EA005080B1 - Способ получения сферических агломератов телитромицина и их применение для приготовления лекарственных форм - Google Patents
Способ получения сферических агломератов телитромицина и их применение для приготовления лекарственных форм Download PDFInfo
- Publication number
- EA005080B1 EA005080B1 EA200200294A EA200200294A EA005080B1 EA 005080 B1 EA005080 B1 EA 005080B1 EA 200200294 A EA200200294 A EA 200200294A EA 200200294 A EA200200294 A EA 200200294A EA 005080 B1 EA005080 B1 EA 005080B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- telithromycin
- preparation
- crystallization
- spherical
- acetone
- Prior art date
Links
- LJVAJPDWBABPEJ-PNUFFHFMSA-N telithromycin Chemical class O([C@@H]1[C@@H](C)C(=O)[C@@H](C)C(=O)O[C@@H]([C@]2(OC(=O)N(CCCCN3C=C(N=C3)C=3C=NC=CC=3)[C@@H]2[C@@H](C)C(=O)[C@H](C)C[C@@]1(C)OC)C)CC)[C@@H]1O[C@H](C)C[C@H](N(C)C)[C@H]1O LJVAJPDWBABPEJ-PNUFFHFMSA-N 0.000 title claims abstract description 21
- 238000000034 method Methods 0.000 title claims abstract description 12
- 238000002360 preparation method Methods 0.000 title abstract description 6
- 238000004519 manufacturing process Methods 0.000 title abstract description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims abstract description 20
- 229960003250 telithromycin Drugs 0.000 claims abstract description 18
- 238000002425 crystallisation Methods 0.000 claims abstract description 9
- 230000008025 crystallization Effects 0.000 claims abstract description 9
- 239000000725 suspension Substances 0.000 claims abstract description 8
- ZAFNJMIOTHYJRJ-UHFFFAOYSA-N Diisopropyl ether Chemical compound CC(C)OC(C)C ZAFNJMIOTHYJRJ-UHFFFAOYSA-N 0.000 claims abstract description 6
- 239000013078 crystal Substances 0.000 claims abstract description 6
- 229920000642 polymer Polymers 0.000 claims abstract description 6
- 239000000203 mixture Substances 0.000 claims abstract description 3
- 239000011248 coating agent Substances 0.000 claims description 3
- 238000000576 coating method Methods 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003094 microcapsule Substances 0.000 abstract description 3
- XCAUINMIESBTBL-UHFFFAOYSA-N lead(ii) sulfide Chemical group [Pb]=S XCAUINMIESBTBL-UHFFFAOYSA-N 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 6
- 239000002245 particle Substances 0.000 description 5
- 238000003756 stirring Methods 0.000 description 5
- 229910052757 nitrogen Inorganic materials 0.000 description 3
- ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 description 2
- 238000005354 coacervation Methods 0.000 description 2
- 238000004090 dissolution Methods 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000005507 spraying Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 1
- 238000012695 Interfacial polymerization Methods 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 238000009529 body temperature measurement Methods 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 229960003276 erythromycin Drugs 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 description 1
- 125000001841 imino group Chemical group [H]N=* 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000012299 nitrogen atmosphere Substances 0.000 description 1
- 238000010899 nucleation Methods 0.000 description 1
- 229920002959 polymer blend Polymers 0.000 description 1
- 239000000523 sample Substances 0.000 description 1
- 239000012798 spherical particle Substances 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 238000002604 ultrasonography Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
-
- 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
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- 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
- A61K9/1682—Processes
- A61K9/1688—Processes resulting in pure drug agglomerate optionally containing up to 5% of excipient
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Oncology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Saccharide Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9910810A FR2797875B1 (fr) | 1999-08-26 | 1999-08-26 | Agglomerats spheriques de telithromycine, leur procede de preparation et leur application dans la preparation de formes pharmaceutiques |
| PCT/FR2000/002393 WO2001014393A2 (fr) | 1999-08-26 | 2000-08-28 | Agglomerats spheriques de telithromycine, leur procede de preparation et leur application dans la preparation de formes pharmaceutiques |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200200294A1 EA200200294A1 (ru) | 2002-08-29 |
