JP6121006B2 - 安定剤として生分解性表面活性ブロックコポリマを含むマイクロカプセル化のためのエマルジョン - Google Patents
安定剤として生分解性表面活性ブロックコポリマを含むマイクロカプセル化のためのエマルジョン Download PDFInfo
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- JP6121006B2 JP6121006B2 JP2016001869A JP2016001869A JP6121006B2 JP 6121006 B2 JP6121006 B2 JP 6121006B2 JP 2016001869 A JP2016001869 A JP 2016001869A JP 2016001869 A JP2016001869 A JP 2016001869A JP 6121006 B2 JP6121006 B2 JP 6121006B2
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- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
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- 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)
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/113—Multiple emulsions, e.g. oil-in-water-in-oil
-
- 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
- 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
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- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Dispersion Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Manufacturing Of Micro-Capsules (AREA)
Description
本出願は、2010年3月26日に出願された前の米国特許仮出願番号第61/317,738号(その全内容は参照により本明細書に組み込まれる)の優先権の恩典を主張する。
下記実施例は、本明細書で主張される化合物、組成物、物品、装置および/または方法がどのように製造され、評価されるかについての完全な開示および説明を当業者に提供するために提示され、純粋に本発明の例示であり、本発明者らが自らの発明とみなす範囲を限定することを意図しない。数値(例えば、量、温度、など)に関しては正確さを確保するように努力しているが、いくらかの誤差およびずれが説明されるべきである。別記されない限り、部は重量部であり、温度は℃で表され、または周囲温度であり、圧力は大気圧、またはその付近である。
酢酸ゴセレリンを含む微粒子調合物を、下記で記載されるダブルエマルジョン、溶媒抽出マイクロカプセル化プロセスを用いて調製した。調合物を水溶液中に溶解されたゴセレリンを用い、これを分散相(DP)溶液に分散させ、よって、ダブルエマルジョンプロセスのプライマリーエマルジョンを形成させることにより調製した。全ての微粒子調合物に対し、生分解性ポリマ50:50ポリ(DL−ラクチド−コ−グリコリド)(Lakeshore Biomatenalsブランド、SurModics Pharmaceuticals、Birmingham、AL)を使用して、DP溶液を調製した。
モデルタンパク質ウシ血清アルブミン(BSA)を使用して、表4に列挙されるバッチを調製した。バッチ00277−138は、1mLの2mg/mL PEG−PLポリマ界面活性剤溶液に溶解させた200mgのBSAを使用して調製した。この調合物を調製するために使用した他の処理条件は全てバッチ00277−067を調製するために使用したものと同じとした。対照として、第2のバッチ、バッチ0277−135を調製し、この場合、200mgのBSAを脱イオン水に溶解し;他の処理条件は全てバッチ00277−058を調製するために使用したものと同じとした。
Claims (3)
- (i)生分解性表面活性ブロックコポリマーを、水溶液としての1つ以上の非混和性相であって、生物活性剤を含む内側水相と混合し、
(ii)生分解性カプセル化ポリマーの有機溶媒溶液に、工程(i)で得られた生分解性表面活性ブロックコポリマーと生物活性剤を含む内側水相との混合物を分散させて、プライマリーエマルジョンを形成し、
(iii)工程(ii)で得られたプライマリーエマルジョンを、外側水性連続相中に乳化させてダブルエマルジョンを形成し、
(iv)前記生分解性カプセル化ポリマーのための有機溶媒を除去する、
ことを含む、微粒子を製造する方法。 - 前記表面活性ブロックコポリマーは非イオン性である、請求項1に記載の方法。
- 前記表面活性ブロックコポリマーは、ポリ(エチレングリコール)、ポリ(ビニルピロリドン)またはポリサッカライドの1つ以上の親水性ブロック;およびポリ(ラクチド)、ポリ(グリコリド)、ポリ(カプロラクトン)、ポリ(バレロラクトン)、ポリ(ヒドロキシブチラート)またはそれらのコポリマーの1つ以上の疎水性ブロックを含む、請求項1または2に記載の方法。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US31773810P | 2010-03-26 | 2010-03-26 | |
US61/317,738 | 2010-03-26 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013501506A Division JP5950901B2 (ja) | 2010-03-26 | 2011-03-25 | 安定剤として生分解性表面活性ブロックコポリマを含むマイクロカプセル化のためのエマルジョン |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2016053089A JP2016053089A (ja) | 2016-04-14 |
JP6121006B2 true JP6121006B2 (ja) | 2017-04-26 |
Family
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Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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JP2013501506A Expired - Fee Related JP5950901B2 (ja) | 2010-03-26 | 2011-03-25 | 安定剤として生分解性表面活性ブロックコポリマを含むマイクロカプセル化のためのエマルジョン |
JP2016001869A Active JP6121006B2 (ja) | 2010-03-26 | 2016-01-07 | 安定剤として生分解性表面活性ブロックコポリマを含むマイクロカプセル化のためのエマルジョン |
Family Applications Before (1)
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JP2013501506A Expired - Fee Related JP5950901B2 (ja) | 2010-03-26 | 2011-03-25 | 安定剤として生分解性表面活性ブロックコポリマを含むマイクロカプセル化のためのエマルジョン |
Country Status (8)
Country | Link |
---|---|
US (1) | US20110236496A1 (ja) |
EP (1) | EP2552412A2 (ja) |
JP (2) | JP5950901B2 (ja) |
