CA2916301C - Preparation of polylactide-polyglycolide microparticles having a sigmoidal release profile - Google Patents
Preparation of polylactide-polyglycolide microparticles having a sigmoidal release profile Download PDFInfo
- Publication number
- CA2916301C CA2916301C CA2916301A CA2916301A CA2916301C CA 2916301 C CA2916301 C CA 2916301C CA 2916301 A CA2916301 A CA 2916301A CA 2916301 A CA2916301 A CA 2916301A CA 2916301 C CA2916301 C CA 2916301C
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- Prior art keywords
- phase
- microparticles
- risperidone
- polymer
- organic solvent
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- 239000011859 microparticle Substances 0.000 title claims description 84
- 238000002360 preparation method Methods 0.000 title claims description 27
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- 229920000954 Polyglycolide Polymers 0.000 title description 2
- 229920000642 polymer Polymers 0.000 claims description 74
- 239000012071 phase Substances 0.000 claims description 73
- 238000000034 method Methods 0.000 claims description 59
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims description 55
- 229960001534 risperidone Drugs 0.000 claims description 52
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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
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
-
- 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
-
- 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
- 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
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J13/00—Colloid chemistry, e.g. the production of colloidal materials or their solutions, not otherwise provided for; Making microcapsules or microballoons
- B01J13/02—Making microcapsules or microballoons
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J3/00—Processes of treating or compounding macromolecular substances
- C08J3/12—Powdering or granulating
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J3/00—Processes of treating or compounding macromolecular substances
- C08J3/12—Powdering or granulating
- C08J3/14—Powdering or granulating by precipitation from solutions
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J2300/00—Characterised by the use of unspecified polymers
- C08J2300/16—Biodegradable polymers
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J2367/00—Characterised by the use of polyesters obtained by reactions forming a carboxylic ester link in the main chain; Derivatives of such polymers
- C08J2367/04—Polyesters derived from hydroxy carboxylic acids, e.g. lactones
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Polymers & Plastics (AREA)
- Dispersion Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
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| EP2013001821 | 2013-06-20 | ||
| EPPCT/EP2013/001821 | 2013-06-20 | ||
| PCT/EP2014/001652 WO2014202214A1 (en) | 2013-06-20 | 2014-06-18 | Preparation of polylactide-polyglycolide microparticles having a sigmoidal release profile |
Publications (2)
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| CA2916301A1 CA2916301A1 (en) | 2014-12-24 |
| CA2916301C true CA2916301C (en) | 2020-01-07 |
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| CA2916301A Active CA2916301C (en) | 2013-06-20 | 2014-06-18 | Preparation of polylactide-polyglycolide microparticles having a sigmoidal release profile |
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| DK (1) | DK3010962T4 (enExample) |
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| FI (1) | FI3010962T4 (enExample) |
| HU (1) | HUE036141T2 (enExample) |
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| SA (1) | SA515370296B1 (enExample) |
| WO (1) | WO2014202214A1 (enExample) |
| ZA (1) | ZA201509354B (enExample) |
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| KR20170036768A (ko) * | 2014-07-30 | 2017-04-03 | 메르크 파텐트 게엠베하 | 미세결정성 셀룰로오스를 포함하는 직접 압축성 조성물 |
| JP2016102093A (ja) * | 2014-11-28 | 2016-06-02 | ニプロ株式会社 | 塩基性の求核化合物を含有するマイクロカプセルの製造方法 |
| US20170079985A1 (en) | 2015-09-21 | 2017-03-23 | Teva Pharmaceuticals International Gmbh | Sustained release olanzapine formulations |