| EA005080B1 true EA005080B1 (ru) | 2004-10-28 |
Family
ID=9549351
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200200294A EA005080B1 (ru) | 1999-08-26 | 2000-08-28 | Способ получения сферических агломератов телитромицина и их применение для приготовления лекарственных форм |
Country Status (34)
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE9902202D0 (sv) * | 1999-06-10 | 1999-06-10 | Astra Ab | Production of aggregates |
| FR2821747B1 (fr) * | 2001-03-09 | 2004-07-02 | Ethypharm Lab Prod Ethiques | Suspension de telithromycine a gout masque |
| BR0215806A (pt) * | 2002-07-19 | 2005-04-26 | Aventis Pharma Sa | Composição oral de telitromicina com paladar mascarado |
| WO2004009059A1 (en) * | 2002-07-19 | 2004-01-29 | Aventis Pharma S.A. | Taste masked oral composition of telithromycin |
| US20040013737A1 (en) * | 2002-07-19 | 2004-01-22 | Philippe Becourt | Taste masked oral composition of telithromycin |
| EP1610878B1 (en) * | 2003-02-21 | 2014-09-03 | University Of Bath | Process for the production of particles |
| WO2005007143A2 (en) * | 2003-07-14 | 2005-01-27 | The Board Of Trustees Of The University Of Illinois | Use of makrolides and ketolides for the treatment of tuberculosis |
| WO2007039914A2 (en) * | 2005-10-06 | 2007-04-12 | Alembic Limited | Novel polymorphs of telithromycin |
| US20090075917A1 (en) * | 2007-09-19 | 2009-03-19 | Protia, Llc | Deuterium-enriched telithromycin |
| KR101324862B1 (ko) * | 2011-07-12 | 2013-11-01 | (주)에이에스텍 | 클로피도그렐 황산수소염의 구형 입자, 이를 포함하는 약학적 조성물 및 이의 제조방법 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3468336D1 (en) * | 1983-06-22 | 1988-02-11 | Univ Ohio State Res Found | Small particle formation |
| JPH02227130A (ja) * | 1989-02-28 | 1990-09-10 | Taisho Pharmaceut Co Ltd | 球形微小凍結粒子の製造法 |
| FR2719587B1 (fr) * | 1994-05-03 | 1996-07-12 | Roussel Uclaf | Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments. |
-
1999
- 1999-08-26 FR FR9910810A patent/FR2797875B1/fr not_active Expired - Fee Related
-
2000
- 2000-08-02 TW TW089115526A patent/TWI272949B/zh not_active IP Right Cessation
- 2000-08-18 CO CO00062195A patent/CO5190666A1/es active IP Right Grant
- 2000-08-25 AR ARP000104426A patent/AR025398A1/es unknown
- 2000-08-28 SI SI200030287T patent/SI1212336T1/xx unknown
- 2000-08-28 PT PT00958756T patent/PT1212336E/pt unknown
- 2000-08-28 DE DE60006976T patent/DE60006976T2/de not_active Expired - Lifetime
- 2000-08-28 HR HR20020167A patent/HRP20020167B1/xx not_active IP Right Cessation
- 2000-08-28 CN CNB008120943A patent/CN1183151C/zh not_active Expired - Fee Related
- 2000-08-28 CZ CZ2002594A patent/CZ2002594A3/cs unknown
- 2000-08-28 EA EA200200294A patent/EA005080B1/ru not_active IP Right Cessation
- 2000-08-28 TR TR2002/00506T patent/TR200200506T2/xx unknown
- 2000-08-28 BR BRPI0013569-0A patent/BR0013569B1/pt not_active IP Right Cessation
- 2000-08-28 AT AT00958756T patent/ATE255590T1/de active
- 2000-08-28 ES ES00958756T patent/ES2209970T3/es not_active Expired - Lifetime
- 2000-08-28 PL PL353137A patent/PL204100B1/pl unknown
- 2000-08-28 UA UA2002032354A patent/UA73523C2/uk unknown
- 2000-08-28 ME MEP-201/08A patent/MEP20108A/xx unknown
- 2000-08-28 KR KR1020027002404A patent/KR100718222B1/ko not_active Expired - Fee Related
- 2000-08-28 US US10/049,874 patent/US6825218B1/en not_active Expired - Fee Related
- 2000-08-28 HK HK03101349.3A patent/HK1049167B/zh not_active IP Right Cessation
- 2000-08-28 IL IL14812800A patent/IL148128A0/xx active IP Right Grant
- 2000-08-28 EP EP00958756A patent/EP1212336B1/fr not_active Expired - Lifetime
- 2000-08-28 DK DK00958756T patent/DK1212336T3/da active
- 2000-08-28 SK SK253-2002A patent/SK287588B6/sk not_active IP Right Cessation
- 2000-08-28 RS YUP-132/02A patent/RS50433B/sr unknown
- 2000-08-28 HU HU0202842A patent/HU229075B1/hu not_active IP Right Cessation
- 2000-08-28 MX MXPA02001988A patent/MXPA02001988A/es active IP Right Grant
- 2000-08-28 WO PCT/FR2000/002393 patent/WO2001014393A2/fr not_active Ceased
- 2000-08-28 JP JP2001518723A patent/JP4871467B2/ja not_active Expired - Fee Related
- 2000-08-28 CA CA2382497A patent/CA2382497C/fr not_active Expired - Fee Related
- 2000-08-28 ME MEP-2008-201A patent/ME00112B/me unknown
- 2000-08-28 AU AU70181/00A patent/AU774385B2/en not_active Ceased
-
2002
- 2002-02-12 IL IL148128A patent/IL148128A/en not_active IP Right Cessation
- 2002-02-26 NO NO20020926A patent/NO322622B1/no not_active IP Right Cessation
- 2002-02-26 ZA ZA200201599A patent/ZA200201599B/en unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |