JP2015508804A - モダフィニルをベースとした医薬組成物を得るための方法、得られる医薬組成物、及びその使用 - Google Patents
モダフィニルをベースとした医薬組成物を得るための方法、得られる医薬組成物、及びその使用 Download PDFInfo
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- JP2015508804A JP2015508804A JP2014559269A JP2014559269A JP2015508804A JP 2015508804 A JP2015508804 A JP 2015508804A JP 2014559269 A JP2014559269 A JP 2014559269A JP 2014559269 A JP2014559269 A JP 2014559269A JP 2015508804 A JP2015508804 A JP 2015508804A
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- modafinil
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
- A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
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- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Anesthesiology (AREA)
- Psychiatry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
- Closures For Containers (AREA)
Abstract
Description
である。
・大きな拡散係数及び小さな粘度係数;
・表面張力がなく、したがって超臨界流体の浸透力が増大する。
次いで種々のパラメータを修正した:
− マンニトール用に担体を変更、
− 活性成分負荷を30%までの負荷レベルに増大、
− Sモダフィニルを使用、
− CO2以外の溶媒、特にテトラフルオロエタン、より特別には1,1,1,2−テトラフルオロエタン。
− S−モダフィニル粒子に関して良好な捕捉効率を有する、均一な滴定製剤の調製;
− DSCプロファイルは、先のタスク中に同じ操作条件下で調製された製剤のプロファイルと類似している;
− 製剤のSEM観察は、Sモダフィニルが、1マイクロメートル程度のサイズの粒子の形態に結晶化されたことを示すようである;
− 溶解動態は、両方のタイプの製剤に関して再現性があり、初期に得られた結果に類似している。超臨界CO2製剤の溶解速度はむしろ遅い。テトラフルオロエタンによる製剤は、より速い溶解プロファイルを有する。
− 成分のそれぞれを計量した後、添加剤を、その重量を増やしながら、混合機に続けて導入する;
− 次いで混合物をシフトさせて、可能性あるクラスターを除去する;
− 次いで得られた混合物を圧密化し、250rpmで1.25mmのアパーチャを有するグリッド上でキャリブレーションする;
− 次いでSVIAC圧縮機での圧縮へと進行させる。
製剤
DASC00512:
Claims (10)
- 超臨界状態の流体にSモダフィニルを可溶化するステップ、次いで前記流体の膨張後に、顆粒として得られる不活性担体により表面に吸収させることによって前記Sモダフィニルを回収するステップからなることを特徴とする、医薬組成物を得るための方法。
- 前記超臨界流体がCO2であることを特徴とする、請求項1に記載の方法。
- 前記超臨界流体がテトラフルオロエタンであることを特徴とする、請求項1に記載の方法。
- 前記担体がマンニトールであることを特徴とする、請求項1から3までのいずれか一項に記載の方法。
- 前記担体が無水ラクトースであることを特徴とする、請求項1から3までのいずれか一項に記載の方法。
- 請求項1から5までのいずれか一項に記載の方法により得られる医薬組成物。
- 経口形態として得られることを特徴とする、請求項6に記載の医薬組成物。
- 前記経口形態がSモダフィニルを25から200mg含有することを特徴とする、請求項7に記載の医薬組成物。
- 前記経口形態がSモダフィニルを50から100mg含有することを特徴とする、請求項8に記載の医薬組成物。
- 前記経口形態が錠剤であることを特徴とする、請求項7から9までのいずれか一項に記載の医薬組成物。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR1200580A FR2987266B1 (fr) | 2012-02-28 | 2012-02-28 | Procede d'obtention d'une composition pharmaceutique a base de modafinil, composition pharmaceutique ainsi obtenue et son application |
PCT/FR2013/000051 WO2013128087A1 (fr) | 2012-02-28 | 2013-02-25 | Procédé d'obtention d'une composition pharmaceutique à base de modafinil, composition pharmaceutique ainsi obtenue et son application |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2015508804A true JP2015508804A (ja) | 2015-03-23 |
JP6026566B2 JP6026566B2 (ja) | 2016-11-16 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP2014559269A Expired - Fee Related JP6026566B2 (ja) | 2012-02-28 | 2013-02-25 | モダフィニルをベースとした医薬組成物を得るための方法、得られる医薬組成物、及びその使用 |
Country Status (32)
Country | Link |
---|---|
US (1) | US9782367B2 (ja) |
EP (1) | EP2819654B1 (ja) |
JP (1) | JP6026566B2 (ja) |
KR (1) | KR101911989B1 (ja) |
CN (1) | CN104168889B (ja) |
AR (1) | AR090168A1 (ja) |
AU (1) | AU2013224830B2 (ja) |
