JP2014501270A - 部分フッ素化アルカンを含むo/wエマルション - Google Patents
部分フッ素化アルカンを含むo/wエマルション Download PDFInfo
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
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- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
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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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
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- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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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
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0026—Blood substitute; Oxygen transporting formulations; Plasma extender
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Abstract
Description
本発明は、(a)式RFRHまたはRFRHRFに従う部分フッ素化アルカンを含む分散相、(b)水性連続相、および(c)少なくとも1つの界面活性剤を含む、物理的に安定なO/Wエマルション形態の新規な液体組成物を提供し、ここで、RFは、20個以下の炭素原子を含む全フッ素化炭化水素セグメントであり、RHは、3〜20個の炭素原子を含む非フッ素化炭化水素セグメントである。全フッ素化化合物は、分散相には存在しない。この組成物は、分散相の平均液滴径が約1μmよりも小さいことをさらに特徴とする。
−ペグ化グリセリド、例えばマクロゴール−15−ヒドロキシステアレート(例、ソルトール(Solutol)(登録商標)HS15)、マクロゴールグリセロールリシノレエート−35(例、クレモフォール(Cremophor)(登録商標)EL)、マクロゴールグリセロールヒドロキシステアレート−40(例、クレモフォール(登録商標)RH40)、マクロゴール−1000−グリセロールモノラウレート、マクロゴール−1000−グリセロールモノステアレート、およびマクロゴール−1000−グリセロールモノオレエートなど;
−ペグ化脂肪酸、例えばマクロゴールステアレート400、ポリオキシル40ステアレート、およびポリオキシル60ステアレートなど;
−ペグ化脂肪アルコール、例えばマクロゴールラウリルエーテル、ポリオキシル20セトステアリルエーテル、およびポリオキシル10オレイルエーテルなど;
−ペグ化ソルビタン脂肪酸エステル、例えばポリソルベート20、ポリソルベート40、ポリソルベート60、およびポリソルベート80(例、Tween(登録商標)20/40/60/80)など;ならびに
−ポリオキシエチレンおよびポリオキシプロピレンのトリブロック共重合体、例えばポロキサマー124、ポロキサマー188、ポロキサマー237、ポロキサマー338、およびポロキサマー407などが挙げられる。上記から、ポリソルベートが特に好ましい。
実施例
Claims (15)
- (a)式
RFRH
または
RFRHRF
に従う部分フッ素化アルカンを含む分散相と;
(b)水性連続相と;
(c)少なくとも1つの界面活性剤と;
を含む、物理的に安定なO/Wエマルションの形態の液体組成物であって
〔式中、
RFは、20個以下の炭素原子を含む全フッ素化炭化水素セグメントであり、RHは、3〜20個の炭素原子を含む非フッ素化炭化水素セグメントである〕、全フッ素化化合物が前記分散相に存在せず、かつ、前記分散相の平均液滴径が約1μmよりも小さい、液体組成物。 - (a)式
RFRH
に従う部分フッ素化アルカンを含む分散相と;
(b)水性連続相と;
(c)少なくとも1つの界面活性剤と;
を含む、物理的に安定なO/Wエマルションの形態の液体組成物であって
〔式中、
RFは、4〜12個の炭素原子を含む直鎖状全フッ素化炭化水素セグメントであり、RHは、4〜8個の炭素原子を含む直鎖状アルキル基である〕、かつ、前記分散相の平均液滴径は、約1μmよりも小さい、液体組成物。 - 前記部分フッ素化アルカンが、F4H5、F4H6、F4H8、F6H6およびF6H8から選択される、請求項1または2に記載の組成物。
- 無菌であり、かつ/または加熱殺菌可能であることをさらに特徴とする、先行する請求項のいずれか一項に記載の組成物。
- 非イオン性界面活性剤を含み、前記水性連続相が塩またはイオン化合物を含むことをさらに特徴とする、先行する請求項のいずれか一項に記載の組成物。
- イオン性界面活性剤を含み、前記水性連続相が、生理学的に許容される非イオン性浸透圧調整剤を含むことをさらに特徴とする、請求項1〜4に記載の組成物。
- 前記連続する水相が、緩衝液およびアミノ酸から選択される化合物を含む、先行する請求項のいずれか一項に記載の組成物。
- 前記分散相が、医薬品有効成分を含む、先行する請求項のいずれか一項に記載の組成物。
- 前記医薬品有効成分がプロポフォールである、請求項8に記載の組成物。
- 前記分散相中のプロポフォールの濃度が、少なくとも約10重量%である、請求項9に記載の組成物。
- 麻酔の導入および/または維持に、または鎮静のために使用するための、請求項9または10に記載の組成物であって、前記使用が、前記組成物を必要とする患者への前記組成物の非経口投与を含む、組成物。
- 前記分散相が、前記エマルションの少なくとも約50重量%に相当する、先行する請求項のいずれか一項に記載の組成物。
- 医薬として使用するための、請求項1〜12に記載の組成物。
- 前記医薬が、局所投与される医薬である、請求項13に記載の医薬として使用するための組成物。
