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1. 发明授权

US07179483B2 Compositions and methods for transdermal oxybutynin therapy 有权
标题翻译：用于透皮奥昔布宁治疗的组合物和方法
公开(公告)号：US07179483B2
公开(公告)日：2007-02-20
申请号：US10913019
申请日：2004-08-06
申请人： Charles D. Ebert , Steven W. Sanders
发明人： Charles D. Ebert , Steven W. Sanders
IPC分类号： A61F13/00 , A61F13/02 , A61L15/16
CPC分类号： A61K31/216 , A61F2013/00646 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/06 , A61K9/1647 , A61K9/7061 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
摘要： The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder. In some aspects, the composition may be presented in the form of an unoccluded or free form topically administered gel.
摘要翻译：本发明提供了用于奥昔布宁的组合物和方法，同时最小化与奥昔布宁治疗相关的不良药物经历的发生率和/或严重程度。在一个方面，这些组合物和方法提供了较低的奥昔布宁代谢物的血浆浓度，例如N-去乙氧基丁啶，其被推定为至少部分地促成一些不良药物经历，同时保持足够的奥昔布宁血浆浓度以有益于奥昔布宁治疗。本发明还提供了符合以下特征的奥昔布宁及其代谢物的异构体，这些特征使不良药物经历的发生率和/或严重程度最小化，以及维持膀胱过度活动症的有益和有效治疗。在一些方面，组合物可以呈局部施用凝胶的未被包裹或游离形式存在。

2. 发明授权

US07029694B2 Compositions and methods for transdermal oxybutynin therapy 有权
公开(公告)号：US07029694B2
公开(公告)日：2006-04-18
申请号：US10286381
申请日：2002-11-01
申请人： Charles D. Ebert , Steven W. Sanders
发明人： Charles D. Ebert , Steven W. Sanders
IPC分类号： A61F13/00 , A61F13/02 , A61K15/16
CPC分类号： A61K9/7061 , A61F2013/00646 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/1647 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
摘要： The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder. In some aspects, the composition may be presented in the form of an unoccluded or free form topically administered gel.

3. 发明授权

US06365178B1 Method of making pressure sensitive adhesive matrix patches for transdermal drug delivery using hydrophilic salts of drugs and hydrophobic pressure sensitive adhesive dispersions 有权
标题翻译：使用药物的亲水盐和疏水性压敏粘合剂分散体制备用于透皮药物递送的压敏粘合剂基质贴剂的方法
公开(公告)号：US06365178B1
公开(公告)日：2002-04-02
申请号：US09764040
申请日：2001-01-17
申请人： Srinivasan Venkateshwaran , David Fikstad , Charles D. Ebert
发明人： Srinivasan Venkateshwaran , David Fikstad , Charles D. Ebert
IPC分类号： A61K970
CPC分类号： A61K9/7053 , A61K9/7061
摘要： A method of making a pressure sensitive matrix patch for transdermal delivery of a drug is disclosed. The method includes the steps of dissolving a hydrophilic salt form of the drug in the water phase of an aqueous dispersion of a hydrophobic pressure sensitive adhesive, casting the resulting mixture as a thin film, and evaporating the water. The physical stability of the drug in the film is excellent, and crystallization of the drug is inhibited. A method of increasing the transdermal flux of an acidic drug is also disclosed.
摘要翻译：公开了制备用于药物透皮递送的压敏基质贴片的方法。该方法包括以下步骤：将亲水盐形式的药物溶解在疏水性压敏粘合剂的水分散体的水相中，将所得混合物浇铸成薄膜，并蒸发水。药物在膜中的物理稳定性优异，药物的结晶被抑制。还公开了增加酸性药物的经皮通量的方法。

4. 发明授权

US5985317A Pressure sensitive adhesive matrix patches for transdermal delivery of salts of pharmaceutical agents 失效
标题翻译：用于经皮递送药剂的盐的压敏粘合剂基质片剂
公开(公告)号：US5985317A
公开(公告)日：1999-11-16
申请号：US706624
申请日：1996-09-06
申请人： Srinivasan Venkateshwaran , David Fikstad , Charles D. Ebert
发明人： Srinivasan Venkateshwaran , David Fikstad , Charles D. Ebert
IPC分类号： A61K9/70 , A61L15/58 , A61L15/16
CPC分类号： A61K9/703 , A61K9/7053 , A61K9/7061
摘要： A method of transdermally or transmucosally delivering a hydrophilic salt form of a drug with a water-based pressure sensitive hydrophobic adhesive matrix patch optionally containing a permeation enhancer is disclosed. A matrix patch comprising a water-based pressure sensitive hydrophobic adhesive, a hydrophilic salt form of a drug, and optionally a permeation enhancer for transdermal or transmucosal delivery of the hydrophilic salt form of the drug is also disclosed.
摘要翻译：公开了一种透皮或透粘膜递送药物的亲水盐形式的方法，该方法是使用任选含有渗透促进剂的基于水的压敏疏水性粘合剂基质片剂。还公开了一种基质贴剂，其包含水基压敏疏水性粘合剂，药物的亲水盐形式和任选的用于透皮或经粘膜递送亲水盐形式的药物的渗透促进剂。

5. 发明授权

US5849322A Compositions and methods for buccal delivery of pharmaceutical agents 失效
标题翻译：用于颊内输送药剂的组合物和方法
公开(公告)号：US5849322A
公开(公告)日：1998-12-15
申请号：US546994
申请日：1995-10-23
申请人： Charles D. Ebert , Sonia J. Heiber , Mark K. Gutniak
发明人： Charles D. Ebert , Sonia J. Heiber , Mark K. Gutniak
IPC分类号： A61K9/70 , A61K9/00 , A61K9/20 , A61K31/00 , A61K38/00 , A61K38/11 , A61K38/22 , A61K38/23 , A61K38/28 , A61L15/00 , A61P1/00 , A61P1/02 , A61F13/02
CPC分类号： A61K9/006 , A61K9/2086 , Y10S514/953
摘要： A composition for transmucosally administering a drug to the oral cavity comprises an adhesive layer comprising a hydrophilic polymer having one surface adapted to contact a first tissue of the oral cavity and adhere thereto when wet and an opposing surface in contact with and adhering to an adjacent drug-containing layer comprising an effective amount of a drug and optionally an effective amount of a permeation enhancer, wherein the drug-containing layer is adapted to contact and be in drug transfer relationship with a mucosal tissue of the oral cavity when the adhesive layer contacts and adheres to the first tissue. Preferred drugs include peptides, such as glucagon-like insulinotropic peptides. A method of transmucosally administering a drug to the oral cavity is also disclosed.
摘要翻译：用于经口给药至口腔的组合物包括粘合剂层，其包含亲水性聚合物，所述亲水性聚合物具有适于接触口腔的第一组织的一个表面并且在湿润时与其粘合，并且相邻表面与相邻药物接触并粘附包含有效量的药物和任选的有效量的渗透促进剂，其中所述药物含量层适于在粘合剂层接触时与口腔的粘膜组织接触并与药物转移关系，并且粘附到第一组织。优选的药物包括肽，例如胰高血糖素样促胰岛素肽。还公开了将药物经口给药至口腔的方法。

6. 发明授权

US5516523A Transmucosal delivery of macromolecular drugs 失效
标题翻译：粘膜递送大分子药物
公开(公告)号：US5516523A
公开(公告)日：1996-05-14
申请号：US243415
申请日：1994-05-16
申请人： Sonia J. Heiber , Charles D. Ebert , Sirish C. Dave
发明人： Sonia J. Heiber , Charles D. Ebert , Sirish C. Dave
IPC分类号： A61K9/70 , A61K9/00 , A61K47/28 , A61F13/02
CPC分类号： A61K9/006 , Y10S514/953
摘要： A method and system for mucosally administering a macromolecular drug to mucosa of the oral cavity is shown. The system comprises an inner drug/enhancer/polymer layer having one surface adapted to contact and adhere to the mucosal tissue of the oral cavity and an opposing surface in contact with and adhering to an overlying inert layer. The inner layer contains from about two to sixty percent by weight of a bile salt enhancer, five to sixty five percent by weight of a hydrophilic polymer which is water soluble or swellable and an effective amount of a macromolecular drug having a molecular weight of at least 500 daltons. Polysaccharides, polypeptides and proteins are preferred forms of macromolecular drugs. The bile salt enhancer facilitates the delivery of macromolecules such as low molecular weight heparin and calcitonin. The polymer serves as a plasticizer to prevent the crystallization and/or aggregation of such macromolecular drugs. Hydroxypropyl cellulose is a particularly suitable polymer.
摘要翻译：显示了将大分子药物粘贴到口腔粘膜的方法和系统。该系统包括内部药物/增强剂/聚合物层，其具有适于接触并粘附到口腔的粘膜组织的一个表面和与上覆惰性层接触并粘附到上覆惰性层的相对表面。内层含有约百分之二至百分之六十重量百分比的胆汁盐增强剂，五至六十五重量％的亲水性聚合物，其是水溶性或可膨胀的，有效量的分子量至少为 500道尔顿多糖，多肽和蛋白质是大分子药物的优选形式。胆盐增强剂促进大分子如低分子量肝素和降钙素的递送。聚合物用作增塑剂以防止这种大分子药物的结晶和/或聚集。羟丙基纤维素是特别合适的聚合物。

