JP2011506399A - 有機化合物 - Google Patents
有機化合物 Download PDFInfo
- Publication number
- JP2011506399A JP2011506399A JP2010537455A JP2010537455A JP2011506399A JP 2011506399 A JP2011506399 A JP 2011506399A JP 2010537455 A JP2010537455 A JP 2010537455A JP 2010537455 A JP2010537455 A JP 2010537455A JP 2011506399 A JP2011506399 A JP 2011506399A
- Authority
- JP
- Japan
- Prior art keywords
- drug substance
- micronized
- hours
- particle size
- glycopyrrolate
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4015—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
-
- 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
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
Landscapes
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Otolaryngology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
(a) 医薬原体を微粉化して約10μm未満の平均粒子径を得て;そして
(b) 該微粉化医薬原体を、40℃〜120℃の高温の乾燥環境に少なくとも6時間曝す
工程を含む。
好ましくは高温は60℃〜100℃、または適切には60〜90℃である。
好ましくは医薬原体はグリコピロニウム塩、特にグリコピロレートである。
ここで使用する、“凝集する”は、一緒に集まるまたは結合することを意味する。新たに微粉化した医薬原体は、時間と共に自然に合体し、医薬原体の凝集体を形成する傾向にある、微粉末の形を取る傾向にある。これらの凝集体は、あまり細かくない、または粗くさえある粉末に似る。
本発明の方法の好ましい態様において、医薬原体はグリコピロニウム塩、特にグリコピロニウムブロマイドまたはグリコピロレートである。
1kgの結晶性グリコピロレートを、次のパラメータ:分類器速度、17000rpm;製粉ガス圧、4barのHosokawa Alpine(登録商標) 100 AFG流動床カウンタジェットミルを使用して、5%ステアリン酸マグネシウムと共微粉化する。このミルは、1.9mm直径の3個のノズルを備える。
Claims (10)
- 貯蔵中に医薬原体が凝集しおよび/または塊形成する傾向を減らす方法であって:
(a) 医薬原体を微粉化して約10μm未満の平均粒子径とし;そして
(b) 該微粉化医薬原体を、40℃〜120℃の高温の乾燥環境に少なくとも6時間曝する、
各工程を含む、方法。 - 医薬原体を、1種以上の他の医薬原体または1種以上の抗付着剤と共微粉化する、請求項1に記載の方法。
- 高温が60℃〜100℃である、請求項1または2に記載の方法。
- 微粉化医薬原体を、乾燥環境に12〜96時間曝す、請求項1〜3のいずれかに記載の方法。
- 医薬原体がグリコピロニウム塩である、請求項1〜4のいずれかに記載の方法。
- 医薬原体がグリコピロレートである、請求項5に記載の方法。
- 高温が60℃〜120℃である、請求項5に記載の方法。
- 微粉化医薬原体を乾燥環境に12〜72時間曝す、請求項5に記載の方法。
- 請求項1〜8のいずれかに記載の方法を使用して処理されている医薬原体を含む、吸入可能乾燥粉末製剤。
- 噴射剤中に懸濁された医薬原体(ここで、該医薬原体は請求項1〜8のいずれかに記載の方法を使用して処理されている)を含む、定量吸入器において使用するための吸入可能製剤。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP07123164 | 2007-12-13 | ||
PCT/EP2008/067359 WO2009074662A2 (en) | 2007-12-13 | 2008-12-11 | Organic compounds |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2011506399A true JP2011506399A (ja) | 2011-03-03 |
JP2011506399A5 JP2011506399A5 (ja) | 2012-01-19 |
Family
ID=39472711
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010537455A Pending JP2011506399A (ja) | 2007-12-13 | 2008-12-11 | 有機化合物 |
Country Status (13)
Country | Link |
---|---|
US (1) | US20100247658A1 (ja) |
EP (1) | EP2234595B1 (ja) |
JP (1) | JP2011506399A (ja) |
KR (1) | KR20100099281A (ja) |
CN (1) | CN101896162B (ja) |
AU (1) | AU2008334543B2 (ja) |
BR (1) | BRPI0821186A2 (ja) |
CA (1) | CA2708083C (ja) |
ES (1) | ES2396471T3 (ja) |
PL (1) | PL2234595T3 (ja) |
PT (1) | PT2234595E (ja) |
RU (1) | RU2482838C2 (ja) |
WO (1) | WO2009074662A2 (ja) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2016521274A (ja) * | 2013-04-26 | 2016-07-21 | シエシー ファルマセウティチィ ソシエタ ペル アチオニ | 抗ムスカリン化合物の粒径の低減 |
JP2017527621A (ja) * | 2014-09-09 | 2017-09-21 | ベクトゥラ・リミテッド | グリコピロレートを含む製剤、方法、及び装置 |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PL3111926T3 (pl) * | 2009-05-29 | 2020-06-29 | Pearl Therapeutics, Inc. | Kompozycje, sposoby i układy do dostarczania dwóch lub większej liczby środków czynnych do układu oddechowego |
GB201307659D0 (en) | 2013-04-26 | 2013-06-12 | Korea Coast Guard Commissioner | Preparation of drug particles by micronisation |
US9925168B2 (en) | 2016-01-22 | 2018-03-27 | Chiesi Farmaceutici S.P.A. | Preparation of micronized particles of an antimuscarinic compound by hydrodynamic cavitation |
PL3490533T3 (pl) | 2016-07-29 | 2020-11-02 | Inke, S.A. | Sposób stabilizacji rozmiaru cząstek |
