CN1238176A - L－2－氧代噻唑烷－4－羧酸与多元醇的结合使用 - Google Patents
L－2－氧代噻唑烷－4－羧酸与多元醇的结合使用 Download PDFInfo
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- CN1238176A CN1238176A CN99100903A CN99100903A CN1238176A CN 1238176 A CN1238176 A CN 1238176A CN 99100903 A CN99100903 A CN 99100903A CN 99100903 A CN99100903 A CN 99100903A CN 1238176 A CN1238176 A CN 1238176A
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Abstract
本发明涉及L－2－氧代噻唑烷－4－羧酸，即PROCYSTEINE与至少一种选自多元醇的化合物结合使用的方法。本专利还涉及一种含有L－2－氧代噻唑烷－4－羧酸和至少一种选自多元醇的化合物的化妆组合物，以及至少一种多元醇用于稳定L－2－氧代噻唑烷－4－羧酸的用途。
Description
在局部涂敷用的化妆或治疗皮肤病用组合物中使用L-2-氧代噻唑烷-4-羧酸是公知的。
如在专利EP-656,201中所述，这类组合物可以用来预防毛发的衰老或刺激毛发重新生长。
PROCYSTEINE作为人类皮肤的去色素剂或漂白剂也是由专利FR-2,742,658中可知的。
但是，PROCYSTEINE具有一定的不稳定性，特别是当其在有水存在下的时候。因此，当把它加入到化妆组合物中的时候，特别是含水组合物的时候，其效果随时间而减小。另外，加入它的组合物，在储存一定时间后，表现出降解的迹象：出现颜色和气味，这都是使用者不能接受的。
因此，现在就一直需要一种可以在化妆和皮肤病治疗方面使用的含L-2-氧代噻唑烷-4-羧酸的组合物，随着时间的进展这种化合物一直是稳定的。
如今，本申请人发现，L-2-氧代噻唑烷-4-羧酸(Ⅰ)与多元醇(Ⅱ)以特定的重量比一起使用，具有意外的稳定性，特别是在含水介质中一起使用时。
因此，本发明的第一个目标是，将化合物(Ⅰ)所表示的L-2-氧代噻唑烷，即PROCYSTEINE与至少一种属于化合物(Ⅱ)所表示的多元醇类化合物一起使用，分别用[Ⅰ]和[Ⅱ]表示的化合物(Ⅰ)和(Ⅱ)的重量具有[Ⅰ]/[Ⅱ]≤1/4的关系。
优选[Ⅰ]/[Ⅱ]≤1/5，更优选[Ⅰ]/[Ⅱ]≤1/10。
本发明的另一个目标是含有上述的结合以及水的化妆组合物。此组合物含有一种以水为其成分之一的可化妆用载体。该载体的组分将具体选自使本发明的组合物没有刺激性、无毒而且无变态反应的一类物质。
按照本发明的组合物最好包括：
-L-2-氧代噻唑烷-4-羧酸(Ⅰ)
-至少一种多元醇(Ⅱ)
-水
分别用[Ⅰ]和[Ⅱ]表示的化合物(Ⅰ)和(Ⅱ)的重量具有[Ⅰ]/[Ⅱ]≤1/4的关系。
与该组合物的总重量相比，水的重量少于或等于35％(重量)，优选少于或等于30％(重量)，更优选少于或等于20％(重量)。
这种组合物使得能够随时间的进展稳定地携带PROCYSTEINE，而不损失这种活性物的效果。
多元醇定义为一种在其烷基链上具有至少两个羟基的、饱和的或不饱和的、线形的、分支的或环状的烷基类化合物，以及这些多羟基烷基化合物的聚合物(聚醚)。优选涉及具有2-12个碳原子的烷基化合物，更优选具有2-8个碳原子。这种烷基化合物最好具有2或3个碳原子。
按照本发明使用的多元醇具体可以选自：甘油、乙二醇、丙二醇、上述三种化合物的聚合物和共聚物，比如二丙二醇和六羟甲基丙烷。
本发明可以使用的多元醇当中，可以列举：山梨糖醇、己二醇、丁二醇、戊二醇、丁基二甘醇、1,2,3-三羟基己烷。
本发明中可用的多元醇还可以举例如：山梨醇、己二醇、丁二醇、戊二醇、丁基二甘醇和1,2,3-三羟基丙烷。
本发明更特定的目标是如上所述的组合物，其特征在于，它被用来为人类的皮肤或人类的毛发脱除色素或漂白。
本发明还有一个目标是如上所述的组合物，其特征在于，它被用来预防毛发衰老或刺激毛发再生。
最好相对于该组合物的总重量，按照本发明的组合物含有0.01-10％(重量)的L-2-氧代噻唑烷-4-羧酸、优选含有0.1-5％(重量)，更优选含有0.5-3％(重量)。
本发明的组合物可以以所有在正常情况下用于局部涂敷的各种药物形式存在，特别是以水溶液、水醇溶液或油溶液、水包油或油包水乳液或多重乳液、水凝胶或油凝胶、不含水的液态、膏状或固态、依靠小球形成的油在水中分散液等的形式存在，这些小球可以是聚合物的纳米级颗粒，比如纳米球和纳米胶囊，或者离子型或非离子型的类脂小囊。
这种组合物可以是或多或少呈液体状的，具有白色或彩色乳脂状、油膏状、牛奶状、洗剂状、乳浆状、浆状、泡沫状的外观。在必要时可以将其以气溶胶的形式涂敷在皮肤或毛发上。它还可以呈现固体式形状，比如呈现棒状。它可以被用作护肤或化妆产品。它还可以呈香波或护发素的形式。
按照众所周知的方式，该组合物还可以含有在化妆品和皮肤药领域中经常使用的助剂，比如亲水或亲油脂的凝胶剂、亲水或亲油脂的活性物、防腐剂、抗氧剂、溶剂、香精、填料、紫外线吸收剂、颜料、气味吸收剂和着色剂。这些助剂的数量和在化妆品或皮肤药领域中通常使用的相同，比如为组合物总重量的0.01-20％。根据这些助剂的本性不同，它们可以被加在油脂相、水相、类脂小囊和/或纳米级颗粒中。
当本发明的组合物是乳液时，相对于组合物总重量的油脂相含量可以由5％至80％(重量)，优选5-50％(重量)。在呈乳液形状的该组合物中使用的油、乳化剂和助乳化剂选自所研究领域中通常使用的化合物。在该组合物中乳化剂和助乳化剂的含量，相对于该组合物的总重量为0.3-30％(重量)，优选为0.5-20％(重量)。
作为在本发明中使用的油，可以举出矿物油(凡士林油)、动物油(羊毛脂)、合成油(全氢角鲨烯)、硅油(环状聚甲基硅氧烷)和含氟油(全氟聚醚)。也可以使用脂肪醇(鲸蜡醇)、脂肪酸、蜡(巴西棕榈蜡、地蜡)作为脂肪材料。
作为在本发明中使用的乳化剂和助乳化剂，可以举出比如脂肪酸和聚乙二醇的酯(比如PEG-20的硬脂酸酯)和脂肪酸与甘油的酯(比如硬脂酸甘油酯)。
作为亲水凝胶剂，特别可以举出羧基乙烯基聚合物(Carbomer)、丙烯酸类共聚物(比如丙烯酸酯/烷基丙烯酸酯共聚物)、聚丙烯酰胺、多糖、天然树胶和粘土，作为亲油凝胶剂可以举出改性粘土如膨润土、脂肪酸金属盐、疏水二氧化硅和聚乙烯。
作为活性物，可以特别举出维生素、角质溶解剂和/或脱屑剂(水杨酸及其衍生物、α-羟基酸、抗坏血酸及其衍生物)、消炎剂、安定剂和它们的混合物。还可以将本发明的组合使用与其它的脱色素剂(如高氏酸或氢醌及其衍生物)一起使用，这使得可以使后者的使用剂量小于对皮肤产生毒性的剂量。还可以将本发明的组合使用与其它的抗衰老剂和/或毛发再生剂一起使用。在不相容的情况下，这些活性物和/或本发明的组合药剂被加入到小球体中，特别是离子型或非离子型小囊和/或纳米级颗粒(纳米级胶囊和/或纳米级小球)中，使它们在组合物中彼此分开。
该组合物的水相最好被中和，调节pH值到6-8。
本发明的还有一个目标是至少一种多元醇用来稳定PROCYSTEINE的用途。
本发明的再有一个目标是稳定化妆组合物中PROCYSTEINE的方法，此方法包括在所述组合物中加入至少一种选自多元醇的化合物。
实施例
给出如下的实施例是为了说明本发明。给出的百分数是相对于该组合物每种成分总重量的重量百分数。
实施例1：面部脱色素乳脂：
PROCYSTEINE 1％
杏仁油 3％
三乙醇胺 1％
琥珀酸辛烯基酯淀粉铝 3％
尼龙粉 7％
环状聚甲基硅氧烷和二甲基硅氧烷的共聚多 20％
元醇
苯基三甲基硅氧烷 4％
丙二醇 6％
甘油 23％
EDTA 适量
防腐剂 适量
水 31.5
％
实施例2：面部脱色素乳脂：
PROCYSTEINE 1％
杏仁油 3％
填料 10％
环状聚甲基硅氧烷 12.5
％
环状聚甲基硅氧烷和二甲基硅氧烷的共聚多 20％
元醇
苯基三甲基硅氧烷 4％
丙二醇 6％
甘油 23％
EDTA 适量
防腐剂 适量
水 19％
Claims (12)
1．一种结合使用的方法，其特征在于，它包括至少一种由化合物(Ⅰ)所表示的L-2-氧代噻唑烷与至少一种化合物(Ⅱ)所表示属于多元醇类的化合物，而且分别用[Ⅰ]和[Ⅱ]表示的化合物(Ⅰ)和(Ⅱ)的重量具有[Ⅰ]/[Ⅱ]≤1/4的关系。
2．按照权利要求1的结合使用方法，其特征在于，[Ⅰ]/[Ⅱ]≤1/5,优选[Ⅰ]/[Ⅱ]≤1/10。
3．按照前面的权利要求中任意一项的结合使用方法，其特征在于，多元醇是一种在其烷基链上具有至少两个羟基的、饱和的或不饱和的、线形的、分支的或环状的具有2-12个碳原子的烷基类化合物，以及这些多羟基烷基化合物的聚合物。
4．按照前面权利要求的结合使用方法，其特征在于，该多元醇选自：甘油、乙二醇、丙二醇、上述三种化合物的聚合物和共聚物，山梨糖醇、己二醇、丁二醇、戊二醇、丁基二甘醇、1,2,3-三羟基己烷。
5．化妆组合物，其特征在于，它含有：
-L-2-氧代噻唑烷-4-羧酸(Ⅰ)
-至少一种多元醇(Ⅱ)
-水，
分别用[Ⅰ]和[Ⅱ]表示的组分(Ⅰ)和(Ⅱ)的重量具有[Ⅰ]/[Ⅱ]≤1/4的关系。
6．按照权利要求5的化妆组合物，其特征在于，相对于该组合物总重量，水的含量小于或等于35％(重量)，优选小于或等于30％(重量)，更优选小于或等于20％(重量)。
7．按照权利要求5和6中任意一项的组合物，其特征在于，它用于人类皮肤或人类毛发的脱除色素或漂白。
8．按照权利要求5和6中任意一项的组合物，其特征在于，它用于预防毛发衰老或刺激毛发再生。
9．按照权利要求5-8中任意一项的组合物，其特征在于，相对于该组合物的总重量，它含有0.01-10％(重量)的L-2-氧代噻唑烷-4-羧酸，优选含有0.1-5％(重量)，更优选含有0.5-3％(重量)。
10．按照权利要求5-9中任意一项的组合物，其特征在于，水相被中和，调节pH值到6-8。
11．至少一种多元醇用于稳定PROCYSTEINE的用途。
12．在化妆组合物中PROCYSTEINE的稳定化方法，此方法包括在所述组合物中加入至少一种选自多元醇的化合物。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR98/00019 | 1998-01-05 | ||
| FR9800019A FR2773323B1 (fr) | 1998-01-05 | 1998-01-05 | Composition contenant une association de procysteine et de polyol |
