SI9300461B - Beads having a core coated with an antifugal and a polymer - Google Patents
Beads having a core coated with an antifugal and a polymer Download PDFInfo
- Publication number
- SI9300461B SI9300461B SI9300461A SI9300461A SI9300461B SI 9300461 B SI9300461 B SI 9300461B SI 9300461 A SI9300461 A SI 9300461A SI 9300461 A SI9300461 A SI 9300461A SI 9300461 B SI9300461 B SI 9300461B
- Authority
- SI
- Slovenia
- Prior art keywords
- antifungal agent
- polymer
- core
- hydrophilic polymer
- microspheres
- Prior art date
Links
- 229920000642 polymer Polymers 0.000 title claims 2
- 239000011324 bead Substances 0.000 title abstract 4
- 230000001716 anti-fugal effect Effects 0.000 title 1
- 229940121375 antifungal agent Drugs 0.000 claims abstract 8
- 239000003429 antifungal agent Substances 0.000 claims abstract 7
- 229920001477 hydrophilic polymer Polymers 0.000 claims abstract 6
- 239000002552 dosage form Substances 0.000 claims abstract 4
- 239000011248 coating agent Substances 0.000 claims abstract 2
- 238000000576 coating method Methods 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims abstract 2
- 239000004005 microsphere Substances 0.000 claims 9
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 6
- 239000011162 core material Substances 0.000 claims 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- VHVPQPYKVGDNFY-DFMJLFEVSA-N 2-[(2r)-butan-2-yl]-4-[4-[4-[4-[[(2r,4s)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one Chemical compound O=C1N([C@H](C)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@@H]3O[C@](CN4N=CN=C4)(OC3)C=3C(=CC(Cl)=CC=3)Cl)=CC=2)C=C1 VHVPQPYKVGDNFY-DFMJLFEVSA-N 0.000 claims 3
- HUADITLKOCMHSB-AVQIMAJZSA-N 2-butan-2-yl-4-[4-[4-[4-[[(2s,4r)-2-(2,4-difluorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-1,2,4-triazol-3-one Chemical compound O=C1N(C(C)CC)N=CN1C1=CC=C(N2CCN(CC2)C=2C=CC(OC[C@H]3O[C@@](CN4N=CN=C4)(OC3)C=3C(=CC(F)=CC=3)F)=CC=2)C=C1 HUADITLKOCMHSB-AVQIMAJZSA-N 0.000 claims 3
- 229920001688 coating polymer Polymers 0.000 claims 3
- 229960004130 itraconazole Drugs 0.000 claims 3
- 229950005137 saperconazole Drugs 0.000 claims 3
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 238000007789 sealing Methods 0.000 claims 2
- 239000007921 spray Substances 0.000 claims 2
- 230000000843 anti-fungal effect Effects 0.000 claims 1
- 239000007903 gelatin capsule Substances 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 229940031705 hydroxypropyl methylcellulose 2910 Drugs 0.000 claims 1
- 239000000565 sealant Substances 0.000 claims 1
- 238000005507 spraying Methods 0.000 claims 1
- 238000004544 sputter deposition Methods 0.000 claims 1
- 238000001291 vacuum drying Methods 0.000 claims 1
- 239000011247 coating layer Substances 0.000 abstract 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
- A61K9/5073—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
- A61K9/5078—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 with drug-free core
-
- 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
-
- 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
- A61P31/10—Antimycotics
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Processes Of Treating Macromolecular Substances (AREA)
- Materials For Medical Uses (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Claims (9)
- PATENTNI ZAHTEVKI 1. Mikrosfera, ki obsega a) centralno, zaobljeno ali sferično jedro; b) preslojevalni film hidrofilnega polimera in protiglivičnega sredstva; in c) zatesnilno preslojevalni polimerni sloj, označena s tem, da ima jedro premer od okoli 600 do okoli 700 μτη (25-30 zank).
- 2. Mikrosfera po zahtevku 1, označena s tem, da obsega glede na celotno maso mikrosfere a) 20 do 60 mas. % materiala jedra; b) 25 do 50 mas. % hidrofilnega polimera; c) 10 do 25 mas. % protiglivičnega sredstva; in d) 2 do 5 mas. % zatesnilno preslojevalnega polimera.
- 3. Mikrosfera po zahtevku 2, označena s tem, da je material jedra kocka sladkorja z velikostjo 25 do 30 zank, hidrofilni polimer je hidroksipropilmetilceluloza, protiglivično sredstvo pa je itrakonazol ali saperkonazol.
- 4. Mikrosfera po zahtevku 3, označena s tem, da je razmerje m/m protiglivičnega sredstva proti hidrofilnemu polimeru okoli 1:1 do okoli 1:2.
- 5. Mikrosfera po zahtevku 2, označena s tem, da je zatesnilno preslojevalni polimer polietilenglikol.
- 6. Mikrosfera po zahtevku 2, označena s tem, da obsega približno: a) 26 do 28 % sladkorja; b) 32 do 33 % hidroksipropilmetilceluloze 2910 5 mPa.s.; c) 21 do 22 % itrakonazola ali saperkonazola; in d) 3 do 4 % polietilenglikola 20000.
- 7. Farmacevtska dozirna oblika, označena s tem, da obsega učinkovito protiglivično količino mikrosfer po kateremkoli od zahtevkov 1 do 6.
- 8. Dozirna oblika po zahtevku 7, označena s tem, da je dozirna oblika trda želatinska kapsula, ki obsega protiglivično sredstvo itrakonazol ali saperkonazol v obliki mikrosfer po kateremkoli od zahtevkov 1 do 6.
