JP5184373B2 - 発泡組成物 - Google Patents
発泡組成物 Download PDFInfo
- Publication number
- JP5184373B2 JP5184373B2 JP2008550673A JP2008550673A JP5184373B2 JP 5184373 B2 JP5184373 B2 JP 5184373B2 JP 2008550673 A JP2008550673 A JP 2008550673A JP 2008550673 A JP2008550673 A JP 2008550673A JP 5184373 B2 JP5184373 B2 JP 5184373B2
- Authority
- JP
- Japan
- Prior art keywords
- composition
- composition according
- mpa
- foam
- viscosity
- 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.)
- Expired - Fee Related
Links
Classifications
-
- 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
- A61K9/0031—Rectum, anus
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- 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
- A61K9/12—Aerosols; Foams
- A61K9/122—Foams; Dry foams
-
- 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
- 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
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
Description
a)水性担体、潤滑剤、少なくとも1種の界面活性剤、および局所的に作用する医薬として活性な成分、または医薬として許容されるその誘導体を混合して、2から20mPa.sの範囲の粘度を有する均質なエマルジョンを得るステップと、
b)ステップa)で得られるエマルジョンに、少なくとも1種の噴射剤を添加して、発泡組成物を形成するステップ
を含む。典型的には、保存剤およびキレート剤は、ホモジナイザーを用いて最初に水性担体と混合する。次いで増粘剤を、同じ方法で混合する。その後、1種または複数の界面活性剤および潤滑剤を混合し、この混合物を安定化および/または加熱した後に、活性成分を添加する。あるいは活性成分は、開始時に混合する。
医薬の発泡組成物を、表1に示される処方に従って、活性成分としてメタスルホ安息香酸プレドニゾロンナトリウムを用いて配合した。
[実施例2]
モノブロックキャニスター(110ml)に、実験1によるバルクエマルジョン90gを充填し、さらに噴射剤B.I.P.(Avantec−dehonのNovospray nbu/p25;8.110g)を充填し、加圧剤として窒素(0.09g)を、加圧ユニットを使用して添加した結果、圧力が12バールになった。キャニスターを、3mlの絞り弁(Lablabo S.A.)で閉じた。キャニスターは、14回分の投薬量(および20%過量)に合わせて材料を含有し、この用量および膨張体積の再現性は、1回目と14回目の用量の単位体積重量(volumic mass)(g/ml)および膨張体積(ml)をそれぞれ測定することによって確立した(表2)。
Claims (21)
- 治療上有効な量のプレドニゾロンまたは医薬として許容されるその塩を直腸投与するための水性発泡組成物であって、前記治療上有効な量のプレドニゾロンまたは医薬として許容されるその塩に加えて、1〜15%(w/w)の界面活性剤、0.01〜1%(w/w)の増粘剤、0.1〜10%(w/w)のシリコーン潤滑剤、及び4〜12%(w/w)の噴射剤を含み、
前記界面活性剤が少なくとも2種の非イオン性界面活性剤の混合物であり、
前記増粘剤が水溶性セルロースポリマーであり、
前記シリコーン潤滑剤がポリジメチルシロキサンであり、且つ
前記噴射剤が、ブタン、イソブタン、及びプロパンの混合物を含み、
少なくとも26の体積膨張比及び2.0から20.0mPa.sの範囲内の粘度を有する水性発泡組成物。 - 前記体積膨張比が少なくとも28である、請求項1に記載の組成物。
- 前記堆積膨張比が少なくとも30である、請求項2に記載の組成物。
- 前記体積膨張比が70未満である、請求項1〜3のいずれか一項に記載の組成物。
- 前記体積膨張比が60未満である、請求項4に記載の組成物。
- 前記体積膨張比が50未満である、請求項5に記載の組成物。
- 前記医薬として許容されるプレドニゾロンの塩が、メタスルホ安息香酸プレドニゾロンナトリウムである、請求項1から6のいずれか一項に記載の組成物。
- 前記増粘剤が、ヒドロキシプロピルメチルセルロースである、請求項1〜7のいずれか一項に記載の組成物。
- 前記増粘剤が、組成物の0.05%(w/w)から0.5%(w/w)の量である、請求項1〜8のいずれか一項に記載の組成物。
- 前記増粘剤が、組成物の0.1%(w/w)から0.3%(w/w)の量である、請求項9に記載の組成物。
- 前記界面活性剤が、カプリロカプロイルマクロゴールグリセリドおよびモノオレイン酸ポリオキシエチレン80ソルビタンの混合物である、請求項1〜10のいずれか一項に記載の組成物。
- 前記噴射剤を、組成物の6から10%(w/w)の量で含む、請求項1〜11のいずれか一項に記載の組成物。
- 前記噴射剤を、組成物の7から9%(w/w)の量で含む、請求項12に記載の組成物。
- 前記シリコーン潤滑剤を、組成物の0.5%(w/w)から5%(w/w)の量で含む、請求項1〜13のいずれか一項に記載の組成物。
- 前記シリコーン潤滑剤を、組成物の1%(w/w)から3%(w/w)の量で含む、請求項14に記載の組成物。
- 請求項1〜15のいずれか一項に記載の発泡組成物を含む、多回用量加圧エアロゾル容器。
- 前記発泡組成物の粘度が4.0mPa.sから16.0mPa.s未満の範囲である、請求項16に記載の多回用量容器。
- 前記発泡組成物の粘度が6.0mPa.sから10.0mPa.s未満の範囲である、請求項17に記載の多回用量容器。
- 前記発泡組成物の粘度が7.0mPa.sから9.0mPa.s未満の範囲である、請求項18に記載の多回用量容器。
- 絞り弁を有する、請求項16〜19のいずれか一項に記載の多回用量容器。
- a.水性担体、シリコーン潤滑剤、増粘剤、界面活性剤、およびプレドニゾロンまたは医薬として許容されるその塩を混合して、2から20mPa.sの範囲の粘度を有する均質なエマルジョンを得るステップと、
b.ステップa)で得られるエマルジョンに、噴射剤を添加して、発泡組成物を形成するステップ
を含む、請求項1〜15のいずれか一項に記載の発泡組成物の製造方法。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP06100572A EP1810666A1 (en) | 2006-01-19 | 2006-01-19 | Foam-Forming composition |
EP06100572.4 | 2006-01-19 | ||
US76177906P | 2006-01-25 | 2006-01-25 | |
US60/761,779 | 2006-01-25 | ||
PCT/EP2007/000271 WO2007082698A1 (en) | 2006-01-19 | 2007-01-12 | Foam-forming composition |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2009523745A JP2009523745A (ja) | 2009-06-25 |
JP5184373B2 true JP5184373B2 (ja) | 2013-04-17 |
Family
ID=37831688
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2008550673A Expired - Fee Related JP5184373B2 (ja) | 2006-01-19 | 2007-01-12 | 発泡組成物 |
Country Status (6)
Country | Link |
---|---|
EP (1) | EP1981480A1 (ja) |
JP (1) | JP5184373B2 (ja) |
AU (1) | AU2007207116B2 (ja) |
CA (1) | CA2637408C (ja) |
NO (1) | NO20083524L (ja) |
WO (1) | WO2007082698A1 (ja) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL152486A0 (en) | 2002-10-25 | 2003-05-29 | Meir Eini | Alcohol-free cosmetic and pharmaceutical foam carrier |
US20080138296A1 (en) | 2002-10-25 | 2008-06-12 | Foamix Ltd. | Foam prepared from nanoemulsions and uses |
MXPA05004278A (es) | 2002-10-25 | 2005-10-05 | Foamix Ltd | Espuma cosmetica y farmaceutica. |
US9265725B2 (en) | 2002-10-25 | 2016-02-23 | Foamix Pharmaceuticals Ltd. | Dicarboxylic acid foamable vehicle and pharmaceutical compositions thereof |
US9668972B2 (en) | 2002-10-25 | 2017-06-06 | Foamix Pharmaceuticals Ltd. | Nonsteroidal immunomodulating kit and composition and uses thereof |
US7700076B2 (en) | 2002-10-25 | 2010-04-20 | Foamix, Ltd. | Penetrating pharmaceutical foam |
US8900554B2 (en) | 2002-10-25 | 2014-12-02 | Foamix Pharmaceuticals Ltd. | Foamable composition and uses thereof |
US7704518B2 (en) | 2003-08-04 | 2010-04-27 | Foamix, Ltd. | Foamable vehicle and pharmaceutical compositions thereof |
US10117812B2 (en) | 2002-10-25 | 2018-11-06 | Foamix Pharmaceuticals Ltd. | Foamable composition combining a polar solvent and a hydrophobic carrier |
US7820145B2 (en) | 2003-08-04 | 2010-10-26 | Foamix Ltd. | Oleaginous pharmaceutical and cosmetic foam |
US9211259B2 (en) | 2002-11-29 | 2015-12-15 | Foamix Pharmaceuticals Ltd. | Antibiotic kit and composition and uses thereof |
US8795693B2 (en) | 2003-08-04 | 2014-08-05 | Foamix Ltd. | Compositions with modulating agents |
US20080260655A1 (en) | 2006-11-14 | 2008-10-23 | Dov Tamarkin | Substantially non-aqueous foamable petrolatum based pharmaceutical and cosmetic compositions and their uses |
US8636982B2 (en) | 2007-08-07 | 2014-01-28 | Foamix Ltd. | Wax foamable vehicle and pharmaceutical compositions thereof |
US9439857B2 (en) | 2007-11-30 | 2016-09-13 | Foamix Pharmaceuticals Ltd. | Foam containing benzoyl peroxide |
WO2009072007A2 (en) | 2007-12-07 | 2009-06-11 | Foamix Ltd. | Carriers, formulations, methods for formulating unstable active agents for external application and uses thereof |
