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公开(公告)号：US06300452B1
公开(公告)日：2001-10-09
申请号：US09442403
申请日：1999-11-18
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。
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公开(公告)号：US06794464B2
公开(公告)日：2004-09-21
申请号：US10298195
申请日：2002-11-18
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。
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公开(公告)号：US6117442A
公开(公告)日：2000-09-12
申请号：US190607
申请日：1998-11-12
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。
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公开(公告)号：US06476079B1
公开(公告)日：2002-11-05
申请号：US09472126
申请日：1999-12-23
IPC分类号： A16K4732
CPC分类号： A61K9/0024 , A61K9/0039 , A61K31/122 , A61K31/277 , A61K31/4418 , A61K31/50 , A61K31/502 , A61K31/565 , A61K31/569 , A61K31/575 , A61K31/58 , C08G77/18 , C08G77/44 , C08G77/46 , C08G77/50 , C08G77/70 , C08L83/04 , C08L83/12 , Y10S514/843 , C08L2666/14
摘要： A device for the controlled release over a prolonged period of time of a drug having antiprogestinic properties, the device including a core containing the drug, optionally a membrane encasing the core, where at least one of the core and membrane, when present, is made of a siloxane-based elastomer composition including at least one elastomer and optionally a non-crosslinked polymer. The device is characterized in that the elastomer composition includes poly(alkylene oxide) groups and that the poly(alkylene oxide) groups are present in the elastomer or polymer as alkoxy-terminated grafts of polysiloxane units, or as blocks, the grafts or blocks being linked to the polysiloxane units by silicon-carbon bonds, or as a mixture of these forms.
摘要翻译： 一种用于具有抗过药性质的药物在长时间内控制释放的装置，该装置包括含有该药物的核心，任选地包含核心的膜，其中存在核心和膜中的至少一个 的包含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。 该装置的特征在于，弹性体组合物包括聚（环氧烷）基团，并且聚（环氧烷）基团作为烷氧基封端的聚硅氧烷单元的接枝物存在于弹性体或聚合物中，或作为嵌段，所述接枝物或嵌段是 通过硅 - 碳键与聚硅氧烷单元连接，或作为这些形式的混合物。
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公开(公告)号：US06299894B1
公开(公告)日：2001-10-09
申请号：US09568027
申请日：2000-05-10
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。
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6.发明授权Drug delivery device especially for the delivery of progestins and estrogens 有权药物输送装置特别适用于输送孕激素和雌激素
公开(公告)号：US6063395A
公开(公告)日：2000-05-16
申请号：US190606
申请日：1998-11-12
CPC分类号： A61K9/0092 , A61K31/565 , A61K31/569 , A61K31/57 , A61K31/575 , A61K9/0039 , A61K9/0024 , A61K9/0036
摘要： The invention relates to a delivery device for the controlled release of a therapeutically active agent, especially a progestin or an estrogen, over a prolonged period of time, said device including a core which contains the therapeutically active agent, and a membrane encasing the core wherein said 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，特别是孕激素或雌激素的递送装置，所述装置包括含有治疗活性剂的核心和包裹核心的膜，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类弹性体。
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7.发明授权Chromatographic purification of cyclosporing using a high pressure carbon dioxide eluent 失效使用高压二氧化碳洗脱液对环孢菌素进行色谱纯化
公开(公告)号：US5976381A
公开(公告)日：1999-11-02
申请号：US894957
申请日：1997-11-12
申请人： Juhani Lundell , Jarkko Ruohonen , Olli Aaltonen , Martti Alkio , Anneli Hase , Tapani Suortti
发明人： Juhani Lundell , Jarkko Ruohonen , Olli Aaltonen , Martti Alkio , Anneli Hase , Tapani Suortti
CPC分类号： C07K7/645
摘要： A process is provided for the preparation of pure cyclosporin which is purified chromatographically from a mixture of different cyclosporin forms and other substances prepared by fermentation. The process comprises feeding a mixture containing a desired form of cyclosporin with an eluent consisting of high pressure carbon dioxide and an adjuvant, into a chromatography column being packed with particles prepared of silica, and recovering from the eluent flow coming out of the chromatography column a fraction which contains the desired cyclosporin form in adequately pure form.
摘要翻译： PCT No.PCT / FI96 / 00120 Sec。 371日期1997年11月12日 102（e）日期1997年11月12日PCT 1996年3月1日PCT公布。 公开号WO96 / 27607 日期1996年9月12日提供用于制备纯环孢菌素的方法，其由不同环孢菌素形式和通过发酵制备的其它物质的混合物进行色谱纯化。 该方法包括将含有所需形式的环孢菌素的混合物与由高压二氧化碳和佐剂组成的洗脱液加入到填充有由二氧化硅制备的颗粒的色谱柱中，并从色谱柱出来的洗脱液流中回收 含有所需环孢菌素形式的足够纯度的级分。
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公开(公告)号：US5237094A
公开(公告)日：1993-08-17
申请号：US838422
申请日：1992-04-30
申请人： Klaus Lampi , Kauko Nieminen , Jarkko Ruohonen
发明人： Klaus Lampi , Kauko Nieminen , Jarkko Ruohonen
IPC分类号： C07F9/38
CPC分类号： C07F9/3839
摘要： The present invention concerns a novel process for the preparation of methylenebisphosphonic acids of the formula I ##STR1## wherein Q.sup.1 and Q.sup.2 are independently hydrogen or halogen, by hydrolyzing the corresponding methylenebisphosphonic acid tetraester of the formula ##STR2## wherein R has the meaning of a straight or branched alkyl group containing 1 to 4 carbon atoms, and Q.sup.1 and Q.sup.2 have the same meaning as above.
摘要翻译： PCT No.PCT / FI90 / 00197 Sec。 一九九二年四月三十日 102（e）日期1992年4月30日PCT提交1990年8月15日PCT公布。 公开号WO91 / 03480 1991年3月21日。本发明涉及一种制备式I（I）的亚甲基双膦酸的新方法，其中Q1和Q2独立地为氢或卤素，通过水解相应的式（I）的亚甲基双膦酸四酯 （II）其中R具有含有1至4个碳原子的直链或支链烷基，Q1和Q2具有与上述相同的含义。
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