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1. 发明授权

US06794464B2 Membrane or matrix for controlling the permeation rate of drugs 有权
标题翻译：用于控制药物渗透速率的膜或基质
公开(公告)号：US06794464B2
公开(公告)日：2004-09-21
申请号：US10298195
申请日：2002-11-18
申请人： Harri Jukarainen , Tommi Markkula , Juha Ala-Sorvari , Matti Lehtinen , Jarkko Ruohonen
发明人： Harri Jukarainen , Tommi Markkula , Juha Ala-Sorvari , Matti Lehtinen , Jarkko Ruohonen
IPC分类号： C08L8310
CPC分类号： C08L83/12 , A61K9/0024 , A61K9/0036 , A61K9/0039 , A61K9/2027 , A61K9/2031
摘要： A membrane or matrix for controlling the permeation rate of a drug, where the membrane or matrix includes a siloxane-based elastomer composition which contains at least one elastomer and optionally a non-crosslinked polymer. The elastomer composition includes poly(alkylene oxide) groups, and the poly(alkylene oxide) groups are present as blocks in a chain of the elastomer or the polymer, or as blocks and alkoxy-terminated grafts of polysiloxane units, the blocks or blocks and grafts being linked to the polysiloxane units by silicon-carbon bonds, with at least three blocks being present in the elastomer or polymer chain. Methods for the preparation of the elastomer composition are also disclosed.
摘要翻译：用于控制药物渗透速率的膜或基质，其中膜或基质包括含有至少一种弹性体和任选的非交联聚合物的硅氧烷基弹性体组合物。弹性体组合物包括聚（环氧烷）基团，聚（环氧烷）基团作为嵌段存在于弹性体或聚合物的链中，或作为聚硅氧烷单元的嵌段和烷氧基封端的接枝物，嵌段或嵌段接枝物通过硅 - 碳键与聚硅氧烷单元连接，至少有三个嵌段存在于弹性体或聚合物链中。还公开了制备弹性体组合物的方法。

2. 发明授权

US6117442A Drug delivery device, especially for the delivery of androgens 有权
标题翻译：药物输送装置，特别是用于输送雄激素
公开(公告)号：US6117442A
公开(公告)日：2000-09-12
申请号：US190607
申请日：1998-11-12
申请人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
发明人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
IPC分类号： A61K9/52 , A61K9/00 , A61K31/565 , A61K31/568 , A61K47/34 , A61P15/16 , A61P15/18 , A61F13/00
CPC分类号： A61K9/0024
摘要： The invention relates to a delivery device for the controlled release of a therapeutically active agent, especially an androgen, over a prolonged period of time, said device including a core containing the therapeutically active agent, and a membrane encasing the core wherein the membrane is made of an elastomer. According to the invention, the elastomer is a siloxane-based elastomer which includes 3,3,3-trifluoropropyl groups attached to the Si-atoms of the siloxane units.
摘要翻译：本发明涉及用于在更长时间内控制释放治疗活性剂，特别是雄激素的递送装置，所述装置包括含有治疗活性剂的核心和包围核心的膜，其中制成膜的弹性体。根据本发明，弹性体是包含连接到硅氧烷单元的Si原子上的3,3,3-三氟丙基的硅氧烷类弹性体。

3. 发明授权

US06299894B1 Drug delivery device, especially for the delivery of gestodene 有权
标题翻译：药物输送装置，特别是用于递送吉司他丁
公开(公告)号：US06299894B1
公开(公告)日：2001-10-09
申请号：US09568027
申请日：2000-05-10
申请人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
发明人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Ruohonen
IPC分类号： A61F1300
CPC分类号： A61K9/0039
摘要： The invention relates to a delivery device for the controlled release of the therapeutically active agent gestodene, over a prolonged period of time, at a release rate of 0,1-300 &mgr;g/day, said device comprising a core comprising at least said therapeutically active agent, and a membrane encasing said core wherein said membrane is made of an elastomer. According to the invention, the elastomer is a siloxane-based elastomer comprising 3,3,3-trifluoropropyl groups attached to the Si-atoms of the siloxane units, and the release rate of said therapeutically active agent of said delivery device is regulated by the amount of said 3,3,3-trifluoropropyl groups.
摘要翻译：本发明涉及一种递送装置，用于在更长的时间内以0.01至300杯/天的释放速率控制释放治疗活性剂甘露聚糖，所述装置包含至少包含所述治疗活性物质的核心试剂和包封所述芯的膜，其中所述膜由弹性体制成。根据本发明，弹性体是包含连接到硅氧烷单元的Si原子上的3,3,3-三氟丙基的硅氧烷基弹性体，并且所述递送装置的所述治疗活性剂的释放速率由所述3,3,3-三氟丙基的量。

