JP2005521677A - 酸素感受性化合物のための製剤及びその製造方法 - Google Patents
酸素感受性化合物のための製剤及びその製造方法 Download PDFInfo
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- AZKSAVLVSZKNRD-UHFFFAOYSA-M 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide Chemical compound [Br-].S1C(C)=C(C)N=C1[N+]1=NC(C=2C=CC=CC=2)=NN1C1=CC=CC=C1 AZKSAVLVSZKNRD-UHFFFAOYSA-M 0.000 description 1
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- 206010040880 Skin irritation Diseases 0.000 description 1
- 206010042496 Sunburn Diseases 0.000 description 1
- RTAQQCXQSZGOHL-UHFFFAOYSA-N Titanium Chemical compound [Ti] RTAQQCXQSZGOHL-UHFFFAOYSA-N 0.000 description 1
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- 229910052782 aluminium Inorganic materials 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
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- VMGAPWLDMVPYIA-HIDZBRGKSA-N n'-amino-n-iminomethanimidamide Chemical compound N\N=C\N=N VMGAPWLDMVPYIA-HIDZBRGKSA-N 0.000 description 1
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- SOQBVABWOPYFQZ-UHFFFAOYSA-N oxygen(2-);titanium(4+) Chemical class [O-2].[O-2].[Ti+4] SOQBVABWOPYFQZ-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- 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
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
-
- 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
- A61K47/02—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/23—Sulfur; Selenium; Tellurium; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/27—Zinc; Compounds thereof
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/29—Titanium; Compounds thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
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- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Dermatology (AREA)
- Dispersion Chemistry (AREA)
- Emergency Medicine (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
- Anti-Oxidant Or Stabilizer Compositions (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
* PEG: ポリエチレングリコール
** 100gに十分な量(quantity sufficient for 100g)
*** パラベン:パラヒドロキシベンゾエート
本実施例は,その治療作用が米国特許第6153226号に記載されたクリームを生成することを可能にする。これは,プロポリスと組み合わせたBHTが増強された抗ウイルス活性を有することを示す。
− NT:試験しなかった。
− ?+:疑わしい反応:わずかな紅斑のみ
− +:弱い陽性反応(水疱なし):紅斑,浸潤,時折いくつかの丘疹
− ++:強い陽性反応:紅斑,丘疹,小水泡の存在
− +++:水疱を伴う激しい陽性反応
− −:陰性反応
− IR:刺激反応:
E0.5:非常に穏やかな紅斑
E1:穏やかな紅斑
E2:明らかな紅斑
E3:著しい紅斑
各読み取り時間における平均刺激指数を,下記の比により計算した:
A.I.I.=Σ紅斑スコア/志願者数
皮膚刺激のスケール解釈を下記のように行った。
− A.I.I.が0.20未満:非刺激性
− A.I.I.が0.20以上0.50未満:穏やかな刺激性
− A.I.I.が0.50以上1未満:中程度の刺激性
− A.I.I.が1以上:刺激性
結果を下記の表Iにまとめる。
*志願者5:僅かな剥離を伴う皮膚の乾燥
(1)M=男 F=女
− 陰性コントロール培養液は,接触後24時間に基底層の細胞の生存の証拠である暗青/紫色となるべきである。
− 陽性コントロールは,接触後,1時間で細胞死の証拠である白色となるべきである。
− 非刺激性(NI):10分間,1時間,3時間及び24時間で青。
− 非常に穏やかな刺激性(VMI):10分間,1時間,3時間で青,24時間で白。
− 穏やかな刺激性(MI):10分間で青,1時間及び3時間で青/白,24時間で白。
− 刺激性(I):24時間
− 著しい刺激性(VI):10分,1時間,3時間及び24時間で白。
40kgの製剤を入れた容器を,不活性ガス(例えば窒素)の添加のような特別な包装をせずに,単純な蓋で覆い,3年間貯蔵した。
Claims (17)
- 医薬及び/または化粧料製剤中の酸素感受性の活性化合物の酸化を防止する方法であって,