- 臓器移植片の保存および/または貯蔵および/または輸送のための媒体としての、請求項1〜8に記載の組成物の使用。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11150064.1 | 2011-01-04 | ||
EP11150064 | 2011-01-04 | ||
PCT/EP2012/050043 WO2012093113A1 (en) | 2011-01-04 | 2012-01-03 | O/w-emulsions comprising semifluorinated alkanes |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2014501270A true JP2014501270A (ja) | 2014-01-20 |
JP6073244B2 JP6073244B2 (ja) | 2017-02-01 |
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Application Number | Title | Priority Date | Filing Date |
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JP2013546732A Expired - Fee Related JP6073244B2 (ja) | 2011-01-04 | 2012-01-03 | 部分フッ素化アルカンを含むo/wエマルション |
Country Status (15)
Country | Link |
---|---|
US (5) | US20140004197A1 (ja) |
EP (2) | EP2661280B1 (ja) |
JP (1) | JP6073244B2 (ja) |
KR (1) | KR101910213B1 (ja) |
CN (1) | CN103313729B (ja) |
AU (1) | AU2012204932B2 (ja) |
BR (1) | BR112013016661B1 (ja) |
CA (1) | CA2819988C (ja) |
DK (2) | DK3202421T3 (ja) |
ES (2) | ES2675242T3 (ja) |
MX (1) | MX353154B (ja) |
PL (2) | PL2661280T3 (ja) |
PT (2) | PT2661280T (ja) |
TR (2) | TR201808752T4 (ja) |
WO (1) | WO2012093113A1 (ja) |
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CA2883002C (en) | 2012-09-12 | 2019-05-21 | Novaliq Gmbh | Compositions comprising mixtures of semifluorinated alkanes |
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EP2783703A1 (en) * | 2013-03-25 | 2014-10-01 | B. Braun Melsungen AG | Semifluorocarbon compound containing contrast agent |
US10273298B2 (en) | 2013-07-23 | 2019-04-30 | Novaliq Gmbh | Stabilized antibody compositions |
CN112641720A (zh) * | 2014-03-03 | 2021-04-13 | 诺华股份有限公司 | 硫辛酸胆碱酯组合物及使用方法 |
EP3722274B1 (en) | 2015-09-30 | 2023-06-07 | Novaliq GmbH | 2-perfluorobutyl pentane for ophthalmic administration |
CN110403923B (zh) | 2015-09-30 | 2021-09-21 | 诺瓦利克有限责任公司 | 半氟化化合物和其组合物 |
DK3442480T3 (da) | 2016-06-23 | 2020-01-13 | Novaliq Gmbh | Fremgangsmåde til topisk indgivelse |
ES2969758T3 (es) | 2016-09-22 | 2024-05-22 | Novaliq Gmbh | Composiciones farmacéuticas para usar en la terapia de la blefaritis |
CN109906085B (zh) | 2016-09-23 | 2024-03-08 | 诺瓦利克有限责任公司 | 含有环孢素的眼用组合物 |
AU2018253944B2 (en) | 2017-04-21 | 2022-09-15 | Dermaliq Therapeutics, Inc. | Iodine compositions |
WO2018202835A1 (en) | 2017-05-05 | 2018-11-08 | Novaliq Gmbh | Process for the production of semifluorinated alkanes |
EP3621601A1 (en) | 2017-05-12 | 2020-03-18 | Novaliq GmbH | Pharmaceutical compositions comprosing semifluorinated alkanes for the treatment of contact lense-related conditions |
US11723861B2 (en) | 2017-09-27 | 2023-08-15 | Novaliq Gmbh | Ophthalmic compositions comprising latanoprost for use in the treatment of ocular diseases |
US11896559B2 (en) | 2017-10-04 | 2024-02-13 | Novaliq Gmbh | Opthalmic compositions comprising F6H8 |
