YMTINGFKWWXKFG-UHFFFAOYSA-N fenofibrate Chemical compound C1=CC(OC(C)(C)C(=O)OC(C)C)=CC=C1C(=O)C1=CC=C(Cl)C=C1 YMTINGFKWWXKFG-UHFFFAOYSA-N 0.000 description 3
- 229960002297 fenofibrate Drugs 0.000 description 3
- 238000000265 homogenisation Methods 0.000 description 3
- 230000003993 interaction Effects 0.000 description 3
- 239000002105 nanoparticle Substances 0.000 description 3
- -1 neuroleptics Substances 0.000 description 3
- 238000001556 precipitation Methods 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- RUDATBOHQWOJDD-UZVSRGJWSA-N ursodeoxycholic acid Chemical compound C([C@H]1C[C@@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 RUDATBOHQWOJDD-UZVSRGJWSA-N 0.000 description 3
- 229960001661 ursodiol Drugs 0.000 description 3
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- 235000010469 Glycine max Nutrition 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 239000001961 anticonvulsive agent Substances 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 238000004108 freeze drying Methods 0.000 description 2
- 239000007972 injectable composition Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 229940042880 natural phospholipid Drugs 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 238000000527 sonication Methods 0.000 description 2
- 238000013112 stability test Methods 0.000 description 2
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 description 1
- 108010036941 Cyclosporins Proteins 0.000 description 1
- 229920005682 EO-PO block copolymer Polymers 0.000 description 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 229920002359 Tetronic® Polymers 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 239000000674 adrenergic antagonist Substances 0.000 description 1
- 230000000202 analgesic effect Effects 0.000 description 1
- 229940035674 anesthetics Drugs 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000001078 anti-cholinergic effect Effects 0.000 description 1
- 230000003556 anti-epileptic effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000001022 anti-muscarinic effect Effects 0.000 description 1
- 230000000840 anti-viral effect Effects 0.000 description 1
- 239000003416 antiarrhythmic agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 229940125681 anticonvulsant agent Drugs 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 229960003965 antiepileptics Drugs 0.000 description 1
- 239000003429 antifungal agent Substances 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 239000002220 antihypertensive agent Substances 0.000 description 1
- 229940030600 antihypertensive agent Drugs 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 229940034982 antineoplastic agent Drugs 0.000 description 1
- 239000000164 antipsychotic agent Substances 0.000 description 1
- 239000003443 antiviral agent Substances 0.000 description 1
- 239000002249 anxiolytic agent Substances 0.000 description 1
- 230000000949 anxiolytic effect Effects 0.000 description 1
- 229940005530 anxiolytics Drugs 0.000 description 1
- 238000013459 approach Methods 0.000 description 1
- 239000012736 aqueous medium Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 239000002981 blocking agent Substances 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 230000000718 cholinopositive effect Effects 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 229940039227 diagnostic agent Drugs 0.000 description 1
- 239000000032 diagnostic agent Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 150000002016 disaccharides Chemical class 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 229940088679 drug related substance Drugs 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000004744 fabric Substances 0.000 description 1
- 239000013020 final formulation Substances 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000003193 general anesthetic agent Substances 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 230000005660 hydrophilic surface Effects 0.000 description 1
- 239000003326 hypnotic agent Substances 0.000 description 1
- 230000000147 hypnotic effect Effects 0.000 description 1
- 238000003384 imaging method Methods 0.000 description 1
- 230000001506 immunosuppresive effect Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 231100001231 less toxic Toxicity 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 239000000693 micelle Substances 0.000 description 1
- 238000003801 milling Methods 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000000472 muscarinic agonist Substances 0.000 description 1
- 239000003149 muscarinic antagonist Substances 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- 235000015097 nutrients Nutrition 0.000 description 1
- 125000001117 oleyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])/C([H])=C([H])\C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 150000003905 phosphatidylinositols Chemical class 0.000 description 1
- 229920001983 poloxamer Polymers 0.000 description 1
- 229920001993 poloxamer 188 Polymers 0.000 description 1
- 229920001987 poloxamine Polymers 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 238000005185 salting out Methods 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 229940125723 sedative agent Drugs 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- 238000005549 size reduction Methods 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000008347 soybean phospholipid Substances 0.000 description 1
- 239000012798 spherical particle Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
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
- A61K9/48—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
- A61K9/51—Nanocapsules; Nanoparticles
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S977/00—Nanotechnology
- Y10S977/902—Specified use of nanostructure
- Y10S977/904—Specified use of nanostructure for medical, immunological, body treatment, or diagnosis
- Y10S977/926—Topical chemical, e.g. cosmetic or sunscreen
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Physics & Mathematics (AREA)
- Biomedical Technology (AREA)
- Nanotechnology (AREA)
- Optics & Photonics (AREA)
- Medicinal Preparation (AREA)
- Manufacturing Of Micro-Capsules (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7980998P | 1998-03-30 | 1998-03-30 | |
| US79809P | 1998-03-30 | ||
| PCT/US1999/006746 WO1999049846A2 (en) | 1998-03-30 | 1999-03-29 | Compositions containing microparticles of water-insoluble substances and method for their preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE69929959D1 DE69929959D1 (de) | 2006-04-27 |
| DE69929959T2 true DE69929959T2 (de) | 2006-11-02 |
Family
ID=22152962
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69929959T Expired - Lifetime DE69929959T2 (de) | 1998-03-30 | 1999-03-29 | Zubereitungen enthaltend mikropartikel von wasserunlöslichen substanzen, sowie verfahren zu deren herstellung |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US6387409B1 (enExample) |
| EP (1) | EP1067914B1 (enExample) |
| JP (2) | JP4709378B2 (enExample) |
| KR (1) | KR100628341B1 (enExample) |
| CN (1) | CN1303278B (enExample) |
| AT (1) | ATE318132T1 (enExample) |
| AU (1) | AU761205B2 (enExample) |
| CA (1) | CA2326456C (enExample) |
| DE (1) | DE69929959T2 (enExample) |
| ES (1) | ES2257041T3 (enExample) |
| IL (3) | IL138765A0 (enExample) |
| SE (1) | SE0003429L (enExample) |
| TW (1) | TWI267383B (enExample) |
| WO (1) | WO1999049846A2 (enExample) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7255877B2 (en) | 1996-08-22 | 2007-08-14 | Jagotec Ag | Fenofibrate microparticles |
| US6465016B2 (en) | 1996-08-22 | 2002-10-15 | Research Triangle Pharmaceuticals | Cyclosporiine particles |
| DE69929959T2 (de) * | 1998-03-30 | 2006-11-02 | Jagotec Ag | Zubereitungen enthaltend mikropartikel von wasserunlöslichen substanzen, sowie verfahren zu deren herstellung |
| US6979456B1 (en) | 1998-04-01 | 2005-12-27 | Jagotec Ag | Anticancer compositions |
| KR100635456B1 (ko) | 1998-05-29 | 2006-10-18 | 스키에파마 캐나다 인코포레이티드 | 열보호화 마이크로입자 조성물 및 그의 말단의 스팀멸균방법 |
| HK1042856B (zh) | 1998-11-20 | 2007-07-27 | Skyepharma Canada Inc. | 可分散的磷脂稳定的微粒 |
| CN1213733C (zh) * | 1998-11-20 | 2005-08-10 | 斯凯伊药品加拿大公司 | 制备稳定的不溶性微粒的悬浮液的方法 |
| DE60020382T2 (de) * | 1999-09-21 | 2006-01-26 | Skyepharma Canada Inc., Verdun | Oberflächenmodifizierte teilchenförmige zusammensetzungen biologisch aktiver stoffe |
| US7276249B2 (en) * | 2002-05-24 | 2007-10-02 | Elan Pharma International, Ltd. | Nanoparticulate fibrate formulations |
| US20080241070A1 (en) * | 2000-09-21 | 2008-10-02 | Elan Pharma International Ltd. | Fenofibrate dosage forms |
| US20030224058A1 (en) * | 2002-05-24 | 2003-12-04 | Elan Pharma International, Ltd. | Nanoparticulate fibrate formulations |
| US9700866B2 (en) | 2000-12-22 | 2017-07-11 | Baxter International Inc. | Surfactant systems for delivery of organic compounds |
| US6977085B2 (en) | 2000-12-22 | 2005-12-20 | Baxter International Inc. | Method for preparing submicron suspensions with polymorph control |
| US8067032B2 (en) | 2000-12-22 | 2011-11-29 | Baxter International Inc. | Method for preparing submicron particles of antineoplastic agents |
| US6607784B2 (en) | 2000-12-22 | 2003-08-19 | Baxter International Inc. | Microprecipitation method for preparing submicron suspensions |
| US6884436B2 (en) | 2000-12-22 | 2005-04-26 | Baxter International Inc. | Method for preparing submicron particle suspensions |
| US6951656B2 (en) | 2000-12-22 | 2005-10-04 | Baxter International Inc. | Microprecipitation method for preparing submicron suspensions |
| US7193084B2 (en) | 2000-12-22 | 2007-03-20 | Baxter International Inc. | Polymorphic form of itraconazole |
| US20030054042A1 (en) * | 2001-09-14 | 2003-03-20 | Elaine Liversidge | Stabilization of chemical compounds using nanoparticulate formulations |
| US20060003012A9 (en) | 2001-09-26 | 2006-01-05 | Sean Brynjelsen | Preparation of submicron solid particle suspensions by sonication of multiphase systems |
| CN1558755A (zh) | 2001-09-26 | 2004-12-29 | ���ع��ʹ�˾ | 通过分散和除去溶剂或液相制备亚微米大小的纳米颗粒 |
| US7112340B2 (en) | 2001-10-19 | 2006-09-26 | Baxter International Inc. | Compositions of and method for preparing stable particles in a frozen aqueous matrix |
| WO2003084518A2 (fr) | 2002-04-09 | 2003-10-16 | Flamel Technologies | Suspension orale de microcapsules de principes actifs |
| US20070264348A1 (en) * | 2002-05-24 | 2007-11-15 | Elan Pharma International, Ltd. | Nanoparticulate fibrate formulations |
| FR2842736B1 (fr) | 2002-07-26 | 2005-07-22 | Flamel Tech Sa | Formulation pharmaceutique orale sous forme d'une pluralite de microcapsules permettant la liberation prolongee de principe(s) actif(s) peu soluble(s) |
| FR2842735B1 (fr) | 2002-07-26 | 2006-01-06 | Flamel Tech Sa | Microcapsules a liberation modifiee de principes actifs peu solubles pour l'administration per os |
| CN1243538C (zh) * | 2002-11-21 | 2006-03-01 | 武汉利元亨药物技术有限公司 | 熊果酸豆磷脂纳米粒冻干粉针及制备方法 |
| GB0302672D0 (en) * | 2003-02-06 | 2003-03-12 | Astrazeneca Ab | Pharmaceutical formulations |
| US6931888B2 (en) * | 2003-02-07 | 2005-08-23 | Ferro Corporation | Lyophilization method and apparatus for producing particles |
| US20040178135A1 (en) * | 2003-03-13 | 2004-09-16 | Beplate Douglas K. | Filtering device incorporating nanoparticles |
| MXPA05012467A (es) * | 2003-05-19 | 2006-02-22 | Baxter Int | Particulas solidas que comprenden un anticonvulsivo o un inmunosupresor revestido con uno o mas modificadores de superficie. |
| EA200600877A1 (ru) * | 2003-10-31 | 2006-12-29 | Тева Фармасьютикал Индастриз, Лтд. | Наночастицы для доставки лекарств |
| US20070224278A1 (en) * | 2003-11-12 | 2007-09-27 | Lyons Robert T | Low immunogenicity corticosteroid compositions |
| US20060141049A1 (en) * | 2003-11-12 | 2006-06-29 | Allergan, Inc. | Triamcinolone compositions for intravitreal administration to treat ocular conditions |
| US20050250737A1 (en) * | 2003-11-12 | 2005-11-10 | Allergan, Inc. | Therapeutic ophthalmic compositions containing retinal friendly excipients and related methods |
| US20050101582A1 (en) | 2003-11-12 | 2005-05-12 | Allergan, Inc. | Compositions and methods for treating a posterior segment of an eye |
| WO2005072701A1 (en) | 2004-01-20 | 2005-08-11 | Allergan, Inc. | Compositions for localized therapy of the eye, comprising preferably triamcinolone acetonide and hyaluronic acid |
| US20050170063A1 (en) * | 2004-01-29 | 2005-08-04 | Lalit Chordia | Production of powder and viscous material |
| US8119154B2 (en) | 2004-04-30 | 2012-02-21 | Allergan, Inc. | Sustained release intraocular implants and related methods |
| US8147865B2 (en) | 2004-04-30 | 2012-04-03 | Allergan, Inc. | Steroid-containing sustained release intraocular implants and related methods |
| AU2005271700B2 (en) * | 2004-07-12 | 2010-11-11 | Allergan, Inc. | Opthalmic compositions and methods for treating ophthalmic conditions |
| WO2006057429A1 (ja) * | 2004-11-24 | 2006-06-01 | Nanocarrier Co., Ltd. | ブロックコポリマーのモーフォロジ-の変化方法 |
| BRPI0612071A2 (pt) * | 2005-06-14 | 2010-10-19 | Baxter Int | formulações farmacêuticas para minimizar interações entre fármacos |
| WO2007008697A2 (en) * | 2005-07-08 | 2007-01-18 | University Of Chicago | Compositions and methods for refolding of denatured proteins |
| WO2007059515A2 (en) * | 2005-11-15 | 2007-05-24 | Baxter International, Inc. | Compositions of lipoxygenase inhibitors |
| WO2008080047A2 (en) * | 2006-12-23 | 2008-07-03 | Baxter International Inc. | Magnetic separation of fine particles from compositions |
| US8722736B2 (en) * | 2007-05-22 | 2014-05-13 | Baxter International Inc. | Multi-dose concentrate esmolol with benzyl alcohol |
| US8426467B2 (en) * | 2007-05-22 | 2013-04-23 | Baxter International Inc. | Colored esmolol concentrate |
| US20080293814A1 (en) * | 2007-05-22 | 2008-11-27 | Deepak Tiwari | Concentrate esmolol |
| MX2010001311A (es) * | 2007-07-31 | 2010-04-21 | Otsuka Pharma Co Ltd | Metodo para producir una suspensi?n de aripiprazol y formulacion liofilizada. |
| EP2200613B1 (en) | 2007-09-21 | 2018-09-05 | The Johns Hopkins University | Phenazine derivatives and uses thereof |
| CN103228266B (zh) | 2010-10-29 | 2017-11-14 | 健康科学西部大学 | 三元混合物制剂 |
| WO2014004507A1 (en) * | 2012-06-27 | 2014-01-03 | Shell Oil Company | Fuel and engine oil composition and its use |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5091187A (en) | 1990-04-26 | 1992-02-25 | Haynes Duncan H | Phospholipid-coated microcrystals: injectable formulations of water-insoluble drugs |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| MX9201782A (es) | 1991-04-19 | 1992-10-01 | Sandoz Ag | Particulas de sustancias biologicamente activas, sustancialmente insolubles en agua, proceso para su produccion y composicion farmaceutica que las contiene. |
| US5298262A (en) | 1992-12-04 | 1994-03-29 | Sterling Winthrop Inc. | Use of ionic cloud point modifiers to prevent particle aggregation during sterilization |
| US5340564A (en) | 1992-12-10 | 1994-08-23 | Sterling Winthrop Inc. | Formulations comprising olin 10-G to prevent particle aggregation and increase stability |
| US5336507A (en) | 1992-12-11 | 1994-08-09 | Sterling Winthrop Inc. | Use of charged phospholipids to reduce nanoparticle aggregation |
| US5326552A (en) | 1992-12-17 | 1994-07-05 | Sterling Winthrop Inc. | Formulations for nanoparticulate x-ray blood pool contrast agents using high molecular weight nonionic surfactants |
