CN1195991A - 预防和/或治疗毛发损失的制剂 - Google Patents
预防和/或治疗毛发损失的制剂 Download PDFInfo
- Publication number
- CN1195991A CN1195991A CN96196927A CN96196927A CN1195991A CN 1195991 A CN1195991 A CN 1195991A CN 96196927 A CN96196927 A CN 96196927A CN 96196927 A CN96196927 A CN 96196927A CN 1195991 A CN1195991 A CN 1195991A
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- 238000002360 preparation method Methods 0.000 title claims abstract description 9
- 230000001225 therapeutic effect Effects 0.000 claims abstract description 6
- 239000013543 active substance Substances 0.000 claims description 16
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- 201000004384 Alopecia Diseases 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 208000024963 hair loss Diseases 0.000 claims description 6
- 230000003676 hair loss Effects 0.000 claims description 6
- 239000010410 layer Substances 0.000 claims description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 239000004820 Pressure-sensitive adhesive Substances 0.000 claims description 3
- 239000011241 protective layer Substances 0.000 claims description 3
- -1 Methyl Chemical group 0.000 claims description 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 239000011737 fluorine Substances 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 2
- 229910052736 halogen Inorganic materials 0.000 claims description 2
- 150000002367 halogens Chemical class 0.000 claims description 2
- 230000007246 mechanism Effects 0.000 claims description 2
- 239000012528 membrane Substances 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 125000004218 chloromethyl group Chemical group [H]C([H])(Cl)* 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 230000002265 prevention Effects 0.000 abstract description 3
- 210000004209 hair Anatomy 0.000 abstract description 2
- 210000002268 wool Anatomy 0.000 abstract 1
- 241001465754 Metazoa Species 0.000 description 2
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical compound [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000002674 ointment Substances 0.000 description 2
- 229920001296 polysiloxane Polymers 0.000 description 2
- 229910052710 silicon Inorganic materials 0.000 description 2
- 239000010703 silicon Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 241001355260 Cissus Species 0.000 description 1
- 235000017003 Cissus Nutrition 0.000 description 1
- 235000017014 Cissus repens Nutrition 0.000 description 1
- 229930182650 Muricin Natural products 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000002778 food additive Substances 0.000 description 1
- 235000013373 food additive Nutrition 0.000 description 1
- 239000000155 melt Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 229940100471 muricin Drugs 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 239000002574 poison Substances 0.000 description 1
- 231100000614 poison Toxicity 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 239000003128 rodenticide Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- PJVWKTKQMONHTI-UHFFFAOYSA-N warfarin Chemical class OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/695—Silicon compounds
-
- 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
- A61K8/58—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
- A61K8/585—Organosilicon compounds
-
- 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
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