4. 发明授权

US06300452B1 Block copolymers and preparation thereof 有权
标题翻译：嵌段共聚物及其制备方法
公开(公告)号：US06300452B1
公开(公告)日：2001-10-09
申请号：US09442403
申请日：1999-11-18
申请人： Harri Jukarainen , Jarkko Ruohonen , Matti Lehtinen , Juha Ala-Sorvari , Jukka Seppälä
发明人： Harri Jukarainen , Jarkko Ruohonen , Matti Lehtinen , Juha Ala-Sorvari , Jukka Seppälä
IPC分类号： C08G7746
CPC分类号： C08G77/46 , C08F290/062 , C08F290/068
摘要： The invention relates to a new polysiloxane-based block copolymer having a formula T(AB)xAT (I) wherein A=—(SiR′R″O)nSiR′R″—, wherein R′ and R″ are the the same or different and represent a lower alkyl group or a phenyl group, wherein said alkyl or phenyl group may be substituted or unsubstituted; B is polyalkylene oxide of formula wherein R is hydrogen, lower alkyl, or phenyl; R1 is hydrogen or lower alkyl; y is 2-6; m is 1-30; n is 1-3000; and x is 0-100.
摘要翻译：本发明涉及一种新的聚硅氧烷基嵌段共聚物，其具有式（A） - （SiR'R''O）nSiR'R“ - ，其中R'和R”相同或不同，表示低级烷基或苯基，其中所述烷基或苯基可以是取代的或未取代的; B是式（Ⅳ）的聚环氧烷，R是氢，低级烷基或苯基; R 1是氢或低级烷基; y为2-6; m为1-30; n为1-3000; x为0-100。

5. 发明授权

US06056976A Elastomer, its preparation and use 有权
标题翻译：弹性体，其制备和使用
公开(公告)号：US06056976A
公开(公告)日：2000-05-02
申请号：US190608
申请日：1998-11-12
申请人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Rughonen
发明人： Tommi Markkula , Juha Ala-Sorvari , Harri Jukarainen , Matti Lehtinen , Jarkko Rughonen
IPC分类号： A61L27/00 , A61K9/00 , A61K9/20 , A61K9/52 , A61K9/58 , C08G77/24 , C08J5/18 , C08K3/36 , C08K5/54 , C08L83/04 , C08L83/08 , A61K9/14
CPC分类号： A61K9/0039 , A61K9/009 , A61K9/2036
摘要： The invention relates to a siloxane-based elastomer intended for controlling the permeation of drugs, wherein the elastomer includes 3,3,3,-trifluoropropyl groups attached to the Si-atoms of the siloxane units.The invention relates also to a method for the preparation of a siloxane-based elastomer including 3,3,3,-trifluoropropyl substituents, where the elastomer is intended for controlling the permeation of drugs.In the method eitheri) a 3,3,3,-trifluoropropyl-substituted vinyl-functional polysiloxane component and a silicon hydride-functional crosslinking agent are crosslinked in the presence of a catalyst, orii) a 3,3,3,-trifluoropropyl-substituted polysiloxane component is crosslinked in the presence of a peroxide catalyst.
摘要翻译：本发明涉及一种旨在控制药物渗透性的硅氧烷基弹性体，其中弹性体包括连接到硅氧烷单元的Si原子上的3,3,3-三氟丙基。本发明还涉及制备包含3,3,3-三氟丙基取代基的硅氧烷基弹性体的方法，其中弹性体用于控制药物的渗透。在该方法中，i）3,3,3,3-三氟丙基取代的乙烯基官能聚硅氧烷组分和硅氢化物官能的交联剂在催化剂存在下进行交联，或ii）3,3,3，三氟丙基取代的聚硅氧烷组分在过氧化物催化剂存在下交联。