CN112972384B (zh) * | 2019-12-02 | 2022-03-18 | 长风药业股份有限公司 | 一种格隆溴铵和茚达特罗原料药微粉混合物的制备方法 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH10510292A (ja) * | 1995-04-05 | 1998-10-06 | ジェネンテク・インコーポレイテッド | 塩化ナトリウムエアゾル製剤の調製 |
JP2003530344A (ja) * | 2000-04-07 | 2003-10-14 | アラキス リミテッド | 呼吸器疾患の治療 |
JP2007535522A (ja) * | 2004-04-30 | 2007-12-06 | ベクトゥラ・リミテッド | 医薬組成物 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SE9101090D0 (sv) * | 1991-04-11 | 1991-04-11 | Astra Ab | Process for conditioning of water-soluble substances |
US6613795B2 (en) * | 1996-11-11 | 2003-09-02 | Christian Noe | Enantiomerically pure basic arylcycloalkylhydroxycarboxylic esters, processes for their preparation and their use in medicaments |
PT1920763E (pt) * | 2000-11-30 | 2014-06-25 | Vectura Ltd | Composições farmacêuticas para inalação |
MXPA06003769A (es) * | 2003-11-04 | 2006-07-03 | Shire Lab Inc | Liberacion sostenida de moleculas farmacologicamente activas cargadas positivamente a partir de una matriz que contiene polimeros con atomos de oxigeno polarizados. |
KR20120091378A (ko) * | 2004-03-23 | 2012-08-17 | 노파르티스 아게 | 제약 조성물 |
EP1834624A4 (en) * | 2005-01-07 | 2011-05-04 | Eisai R&D Man Co Ltd | MEDICAL COMPOSITION AND MANUFACTURING METHOD THEREFOR |
GB0613161D0 (en) * | 2006-06-30 | 2006-08-09 | Novartis Ag | Organic Compounds |
-
2008
- 2008-12-11 PL PL08859423T patent/PL2234595T3/pl unknown
- 2008-12-11 EP EP08859423A patent/EP2234595B1/en active Active
- 2008-12-11 CA CA2708083A patent/CA2708083C/en not_active Expired - Fee Related
- 2008-12-11 JP JP2010537455A patent/JP2011506399A/ja active Pending
- 2008-12-11 CN CN2008801205425A patent/CN101896162B/zh not_active Expired - Fee Related
- 2008-12-11 BR BRPI0821186-8A patent/BRPI0821186A2/pt not_active IP Right Cessation
- 2008-12-11 ES ES08859423T patent/ES2396471T3/es active Active
- 2008-12-11 KR KR1020107015330A patent/KR20100099281A/ko not_active Application Discontinuation
- 2008-12-11 WO PCT/EP2008/067359 patent/WO2009074662A2/en active Application Filing
- 2008-12-11 US US12/745,790 patent/US20100247658A1/en not_active Abandoned
- 2008-12-11 PT PT88594239T patent/PT2234595E/pt unknown
- 2008-12-11 AU AU2008334543A patent/AU2008334543B2/en not_active Ceased
- 2008-12-11 RU RU2010128246/15A patent/RU2482838C2/ru not_active IP Right Cessation
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH10510292A (ja) * | 1995-04-05 | 1998-10-06 | ジェネンテク・インコーポレイテッド | 塩化ナトリウムエアゾル製剤の調製 |
JP2003530344A (ja) * | 2000-04-07 | 2003-10-14 | アラキス リミテッド | 呼吸器疾患の治療 |
JP2007535522A (ja) * | 2004-04-30 | 2007-12-06 | ベクトゥラ・リミテッド | 医薬組成物 |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2016521274A (ja) * | 2013-04-26 | 2016-07-21 | シエシー ファルマセウティチィ ソシエタ ペル アチオニ | 抗ムスカリン化合物の粒径の低減 |
JP2017527621A (ja) * | 2014-09-09 | 2017-09-21 | ベクトゥラ・リミテッド | グリコピロレートを含む製剤、方法、及び装置 |
Also Published As
Publication number | Publication date |
---|---|
AU2008334543B2 (en) | 2011-07-28 |
EP2234595A2 (en) | 2010-10-06 |
EP2234595B1 (en) | 2012-11-28 |
CN101896162A (zh) | 2010-11-24 |
BRPI0821186A2 (pt) | 2015-06-16 |
CA2708083C (en) | 2016-06-28 |
RU2010128246A (ru) | 2012-01-20 |
PT2234595E (pt) | 2013-01-24 |
KR20100099281A (ko) | 2010-09-10 |
RU2482838C2 (ru) | 2013-05-27 |
CA2708083A1 (en) | 2009-06-18 |
US20100247658A1 (en) | 2010-09-30 |
AU2008334543A1 (en) | 2009-06-18 |
PL2234595T3 (pl) | 2013-04-30 |
WO2009074662A2 (en) | 2009-06-18 |
CN101896162B (zh) | 2013-06-05 |
WO2009074662A3 (en) | 2009-09-24 |
ES2396471T3 (es) | 2013-02-21 |
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