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1. 发明专利

CA2904432A1 HIGH DRUG LOAD BUPRENORPHINE MICROSPHERES AND METHOD OF PRODUCING THE SAME 未知
公开(公告)号：CA2904432A1
公开(公告)日：2014-09-18
申请号：CA2904432
申请日：2014-03-14
申请人： THANOO BAGAVATHIKANUN CHITHAMBARA , OAKWOOD LAB LLC , RICHEY TRACY
发明人： THANOO BAGAVATHIKANUN CHITHAMBARA , RICHEY TRACY
IPC分类号： A61K47/32 , A61K9/16 , A61K9/48 , A61K31/485 , A61K47/30
摘要： A sustained release microsphere formulation with a high drug load may be formed by a continuous oil-in-water emulsion process by combining an organic dispersed phase with an aqueous continuous phase. The dispersed phase may include an encapsulating polymer, a primary solvent, such as dichloromethane, a pharmaceutically effective amount of an active agent having a solubility relative to the dispersed phase, and a co-solvent, such as benzyl alcohol, which is capable of increasing the solubility of the active agent relative to the dispersed phase. The continuous phase may include an aqueous solution of polyvinyl alcohol and water.

2. 发明专利

ES2717942T3 Microesferas de buprenorfina de alta carga de fármaco y método de producción de las mismas 未知
公开(公告)号：ES2717942T3
公开(公告)日：2019-06-26
申请号：ES14764439
申请日：2014-03-14
申请人： OAKWOOD LABORATORIES LLC , RICHEY TRACY , THANOO BAGAVATHIKANUN CHITHAMBARA
发明人： RICHEY TRACY , THANOO BAGAVATHIKANUN
IPC分类号： A61K31/485 , A61K9/10 , A61K9/50

3. 发明申请

WO2014144309A1 SUSTAINED RELEASE MICROSPHERES AND METHOD OF PRODUCING THE SAME 审中-公开
标题翻译：可持续释放微生物及其生产方法
公开(公告)号：WO2014144309A1
公开(公告)日：2014-09-18
申请号：PCT/US2014/028657
申请日：2014-03-14
申请人： OAKWOOD LABORATORIES , RICHEY, Tracy , THANOO, Bagavathikanun, Chithambara
发明人： RICHEY, Tracy , THANOO, Bagavathikanun, Chithambara
IPC分类号： A61K9/48 , A61K9/16 , A61K47/10 , A61K47/30
CPC分类号： A61K9/1694 , A61K9/1647 , A61K31/573
摘要： A method of making a sustained release microsphere formulation, wherein the release rate of a bioactive ingredient is manipulated by controlling the crystallinity of said bioactive ingredient, includes the steps of combining the active ingredient and an encapsulating polymer in at least one solvent, or mixtures thereof, to form a dispersed phase and processing the dispersed phase without filtering, filtering the combined dispersed phase with a hydrophobic or a hydrophilic filter, or filtering the active ingredient and encapsulating polymer individually with a hydrophobic or hydrophilic filter before combining them to form the dispersed phase. The dispersed phase is then combined with a continuous phase to form the microsphere formulation.
摘要翻译：一种制备持续释放微球制剂的方法，其中通过控制所述生物活性成分的结晶度来操纵生物活性成分的释放速率，包括将活性成分与包封聚合物组合在至少一种溶剂或其混合物中的步骤，以形成分散相并处理分散相而不进行过滤，用疏水或亲水过滤器过滤组合的分散相，或者在将它们组合之前用疏水或亲水过滤器单独过滤活性成分和包封聚合物以形成分散相。然后将分散相与连续相组合以形成微球体制剂。

4. 发明专利

CA2909303C SUSTAINED RELEASE MICROSPHERES AND METHOD OF PRODUCING THE SAME 未知
公开(公告)号：CA2909303C
公开(公告)日：2021-10-19
申请号：CA2909303
申请日：2014-03-14
申请人： RICHEY TRACY , THANOO BAGAVATHIKANUN CHITHAMBARA , OAKWOOD LABORATORIES LLC
发明人： RICHEY TRACY , THANOO BAGAVATHIKANUN CHITHAMBARA
IPC分类号： A61K9/48 , A61K9/16 , A61K47/10 , A61K47/30
摘要： A method of making a sustained release microsphere formulation, wherein the release rate of a bioactive ingredient is manipulated by controlling the crystallinity of said bioactive ingredient, includes the steps of combining the active ingredient and an encapsulating polymer in at least one solvent, or mixtures thereof, to form a dispersed phase and processing the dispersed phase without filtering, filtering the combined dispersed phase with a hydrophobic or a hydrophilic filter, or filtering the active ingredient and encapsulating polymer individually with a hydrophobic or hydrophilic filter before combining them to form the dispersed phase. The dispersed phase is then combined with a continuous phase to form the microsphere formulation.

5. 发明专利

ES2697696T3 Microesferas de liberación sostenida y método de producción de las mismas 未知
公开(公告)号：ES2697696T3
公开(公告)日：2019-01-25
申请号：ES14762738
申请日：2014-03-14
申请人： OAKWOOD LABORATORIES LLC , RICHEY TRACY , THANOO BAGAVATHIKANUN CHITHAMBARA
发明人： RICHEY TRACY , THANOO BAGAVATHIKANUN CHITHAMBARA
IPC分类号： A61K9/48 , A61K9/16 , A61K47/10 , A61K47/30
摘要： Un método de fabricación de una formulación de microesferas de liberación sostenida, en donde la velocidad de liberación de un ingrediente bioactivo se manipula controlando la cristalinidad de dicho ingrediente bioactivo, que comprende las etapas de: (a) esterilizar un ingrediente activo para formar un ingrediente activo esterilizado; en donde el ingrediente activo es betametasona; (b) disolver un polímero de encapsulado en un disolvente o mezclas de los mismos; en donde el polímero de encapsulado se selecciona a partir de una polilactida o polilactida-co-glicolida; (c) filtrar el resultado de la etapa (b); en donde dicho filtrado se consigue con un filtro hidrófobo o hidrófilo; (d) combinar (a) y la etapa (c) para formar una fase dispersa, (e) combinar la fase dispersa con una fase continua para formar la formulación de microesferas.

6. 发明专利

CA2909303A1 SUSTAINED RELEASE MICROSPHERES AND METHOD OF PRODUCING THE SAME 未知
公开(公告)号：CA2909303A1
公开(公告)日：2014-09-18
申请号：CA2909303
申请日：2014-03-14
申请人： OAKWOOD LAB , RICHEY TRACY , THANOO BAGAVATHIKANUN CHITHAMBARA
发明人： RICHEY TRACY , THANOO BAGAVATHIKANUN CHITHAMBARA
IPC分类号： A61K9/48 , A61K9/16 , A61K47/10 , A61K47/30
摘要： A method of making a sustained release microsphere formulation, wherein the release rate of a bioactive ingredient is manipulated by controlling the crystallinity of said bioactive ingredient, includes the steps of combining the active ingredient and an encapsulating polymer in at least one solvent, or mixtures thereof, to form a dispersed phase and processing the dispersed phase without filtering, filtering the combined dispersed phase with a hydrophobic or a hydrophilic filter, or filtering the active ingredient and encapsulating polymer individually with a hydrophobic or hydrophilic filter before combining them to form the dispersed phase. The dispersed phase is then combined with a continuous phase to form the microsphere formulation.

7. 发明申请

WO2014143839A1 HIGH DRUG LOAD BUPRENORPHINE MICROSPHERES AND METHOD OF PRODUCING THE SAME 审中-公开
标题翻译：高剂量负载布地尼定微生物及其生产方法
公开(公告)号：WO2014143839A1
公开(公告)日：2014-09-18
申请号：PCT/US2014/027982
申请日：2014-03-14
申请人： OAKWOOD LABORATORIES LLC , RICHEY, Tracy , THANOO, Bagavathikanun, Chithambara
发明人： RICHEY, Tracy , THANOO, Bagavathikanun, Chithambara
IPC分类号： A61K47/32 , A61K47/30 , A61K9/16 , A61K9/48 , A61K31/485
CPC分类号： A61K9/5031 , A61K9/10 , A61K9/1647 , A61K9/5089 , A61K31/485
摘要： A sustained release microsphere formulation with a high drug load may be formed by a continuous oil-in-water emulsion process by combining an organic dispersed phase with an aqueous continuous phase. The dispersed phase may include an encapsulating polymer, a primary solvent, such as dichloromethane, a pharmaceutically effective amount of an active agent having a solubility relative to the dispersed phase, and a co-solvent, such as benzyl alcohol, which is capable of increasing the solubility of the active agent relative to the dispersed phase. The continuous phase may include an aqueous solution of polyvinyl alcohol and water.
摘要翻译：具有高药物负荷的缓释微球制剂可以通过将有机分散相与含水连续相组合而通过连续的水包油乳液方法形成。分散相可以包括包封聚合物，主要溶剂如二氯甲烷，药物有效量的具有相对于分散相的溶解度的活性剂，以及能够增加的共溶剂如苄醇活性剂相对于分散相的溶解度。连续相可以包括聚乙烯醇和水的水溶液。