6. 发明授权

US07294345B2 Otorhinological delivery device 有权
标题翻译：耳道输送装置
公开(公告)号：US07294345B2
公开(公告)日：2007-11-13
申请号：US10542420
申请日：2004-01-14
申请人： Timo Haapakumpu , Harri Jukarainen , Juha Ala-Sorvari , Henry Rankonen , Frederik E. Riphagen , Wolfgang Arnold
发明人： Timo Haapakumpu , Harri Jukarainen , Juha Ala-Sorvari , Henry Rankonen , Frederik E. Riphagen , Wolfgang Arnold
IPC分类号： A61F11/00
CPC分类号： A61K9/0046 , A61K9/0043 , A61L31/06 , A61L31/16 , Y10S514/953 , C08L83/04
摘要： The invention relates to an otorhinological delivery device comprising at least one pharmaceutically active agent. According to the invention the device comprises a core comprising said at least one pharmaceutically active agent wherein said core is made of an elastomer composition selected from the group consisting of poly(dimethylsiloxane), a siloxane-based elastomer comprising 3,3,3-trifluoropropyl groups attached to the Siatoms of the siloxane units, a siloxane-based elastomer comprising poly(alkylene oxide) groups and mixtures thereof, and a membrane encasing said core, said membrane being made of a same or a different elastomer composition than said core, said elastomer composition being selected from the group consisting of poly(dimethylsiloxane), a siloxane-based elastomer comprising 3,3,3-trifluoropropyl groups attached to the Siatoms of the siloxane units, a siloxane-based elastomer comprising poly(alkylene oxide) groups and mixtures thereof. The invention is characterized in that the pharmaceutically active agent is selected from the group comprising anti-allergic agents, anti-inflammatory agents, anti-fungicides, glucocorticoids and mixtures thereof.
摘要翻译：本发明涉及包含至少一种药物活性剂的运输装置。根据本发明，该装置包括一种包含所述至少一种药物活性剂的核心，其中所述核心由弹性体组合物制成，所述弹性体组合物选自聚（二甲基硅氧烷），包含3,3,3-三氟丙基连接到硅氧烷单元的硅原子的基团，包含聚（环氧烷）基团的硅氧烷基弹性体及其混合物，以及包围所述芯的膜，所述膜由与所述芯相同或不同的弹性体组合物制成，所述弹性体组合物选自聚（二甲基硅氧烷），包含连接到硅氧烷单元的硅原子上的3,3,3-三氟丙基的硅氧烷基弹性体，包含聚（氧化烯）基团的硅氧烷基弹性体和其混合物。本发明的特征在于药物活性剂选自抗过敏剂，抗炎剂，抗真菌剂，糖皮质激素及其混合物。

7. 发明申请

US20060067982A1 Otorhinological delivery device 有权
标题翻译：耳道输送装置
公开(公告)号：US20060067982A1
公开(公告)日：2006-03-30
申请号：US10542420
申请日：2004-01-14
申请人： Timo Haapakumpu , Harri Jukarainen , Juha Ala-Sorvari , Frederik Riphagen , Wolfgang Arnold
发明人： Timo Haapakumpu , Harri Jukarainen , Juha Ala-Sorvari , Frederik Riphagen , Wolfgang Arnold
IPC分类号： A61F11/00
CPC分类号： A61K9/0046 , A61K9/0043 , A61L31/06 , A61L31/16 , Y10S514/953 , C08L83/04
摘要： The invention relates to an otorhinological delivery device comprising at least one pharmaceutically active agent. According to the invention the device comprises a core comprising said at least one pharmaceutically active agent wherein said core is made of an elastomer composition selected from the group consisting of poly(dimethylsiloxane), a siloxane-based elastomer comprising 3,3,3-trifluoropropyl groups attached to the Siatoms of the siloxane units, a siloxane-based elastomer comprising poly(alkylene oxide) groups and mixtures thereof, and a membrane encasing said core, said membrane being made of a same or a different elastomer composition than said core, said elastomer composition being selected from the group consisting of poly(dimethylsiloxane), a siloxane-based elastomer comprising 3,3,3-trifluoropropyl groups attached to the Siatoms of the siloxane units, a siloxane-based elastomer comprising poly(alkylene oxide) groups and mixtures thereof. The invention is characterized in that the pharmaceutically active agent is selected from the group comprising anti-allergic agents, anti-inflammatory agents, anti-fungicides, glucocorticoids and mixtures thereof.
摘要翻译：本发明涉及包含至少一种药物活性剂的运输装置。根据本发明，该装置包括一种包含所述至少一种药物活性剂的核心，其中所述核心由弹性体组合物制成，所述弹性体组合物选自聚（二甲基硅氧烷），包含3,3,3-三氟丙基连接到硅氧烷单元的硅原子的基团，包含聚（环氧烷）基团的硅氧烷基弹性体及其混合物，以及包围所述芯的膜，所述膜由与所述芯相同或不同的弹性体组合物制成，所述弹性体组合物选自聚（二甲基硅氧烷），包含连接到硅氧烷单元的硅原子上的3,3,3-三氟丙基的硅氧烷基弹性体，包含聚（氧化烯）基团的硅氧烷基弹性体和其混合物。本发明的特征在于药物活性剂选自抗过敏剂，抗炎剂，抗真菌剂，糖皮质激素及其混合物。

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