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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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Birds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Cosmetics (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
一种透皮治疗系统形式的含毒鼠硅的制剂,它适于预防和/或治疗毛发损失。
Description
本发明涉及用于预防和/或治疗毛发损失的透皮治疗系统(TTS)。
由德国专利说明书2615654已知取代毒鼠硅的作为毛发恢复剂的效力。所施用化合物的良好耐受性被特别强调。根据该文献，其给药效果可以通过作为食品添加剂或通过涂抹软膏或悬浮剂而达到，前者特别适用于动物给药。如果每周给药几次，治疗期大约在几个月之内。但是，现有技术仍不尽人意，原因在于需要很高的患者的配合性；另外，由于使用软膏或悬浮剂相关的已知缺陷，给药的活性物质的量难以控制。
正是由现有技术的这一情况出发，本发明的目的是在使用取代毒鼠硅预防和/或治疗毛发损失时，提供一种克服了上述缺陷的一种新的应用方式。
这一目的之达到是基于如下事实，即，制备透皮治疗系统的含下式取代毒鼠硅的制剂：
式中的定义如下：
R＝H或CH3，
Z＝一双键基团，包括1-3个碳原子和任选被氟取代，和
X＝H，低级烷基，芳基，卤素，CF3，CN，NH2，SH，CNS，R1M，(R2O)2P(O)，R3C(O)M，其中；
R1＝含1-4个碳原子的直链或支链的烷基，芳基，芳烷基，烷芳基，
M＝O，S
R2＝甲基、乙基、R3＝1-4个碳原子的烷基，1-4个碳原子的氟代烷基，或芳基。
治疗系统(TTS)含一种或多种活性物质，它们在一确定时间内以预定的速率连续释放于一确定的用药部位(Heilmann，Therapeutische Systeme-Konzept und Realisation programmierter Arzneiverabreichung，第四版，Ferdinand Enke Verlag Stuttgart，1984，26页)。
在这些治疗系统中，具有透皮作用的贴片根据本发明是优选的，一个原因在于毒鼠硅由于球形分子形状而适于皮肤渗透。
贴片形式的TTS对本领域技术人员而言是已知的。一般地，它们包括一不渗透的支持层，与其连接的活性物质库，一控制活性物质释放的膜(当没有其它控制机制时)，一种将贴片固定于皮肤上的压力敏感粘接装置，和如果必要，一种在使用前可以去除的保护层。如果活性物质库可以自行粘接，则TTS可以如下制备：在一合适的溶剂中均匀混合活性物质，辅剂和压力敏感粘接聚合物，将溶液摊铺于支持层上，除去溶剂，和使用保护层。也可以颠倒层的顺序。
原则上活性物质库也可以由熔化物制备。根据本发明所用的活性物质的一种合成方法，描述于德国专利说明书2522982。由于其良好的耐受性，1-(氯甲基)毒鼠硅和1-(乙氧基)毒鼠硅是特别优选的。
来自毒鼠硅系列的至少一种活性物质在库中的浓度至约0.1～50％(重量)，优选3～25％(重量)，和最优选5～15％(重量)。然后根据层厚度和库尺寸的选择可以调节每个贴片中的剂量。在其它方面，取决于病人的年龄和皮肤表面。以及毛发损失的类型和程度。
当用于动物时，相似的方案也是可行的。
含毒鼠硅的TTS提供了一种药剂的应用形式，该药剂可以在更长的时间内使用以预防和治疗毛发损失，它可使一个单剂给药的有效期延续几周或几个月，并确保了活性物质的理想剂量。另外，毒鼠硅的全身作用可以使局部给药成为不必要。
Claims (6)
1.一种预防和/或治疗毛发损失的制剂，含有下式的活性物质毒鼠硅：其中，
R＝H或CH3，
Z＝一双键基团，包括1-3个碳原子和任选被氟取代，和
X＝H，低级烷基，芳基，卤素，CF3，CN，NH2，SH，CNS，R1M，(R2O)2P(O)，R3C(O)M，R1＝含1-4个碳原子的直链或支链烷基，芳基，芳烷基，烷芳基，M＝O、S，R2＝甲基、乙基，R3＝1-4个碳原子的烷基，1-4个碳原子的氟代烷基，或芳基，该制剂的特征在于其采用透皮治疗系统的形式。
2.权利要求1的制剂，其特征在于它是一种贴片。
3.权利要求2的制剂，其特征在于贴片包括一不渗透的支持层，与其连接的活性物质库，当没有其它控制机制时有一控制活性物质释放的膜，一种将贴片固定于皮肤上的压力敏感粘接装置，和如有必要，一种在使用前可以去除的保护层。
4.根据权利要求1-3中一项或几项的制剂，其特征在于它含0.1～50％(重量)，优选3～25％(重量)，和最优选5～15％(重量)的活性物质。
5.根据权利要求1-4中一项或几项的制剂，其特征在于它含作为活性物质的1-(氯甲基)-毒鼠硅。
6.根据权利要求1-4中一项或几项的制剂，其特征在于它含作为活性物质的1-(乙氧基)-毒鼠硅。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19534201.1 | 1995-09-15 | ||
| DE19534201A DE19534201A1 (de) | 1995-09-15 | 1995-09-15 | Zubereitung zur Prophylaxe und/oder Behandlung von Woll- und Haarausfall |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1195991A true CN1195991A (zh) | 1998-10-14 |
Family
ID=7772231
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN96196927A Pending CN1195991A (zh) | 1995-09-15 | 1996-08-29 | 预防和/或治疗毛发损失的制剂 |
Country Status (19)
| Country | Link |
|---|---|
| EP (1) | EP0850065B1 (zh) |
| JP (1) | JPH11512404A (zh) |
| KR (1) | KR19990044130A (zh) |
| CN (1) | CN1195991A (zh) |
| AT (1) | ATE184487T1 (zh) |
| AU (1) | AU701327B2 (zh) |
| CA (1) | CA2232026A1 (zh) |
| CZ (1) | CZ70098A3 (zh) |
| DE (2) | DE19534201A1 (zh) |
| ES (1) | ES2139382T3 (zh) |
| GR (1) | GR3032072T3 (zh) |
| HU (1) | HUP0400916A2 (zh) |
| IL (1) | IL123382A0 (zh) |
| NO (1) | NO981020L (zh) |
| NZ (1) | NZ316938A (zh) |
| PL (1) | PL325557A1 (zh) |
| SK (1) | SK22698A3 (zh) |
| WO (1) | WO1997009990A1 (zh) |
| ZA (1) | ZA967711B (zh) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6447858B2 (ja) * | 2016-07-08 | 2019-01-09 | Ｙａｎｃｈｅｒｓ株式会社 | 固形癌治療剤 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU686731A1 (ru) * | 1973-07-26 | 1979-09-25 | Иркутский институт органической химии СО АН СССР | Стимул тор роста волос ного покрова |
| DE2530255C3 (de) * | 1975-07-07 | 1978-08-31 | Irkutskij Institut Organitscheskoj Chimii Sibirskogo Otdelenija Akademii Nauk Ssr, Irkutsk (Sowjetunion) | l-(ChIormethyl)silatran, seine Herstellung und dieses enthaltende Zubereitungen |
| GB1465455A (en) * | 1975-07-14 | 1977-02-23 | Ir I Orch Khim Sib | Medicinal preparation ofr healing wounds and treating dermatites |
| US4055637A (en) * | 1975-08-15 | 1977-10-25 | Mikhail Grigorievich Voronkov | Medicinal preparation for healing wounds and treating dermatites using 1-(chloromethyl)silatrane |
| FR2321295A1 (fr) * | 1975-08-22 | 1977-03-18 | Ir I Orch | Produits medicamenteux pour cicatriser les plaies et traiter les dermatites |
| DE2615654C3 (de) * | 1976-04-09 | 1980-10-30 | Irkutskij Institut Organitscheskoj Chimii Sibirskogo Otdelenija Akademii Nauk Ssr, Irkutsk (Sowjetunion) | Salbenpräparat zur Intensivierung des WoIl- und Haarwachstums |
| JPS6176494A (ja) * | 1984-09-21 | 1986-04-18 | Tokuyama Soda Co Ltd | シラトラン化合物 |
-
1995
- 1995-09-15 DE DE19534201A patent/DE19534201A1/de not_active Withdrawn
-
1996
- 1996-08-29 WO PCT/EP1996/003783 patent/WO1997009990A1/de not_active Application Discontinuation
- 1996-08-29 EP EP96930118A patent/EP0850065B1/de not_active Expired - Lifetime
- 1996-08-29 DE DE59603099T patent/DE59603099D1/de not_active Expired - Fee Related
- 1996-08-29 AU AU69293/96A patent/AU701327B2/en not_active Ceased
- 1996-08-29 PL PL96325557A patent/PL325557A1/xx unknown
- 1996-08-29 ES ES96930118T patent/ES2139382T3/es not_active Expired - Lifetime
- 1996-08-29 JP JP9511606A patent/JPH11512404A/ja not_active Ceased
- 1996-08-29 CA CA002232026A patent/CA2232026A1/en not_active Abandoned
- 1996-08-29 HU HU0400916A patent/HUP0400916A2/hu unknown
- 1996-08-29 CN CN96196927A patent/CN1195991A/zh active Pending
- 1996-08-29 KR KR1019980701363A patent/KR19990044130A/ko not_active Application Discontinuation
- 1996-08-29 SK SK226-98A patent/SK22698A3/sk unknown
- 1996-08-29 NZ NZ316938A patent/NZ316938A/xx unknown
- 1996-08-29 CZ CZ98700A patent/CZ70098A3/cs unknown
- 1996-08-29 IL IL12338296A patent/IL123382A0/xx unknown
- 1996-08-29 AT AT96930118T patent/ATE184487T1/de active
- 1996-09-12 ZA ZA967711A patent/ZA967711B/xx unknown
-
1998
- 1998-03-09 NO NO981020A patent/NO981020L/no not_active Application Discontinuation
-
1999
- 1999-12-08 GR GR990403163T patent/GR3032072T3/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DE19534201A1 (de) | 1997-03-20 |
| CZ70098A3 (cs) | 1998-07-15 |
| ATE184487T1 (de) | 1999-10-15 |
| SK22698A3 (en) | 1998-07-08 |
| EP0850065B1 (de) | 1999-09-15 |
| KR19990044130A (ko) | 1999-06-25 |
| NZ316938A (en) | 1999-02-25 |
| HUP0400916A2 (hu) | 2004-11-29 |
| DE59603099D1 (de) | 1999-10-21 |
| AU701327B2 (en) | 1999-01-28 |
| AU6929396A (en) | 1997-04-01 |
| EP0850065A1 (de) | 1998-07-01 |
| NO981020D0 (no) | 1998-03-09 |
| WO1997009990A1 (de) | 1997-03-20 |
| PL325557A1 (en) | 1998-08-03 |
| NO981020L (no) | 1998-03-09 |
| IL123382A0 (en) | 1998-09-24 |
| ZA967711B (en) | 1997-03-26 |
| MX9802027A (es) | 1998-10-31 |
| JPH11512404A (ja) | 1999-10-26 |
| CA2232026A1 (en) | 1997-03-20 |
| GR3032072T3 (en) | 2000-03-31 |
| ES2139382T3 (es) | 2000-02-01 |
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| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |