JP2007518783A - Dopeおよびp80の非ラメラ組成物 - Google Patents
Dopeおよびp80の非ラメラ組成物 Download PDFInfo
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- JP2007518783A JP2007518783A JP2006550277A JP2006550277A JP2007518783A JP 2007518783 A JP2007518783 A JP 2007518783A JP 2006550277 A JP2006550277 A JP 2006550277A JP 2006550277 A JP2006550277 A JP 2006550277A JP 2007518783 A JP2007518783 A JP 2007518783A
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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
- A61K9/127—Liposomes
- A61K9/1274—Non-vesicle bilayer structures, e.g. liquid crystals, tubules, cubic phases, cochleates; Sponge phases
-
- 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
- A61K31/66—Phosphorus compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
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- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Dispersion Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
Description
a)少なくとも50%のジオレオイルホスファチジルエタノールアミン(DOPE)と、
b)1〜50%のポリソルベート80(P80)と、
を含み(全ての部はa+bの重量の合計に対する重量比で示される)、
非ラメラ粒子を含むか又は水性流体と接触させると非ラメラ粒子を形成する粒子組成物を提供する。
DOPE(アヴァンティポーラーリピッズ(Avanti Polar Lipids)社、米国、0.80g)とP80(0.2g)を脱イオン水(49.0g)中で混合し、マグネチックスターラーで24時間攪拌することによって、キュービックおよびラメラ粒子の分散液を形成した。
実施例1で調製した分散液の相挙動を、周囲温度での10日間の保存の前後に調べた。粒度または相挙動の変化は見られなかった。
3.1 溶血
実施例1により得られた分散液(白色)を、ミクロ流動化装置において周囲温度で10分間(8回)高圧(350バール)で均質化し、オートクレーブ(120℃、20分)し、室温まで冷却した。
実施例3.1と同様にDOPE/P80製剤を調製し、ウサギモデルにおいて発熱性試験を行った。組成物は、少なくとも5ml/kg(全両親媒性物質5重量%)の用量までは非発熱性であることがわかった。
実施例3.1と同様にDOPE/P80およびGMOを基剤とする組成物を調製し、ラットモデルにおいて急性毒性試験を行った。
Claims (13)
- a)少なくとも50%のジオレオイルホスファチジルエタノールアミン(DOPE)と、
b)1〜50%のポリソルベート80(P80)と、
を含み(全ての部はa+bの重量の合計に対する重量比で示される)、
非ラメラ粒子を含むか又は水性流体と接触させると非ラメラ粒子を形成する粒子組成物。 - a)少なくとも50%のジオレオイルホスファチジルエタノールアミン(DOPE)と、
b)1〜50%のポリソルベート80(P80)と、
c)必要に応じて溶媒と、
からなる両親媒性担体製剤を含み(全ての部はa+bの重量の合計に対する重量比で示される)、
非ラメラ粒子を含むか又は水性流体と接触させると非ラメラ粒子を形成し、
該担体製剤は、ラットにおいて、対象の1kgあたりの成分a+bが少なくとも1000mgまでのレベルでは急性毒性を示さない粒子組成物。 - a)少なくとも50%のジオレオイルホスファチジルエタノールアミン(DOPE)と、
b)1〜50%のポリソルベート80(P80)と、
c)必要に応じて溶媒と、
からなる両親媒性担体製剤を含み(全ての部はa+bの重量の合計に対する重量比で示される)、
非ラメラ粒子を含むか又は水性流体と接触させると非ラメラ粒子を形成し、
該担体製剤は、ウサギにおいて、対象の1kgあたりの成分a+bの5%分散液が少なくとも5mlまでのレベルで非経口投与した場合、発熱性を示さない粒子組成物。 - 少なくとも1つの活性剤をさらに含む請求項1から3のいずれかに記載の組成物。
- 少なくとも50%の非ラメラ粒子を含む請求項1から4のいずれかに記載の組成物。
- 水性流体と接触すると少なくとも50%の非ラメラ粒子を形成する請求項1から4のいずれかに記載の組成物。
- 前記水性流体が体液である請求項6に記載の組成物。
- 前記粒子の平均粒度が10〜150μmである請求項1から7のいずれかに記載の組成物。
- 前記粒子がコロイド状である請求項1から7のいずれかに記載の組成物。
- 前記粒子が、少なくとも10日の室温での保存に対して相挙動および粒度の点で安定している請求項9に記載の組成物。
- 乾燥粉末状である請求項1から10のいずれかに記載の組成物。
- 請求項1から11のいずれかに記載の組成物を含む医薬製剤。
- 少なくとも1つの製薬上許容可能な担体または賦形剤をさらに含む請求項12に記載の製剤。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0401513.7 | 2004-01-23 | ||
GBGB0401513.7A GB0401513D0 (en) | 2004-01-23 | 2004-01-23 | Compositions |
PCT/GB2005/000200 WO2005070392A2 (en) | 2004-01-23 | 2005-01-21 | Non-lamellar compositions of dioleoyl phosphatidylethanolamine and polysorbate 80 |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2007518783A true JP2007518783A (ja) | 2007-07-12 |
JP4920425B2 JP4920425B2 (ja) | 2012-04-18 |
Family
ID=31971358
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006550277A Expired - Fee Related JP4920425B2 (ja) | 2004-01-23 | 2005-01-21 | Dopeおよびp80の非ラメラ組成物 |
Country Status (8)
Country | Link |
---|---|
US (1) | US8187629B2 (ja) |
EP (1) | EP1713445B1 (ja) |
JP (1) | JP4920425B2 (ja) |
AT (1) | ATE489941T1 (ja) |
CA (1) | CA2554051C (ja) |
DE (1) | DE602005025082D1 (ja) |
GB (1) | GB0401513D0 (ja) |
WO (1) | WO2005070392A2 (ja) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE602005026998D1 (de) * | 2005-01-14 | 2011-04-28 | Camurus Ab | Somatostatin-analog-formulierungen |