| JP2020511483A (ja) | 2017-03-20 | 2020-04-16 | テバ・ファーマシューティカルズ・インターナショナル・ゲーエムベーハーＴｅｖａ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｔｅｒｎａｔｉｏｎａｌ ＧｍｂＨ | 徐放性オランザピン製剤 |
| KR102047983B1 (ko) * | 2017-11-30 | 2019-11-22 | 주식회사 지투지바이오 | 안전성 및 저장 안정성이 향상된 생분해성 미립구의 제조방법 |
| GR1009870B (el) * | 2019-07-09 | 2020-11-12 | Φαρματεν Α.Β.Ε.Ε. | Φαρμακευτικο σκευασμα που περιλαμβανει ενα ατυπο αντιψυχωσικο φαρμακο και μεθοδος παρασκευης αυτου |
| WO2021134623A1 (zh) * | 2019-12-31 | 2021-07-08 | 广州帝奇医药技术有限公司 | 一种叔胺药物组合物及其产业化批量制备方法 |
| EP4125823A1 (en) | 2020-03-30 | 2023-02-08 | Biological E Limited | Risperidone microspheres, process for their prepartion and uses thereof |
| KR102259589B1 (ko) * | 2020-11-30 | 2021-06-02 | (주)인벤티지랩 | 미소구체 제조 시스템 및 미소구체 제조 방법 |
| EP4277661A1 (en) | 2021-01-18 | 2023-11-22 | Anton Frenkel | Pharmaceutical dosage form |
| EP4297753A4 (en) * | 2021-02-24 | 2025-01-01 | Oakwood Laboratories, Llc | Microsphere formulations comprising lurasidone and methods for making and using the same |
| WO2023281406A1 (en) | 2021-07-06 | 2023-01-12 | Mark Hasleton | Treatment of serotonin reuptake inhibitor withdrawal syndrome |
| GR1010327B (el) * | 2021-10-06 | 2022-10-17 | Φαρματεν Α.Β.Ε.Ε., | Παρατεταμενης αποδεσμευσης ενεσιμο φαρμακευτικο σκευασμα λεβοθυροξινης και μεθοδος παρασκευης αυτου |
| WO2025135778A1 (ko) * | 2023-12-18 | 2025-06-26 | 주식회사 포스테라헬스사이언스 | 약물의 특성에 따른 활성형 미립자의 제조 방법, 이의 제조 방법으로 제조된 활성형 미립자 및 상기 활성형 미립자를 이용한 약물을 포함하는 장기 지속 제형의 제조 방법 |
| WO2025207396A1 (en) * | 2024-03-27 | 2025-10-02 | Avidence Therapeutics, Inc. | Microsphere-based injectable rofecoxib formulation |
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| US5478564A (en) * | 1990-02-22 | 1995-12-26 | Teva Pharmaceutical Industries, Ltd. | Preparation of microparticles for controlled release of water-soluble substances |
| US5288496A (en) * | 1990-05-15 | 1994-02-22 | Stolle Research & Development Corporation | Growth promoters for animals |
| AU722884B2 (en) * | 1996-01-24 | 2000-08-10 | United States Government Represented By The Secretary Of The Army | Novel "burst-free" sustained release poly-(lactide/glycolide) microspheres |
| US5792477A (en) * | 1996-05-07 | 1998-08-11 | Alkermes Controlled Therapeutics, Inc. Ii | Preparation of extended shelf-life biodegradable, biocompatible microparticles containing a biologically active agent |
| US6194006B1 (en) * | 1998-12-30 | 2001-02-27 | Alkermes Controlled Therapeutics Inc. Ii | Preparation of microparticles having a selected release profile |
| US6264987B1 (en) | 2000-05-19 | 2001-07-24 | Alkermes Controlled Therapeutics Inc. Ii | Method for preparing microparticles having a selected polymer molecular weight |
| US7690026B2 (en) * | 2005-08-22 | 2010-03-30 | Microsoft Corporation | Distributed single sign-on service |
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- 2014-06-18 CA CA2916301A patent/CA2916301C/en active Active
- 2014-06-18 PT PT147335244T patent/PT3010962T/pt unknown
- 2014-06-18 WO PCT/EP2014/001652 patent/WO2014202214A1/en not_active Ceased
- 2014-06-18 RU RU2016101418A patent/RU2658004C2/ru active
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Also Published As
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| DK3010962T4 (da) | 2023-04-17 |
| DK3010962T3 (en) | 2017-10-23 |
| ES2640486T5 (es) | 2023-04-28 |
| AU2014283692A1 (en) | 2016-01-21 |
| AU2014283692B2 (en) | 2017-04-27 |
| ZA201509354B (en) | 2017-07-26 |
| CN105308101B (zh) | 2018-10-23 |
| WO2014202214A1 (en) | 2014-12-24 |
| US20160143851A1 (en) | 2016-05-26 |
| LT3010962T (lt) | 2017-09-25 |
| RU2016101418A (ru) | 2017-07-25 |
| PT3010962T (pt) | 2017-09-05 |
| RU2658004C2 (ru) | 2018-06-19 |
| US9943484B2 (en) | 2018-04-17 |
| SA515370296B1 (ar) | 2017-10-12 |
| ES2640486T3 (es) | 2017-11-03 |
| JP6464154B2 (ja) | 2019-02-06 |
| JP2017507895A (ja) | 2017-03-23 |
| CN105308101A (zh) | 2016-02-03 |
| CA2916301A1 (en) | 2014-12-24 |
| FI3010962T4 (fi) | 2023-05-04 |
| HUE036141T2 (hu) | 2018-06-28 |
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Effective date: 20170418 |