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| Publication Number | Publication Date |
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| CN1238176A true CN1238176A (zh) | 1999-12-15 |
| CN1144578C CN1144578C (zh) | 2004-04-07 |
Family
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| Application Number | Title | Priority Date | Filing Date |
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| CNB991009037A Expired - Fee Related CN1144578C (zh) | 1998-01-05 | 1999-01-05 | L-2-氧代噻唑烷-4-羧酸与多元醇的结合使用 |
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| Country | Link |
|---|---|
| EP (1) | EP0931541B1 (zh) |
| JP (1) | JP2980605B2 (zh) |
| KR (1) | KR100318105B1 (zh) |
| CN (1) | CN1144578C (zh) |
| BR (1) | BR9805626A (zh) |
| CA (1) | CA2256085C (zh) |
| DE (1) | DE69813499T2 (zh) |
| ES (1) | ES2196515T3 (zh) |
| FR (1) | FR2773323B1 (zh) |
| ID (1) | ID22556A (zh) |
| MY (1) | MY133079A (zh) |
| SG (1) | SG72895A1 (zh) |
| TW (1) | TW516969B (zh) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104592146A (zh) * | 2015-01-19 | 2015-05-06 | 烟台腾辉化工有限公司 | 一种l-2-氧代噻唑烷-4-羧酸的制备工艺 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2790953B1 (fr) * | 1999-03-19 | 2002-08-09 | Oreal | Composition a phase aqueuse continue renfermant de l'acide l-2-oxothiazolidine 4-carboxylique |
| US6752830B1 (en) | 1999-07-20 | 2004-06-22 | Ethicon, Inc. | Apparatus and method for reconstructing a ligament |
| CA2353206C (en) * | 2000-07-19 | 2009-07-14 | Ethicon, Inc. | Apparatus and method for reconstructing a ligament |
| FR2816838B1 (fr) * | 2000-11-17 | 2004-12-03 | Oreal | Utilisation de derives de l'acide 2-oxothiazolidine- 4-carboxylique comme agents prodesquamants |
| US6562321B2 (en) | 2000-12-20 | 2003-05-13 | Avon Products, Inc. | Compositions and methods for treating hyperpigmentation |
| FR2908985B1 (fr) * | 2006-11-29 | 2009-02-13 | Oreal | Utilisation de l'octane 1,2 diol comme agent antioxydant. |
| JP5378713B2 (ja) * | 2008-06-19 | 2013-12-25 | 日本理化学薬品株式会社 | 外用組成物 |
| US8685472B2 (en) * | 2010-03-01 | 2014-04-01 | Access Business Group International Llc | Skin whitening composition containing chia seed extract |