7. 发明授权

US5227169A Sorbitan esters as skin permeation enhancers 失效
公开(公告)号：US5227169A
公开(公告)日：1993-07-13
申请号：US848110
申请日：1992-03-09
申请人： Sonia Heiber , Dinesh Patel , Charles D. Ebert
发明人： Sonia Heiber , Dinesh Patel , Charles D. Ebert
IPC分类号： A61K9/00 , A61K9/70 , A61K47/26
CPC分类号： A61K9/703 , A61K47/26 , A61K9/0014 , A61K9/7061
摘要： Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions contain a sorbitan ester in addition to the selected pharmacologically active agent, and may also contain a C.sub.1 -C.sub.4 aliphatic alcohol. Methods and transdermal drug delivery systems for using the compositions are also provided.

8. 发明授权

US07081251B2 Compositions and methods for minimizing adverse drug experiences associated with oxybutynin therapy 有权
公开(公告)号：US07081251B2
公开(公告)日：2006-07-25
申请号：US10731041
申请日：2003-12-08
申请人： Steven W. Sanders , Charles D. Ebert
发明人： Steven W. Sanders , Charles D. Ebert
IPC分类号： A61F13/00
CPC分类号： A61K9/0024 , A61K9/0014 , A61K9/0019 , A61K9/1647 , A61K9/7061 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
摘要： The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder.

9. 发明授权

US07081250B2 Compositions and methods for minimizing adverse drug experiences associated with oxybutynin therapy 有权
公开(公告)号：US07081250B2
公开(公告)日：2006-07-25
申请号：US10731040
申请日：2003-12-08
申请人： Steven W. Sanders , Charles D. Ebert
发明人： Steven W. Sanders , Charles D. Ebert
IPC分类号： A61F13/00
CPC分类号： A61K9/0024 , A61K9/0014 , A61K9/0019 , A61K9/1647 , A61K9/7061 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
摘要： The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and/or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder.

10. 发明授权

US5780050A Drug delivery compositions for improved stability of steroids 失效
标题翻译：用于改善类固醇稳定性的药物输送组合物
公开(公告)号：US5780050A
公开(公告)日：1998-07-14
申请号：US504430
申请日：1995-07-20
申请人： Uday Jain , Srinivasan Venkateshwaran , Charles D. Ebert
发明人： Uday Jain , Srinivasan Venkateshwaran , Charles D. Ebert
IPC分类号： A61K9/70 , A61K31/565 , A61K31/57 , A61K47/04 , A61K47/10 , A61K47/14 , A61K47/16 , A61K47/20 , A61K47/30 , A61K47/32 , A61K47/44 , A61P5/24 , A61P5/38 , A61F13/00
CPC分类号： A61K9/7061 , A61K31/568 , A61K31/569 , A61K31/57 , A61K31/573 , A61K31/575
摘要： A stabilized patch device for transdermal drug delivery of steroid drugs containing a 3-keto-4-en functional group is described, wherein the patch comprises an effective amount of the steroid drug and a carrier that is free of acid functional groups. The device can further contain additives such as a penetration enhancer or excipient, so long as such additives are also free of acid functional groups. The device can be either a matrix patch or a liquid reservoir patch. In a matrix patch, the carrier is a biocompatible polymeric adhesive with which the steroid drug is intimately admixed. The adhesive is preferably an acrylic polymer or copolymer. In a liquid reservoir patch, the carrier is a controlled-viscosity composition containing a thinner or thickener. Preferred steroid drugs include certain corticosteroids and sex hormones, such as progestins and androgens. A method of stabilizing such steroid drugs during storage in transdermal patches is also disclosed.
摘要翻译：描述了一种用于经皮药物递送含有3-酮-4-烯官能团的类固醇药物的稳定补片装置，其中补片包含有效量的类固醇药物和不含酸官能团的载体。该装置可以进一步含有添加剂如渗透促进剂或赋形剂，只要这些添加剂也不含酸官能团。该装置可以是矩阵补丁或液体储存器补丁。在基质贴剂中，载体是与类固醇药物紧密混合的生物相容的聚合物粘合剂。粘合剂优选为丙烯酸类聚合物或共聚物。在液体储存贴片中，载体是含有较薄或增稠剂的受控粘度组合物。优选的类固醇药物包括某些皮质类固醇和性激素，如孕激素和雄激素。还公开了在透皮贴剂储存期间稳定这种类固醇药物的方法。

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