8. 发明申请

WO2011087496A1 MICROSPHERES FOR THE SUSTAINED RELEASE OF OCTREOTIDE WITHOUT AN INITIAL TIME LAG 审中-公开
标题翻译：在没有初始时间段的情况下持续释放奥曲肽的MICROSPHERES
公开(公告)号：WO2011087496A1
公开(公告)日：2011-07-21
申请号：PCT/US2010/020895
申请日：2010-01-13
申请人： OAKWOOD LABORATORIES LLC , THANOO, Bagavathikanun, Chithambara , JOHNS, Gonto
发明人： THANOO, Bagavathikanun, Chithambara , JOHNS, Gonto
IPC分类号： A01N37/18
CPC分类号： A61K9/1647 , A61K9/0024
摘要： Microspheres for releasing an octreotide compound without an initial time lag include a poly(D,L-lactide-co-glycolide) polymer (PLGA polymer) matrix having a ratio of lactide to glycolide ranging from 80:20 to 90: 10 mol%. The polymer has a molecular weight ranging from about 6000 to 16000. The octreotide compound is dispersed in the polymer matrix. The microspheres can be made by forming a dispersed phase by combining the above polymer, dichloromethane, the octreotide compound, methanol and acetic acid. A target loading of the octreotide compound in the dispersed phase ranges from 7 to 12% by weight. Polyvinyl alcohol is dissolved in water to form a continuous phase. The dispersed phase is mixed in the continuous phase to form a microsphere suspension. The dichloromethane, acetic acid, methanol and polyvinyl alcohol are removed from the microsphere suspension. Residual dichloromethane and methanol are removed from the microspheres by washing.
摘要翻译：用于释放没有初始时滞的奥曲肽化合物的微球包括丙交酯与乙交酯的比率为80:20至90:10mol％的聚（D，L-丙交酯 - 共 - 乙交酯）聚合物（PLGA聚合物）基质。聚合物的分子量范围为约6000至16000.奥曲肽化合物分散在聚合物基质中。可以通过将上述聚合物，二氯甲烷，奥曲肽化合物，甲醇和乙酸组合形成分散相来制备微球。奥曲肽化合物在分散相中的靶装载量为7至12重量％。将聚乙烯醇溶于水中形成连续相。将分散相在连续相中混合以形成微球悬浮液。从微球悬浮液中除去二氯甲烷，乙酸，甲醇和聚乙烯醇。通过洗涤从微球中除去残留的二氯甲烷和甲醇。

9. 发明申请

WO2012112747A2 MANUFACTURE OF MICROSPHERES USING A HYDROCYCLONE 审中-公开
标题翻译：使用氢氯酸盐制备微球
公开(公告)号：WO2012112747A2
公开(公告)日：2012-08-23
申请号：PCT/US2012/025378
申请日：2012-02-16
申请人： OAKWOOD LABORATORIES, LLC , THANOO, Bagavathikanun, Chithambara , SMITH, Edward, Caldwell , SMITH, Mark
发明人： THANOO, Bagavathikanun, Chithambara , SMITH, Edward, Caldwell , SMITH, Mark
IPC分类号： B01J19/20 , B01J2/08 , B01J4/00 , B01J13/02
CPC分类号： F04F5/44 , F04B43/12
摘要： This disclosure features a system for processing microspheres. A vessel contains a suspension of solidified microspheres comprising polymer and an active agent. A hydrocyclone has a fluid inlet, a first fluid outlet and a second fluid outlet. The fluid inlet is in fluid communication with the vessel and receives the suspension. The second fluid outlet contains a flow of the suspension having concentrated microspheres. The first fluid outlet contains a flow of a relatively large amount of liquid compared to the flow from the second fluid outlet. Also featured is a method of processing the microspheres using the hydrocyclone.
摘要翻译：该公开内容特征在于用于处理微球体的系统。容器含有包含聚合物和活性剂的固化微球的悬浮液。水力旋流器具有流体入口，第一流体出口和第二流体出口。流体入口与容器流体连通并接收悬架。第二流体出口含有具有浓缩微球的悬浮液流。与来自第二流体出口的流相比，第一流体出口含有相对大量的液体流。还特征在于使用水力旋流器处理微球的方法。

10. 发明申请

WO2010065513A1 METHOD OF MAKING SUSTAINED RELEASE MICROPARTICLES 审中-公开
标题翻译：制备持续释放微生物的方法
公开(公告)号：WO2010065513A1
公开(公告)日：2010-06-10
申请号：PCT/US2009/066212
申请日：2009-12-01
申请人： OAKWOOD LABORATORIES, LLC , THANOO, Bagavathikanun, Chithambara , JOHNS, Gonto, III , WOO, Byung, Ho
发明人： THANOO, Bagavathikanun, Chithambara , JOHNS, Gonto, III , WOO, Byung, Ho
IPC分类号： A61K9/14
CPC分类号： A61K31/519 , A61K9/1647 , A61K9/1682 , A61K9/1694
摘要： Various embodiments of a method of preparing sustained release microparticles are described. In one embodiment, the method includes the steps of forming a dispersed phase of an active agent in a polymer and combining the dispersed phase with a continuous phase to form a microparticle dispersion. The method further includes the step of adding a measured amount of a dilution composition to the microparticle dispersion. It has been found herein that the various embodiments for preparing sustained release microparticles using various amounts of the dilution composition alters the release rate of the sustained microparticle for the specific active agent.
摘要翻译：描述了制备缓释微粒的方法的各种实施方案。在一个实施方案中，该方法包括以下步骤：在聚合物中形成活性剂的分散相并将分散相与连续相组合以形成微粒分散体。该方法还包括将测量量的稀释组合物加入到微粒分散体中的步骤。已经发现，使用各种量的稀释组合物制备缓释微粒的各种实施方案改变了用于特定活性剂的持续微粒的释放速率。

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