少なくとも1種類の強い酸化防止剤と少なくとも1種類の弱い酸化防止剤を入れることからなり,前記強い酸化防止剤が前記活性化合物より前に酸素と反応し,前記弱い酸化防止剤が残留酸素と反応して,酸化後,高いコーティング性を有し,微粉化により前記活性化合物の周囲に集まって保護層を形成する粒子を形成することを特徴とする方法。 - 酸化が防止されるべき酸素感受性活性化合物を含有する医薬及び/または化粧料製剤であって,前記活性化合物に加えて,少なくとも1種類の強い酸化防止剤と,微粉化により高いコーティング性を有する少なくとも1種類の弱い酸化防止剤を含有することを特徴とする製剤。
- 前記活性化合物が,2,6−ジ−第三ブチルフェノール誘導体である請求項2記載の製剤。
- 前記活性化合物が,本製剤の総重量の1〜10重量%,好ましくは5重量%の範囲の量で存在する請求項2記載の製剤。
- 前記弱い酸化防止剤が金属酸化物である請求項2記載の製剤。
- 前記弱い酸化防止剤が,全量で,本製剤の総重量の5.1〜12重量%,好ましくは5.5重量%の範囲の量で存在することを特徴とする請求項5記載の製剤。
- 2種類の弱い酸化防止剤を含むことを特徴とする請求項2記載の製剤。
- 前記2種類の酸化防止剤が本製剤の総重量の0.1〜2重量%,好ましくは0.5重量%の範囲の量で存在する酸化亜鉛と本製剤の総重量の5〜10重量%,好ましくは5重量%の範囲の量で存在する二酸化チタンであることを特徴とする請求項7記載の製剤。
- 前記強い酸化防止剤が二亜硫酸ナトリウムであることを特徴とする請求項2記載の製剤。
- 前記強い酸化防止剤が,本製剤の総重量の0.05〜0.1重量%,好ましくは0.05重量%の範囲の量で存在することを特徴とする請求項9記載の製剤。
- 前記製剤が,油相と水相の二相製剤である特徴とする請求項2記載の製剤。
- 前記製剤の粒子が0.1〜2μm,より好ましくは0.2μm未満の大きさを有することを特徴とする前記請求項のいずれか1項記載の製剤。
- 前記油相が前記活性化合物及び前記弱い酸化防止剤を含むことを特徴とする請求項1〜12のいずれか1項記載の製剤。
- 前記水相が前記強い酸化防止剤を含むことを特徴とする請求項1〜13のいずれか1項記載の製剤。
- 下記の5つの混合物を含むことを特徴とする請求項1〜14のいずれか1項記載の製剤。
−ステアリン酸グリセリル,セテアリールアルコール,セチルパルミテート及びココグリセリド,PEG−6ステアレート,PEG−32ステアレート,トリグリセリドを含む混合物A,
−前記活性化合物及び前記弱い酸化防止剤を含む混合物A’,
−脱塩水及びグリセロールを含む混合物B,
−防腐剤を含む混合物C,
−脱塩水及び前記強い酸化防止剤を含む混合物D。 - 下記の6つの混合物を含むことを特徴とする請求項1〜15のいずれか1項記載の製剤。
−ステアリン酸グリセリル,セテアリールアルコール,セチルパルミテート及びココグリセリド,PEG−6ステアレート,PEG−32ステアレート,トリグリセリドを含む混合物A,
−前記活性化合物及び前記弱い酸化防止剤を含む混合物A’,
−脱塩水及びグリセロールを含む混合物B,
−防腐剤を含む混合物C,
−脱塩水及び前記強い酸化防止剤を含む混合物D,
−プロポリス及びテペスコフイテグリコール抽出物を含む混合物E。 - 少なくとも1種類の活性化合物,少なくとも1種類の強い酸化防止剤及び少なくとも1種類の弱い酸化防止剤を含み,前記強い酸化防止剤が前記活性化合物より前に酸素と反応し,前記弱い酸化防止剤が残留酸素と反応して,酸化後,高いコーティング性を有し,微粉化により前記活性化合物の周囲に集まって保護層を形成する粒子を形成する酸素感受性化合物製剤の製造方法であって,
a)混合物Aを70〜75℃に加熱し,その後混合物A’の成分を一つずつ添加し,
b)混合物Bを70〜75℃に加熱し,その後反応混合物に添加し,
c)全混合物を60〜65℃に冷却し,その後混合物Cを添加し,
d)該混合物を40〜45℃の温度に合わせ,混合物Dを添加し,
e)所望により,混合物Eを35℃で添加し,
f)温度が約25〜30℃に降下するまで撹拌を続ける
ことを特徴とする方法。
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FR0201456A FR2835522B1 (fr) | 2002-02-06 | 2002-02-06 | Preparation pour composes sensibles a l'oxydation et son procede de fabrication |
PCT/FR2003/000386 WO2003066101A1 (fr) | 2002-02-06 | 2003-02-04 | Préparation pour composées sensibles a l'oxydation et son procédé de fabrication |
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JP2005521677A true JP2005521677A (ja) | 2005-07-21 |
JP2005521677A5 JP2005521677A5 (ja) | 2010-09-02 |
JP4614262B2 JP4614262B2 (ja) | 2011-01-19 |
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US (1) | US20050175644A1 (ja) |
EP (1) | EP1478402A1 (ja) |
JP (1) | JP4614262B2 (ja) |
AU (1) | AU2003222364A1 (ja) |
BR (1) | BR0307486A (ja) |
CA (1) | CA2475218C (ja) |
FR (1) | FR2835522B1 (ja) |
IL (1) | IL163365A (ja) |
WO (1) | WO2003066101A1 (ja) |
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FR2867683B1 (fr) * | 2004-03-22 | 2012-12-21 | Lm Cosmetics | Compositions cosmetiques ou dermatologiques et leurs applications |
US8048919B2 (en) * | 2004-06-28 | 2011-11-01 | Archer Daniels Midland Company | Use of ethyl lactate as an excipient for pharmaceutical compositions |
