CN1280507A - 含米诺地尔的液体组合物 - Google Patents
含米诺地尔的液体组合物 Download PDFInfo
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- 229960003632 minoxidil Drugs 0.000 title claims abstract description 26
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- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- 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
- A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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Abstract
含米诺地尔的液体组合物随时间延长易于变色,因此降低了商品价值。然而,含米诺地尔和氨基酸的液体制剂可防止随时间延长而变色,因此本发明能在市场上给出优良的液体组合物。
Description
技术领域
本发明涉及能防止随时间延长而变色的含米诺地尔的液体组合物。
背景技术
由于具有头发生长作用，米诺地尔是用作外用头发生长剂的组分。
然而，当以液体状态贮存时，米诺地尔具有易于随时间延长而变色的缺点，并因此导致商品价值降低。含米诺地尔的液体制剂的变色机理尚未弄清楚，但据假定是与光的作用有关。因此，在市场上需要使用遮光容器来装盛含米诺地尔的液体制剂。然而，这些容器不便于使用，例如，容器中剩余含量不清楚。
一般情况下，是使用抗氧化剂和抗螯合剂来改善含易变色组分的液体制剂，但是使用抗氧化剂和抗螯合剂不能充分地防止含米诺地尔的液体制剂随时间延长而变色。
另一方面，为了使制剂变色显得不太显著，据认为开始时可先将制剂着色。但是，因为头发生长制剂是通过涂在头皮上来使用的，先进行着色的制剂会由于污染衣服和床上用品而令人不快。
本发明的公开
通过大量研究以防止含米诺地尔的液体制剂变色，本发明者已经发现，通过加入氨基酸、尤其是牛磺酸，可令人惊奇地防止含米诺地尔的液体制剂变色，由此完成了本发明。
也就是说，本发明涉及含米诺地尔和氨基酸的液体组合物。
依据本发明，氨基酸是指可加入外用液体制剂中的所有氨基酸，并包括它们的盐。
在本发明氨基酸中，从防止变色的角度考虑，氨基酸优选为含硫的氨基酸(例如牛磺酸、半胱氨酸、胱氨酸、蛋氨酸或高半胱氨酸)，尤其是牛磺酸。
在本发明液体组合物中，按液体制剂的重量计，米诺地尔的浓度优选为0．1％-5％。当米诺地尔的浓度低于0．1％时，其头发生长作用就很弱，当大于5％时，就难以设计该制剂。
依据本发明，氨基酸的含量越高，阻止该液体制剂变色的作用就越强，但是按1重量份的米诺地尔计，氨基酸的含量优选为0．01-20重量份。
在本发明液体组合物中，溶剂优选为含水有机溶剂，这是因为氨基酸不能溶于单独的有机溶剂，而米诺地尔不能溶于单独的水。水含量优选为10％-50％(体积比)。本发明所用有机溶剂必须能与水均相混合，并且当用作皮肤外用制剂时不能有任何副作用。鉴于此，有机溶剂的优选实例是具有1-6个碳原子的醇(例如乙醇、丙醇、异丙醇、乙二醇、丙二醇、1，3-丁二醇、甘油等)，特别优选的溶剂是选自乙醇、丙二醇和1，3-丁二醇的一种或多种醇。
依据本发明，从防止变色角度考虑，当用纯化水稀释20倍时，液体制剂的的pH优选被调节至4-9。
根据本发明，米诺地尔的液体组合物的保存容器可以选用普通液体制剂常用的容器，特别优选采用PET、玻璃、聚乙烯、聚丙烯等材料。
本发明的液体组合物可采用制备液体制剂的常规方法来制备，不过配合氨基酸时，从氨基酸溶解的角度来说，最好先用水溶解再与有机溶剂混合，因为氨基酸在含水有机溶剂中的溶解速度慢。
本发明的液体制剂中可以配合外用液体制剂中常用的成分(助溶剂、增稠剂、吸收促进剂、pH调节剂等)。
根据本发明，在组合物中组合氨基酸，不仅确认有防止变色的作用，另外还可望显示出氨基酸所具有的药理作用(抗炎作用、降低皮肤刺激作用、止痒作用等)。
实施本发明的最佳方式
通过下述实施例和实验来更详细地说明本发明。实施例1
将1克米诺地尔、0．04g牛磺酸、10g丙二醇、60g乙醇以及使总体积为100ml的纯化水在搅拌下溶解，因此获得了液体制剂。对比实施例1
按照与实施例1相同的方法，除了不使用牛磺酸之外采用相同配方，制得了对比液体制剂。实验1
将实施例1和对比实施例1所得液体制剂置于3个透明的玻璃瓶中，在室温用3000lux的光照射34天。在实验开始和结束时于420nm波长、1cm比色皿长度测定吸光度。结果如表1所示。表l
实施例2
| 实施例1 | 对比实施例1 | |||||
| 检品1 | 检品2 | 检品3 | 检品1 | 检品2 | 检品3 | |
| 实验开始时实验结束时 | 0．0020．056 | 0．0020．050 | 0．0020．058 | 0．0010．090 | 0．0010．077 | 0．0010．097 |
将1克米诺地尔、0．1g牛磺酸、10g丙二醇、60g乙醇以及使总体积为100ml的纯化水在搅拌下溶解，因此获得了液体制剂。实验2
将实施例2和对比实施例1所得液体制剂分置于3个透明的玻璃瓶中，通过窗户接受日光照射、在室温放置6个月。30天和6个月后，让3个不知道液体制剂组成的检验员用目测判断变色情况。此外，在实验开始和6个月后，于420nm波长、1cm比色皿长度测定吸光度。结果如表2所示。表2
| 实施例2 | 对比实施例1 | |
| 颜色 吸光度 | 颜色 吸光度 | |
| 实验开始时 | 无色 0．002 | 无色 0．002 |
| 30天 | 无色 - | 浅黄色 - |
| 6个月 | 浅黄色 0．152 | 深黄色 0．508 |
工业实用性
本发明能防止含米诺地尔的液体制剂变色，因此在商业上可用作优良的头发生长制剂。
Claims (10)
1．含有米诺地尔和氨基酸的液体组合物。
2．权利要求1的液体组合物，其中所述氨基酸是含硫氨基酸。
3．权利要求1的液体组合物，其中所述氨基酸是牛磺酸。
4．权利要求1的液体组合物，其中按1重量份的米诺地尔计，氨基酸的含量是0．01-20重量份。
5．权利要求1-4任一项的液体组合物，其中所用溶剂是水和具有1-6个碳原子的醇的混合物。
6．权利要求5的液体组合物，其中水在水和具有1-6个碳原子的醇的混合物中的含量为10％-50％(体积比)。
7．权利要求5的液体组合物，其中所述具有1-6个碳原子的醇是选自乙醇、丙二醇和1，3-丁二醇的一种或多种醇。
8．权利要求1-7任一项的液体组合物，其中按整个制剂的总重量计，米诺地尔的含量为0．1％-5％。
9．防止含米诺地尔的液体组合物变色的活性剂，其中所述活性剂含氨基酸作为有效组分。
10．防止含米诺地尔的液体组合物变色的方法，其特征在于加入氨基酸。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP333060/1997 | 1997-12-03 | ||
| JP33306097 | 1997-12-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1280507A true CN1280507A (zh) | 2001-01-17 |
Family
ID=18261827
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN98811791A Pending CN1280507A (zh) | 1997-12-03 | 1998-12-02 | 含米诺地尔的液体组合物 |
Country Status (12)
| Country | Link |
|---|---|
| EP (1) | EP1050310A1 (zh) |
| JP (1) | JP4390030B2 (zh) |
| KR (1) | KR20010032724A (zh) |
| CN (1) | CN1280507A (zh) |
| AU (1) | AU736407B2 (zh) |
| BR (1) | BR9815347A (zh) |
| CA (1) | CA2311731A1 (zh) |
| ID (1) | ID24902A (zh) |
| NO (1) | NO20002797L (zh) |
| NZ (1) | NZ504825A (zh) |
| TW (1) | TW592716B (zh) |
| WO (1) | WO1999027966A1 (zh) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1813699B (zh) * | 2001-06-14 | 2012-04-18 | 大塚制药株式会社 | 药物组合物 |
| CN115501178A (zh) * | 2022-08-26 | 2022-12-23 | 山东京卫制药有限公司 | 含有米诺地尔的稳定的液体组合物及其制备方法 |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4610040B2 (ja) | 2000-04-04 | 2011-01-12 | 東レ・ダウコーニング株式会社 | 育毛剤用添加剤及び育毛剤組成物 |
| ATE368463T1 (de) * | 2001-05-15 | 2007-08-15 | Taisho Pharmaceutical Co Ltd | Minoxidil-enthaltende flüssige zusammensetzung |
| JP2005075735A (ja) * | 2003-08-28 | 2005-03-24 | Rohto Pharmaceut Co Ltd | オキシメタゾリン含有組成物 |
| JP6261874B2 (ja) * | 2013-04-24 | 2018-01-17 | ロート製薬株式会社 | ミノキシジル含有外用組成物 |
| JP6244101B2 (ja) * | 2013-04-24 | 2017-12-06 | ロート製薬株式会社 | ミノキシジル含有外用組成物 |
| JP2017210480A (ja) * | 2017-08-07 | 2017-11-30 | ロート製薬株式会社 | ミノキシジル含有外用組成物 |
| JP2017226692A (ja) * | 2017-09-05 | 2017-12-28 | ロート製薬株式会社 | ミノキシジル含有外用組成物 |