CA (1) | CA2863042A1 (ja) |
CL (1) | CL2014002202A1 (ja) |
CY (1) | CY1117049T1 (ja) |
DK (1) | DK2819654T3 (ja) |
EA (1) | EA024459B1 (ja) |
ES (1) | ES2554794T3 (ja) |
FR (1) | FR2987266B1 (ja) |
HK (1) | HK1198931A1 (ja) |
HR (1) | HRP20151280T1 (ja) |
HU (1) | HUE027141T2 (ja) |
IL (1) | IL234008A (ja) |
IN (1) | IN2014DN06573A (ja) |
MA (1) | MA37284B1 (ja) |
MX (1) | MX349970B (ja) |
NZ (1) | NZ628007A (ja) |
PH (1) | PH12014501838B1 (ja) |
PL (1) | PL2819654T3 (ja) |
PT (1) | PT2819654E (ja) |
RS (1) | RS54435B1 (ja) |
SG (1) | SG11201404812QA (ja) |
SI (1) | SI2819654T1 (ja) |
SM (1) | SMT201600029B (ja) |
TW (1) | TWI543779B (ja) |
UA (1) | UA113539C2 (ja) |
WO (1) | WO2013128087A1 (ja) |
Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
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US5618845A (en) * | 1994-10-06 | 1997-04-08 | Cephalon, Inc. | Acetamide derivative having defined particle size |
JP2003525895A (ja) * | 2000-03-09 | 2003-09-02 | アストラゼネカ・アクチエボラーグ | 固形分散剤の製造方法 |
US20060024370A1 (en) * | 2004-07-29 | 2006-02-02 | Cephalon France | Modafinil oral lyophilizate |
WO2007013962A2 (en) * | 2005-07-21 | 2007-02-01 | Neurohealing Pharmaceuticals, Inc. | Rapid onset and short term modafinil compositions and methods of use thereof |
US20070275057A1 (en) * | 2007-07-11 | 2007-11-29 | Hikma Pharmaceuticals | Formulation and Process for the Preparation of Modafinil |
JP2009543803A (ja) * | 2006-07-12 | 2009-12-10 | エラン・ファルマ・インターナショナル・リミテッド | モダフィニルのナノ粒子製剤 |
JP2011526836A (ja) * | 2009-06-23 | 2011-10-20 | ザ インダストリイ アンド コーパレイション イン チョンナム ナショナル ユニヴァシティ | 均一な粒度分布を有する超微細粒子の新規な製造方法及び装置 |
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CN1249932A (zh) * | 1999-09-29 | 2000-04-12 | 付俊昌 | 一种莫达芬尼及其光学对映体l及d异构体的新用途 |
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US6919378B2 (en) | 2000-10-11 | 2005-07-19 | Cephalon, Inc. | Pharmaceutical solutions of modafinil compounds |
KR100911779B1 (ko) | 2001-05-25 | 2009-08-12 | 세파론, 인코포레이티드 | 모다피닐을 포함하는 고형 제약 제제 |
US20040048931A1 (en) | 2002-07-12 | 2004-03-11 | Craig Heacock | Modafinil pharmaceutical compositions |
US20040121003A1 (en) | 2002-12-19 | 2004-06-24 | Acusphere, Inc. | Methods for making pharmaceutical formulations comprising deagglomerated microparticles |
GB0523653D0 (en) * | 2005-11-21 | 2005-12-28 | Novartis Ag | Organic compounds |
CA2615452C (en) * | 2005-07-15 | 2015-03-31 | Micell Technologies, Inc. | Polymer coatings containing drug powder of controlled morphology |
FR2943543B1 (fr) | 2009-03-31 | 2013-02-08 | Separex Sa | Procede de preparation de compositions pharmaceutiques comprenant des particules fines de substance active. |
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2012
- 2012-02-28 FR FR1200580A patent/FR2987266B1/fr not_active Expired - Fee Related
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2013
- 2013-02-25 RS RS20150789A patent/RS54435B1/en unknown
- 2013-02-25 PT PT137152625T patent/PT2819654E/pt unknown
- 2013-02-25 UA UAA201409665A patent/UA113539C2/uk unknown
- 2013-02-25 PL PL13715262T patent/PL2819654T3/pl unknown
- 2013-02-25 MA MA37284A patent/MA37284B1/fr unknown
- 2013-02-25 WO PCT/FR2013/000051 patent/WO2013128087A1/fr active Application Filing
- 2013-02-25 AU AU2013224830A patent/AU2013224830B2/en not_active Ceased
- 2013-02-25 JP JP2014559269A patent/JP6026566B2/ja not_active Expired - Fee Related
- 2013-02-25 IN IN6573DEN2014 patent/IN2014DN06573A/en unknown
- 2013-02-25 DK DK13715262.5T patent/DK2819654T3/en active
- 2013-02-25 US US14/381,699 patent/US9782367B2/en not_active Expired - Fee Related
- 2013-02-25 EP EP13715262.5A patent/EP2819654B1/fr active Active
- 2013-02-25 HU HUE13715262A patent/HUE027141T2/hu unknown
- 2013-02-25 ES ES13715262.5T patent/ES2554794T3/es active Active
- 2013-02-25 EA EA201400962A patent/EA024459B1/ru not_active IP Right Cessation
- 2013-02-25 SG SG11201404812QA patent/SG11201404812QA/en unknown
- 2013-02-25 NZ NZ628007A patent/NZ628007A/en not_active IP Right Cessation
- 2013-02-25 CA CA 2863042 patent/CA2863042A1/fr not_active Abandoned
- 2013-02-25 SI SI201330097T patent/SI2819654T1/sl unknown
- 2013-02-25 CN CN201380011313.0A patent/CN104168889B/zh not_active Expired - Fee Related
- 2013-02-25 KR KR1020147023178A patent/KR101911989B1/ko active IP Right Grant
- 2013-02-25 MX MX2014010236A patent/MX349970B/es active IP Right Grant
- 2013-02-26 TW TW102106626A patent/TWI543779B/zh not_active IP Right Cessation
- 2013-02-27 AR ARP130100595 patent/AR090168A1/es unknown
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2014
- 2014-08-07 IL IL234008A patent/IL234008A/en active IP Right Grant
- 2014-08-14 PH PH12014501838A patent/PH12014501838B1/en unknown
- 2014-08-19 CL CL2014002202A patent/CL2014002202A1/es unknown
- 2014-12-12 HK HK14112529.9A patent/HK1198931A1/xx not_active IP Right Cessation
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2015
- 2015-11-26 HR HRP20151280TT patent/HRP20151280T1/hr unknown
- 2015-12-09 CY CY20151101120T patent/CY1117049T1/el unknown
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2016
- 2016-01-29 SM SM201600029T patent/SMT201600029B/it unknown
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5618845A (en) * | 1994-10-06 | 1997-04-08 | Cephalon, Inc. | Acetamide derivative having defined particle size |
JP2003525895A (ja) * | 2000-03-09 | 2003-09-02 | アストラゼネカ・アクチエボラーグ | 固形分散剤の製造方法 |
US20060024370A1 (en) * | 2004-07-29 | 2006-02-02 | Cephalon France | Modafinil oral lyophilizate |
WO2007013962A2 (en) * | 2005-07-21 | 2007-02-01 | Neurohealing Pharmaceuticals, Inc. | Rapid onset and short term modafinil compositions and methods of use thereof |
JP2009543803A (ja) * | 2006-07-12 | 2009-12-10 | エラン・ファルマ・インターナショナル・リミテッド | モダフィニルのナノ粒子製剤 |
US20070275057A1 (en) * | 2007-07-11 | 2007-11-29 | Hikma Pharmaceuticals | Formulation and Process for the Preparation of Modafinil |
JP2011526836A (ja) * | 2009-06-23 | 2011-10-20 | ザ インダストリイ アンド コーパレイション イン チョンナム ナショナル ユニヴァシティ | 均一な粒度分布を有する超微細粒子の新規な製造方法及び装置 |
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