ES2400034T3 (es) | 2005-01-14 | 2013-04-05 | Camurus Ab | Formulaciones bioadhesivas tópicas |
US9649382B2 (en) | 2005-01-14 | 2017-05-16 | Camurus Ab | Topical bioadhesive formulations |
KR101245022B1 (ko) | 2005-01-21 | 2013-03-19 | 카무러스 에이비 | 약제학적 지질 조성물 |
DK1888031T3 (da) * | 2005-06-06 | 2013-02-18 | Camurus Ab | GLP-1-analogformuleringer |
GB0711656D0 (en) | 2007-06-15 | 2007-07-25 | Camurus Ab | Formulations |
GB0716385D0 (en) | 2007-08-22 | 2007-10-03 | Camurus Ab | Formulations |
GB0815435D0 (en) | 2008-08-22 | 2008-10-01 | Camurus Ab | Formulations |
PE20141297A1 (es) | 2011-12-05 | 2014-10-09 | Camurus Ab | Formulaciones peptidicas robustas de liberacion controlada |
MX350964B (es) | 2012-05-25 | 2017-09-27 | Camurus Ab | Formulaciones de agonistas del receptor de somatostatina. |
WO2024047037A1 (en) * | 2022-08-30 | 2024-03-07 | ETH Zürich | Compositions for parenteral sustained release delivery of hydrophilic drugs |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001080897A2 (en) * | 2000-04-21 | 2001-11-01 | Vical Incorporated | Compositions and methods for in vivo delivery of polynucleotide-based therapeutics |
JP2005529949A (ja) * | 2002-06-13 | 2005-10-06 | リオトロピック セラピュティックス アイエヌシー. | 被覆粒子、製造方法および使用 |
JP2007501213A (ja) * | 2003-08-04 | 2007-01-25 | カムルス エービー | 両親媒性粒子に活性因子を装填する方法 |
JP2007518784A (ja) * | 2004-01-23 | 2007-07-12 | カムルス エービー | 三元非ラメラ脂質組成物 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2133391T3 (es) * | 1991-10-04 | 1999-09-16 | Gs Dev Ab | Particulas, metodo para preparar dichas particulas y usos de las mismas. |
US6120794A (en) * | 1995-09-26 | 2000-09-19 | University Of Pittsburgh | Emulsion and micellar formulations for the delivery of biologically active substances to cells |
EP0935415B1 (en) * | 1996-05-01 | 2006-11-22 | Imarx Pharmaceutical Corp. | In vitro methods for delivering nucleic acids into a cell |
-
2004
- 2004-01-23 GB GBGB0401513.7A patent/GB0401513D0/en not_active Ceased
-
2005
- 2005-01-21 DE DE602005025082T patent/DE602005025082D1/de active Active
- 2005-01-21 JP JP2006550277A patent/JP4920425B2/ja not_active Expired - Fee Related
- 2005-01-21 US US10/586,778 patent/US8187629B2/en active Active
- 2005-01-21 EP EP05701963A patent/EP1713445B1/en active Active
- 2005-01-21 WO PCT/GB2005/000200 patent/WO2005070392A2/en active Application Filing
- 2005-01-21 CA CA2554051A patent/CA2554051C/en not_active Expired - Fee Related
- 2005-01-21 AT AT05701963T patent/ATE489941T1/de not_active IP Right Cessation
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001080897A2 (en) * | 2000-04-21 | 2001-11-01 | Vical Incorporated | Compositions and methods for in vivo delivery of polynucleotide-based therapeutics |
JP2005529949A (ja) * | 2002-06-13 | 2005-10-06 | リオトロピック セラピュティックス アイエヌシー. | 被覆粒子、製造方法および使用 |
JP2007501213A (ja) * | 2003-08-04 | 2007-01-25 | カムルス エービー | 両親媒性粒子に活性因子を装填する方法 |
JP2007501115A (ja) * | 2003-08-04 | 2007-01-25 | カムルス エービー | 両親媒性粒子の特性を改良する方法 |
JP2007518784A (ja) * | 2004-01-23 | 2007-07-12 | カムルス エービー | 三元非ラメラ脂質組成物 |
Also Published As
Publication number | Publication date |
---|---|
US20070281030A1 (en) | 2007-12-06 |
US8187629B2 (en) | 2012-05-29 |
WO2005070392A3 (en) | 2006-01-26 |
JP4920425B2 (ja) | 2012-04-18 |
WO2005070392A2 (en) | 2005-08-04 |
EP1713445B1 (en) | 2010-12-01 |
GB0401513D0 (en) | 2004-02-25 |
EP1713445A2 (en) | 2006-10-25 |
DE602005025082D1 (de) | 2011-01-13 |
CA2554051C (en) | 2013-11-26 |
CA2554051A1 (en) | 2005-08-04 |
ATE489941T1 (de) | 2010-12-15 |
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