- 9. Postopek za pripravo mikrosfer po kateremkoli od zahtevkov 1 do 6, označen s tem, da a) preslojimo jedra z velikostjo 25 do 30 zank z naprševanjem z raztopino protiglivičnega sredstva in hidrofilnega polimera v organskem topilu, ki obstoji iz metilenklorida in etanola v granulatoiju s fluidizirano blazino, opremljenem z Wursteijevim vstavkom (razprševanje na dnu). b) dobljena preslojena jedra sušimo v vakuumskem sušilnem bobnu; in c) posušena jedra zatesnilno preslojimo z naprševanjem z raztopino zatesnilnopres-lojevalnega polimera v organskem topilu, ki obstoji iz metilenklorida in etanola, v granulatoiju s fluidizirano blazino, opremljenem z Wursterjevim vstavkom (razprševanje na dnu).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP92202664 | 1992-09-03 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SI9300461A SI9300461A (en) | 1994-03-31 |
| SI9300461B true SI9300461B (en) | 2001-12-31 |
Family
ID=8210890
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI9300461A SI9300461B (en) | 1992-09-03 | 1993-09-03 | Beads having a core coated with an antifugal and a polymer |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US5633015A (sl) |
| EP (1) | EP0658103B1 (sl) |
| JP (1) | JP2865869B2 (sl) |
| KR (1) | KR0151893B1 (sl) |
| CN (1) | CN1034714C (sl) |
| AP (1) | AP444A (sl) |
| AT (1) | ATE145327T1 (sl) |
| AU (1) | AU665867B2 (sl) |
| CA (1) | CA2142848C (sl) |
| CY (1) | CY2105B1 (sl) |
| CZ (1) | CZ283403B6 (sl) |
| DE (1) | DE69306119T2 (sl) |
| DK (1) | DK0658103T3 (sl) |
| ES (1) | ES2097536T3 (sl) |
| FI (1) | FI112437B (sl) |
| GR (1) | GR3022198T3 (sl) |
| HK (1) | HK1006000A1 (sl) |
| HR (1) | HRP931158B1 (sl) |
| HU (1) | HU220614B1 (sl) |
| IL (1) | IL106871A (sl) |
| MX (1) | MX9305438A (sl) |
| MY (1) | MY109369A (sl) |
| NO (1) | NO307953B1 (sl) |
| NZ (1) | NZ255379A (sl) |
| OA (1) | OA10130A (sl) |
| PH (1) | PH30929A (sl) |
| PL (2) | PL174178B1 (sl) |
| RU (1) | RU2125445C1 (sl) |
| SG (1) | SG48801A1 (sl) |
| SI (1) | SI9300461B (sl) |
| TW (1) | TW376322B (sl) |
| WO (1) | WO1994005263A1 (sl) |
| ZA (1) | ZA936493B (sl) |
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| US5846971A (en) * | 1996-06-28 | 1998-12-08 | Schering Corporation | Oral antifungal composition |
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| GB9623634D0 (en) | 1996-11-13 | 1997-01-08 | Bpsi Holdings Inc | Method and apparatus for the coating of substrates for pharmaceutical use |
| FR2758459B1 (fr) * | 1997-01-17 | 1999-05-07 | Pharma Pass | Composition pharmaceutique de fenofibrate presentant une biodisponibilite elevee et son procede de preparation |
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| FR2514261B1 (fr) * | 1981-10-08 | 1986-08-22 | Aec Chim Organ Biolog | Nouvelle composition pour l'enrobage des aliments et des medicaments et granules ainsi enrobes |
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| US5213811A (en) * | 1991-09-13 | 1993-05-25 | Sterling Drug Inc. | Oral sustained-release drug compositions |
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1993
- 1993-08-13 PH PH46686A patent/PH30929A/en unknown
- 1993-08-26 TW TW082106900A patent/TW376322B/zh not_active IP Right Cessation
- 1993-08-27 US US08/432,188 patent/US5633015A/en not_active Expired - Lifetime
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- 1993-08-27 RU RU95108537A patent/RU2125445C1/ru active
- 1993-08-27 DK DK93919206.8T patent/DK0658103T3/da active
- 1993-08-27 KR KR1019950700756A patent/KR0151893B1/ko not_active Expired - Lifetime
- 1993-08-27 HU HU9500642A patent/HU220614B1/hu unknown
- 1993-08-27 WO PCT/EP1993/002327 patent/WO1994005263A1/en not_active Ceased
- 1993-08-27 AU AU49546/93A patent/AU665867B2/en not_active Expired
- 1993-08-27 PL PL93318659A patent/PL174178B1/pl unknown
- 1993-08-27 CZ CZ95542A patent/CZ283403B6/cs not_active IP Right Cessation
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- 1993-08-27 EP EP93919206A patent/EP0658103B1/en not_active Expired - Lifetime
- 1993-08-27 DE DE69306119T patent/DE69306119T2/de not_active Expired - Lifetime
- 1993-08-27 AT AT93919206T patent/ATE145327T1/de active
- 1993-08-27 PL PL93307791A patent/PL172676B1/pl unknown
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- 1993-09-02 AP APAP/P/1993/000563A patent/AP444A/en active
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- 1993-09-02 HR HR92202664.6A patent/HRP931158B1/xx not_active IP Right Cessation
- 1993-09-02 CN CN93117313A patent/CN1034714C/zh not_active Expired - Lifetime
- 1993-09-03 MX MX9305438A patent/MX9305438A/es unknown
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1995
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- 1995-03-02 NO NO950829A patent/NO307953B1/no not_active IP Right Cessation
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