KR101340514B1 (ko) * | 2007-01-24 | 2013-12-12 | 삼성디스플레이 주식회사 | 박막 트랜지스터 기판 및 이의 제조 방법 |
FR2933616B1 (fr) * | 2008-07-10 | 2011-08-19 | Robert Vachy | "compositions renfermant une association de propolis et d'un derive phenolique et leurs applications biologiques" |
DE102009048974A1 (de) * | 2009-10-09 | 2011-04-14 | Beiersdorf Ag | Kosmetische oder dermatologische Zubereitungen mit Kombinationen aus öllöslichen kosmetischen oder dermatologischen Wirkstoffen und einem oder mehreren Sulfiten (Bisulfiten oder Disulfiten) |
DE102009048977A1 (de) * | 2009-10-09 | 2011-04-14 | Beiersdorf Ag | Kosmetische oder dermatologische Zubereitungen mit Kombinationen aus 4-n-Butylresorcin und einem oder mehreren Sulfiten, insbesondere Hydrogensulfiten und/oder Disulfiten |
EP2640667A4 (en) | 2010-11-15 | 2014-11-19 | Archer Daniels Midland Co | COMPOSITIONS AND USES FOR CONVERTING CONTAMINANTS |
KR102348583B1 (ko) * | 2020-04-29 | 2022-01-07 | 주식회사 닥터이엘 | 천연색소 변색방지용 조성물 |
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2002
- 2002-02-06 FR FR0201456A patent/FR2835522B1/fr not_active Expired - Fee Related
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2003
- 2003-02-04 CA CA2475218A patent/CA2475218C/fr not_active Expired - Fee Related
- 2003-02-04 JP JP2003565524A patent/JP4614262B2/ja not_active Expired - Fee Related
- 2003-02-04 AU AU2003222364A patent/AU2003222364A1/en not_active Abandoned
- 2003-02-04 WO PCT/FR2003/000386 patent/WO2003066101A1/fr active Application Filing
- 2003-02-04 US US10/503,360 patent/US20050175644A1/en not_active Abandoned
- 2003-02-04 EP EP03717383A patent/EP1478402A1/fr not_active Withdrawn
- 2003-02-04 BR BR0307486-2A patent/BR0307486A/pt not_active IP Right Cessation
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2004
- 2004-07-30 ZA ZA200406128A patent/ZA200406128B/en unknown
- 2004-08-05 IL IL163365A patent/IL163365A/en not_active IP Right Cessation
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JPH02117688A (ja) * | 1988-06-28 | 1990-05-02 | Julio Tellez Perez | ミモザ・テヌイフローラ(Mimosa Tenuiflora)活性成分に基づく表面組織再生機能保有の薬用生成物質とその調製方法 |
US6153226A (en) * | 1990-03-12 | 2000-11-28 | Fileco | Therapeutic composition containing a phenol compound and propolis, which is useful against lipid capsid viruses, especially herpes viruses |
US5352681A (en) * | 1991-06-07 | 1994-10-04 | Byk Nederland Bv | Pharmaceutical enema preparation |
JP2001518111A (ja) * | 1997-03-25 | 2001-10-09 | バイヤースドルフ・アクチエンゲゼルシヤフト | 乳化剤を含まない水中油型の微細分散系 |
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AU2003222364A1 (en) | 2003-09-02 |
ZA200406128B (en) | 2006-07-26 |
FR2835522A1 (fr) | 2003-08-08 |
CA2475218A1 (fr) | 2003-08-14 |
US20050175644A1 (en) | 2005-08-11 |
BR0307486A (pt) | 2004-12-07 |
IL163365A (en) | 2008-07-08 |
JP4614262B2 (ja) | 2011-01-19 |
WO2003066101A1 (fr) | 2003-08-14 |
CA2475218C (fr) | 2012-09-11 |
EP1478402A1 (fr) | 2004-11-24 |
FR2835522B1 (fr) | 2006-04-07 |
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