US20090239289A1 (en) * | 2008-03-19 | 2009-09-24 | Ipser Reid M | Drain Foam Composition and Method of Using the Same |
WO2009150530A2 (en) * | 2008-06-11 | 2009-12-17 | Ferring International Center Sa | Novel foam composition |
WO2010125470A2 (en) | 2009-04-28 | 2010-11-04 | Foamix Ltd. | Foamable vehicle and pharmaceutical compositions comprising aprotic polar solvents and uses thereof |
WO2011013008A2 (en) | 2009-07-29 | 2011-02-03 | Foamix Ltd. | Non surface active agent non polymeric agent hydro-alcoholic foamable compositions, breakable foams and their uses |
CA2769625C (en) | 2009-07-29 | 2017-04-11 | Foamix Ltd. | Non surfactant hydro-alcoholic foamable compositions, breakable foams and their uses |
CA2776474C (en) | 2009-10-02 | 2021-01-12 | Foamix Ltd. | Topical tetracycline compositions |
US9849142B2 (en) | 2009-10-02 | 2017-12-26 | Foamix Pharmaceuticals Ltd. | Methods for accelerated return of skin integrity and for the treatment of impetigo |
JP2015168654A (ja) * | 2014-03-07 | 2015-09-28 | 三笠製薬株式会社 | NSAIDs含有泡沫化製剤用水性組成物 |
MX2020012139A (es) | 2016-09-08 | 2021-01-29 | Vyne Pharmaceuticals Inc | Composiciones y metodos para tratar rosacea y acne. |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SE9000485D0 (sv) * | 1990-02-09 | 1990-02-09 | Pharmacia Ab | Foamable composition for pharmaceutical use, use thereof and method of treatment |
IT1243379B (it) * | 1990-07-27 | 1994-06-10 | Giuliani Spa | Composizione farmaceutica adatta alla somministrazione rettale di principi attivi che esplicano un'azione di medicazione a livello del colon prevalentemente di tipo topico |
FR2713486B1 (fr) * | 1993-12-14 | 1996-02-09 | Scophysa | Nouvelles compositions pour mousses, notamment mousses rectales, et mousses ainsi obtenues. |
GB9414699D0 (en) * | 1994-07-21 | 1994-09-07 | Slagel David | Aqueous foamable composition |
SE9703226D0 (sv) * | 1997-09-08 | 1997-09-08 | Astra Ab | New pharmaceutical composition |
MXPA05004278A (es) * | 2002-10-25 | 2005-10-05 | Foamix Ltd | Espuma cosmetica y farmaceutica. |
US20050069499A1 (en) * | 2003-09-25 | 2005-03-31 | Moshe Arkin | Foamable compositions, processes of preparing same and uses thereof |
-
2007
- 2007-01-12 EP EP07702743A patent/EP1981480A1/en not_active Withdrawn
- 2007-01-12 JP JP2008550673A patent/JP5184373B2/ja not_active Expired - Fee Related
- 2007-01-12 WO PCT/EP2007/000271 patent/WO2007082698A1/en active Application Filing
- 2007-01-12 CA CA2637408A patent/CA2637408C/en not_active Expired - Fee Related
- 2007-01-12 AU AU2007207116A patent/AU2007207116B2/en not_active Ceased
-
2008
- 2008-08-13 NO NO20083524A patent/NO20083524L/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
EP1981480A1 (en) | 2008-10-22 |
JP2009523745A (ja) | 2009-06-25 |
AU2007207116A1 (en) | 2007-07-26 |
AU2007207116B2 (en) | 2012-08-02 |
CA2637408A1 (en) | 2007-07-26 |
WO2007082698A1 (en) | 2007-07-26 |
NO20083524L (no) | 2008-08-13 |
CA2637408C (en) | 2013-12-03 |
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