JP2006515592A - 味覚マスキングが必要な活性物質の経口調剤のための化合物 - Google Patents
味覚マスキングが必要な活性物質の経口調剤のための化合物 Download PDFInfo
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- JP2006515592A JP2006515592A JP2004563271A JP2004563271A JP2006515592A JP 2006515592 A JP2006515592 A JP 2006515592A JP 2004563271 A JP2004563271 A JP 2004563271A JP 2004563271 A JP2004563271 A JP 2004563271A JP 2006515592 A JP2006515592 A JP 2006515592A
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- glycerol ester
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Classifications
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- 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
- B01J2/00—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic
- B01J2/02—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic by dividing the liquid material into drops, e.g. by spraying, and solidifying the drops
- B01J2/04—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic by dividing the liquid material into drops, e.g. by spraying, and solidifying the drops in a gaseous medium
-
- 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
-
- 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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- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
あらかじめ60℃のオーブンで融解したプレシロールを2400g、ジャケット基準温度を75℃に設定したジャケット付き反応器に導入した。ダイズレシチンを78g加えた。ダイズレシチンが溶解した時に、基準温度を65℃に低下し、プリスチナマイシンを540g加えた。混合物を20分間、300rpmで撹拌し、ついで懸濁物をボールミル(ball mill)に注ぎ込んだ。
− 0〜100μmの粒子径のものが26%
− 100〜315μmの粒子径のものが62%
− 315〜500μmの粒子径のものが12%
− 500μmを超える粒子径のものが1%。
プレシロールを704g、ジャケット基準温度を75℃に設定したジャケット付き反応器に導入した。プレシロールが溶解した時に、ダイズレシチンを18g加えた。ダイズレシチンが溶解した時に、参照温度を65℃に低下させ、あらかじめエアジェット型ミクロナイザーで微粉化し、粉砕後の平均直径が2μmである、プリスチナマイシンを182g加えた。混合物を45分間、800rpmで撹拌し、均質な懸濁物を得た。
− 0〜100μmの粒子径のものが30%
− 100〜315μmの粒子径のものが54%
− 315〜500μmの粒子径のものが11%
− 500μmを超える粒子径のものが5%。
プレシロールを907g、ジャケット基準温度を70℃に設定したジャケット付き反応器に導入した。プレシロールが溶解した時に、ダイズレシチンを23g加えた。ダイズレシチンが溶解した時に、平均直径が114μmの未粉砕テリスロマイシン207gを導入した。混合物を50分間、500rpmで撹拌し、均質な液を得た。テリスロマイシンは可視的にプレシロール中に溶解する。
− 0〜100μmの粒子径のものが59%
− 100〜315μmの粒子径のものが38%
− 315〜500μmの粒子径のものが3%。
プレシロールを782g、および、カルナウバ蝋を115g、ジャケット基準温度を95℃に設定したジャケット付き反応器に導入した。脂質が溶解した時に、ダイズレシチンを23g加えた。ダイズレシチンが溶解した時に、平均直径が114μmの未粉砕テリスロマイシン230gを導入した。混合物を60分間、500rpmで撹拌し、均質な液体を得た。
− 0〜100μmの粒子径のものが27%
− 100〜315μmの粒子径のものが50%
− 315〜500μmの粒子径のものが16%
− 500μmを超える粒子径のものが7%。
Claims (8)
- 15〜30%の活性成分を60〜80%のグリセロールエステルまたは脂肪酸と混合し、場合によってはワックスを加え、また界面活性剤を加えることを含み、そして、350μm未満の粒径が得られるようにできるスプレー冷却法により調整されることを特徴とする、受容できない味覚を有する活性成分の経口投与用組成物。
- グリセロールエステルが、ステアリン酸グリセリルまたはパルミトステアリン酸グリセリルから選ばれることを特徴とする、請求項1の組成物。
- グリセロールエステルが、組成物の混合物の総量の50〜85重量%であることを特徴とする、請求項1の組成物。
- グリセロールエステルが、組成物の混合物の総量の60〜80重量%であることを特徴とする、請求項1〜3のいずれかの組成物。
- グリセロールエステルが、組成物の混合物の総量の70〜80重量%であることを特徴とする、請求項1〜4のいずれかの組成物。
- 活性成分が、医薬活性成分であることを特徴とする、請求項1〜5のいずれかの組成物。
- 活性成分を、溶解したグリセロールエステルと混合し、他の賦形剤を加え、ついで、タワーの頭頂部で二重流体ノズルを用いて、冷却ガス流を、場合によっては、向流的に導入するようにスプレーすることにより、スプレー冷却工程を行う、請求項1〜6のいずれかの組成物の製造方法。