SG11202007858VA (en) | 2018-03-02 | 2020-09-29 | Novaliq Gmbh | Pharmaceutical compositions comprising nebivolol |
WO2020064556A1 (en) | 2018-09-27 | 2020-04-02 | Novaliq Gmbh | Topical sunscreen formulation |
SG11202102820VA (en) | 2018-10-12 | 2021-04-29 | Novaliq Gmbh | Ophthalmic composition for treatment of dry eye disease |
US11439653B1 (en) | 2021-03-30 | 2022-09-13 | Epalex Corporation | Fospropofol formulations |
US11628178B2 (en) | 2019-03-26 | 2023-04-18 | Epalex Corporation | Fospropofol methods and compositions |
US11478490B1 (en) | 2021-03-30 | 2022-10-25 | Epalex Corporation | Fospropofol formulations |
US11547714B2 (en) | 2020-02-05 | 2023-01-10 | Epalex Corporation | Fospropofol salts, methods and compositions |
EP3912621A1 (en) * | 2020-05-19 | 2021-11-24 | tesa Labtec GmbH | Propofol for diagnosis of primary headache |
FR3112475B1 (fr) | 2020-07-20 | 2023-11-10 | Naos Inst Of Life Science | formulation écobiologique, compatible avec la vie cellulaire, utilisable dans les domaines cosmétiques, dermopharmaceutiques ou vétérinaires |
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- 2012-01-03 KR KR1020137018703A patent/KR101910213B1/ko active IP Right Grant
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- 2012-01-03 BR BR112013016661-4A patent/BR112013016661B1/pt active IP Right Grant
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- 2012-01-03 JP JP2013546732A patent/JP6073244B2/ja not_active Expired - Fee Related
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- 2012-01-03 PT PT12700455T patent/PT2661280T/pt unknown
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- 2012-01-03 DK DK17159788.3T patent/DK3202421T3/en active
- 2012-01-03 CN CN201280004613.1A patent/CN103313729B/zh active Active
- 2012-01-03 WO PCT/EP2012/050043 patent/WO2012093113A1/en active Application Filing
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2017
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2019
- 2019-01-28 US US16/259,037 patent/US20190224123A1/en not_active Abandoned
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2020
- 2020-04-30 US US16/863,918 patent/US20200360285A1/en not_active Abandoned
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2022
- 2022-12-23 US US18/146,306 patent/US20230139672A1/en active Pending
Patent Citations (3)
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JPH06509022A (ja) * | 1991-07-17 | 1994-10-13 | アライアンス・ファーマスーティカル・コーポレイション | 炭化フッ素および親油性/親フッ素性有機化合物を含む調製物、ならびにそれらの用途 |
JP2000511157A (ja) * | 1995-09-29 | 2000-08-29 | マイネルト,ハッソ | セミフルオロアルカン及びその使用 |
JP2004516265A (ja) * | 2000-12-20 | 2004-06-03 | アンファスター・ファーマスーティカルズ・インコーポレイション | 強化された微生物阻害を有するプロポフォール製剤 |
Non-Patent Citations (1)
Title |
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JPN6015042485; BIOMAT., ART. CELLS & IMMOB. BIOTECH. Vol.21, No.5, 1993, p.583-595 * |
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