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公开(公告)号：US09180093B2
公开(公告)日：2015-11-10
申请号：US13592235
申请日：2012-08-22
申请人： Kumaresh Soppimath , Satish Pejaver , Kanaiyalal R. Patel , Lakkaraju Dasaradhi , Rama Sodum , Hari Desu , Navneet Puri
发明人： Kumaresh Soppimath , Satish Pejaver , Kanaiyalal R. Patel , Lakkaraju Dasaradhi , Rama Sodum , Hari Desu , Navneet Puri
CPC分类号： A61K9/08 , A61K9/0019 , A61K9/19 , A61K31/4965 , A61K31/69 , A61K47/10 , C07B63/04
摘要： Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.
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公开(公告)号：US20110230441A1
公开(公告)日：2011-09-22
申请号：US13051102
申请日：2011-03-18
申请人： Kumaresh Soppimath , Satish Pejaver , Kanaiyalal R. Patel , Lakkaraju Dasaradhi , Rama Sodum , Hari Desu , Navneet Puri
发明人： Kumaresh Soppimath , Satish Pejaver , Kanaiyalal R. Patel , Lakkaraju Dasaradhi , Rama Sodum , Hari Desu , Navneet Puri
CPC分类号： A61K31/69 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K31/4965 , A61K47/10
摘要： Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.
摘要翻译： 硼替佐米的多剂量制剂被提出，其中硼替佐米具有显着改善的稳定性。 特别优选的制剂包括硼替佐米是适合注射的液体形式的制剂，其中溶剂体系主要包含丙二醇。 在其他优选方面，硼替佐米作为具有异双功能路易斯碱的路易斯供体 - 受体复合物存在。
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3.发明申请PROTEIN-ASSISTED DRUG DELIVERY SYSTEM FOR THE TARGETED ADMINISTRATION OF ACTIVE AGENTS 审中-公开蛋白质辅助药物输送系统，用于有针对性的药剂管理公开(公告)号：US20100330158A1
公开(公告)日：2010-12-30
申请号：US12748221
申请日：2010-03-26
CPC分类号： A61K9/1271 , A61K38/164 , Y02A50/473
摘要： The present invention provides a composition and prodrug for targeted drug delivery to the central nervous system of a patient. The inventive composition and prodrug include a pharmaceutically acceptable active agent and at least one protein selected from the group consisting of a fimbrial adhesin protein, a membrane protein, and combinations thereof. The inventive compositions and prodrugs of the present invention selectively target the blood-brain barrier and deliver hydrophilic and lipophilic active agents of varying sizes to the central nervous system.
摘要翻译： 本发明提供了用于靶向药物递送至患者的中枢神经系统的组合物和前药。 本发明的组合物和前药包括药学上可接受的活性剂和至少一种选自纤毛粘连素蛋白，膜蛋白及其组合的蛋白质。 本发明的本发明组合物和前药选择性地靶向血脑屏障，并将不同大小的亲水和亲脂性活性剂递送至中枢神经系统。
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公开(公告)号：US07037516B2
公开(公告)日：2006-05-02
申请号：US10792992
申请日：2004-03-04
IPC分类号： C07K15/00
CPC分类号： A61K9/0024 , A61K9/0019 , A61K9/107 , A61K38/1709 , A61K47/10 , A61K47/26
摘要： The present invention provides compositions comprising biologically-active somatotropin formulated for extended release and methods of preparing and methods of using the same. These compositions comprise somatotropin, at least a first bioavailability-enhancing constituent (BEC), and a substantially non-aqueous, hydrophobic excipient, and optionally a second BEC. The first BEC is typically a surfactant (preferably a non-ionic surfactant) or a cyclodextrin compound. The optional second BEC may comprise (i) amino acids or amino acid derivatives; (ii) hydroxamate derivatives; (iii) non-reducing carbohydrates; (iv) oxo-acid salts; or (v) a mixture of two or more compounds from within the foregoing classes (i)–(iv).
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公开(公告)号：US09107821B2
公开(公告)日：2015-08-18
申请号：US13592228
申请日：2012-08-22
申请人： Kumaresh Soppimath , Satish Pejaver , Kanaiyalal R. Patel , Lakkaraju Dasaradhi , Rama Sodum , Hari Desu , Navneet Puri
发明人： Kumaresh Soppimath , Satish Pejaver , Kanaiyalal R. Patel , Lakkaraju Dasaradhi , Rama Sodum , Hari Desu , Navneet Puri
CPC分类号： A61K9/08 , A61K9/0019 , A61K9/19 , A61K31/4965 , A61K31/69 , A61K47/10 , C07B63/04
摘要： Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.
摘要翻译： 硼替佐米的多剂量制剂被提出，其中硼替佐米具有显着改善的稳定性。 特别优选的制剂包括硼替佐米是适合注射的液体形式的制剂，其中溶剂体系主要包含丙二醇。 在其他优选方面，硼替佐米作为具有异双功能路易斯碱的路易斯供体 - 受体复合物存在。
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公开(公告)号：US20120322763A1
公开(公告)日：2012-12-20
申请号：US13592235
申请日：2012-08-22
申请人： Kumaresh Soppimath , Satish Pejaver , Kanaiyalal R. Patel , Lakkaraju Dasaradhi , Rama Sodum , Hari Desu , Navneet Puri
发明人： Kumaresh Soppimath , Satish Pejaver , Kanaiyalal R. Patel , Lakkaraju Dasaradhi , Rama Sodum , Hari Desu , Navneet Puri
IPC分类号： A61K31/69
CPC分类号： A61K9/08 , A61K9/0019 , A61K9/19 , A61K31/4965 , A61K31/69 , A61K47/10 , C07B63/04
摘要： Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.
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7.发明申请METHODS AND COMPOSITIONS FOR DELIVERY OF TAXANES IN STABLE OIL-IN-WATER EMULSIONS 审中-公开在稳定的水包油乳剂中输送紫杉醇的方法和组合物公开(公告)号：US20110166214A1
公开(公告)日：2011-07-07
申请号：US12986909
申请日：2011-01-07
IPC分类号： A61K31/337 , A61K8/02 , A61P35/04
CPC分类号： A61K31/337 , A61K9/0019 , A61K9/1075 , A61K47/24 , A61K47/44
摘要： The present invention provides methods and compositions for delivery of taxanes in stable oil-in-water emulsion. The inventive emulsion formulation includes an oil phase, aqueous and emulsifier phases. The oil portion includes all or substantial amount of taxane, vegetable oil and medium chain triglycerides; aqueous phase includes an emulsion stabilizer; emulsifier phase reduces the surface tension between oil and aqueous phases to produce a stable oil-in-water emulsion. The inventive compositions produce minimal side effects upon administration.
摘要翻译： 本发明提供了用于在稳定的水包油乳液中递送紫杉烷的方法和组合物。 本发明的乳液制剂包括油相，水相和乳化剂相。 油部分包括所有或大量的紫杉烷，植物油和中链甘油三酯; 水相包括乳液稳定剂; 乳化剂相降低油和水相之间的表面张力，以产生稳定的水包油乳液。 本发明组合物在施用时产生最小的副作用。
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8.发明授权公开(公告)号：US07048938B2
公开(公告)日：2006-05-23
申请号：US10793232
申请日：2004-03-04
IPC分类号： C07K15/00
CPC分类号： A61K38/27 , A61K9/0019 , A61K47/02 , A61K47/18 , A61K47/183 , A61K47/26 , A61K47/44
摘要： The present invention provides compositions which allow for the extended release and enhanced bioavailability of biologically-active polypeptides following parenteral delivery to an animal. More particularly, it concerns compositions comprising biologically-active somatotropin formulated for extended release, methods of preparing these compositions, and methods of using the same. These compositions comprise somatotropin, a bioavailability-enhancing constituent (BEC), and a substantially non-aqueous, hydrophobic excipient. The BEC may comprise (i) amino acids or amino acid derivatives, such as histidine-HCl; (ii) hydroxamate derivatives, such as histidine hydroxamate or suberohydroxamic acid; (iii) non-reducing carbohydrates, such as trehalose or trehalose octaacetate; (iv) oxo-acid salts, such as a mixture of monobasic and dibasic sodium phosphate; or (v) a mixture of two or more compounds from within the foregoing classes (i)–(iv).
摘要翻译： 本发明提供了允许在肠胃外输送到动物后的生物活性多肽的延长释放和增强的生物利用度的组合物。 更具体地，涉及包含用于延长释放的生物活性生长激素配制剂，制备这些组合物的方法和使用该组合物的方法的组合物。 这些组合物包含生长激素，生物利用度增加成分（BEC）和基本上非水性的疏水性赋形剂。 BEC可以包含（i）氨基酸或氨基酸衍生物，例如组氨酸-HCl; （ii）异羟肟酸衍生物，例如羟肟酸组氨酸或苏泊酸肟酸; （iii）非还原性碳水化合物，例如海藻糖或海藻糖八乙酸酯; （iv）含氧酸盐，例如一元和二元磷酸钠的混合物; 或（v）来自上述（i） - （iv）类的两种或更多种化合物的混合物。
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公开(公告)号：US06719992B2
公开(公告)日：2004-04-13
申请号：US09891445
申请日：2001-06-26
IPC分类号： C07K1500
CPC分类号： A61K9/0024 , A61K9/0019 , A61K9/107 , A61K38/1709 , A61K47/10 , A61K47/26
摘要： The present invention provides compositions comprising biologically-active somatotropin formulated for extended release and methods of preparing and methods of using the same. These compositions comprise somatotropin, at least a first bioavailability-enhancing constituent (BEC), and a substantially non-aqueous, hydrophobic excipient, and optionally a second BEC. The first BEC is typically a surfactant (preferably a non-ionic surfactant) or a cyclodextrin compound. The optional second BEC may comprise (i) amino acids or amino acid derivatives; (ii) hydroxamate derivatives; (iii) non-reducing carbohydrates; (iv) oxo-acid salts; or (v) a mixture of two or more compounds from within the foregoing classes (i)-(iv).
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公开(公告)号：US5091185A
公开(公告)日：1992-02-25
申请号：US541114
申请日：1990-06-20
CPC分类号： A61K9/0024 , A61K38/27 , A61K9/5026
摘要： Solid dosage forms of bioactive materials for parenteral administration such as porcine or bovine somatotropin pellets intended for subcutaneous implantation to improve food production of farm animals are coated with polyvinyl alcohol to extend the release characteristics of the material. The polyvinyl alcohol preferably has a molecular weight of from about 20,000 to 100,000, a degree of hydrolysis of at least about 98%, and is applied from an aqueous solution by spray coating to form a continuous uniform covering 3 to 25 .mu.m PVA/mm.sup.2.
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