- 機器が流動床を装備していることを特徴とする、請求項7の製造方法。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0216521A FR2848855B1 (fr) | 2002-12-23 | 2002-12-23 | Compositions pour administration orale de principes actifs necessitant un masquage du gout |
PCT/FR2003/003813 WO2004058137A2 (fr) | 2002-12-23 | 2003-12-19 | Compositions pour administration orale de principes actifs necessitant un masquage du gout |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2006515592A true JP2006515592A (ja) | 2006-06-01 |
JP2006515592A5 JP2006515592A5 (ja) | 2007-01-25 |
JP4676763B2 JP4676763B2 (ja) | 2011-04-27 |
Family
ID=32406402
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2004563271A Expired - Fee Related JP4676763B2 (ja) | 2002-12-23 | 2003-12-19 | 味覚マスキングが必要な活性物質の経口調剤のための化合物 |
Country Status (14)
Country | Link |
---|---|
EP (1) | EP1587500B1 (ja) |
JP (1) | JP4676763B2 (ja) |
AU (1) | AU2003299360B2 (ja) |
BR (1) | BR0317654A (ja) |
CA (1) | CA2510373C (ja) |
CY (1) | CY1115401T1 (ja) |
DK (1) | DK1587500T3 (ja) |
ES (1) | ES2470371T3 (ja) |
FR (1) | FR2848855B1 (ja) |
IL (1) | IL169343A (ja) |
MX (1) | MXPA05005640A (ja) |
PT (1) | PT1587500E (ja) |
SI (1) | SI1587500T1 (ja) |
WO (1) | WO2004058137A2 (ja) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NL1034065C2 (nl) | 2007-06-29 | 2008-12-30 | Friesland Brands Bv | Bereiding van deeltjes. |
FR2959130A1 (fr) | 2010-04-21 | 2011-10-28 | Sanofi Aventis | Procede de preparation de compositions pharmaceutiques destinees a l'administration par voie orale comprenant un ou plusieurs principes actifs et les compositions les comprenant. |
FR2968995B1 (fr) | 2010-12-16 | 2013-03-22 | Sanofi Aventis | Composition pharmaceutioue pour une administration par voie orale destinee a eviter le mesusage |
FR2968992B1 (fr) | 2010-12-16 | 2013-02-08 | Sanofi Aventis | Comprime pharmaceutique orodispersible a base de zolpidem |
FR3000400B1 (fr) | 2012-12-27 | 2019-06-21 | Virbac | Suspension huileuse de metronidazole |
TR201809617T4 (tr) * | 2013-12-04 | 2018-07-23 | Hovione Scientia Ltd | Tat maskeleme formülasyonları içeren kontrast ortamlar. |
FR3027802B1 (fr) | 2014-10-31 | 2018-03-02 | Ethypharm | Granules de principe actif a double masquage de gout, leur procede de preparation et comprimes orodispersibles les contenant |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS63303928A (ja) * | 1987-05-14 | 1988-12-12 | グラクソ・グループ・リミテツド | セフロキシムアクセチル経口製剤 |
JPH04212359A (ja) * | 1990-01-19 | 1992-08-03 | Rhone Poulenc Sante | 粒剤の形状の薬物の製造方法 |
JPH08510989A (ja) * | 1992-10-16 | 1996-11-19 | グラクソ、グループ、リミテッド | ラニチジン組成物 |
JP2000103730A (ja) * | 1998-07-31 | 2000-04-11 | Otsuka Pharmaceut Co Ltd | 服用感が改善された医薬組成物 |
WO2000054811A1 (fr) * | 1999-03-17 | 2000-09-21 | Daiichi Pharmaceutical Co., Ltd. | Compositions medicamenteuses |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS59122425A (ja) * | 1982-12-27 | 1984-07-14 | Kaken Pharmaceut Co Ltd | 持続性製剤およびその製造法 |