| DE4440337A1 (de) | 1994-11-11 | 1996-05-15 | Dds Drug Delivery Services Ges | Pharmazeutische Nanosuspensionen zur Arzneistoffapplikation als Systeme mit erhöhter Sättigungslöslichkeit und Lösungsgeschwindigkeit |
| US5569448A (en) | 1995-01-24 | 1996-10-29 | Nano Systems L.L.C. | Sulfated nonionic block copolymer surfactants as stabilizer coatings for nanoparticle compositions |
| ATE198148T1 (de) * | 1995-02-06 | 2001-01-15 | Elan Pharma Int Ltd | Formulierungen von verbindungen als nanopartikel dispergiert in verdaubaren ölen oder fettsäuren |
| US5510118A (en) | 1995-02-14 | 1996-04-23 | Nanosystems Llc | Process for preparing therapeutic compositions containing nanoparticles |
| WO1997014407A1 (en) * | 1995-10-17 | 1997-04-24 | Research Triangle Pharmaceuticals | Insoluble drug delivery |
| US5686133A (en) | 1996-01-31 | 1997-11-11 | Port Systems, L.L.C. | Water soluble pharmaceutical coating and method for producing coated pharmaceuticals |
| JP2000516244A (ja) * | 1996-08-22 | 2000-12-05 | リサーチ・トライアングル・ファーマシューティカルズ | 水不溶性物質の微粒子を含む組成物およびその製造方法 |
| WO1999029300A1 (en) * | 1997-12-10 | 1999-06-17 | Rtp Pharma Inc. | Self-emulsifying fenofibrate formulations |
| DE69929959T2 (de) * | 1998-03-30 | 2006-11-02 | Jagotec Ag | Zubereitungen enthaltend mikropartikel von wasserunlöslichen substanzen, sowie verfahren zu deren herstellung |
| KR20140029532A (ko) * | 2011-09-30 | 2014-03-10 | 제이엑스 닛코 닛세키 킨조쿠 가부시키가이샤 | 스퍼터링 타깃 및 그 제조 방법 |
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1999
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- 1999-03-29 AT AT99912926T patent/ATE318132T1/de not_active IP Right Cessation
- 1999-03-29 KR KR1020007010469A patent/KR100628341B1/ko not_active Expired - Fee Related
- 1999-03-29 IL IL13876599A patent/IL138765A0/xx active IP Right Grant
- 1999-03-29 AU AU31185/99A patent/AU761205B2/en not_active Ceased
- 1999-03-29 ES ES99912926T patent/ES2257041T3/es not_active Expired - Lifetime
- 1999-03-29 JP JP2000540812A patent/JP4709378B2/ja not_active Expired - Fee Related
- 1999-03-29 WO PCT/US1999/006746 patent/WO1999049846A2/en not_active Ceased
- 1999-03-29 CA CA002326456A patent/CA2326456C/en not_active Expired - Fee Related
- 1999-03-29 EP EP99912926A patent/EP1067914B1/en not_active Expired - Lifetime
- 1999-03-29 IL IL16202399A patent/IL162023A0/xx unknown
- 1999-03-29 CN CN998067113A patent/CN1303278B/zh not_active Expired - Fee Related
- 1999-05-14 TW TW088105042A patent/TWI267383B/zh not_active IP Right Cessation
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2000
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- 2000-09-26 SE SE0003429A patent/SE0003429L/xx not_active Application Discontinuation
- 2000-09-28 IL IL138765A patent/IL138765A/en not_active IP Right Cessation
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Also Published As
| Publication number | Publication date |
|---|---|
| TWI267383B (en) | 2006-12-01 |
| CN1303278A (zh) | 2001-07-11 |
| IL138765A0 (en) | 2001-10-31 |
| ATE318132T1 (de) | 2006-03-15 |
| WO1999049846A3 (en) | 1999-11-18 |
| ES2257041T3 (es) | 2006-07-16 |
| CN1303278B (zh) | 2010-06-23 |
| KR100628341B1 (ko) | 2006-09-27 |
| JP2011037889A (ja) | 2011-02-24 |
| AU761205B2 (en) | 2003-05-29 |
| US6387409B1 (en) | 2002-05-14 |
| SE0003429L (sv) | 2000-11-23 |
| IL162023A0 (en) | 2005-11-20 |
| JP5539839B2 (ja) | 2014-07-02 |
| EP1067914A2 (en) | 2001-01-17 |
| JP2002509876A (ja) | 2002-04-02 |
| WO1999049846A2 (en) | 1999-10-07 |
| DE69929959D1 (de) | 2006-04-27 |
| CA2326456C (en) | 2008-12-23 |
| IL138765A (en) | 2007-09-20 |
| JP4709378B2 (ja) | 2011-06-22 |
| SE0003429D0 (sv) | 2000-09-26 |
| AU3118599A (en) | 1999-10-18 |
| KR20010042103A (ko) | 2001-05-25 |
| CA2326456A1 (en) | 1999-10-07 |
| EP1067914B1 (en) | 2006-02-22 |
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