| EP3727314B1 (en) * | 2017-12-20 | 2021-10-13 | Unilever IP Holdings B.V. | Deodorant compositions |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| USRE34185E (en) * | 1985-03-08 | 1993-02-23 | Rohm And Haas Company | Stabilization of non-aqueous solutions of 3-isothiazolones |
| EP0656201A1 (en) * | 1993-11-09 | 1995-06-07 | Transcend Therapeutics, Inc. | Use of stimulators of glutathione synthesis as hait growth promotors |
| FR2742658B1 (fr) * | 1995-12-22 | 1998-01-30 | Oreal | Utilisation de la procysteine comme agent depigmentant |
-
1998
- 1998-01-05 FR FR9800019A patent/FR2773323B1/fr not_active Expired - Fee Related
- 1998-11-20 ES ES98402902T patent/ES2196515T3/es not_active Expired - Lifetime
- 1998-11-20 EP EP98402902A patent/EP0931541B1/fr not_active Expired - Lifetime
- 1998-11-20 DE DE69813499T patent/DE69813499T2/de not_active Expired - Lifetime
- 1998-11-30 SG SG1998005044A patent/SG72895A1/en unknown
- 1998-11-30 BR BR9805626-3A patent/BR9805626A/pt not_active Application Discontinuation
- 1998-12-09 TW TW087120412A patent/TW516969B/zh active
- 1998-12-10 MY MYPI98005590A patent/MY133079A/en unknown
- 1998-12-16 ID IDP981633A patent/ID22556A/id unknown
- 1998-12-21 KR KR1019980056837A patent/KR100318105B1/ko not_active IP Right Cessation
- 1998-12-24 JP JP10368129A patent/JP2980605B2/ja not_active Expired - Lifetime
-
1999
- 1999-01-04 CA CA002256085A patent/CA2256085C/fr not_active Expired - Fee Related
- 1999-01-05 CN CNB991009037A patent/CN1144578C/zh not_active Expired - Fee Related
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104592146A (zh) * | 2015-01-19 | 2015-05-06 | 烟台腾辉化工有限公司 | 一种l-2-氧代噻唑烷-4-羧酸的制备工艺 |
Also Published As
| Publication number | Publication date |
|---|---|
| KR100318105B1 (ko) | 2002-02-19 |
| JP2980605B2 (ja) | 1999-11-22 |
| CA2256085A1 (fr) | 1999-07-05 |
| ID22556A (id) | 1999-11-04 |
| MY133079A (en) | 2007-10-31 |
| CA2256085C (fr) | 2005-11-08 |
| BR9805626A (pt) | 2000-06-06 |
| DE69813499T2 (de) | 2003-11-20 |
| EP0931541B1 (fr) | 2003-04-16 |
| JPH11255633A (ja) | 1999-09-21 |
| CN1144578C (zh) | 2004-04-07 |
| KR19990066860A (ko) | 1999-08-16 |
| FR2773323A1 (fr) | 1999-07-09 |
| ES2196515T3 (es) | 2003-12-16 |
| DE69813499D1 (de) | 2003-05-22 |
| TW516969B (en) | 2003-01-11 |
| EP0931541A1 (fr) | 1999-07-28 |
| FR2773323B1 (fr) | 2000-02-11 |
| SG72895A1 (en) | 2000-05-23 |
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