JP3155028B2 (ja) * | 1991-06-10 | 2001-04-09 | 大川原化工機株式会社 | 噴霧乾燥造粒装置 |
JPH05309314A (ja) * | 1992-05-07 | 1993-11-22 | Sumitomo Pharmaceut Co Ltd | コーティング方法 |
NZ505123A (en) * | 1997-12-19 | 2003-07-25 | Smithkline Beecham Corp | Process for manufacturing bite-dispersion tablets by compressing medicaments and other ingredients into granulates then compressing the granulates and other ingredients into tablets, and the tablets thereof |
US6209479B1 (en) * | 1998-12-30 | 2001-04-03 | Aeromatic-Fielder Ag | Apparatus for coating tablets |
-
2002
- 2002-12-23 FR FR0216521A patent/FR2848855B1/fr not_active Expired - Fee Related
-
2003
- 2003-12-19 BR BR0317654-1A patent/BR0317654A/pt not_active IP Right Cessation
- 2003-12-19 EP EP03799644.4A patent/EP1587500B1/fr not_active Expired - Lifetime
- 2003-12-19 ES ES03799644.4T patent/ES2470371T3/es not_active Expired - Lifetime
- 2003-12-19 DK DK03799644.4T patent/DK1587500T3/da active
- 2003-12-19 WO PCT/FR2003/003813 patent/WO2004058137A2/fr active Application Filing
- 2003-12-19 AU AU2003299360A patent/AU2003299360B2/en not_active Ceased
- 2003-12-19 MX MXPA05005640A patent/MXPA05005640A/es active IP Right Grant
- 2003-12-19 SI SI200332356T patent/SI1587500T1/sl unknown
- 2003-12-19 CA CA2510373A patent/CA2510373C/fr not_active Expired - Fee Related
- 2003-12-19 JP JP2004563271A patent/JP4676763B2/ja not_active Expired - Fee Related
- 2003-12-19 PT PT37996444T patent/PT1587500E/pt unknown
-
2005
- 2005-06-22 IL IL169343A patent/IL169343A/en not_active IP Right Cessation
-
2014
- 2014-06-12 CY CY20141100434T patent/CY1115401T1/el unknown
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS63303928A (ja) * | 1987-05-14 | 1988-12-12 | グラクソ・グループ・リミテツド | セフロキシムアクセチル経口製剤 |
JPH04212359A (ja) * | 1990-01-19 | 1992-08-03 | Rhone Poulenc Sante | 粒剤の形状の薬物の製造方法 |
JPH08510989A (ja) * | 1992-10-16 | 1996-11-19 | グラクソ、グループ、リミテッド | ラニチジン組成物 |
JP2000103730A (ja) * | 1998-07-31 | 2000-04-11 | Otsuka Pharmaceut Co Ltd | 服用感が改善された医薬組成物 |
WO2000054811A1 (fr) * | 1999-03-17 | 2000-09-21 | Daiichi Pharmaceutical Co., Ltd. | Compositions medicamenteuses |
Also Published As
Publication number | Publication date |
---|---|
FR2848855A1 (fr) | 2004-06-25 |
EP1587500A2 (fr) | 2005-10-26 |
PT1587500E (pt) | 2014-06-24 |
AU2003299360B2 (en) | 2009-10-29 |
CY1115401T1 (el) | 2017-01-04 |
AU2003299360A1 (en) | 2004-07-22 |
CA2510373C (fr) | 2014-09-30 |
WO2004058137A3 (fr) | 2005-04-14 |
MXPA05005640A (es) | 2005-07-27 |
WO2004058137A2 (fr) | 2004-07-15 |
ES2470371T3 (es) | 2014-06-23 |
IL169343A0 (en) | 2007-07-04 |
FR2848855B1 (fr) | 2005-02-11 |
CA2510373A1 (fr) | 2004-07-15 |
SI1587500T1 (sl) | 2014-07-31 |
JP4676763B2 (ja) | 2011-04-27 |
EP1587500B1 (fr) | 2014-03-12 |
BR0317654A (pt) | 2005-12-20 |
DK1587500T3 (da) | 2014-06-23 |
IL169343A (en) | 2011-06-30 |
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