| JP2018199738A (ja) * | 2018-10-02 | 2018-12-20 | ロート製薬株式会社 | ミノキシジル含有外用組成物 |
| JP2018199739A (ja) * | 2018-10-02 | 2018-12-20 | ロート製薬株式会社 | ミノキシジル含有外用組成物 |
| CN109431996B (zh) * | 2018-12-28 | 2021-09-10 | 浙江万晟药业有限公司 | 一种含米诺地尔的外用剂组合物及其制备方法 |
| JP2020189883A (ja) * | 2020-08-24 | 2020-11-26 | ロート製薬株式会社 | ミノキシジル含有外用組成物 |
| BR102021003531A2 (pt) | 2021-02-24 | 2022-08-30 | Eurofarma Laboratorios S.A. | Composição farmacêutica tópica espumável |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5235729B2 (zh) * | 1973-02-12 | 1977-09-10 | ||
| JPS5195120A (en) * | 1975-02-10 | 1976-08-20 | Tenganekino seizoho | |
| JPS5888306A (ja) * | 1981-11-19 | 1983-05-26 | Takeo Kinji | 養毛化粧料 |
-
1998
- 1998-12-02 AU AU13507/99A patent/AU736407B2/en not_active Ceased
- 1998-12-02 CN CN98811791A patent/CN1280507A/zh active Pending
- 1998-12-02 WO PCT/JP1998/005446 patent/WO1999027966A1/ja not_active Application Discontinuation
- 1998-12-02 BR BR9815347-1A patent/BR9815347A/pt not_active IP Right Cessation
- 1998-12-02 KR KR1020007006013A patent/KR20010032724A/ko not_active Application Discontinuation
- 1998-12-02 NZ NZ504825A patent/NZ504825A/en unknown
- 1998-12-02 ID IDW20001043A patent/ID24902A/id unknown
- 1998-12-02 CA CA002311731A patent/CA2311731A1/en not_active Abandoned
- 1998-12-02 JP JP2000522951A patent/JP4390030B2/ja not_active Expired - Lifetime
- 1998-12-02 EP EP98957141A patent/EP1050310A1/en not_active Withdrawn
-
1999
- 1999-05-26 TW TW088108677A patent/TW592716B/zh not_active IP Right Cessation
-
2000
- 2000-05-31 NO NO20002797A patent/NO20002797L/no not_active Application Discontinuation
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1813699B (zh) * | 2001-06-14 | 2012-04-18 | 大塚制药株式会社 | 药物组合物 |
| CN115501178A (zh) * | 2022-08-26 | 2022-12-23 | 山东京卫制药有限公司 | 含有米诺地尔的稳定的液体组合物及其制备方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20010032724A (ko) | 2001-04-25 |
| JP4390030B2 (ja) | 2009-12-24 |
| AU736407B2 (en) | 2001-07-26 |
| TW592716B (en) | 2004-06-21 |
| NO20002797D0 (no) | 2000-05-31 |
| CA2311731A1 (en) | 1999-06-10 |
| EP1050310A1 (en) | 2000-11-08 |
| BR9815347A (pt) | 2000-10-10 |
| WO1999027966A1 (fr) | 1999-06-10 |
| NZ504825A (en) | 2001-11-30 |
| AU1350799A (en) | 1999-06-16 |
| ID24902A (id) | 2000-08-31 |
| NO20002797L (no) | 2000-05-31 |
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