CN (1) | CN103209685A (ja) |
AU (1) | AU2011230601B2 (ja) |
CA (1) | CA2794195A1 (ja) |
RU (1) | RU2617057C2 (ja) |
WO (1) | WO2011119903A2 (ja) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20130248176A1 (en) * | 2012-03-23 | 2013-09-26 | Glori Energy Inc. | Ultra low concentration surfactant flooding |
CN111315365A (zh) * | 2017-09-26 | 2020-06-19 | 纳奥米有限公司 | 用于通过双乳液技术制备微粒的方法 |
KR20200092940A (ko) * | 2017-10-06 | 2020-08-04 | 유니베르시떼 드 보르도 | 신규한 폴리머 유화제 및 소수성 또는 친수성 활성 화합물의 캡슐화를 위한 그의 용도 |
RU2702012C2 (ru) * | 2017-10-24 | 2019-10-03 | федеральное государственное бюджетное образовательное учреждение высшего образования "Волгоградский государственный медицинский университет" Министерства здравоохранения Российской Федерации | Способ получения фармацевтической композиции, содержащей пентоксифиллин |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5543158A (en) * | 1993-07-23 | 1996-08-06 | Massachusetts Institute Of Technology | Biodegradable injectable nanoparticles |
US5565215A (en) * | 1993-07-23 | 1996-10-15 | Massachusettes Institute Of Technology | Biodegradable injectable particles for imaging |
KR20010030891A (ko) * | 1997-10-03 | 2001-04-16 | 마크로메드 인코퍼레이션 | 가역적 열 겔화 성질을 갖는 생분해성 저분자량 트리블럭폴리(락티드-코-글리콜리드) 폴리에틸렌 글리콜 공중합체 |
KR100274842B1 (ko) * | 1998-10-01 | 2001-03-02 | 김효근 | 미립구를 이용한 레티노익산의 서방형 약물방출 시스템 |
GB0114197D0 (en) * | 2001-06-11 | 2001-08-01 | Syngenta Ltd | Reactive polymeric surfactants |
US6592899B2 (en) * | 2001-10-03 | 2003-07-15 | Macromed Incorporated | PLA/PLGA oligomers combined with block copolymers for enhancing solubility of a drug in water |
JP3916481B2 (ja) * | 2002-02-22 | 2007-05-16 | 三井化学株式会社 | 両親媒性共重合体 |
WO2003086369A2 (en) * | 2002-04-05 | 2003-10-23 | Valorisation-Recherche, Societe En Commandite | Stealthy polymeric biodegradable nanospheres and uses thereof |
US20080124400A1 (en) * | 2004-06-24 | 2008-05-29 | Angiotech International Ag | Microparticles With High Loadings Of A Bioactive Agent |
WO2006123361A2 (en) * | 2005-03-01 | 2006-11-23 | Sun Pharmaceutical Industries Limited | Microspheres containing goserelin or a pharmaceutically acceptable salt thereof |
EP1959925B1 (en) * | 2005-12-02 | 2016-11-23 | (OSI) Eyetech, Inc. | Controlled release microparticles |
JP2008088158A (ja) * | 2006-09-05 | 2008-04-17 | Toray Ind Inc | 親水性活性物質含有微粒子の製造方法 |
-
2011
- 2011-03-25 AU AU2011230601A patent/AU2011230601B2/en not_active Ceased
- 2011-03-25 JP JP2013501506A patent/JP5950901B2/ja not_active Expired - Fee Related
- 2011-03-25 US US13/071,633 patent/US20110236496A1/en not_active Abandoned
- 2011-03-25 CN CN2011800153779A patent/CN103209685A/zh active Pending
- 2011-03-25 WO PCT/US2011/029900 patent/WO2011119903A2/en active Application Filing
- 2011-03-25 EP EP11712434A patent/EP2552412A2/en not_active Withdrawn
- 2011-03-25 RU RU2012145462A patent/RU2617057C2/ru not_active IP Right Cessation
- 2011-03-25 CA CA2794195A patent/CA2794195A1/en not_active Abandoned
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2016
- 2016-01-07 JP JP2016001869A patent/JP6121006B2/ja active Active
Also Published As
Publication number | Publication date |
---|---|
CA2794195A1 (en) | 2011-09-29 |
WO2011119903A3 (en) | 2012-05-03 |
JP5950901B2 (ja) | 2016-07-13 |
JP2016053089A (ja) | 2016-04-14 |
RU2012145462A (ru) | 2014-05-10 |
WO2011119903A2 (en) | 2011-09-29 |
RU2617057C2 (ru) | 2017-04-19 |
EP2552412A2 (en) | 2013-02-06 |
AU2011230601B2 (en) | 2015-04-02 |
AU2011230601A1 (en) | 2012-10-11 |
US20110236496A1 (en) | 2011-09-29 |
CN103209685A (zh) | 2013-07-17 |
JP2013523653A (ja) | 2013-06-17 |
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