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公开(公告)号：US5626866A
公开(公告)日：1997-05-06
申请号：US544110
申请日：1995-10-17
Applicant: Charles D. Ebert , Srinivasan Venkateshwaran , Werner Heiber , Suresh Borsadia
Inventor： Charles D. Ebert , Srinivasan Venkateshwaran , Werner Heiber , Suresh Borsadia
IPC: A61K9/70 , A61K31/465 , A61F13/00 , A61F13/02
CPC classification number: A61K9/703 , A61K9/7061
Abstract: A method for making a transdermal drug delivery device for heat sensitive and volatile drugs is disclosed. The device contains a drug-containing adhesive composite layer having an impermeable backing material laminated to the distal surface thereof and a proximal peelable impermeable backing material adapted for removal for administering a drug to the skin or mucosa laminated to the proximal surface thereof. The method comprising the steps of providing first and second adhesive laminates each comprising a drug permeable adhesive layer having laminated to one surface one of said backing materials and having the opposing surface exposed. The drug, in gelled form and optionally containing additives such as enhancers and preservatives, is extruded onto at least one exposed surface of the first or second adhesive laminate followed by laminating together the exposed surfaces of the first and second adhesive laminate such that the adhesive layers and gelled drug are combined to form the drug-containing adhesive composite layer having the distal and proximal surfaces covered by the respective backing materials. The adhesives used in making up the laminates may be the same or different provided the drug is compatible with the adhesive. The process is particularly adaptable to the formulation of nicotine-containing patches. Drug delivery devices made according to the disclosed method and a method of using these drug delivery devices are also described.
Abstract translation: 公开了制备用于热敏和挥发性药物的透皮药物递送装置的方法。 该装置含有含有药物的粘合剂复合层，其具有层压到其远端表面的不可渗透的背衬材料和适于去除的药物的近侧可剥离的不渗透背衬材料，以将药物施用于层压到其近侧表面的皮肤或粘膜。 该方法包括以下步骤：提供第一和第二粘合剂层压体，每个粘合层压板包括药物可渗透的粘合剂层，该粘合剂层层压到所述背衬材料的一个表面并且具有暴露的相对表面。 将胶体形式的药物和任选地含有添加剂如增强剂和防腐剂的药物挤压到第一或第二粘合层压体的至少一个暴露表面上，然后将第一和第二粘合层压体的暴露表面层压在一起，使得粘合剂层 并且凝胶化药物组合以形成具有由各个背衬材料覆盖的远侧和近侧表面的含药物的粘合剂复合材料层。 用于组合层压体的粘合剂可以相同或不同，只要药物与粘合剂相容即可。 该方法特别适用于含尼古丁的贴剂的制剂。 还描述了根据所公开的方法制备的药物递送装置和使用这些药物递送装置的方法。
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12.发明授权公开(公告)号：US07081251B2
公开(公告)日：2006-07-25
申请号：US10731041
申请日：2003-12-08
Applicant: Steven W. Sanders , Charles D. Ebert
Inventor： Steven W. Sanders , Charles D. Ebert
IPC: A61F13/00
CPC classification number: A61K9/0024 , A61K9/0014 , A61K9/0019 , A61K9/1647 , A61K9/7061 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
Abstract: 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.
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13.发明授权公开(公告)号：US07081250B2
公开(公告)日：2006-07-25
申请号：US10731040
申请日：2003-12-08
Applicant: Steven W. Sanders , Charles D. Ebert
Inventor： Steven W. Sanders , Charles D. Ebert
IPC: A61F13/00
CPC classification number: A61K9/0024 , A61K9/0014 , A61K9/0019 , A61K9/1647 , A61K9/7061 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
Abstract: 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.
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公开(公告)号：US5212199A
公开(公告)日：1993-05-18
申请号：US871643
申请日：1992-04-21
Applicant: Sonia Heiber , Dinesh Patel , Charles D. Ebert
Inventor： Sonia Heiber , Dinesh Patel , Charles D. Ebert
CPC classification number: A61K9/703 , A61K47/26 , A61K9/0014 , A61K9/7061 , Y10S514/946 , Y10S514/947
Abstract: 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.
Abstract translation: 提供了皮肤渗透增强剂组合物，其增加皮肤对透皮给药的药理学活性剂的渗透性。 该组合物除了所选择的药理学活性剂外还含有脱水山梨醇酯，并且还可以含有C 1 -C 4脂族醇。 还提供了用于使用组合物的方法和透皮药物递送系统。
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公开(公告)号：US07179483B2
公开(公告)日：2007-02-20
申请号：US10913019
申请日：2004-08-06
Applicant: Charles D. Ebert , Steven W. Sanders
Inventor： Charles D. Ebert , Steven W. Sanders
CPC classification number: A61K31/216 , A61F2013/00646 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/06 , A61K9/1647 , A61K9/7061 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
Abstract: 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.
Abstract translation: 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。
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Patent Agency Ranking
公开(公告)号：US07029694B2
公开(公告)日：2006-04-18
申请号：US10286381
申请日：2002-11-01
Applicant: Charles D. Ebert , Steven W. Sanders
Inventor： Charles D. Ebert , Steven W. Sanders
CPC classification number: A61K9/7061 , A61F2013/00646 , A61K9/0014 , A61K9/0019 , A61K9/0024 , A61K9/1647 , A61K31/216 , A61K47/10 , A61K47/14 , A61K47/38 , A61K2300/00
Abstract: 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.
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公开(公告)号：US5849322A
公开(公告)日：1998-12-15
申请号：US546994
申请日：1995-10-23
Applicant: Charles D. Ebert , Sonia J. Heiber , Mark K. Gutniak
Inventor： Charles D. Ebert , Sonia J. Heiber , Mark K. Gutniak
IPC: 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 classification number: A61K9/006 , A61K9/2086 , Y10S514/953
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US5516523A
公开(公告)日：1996-05-14
申请号：US243415
申请日：1994-05-16
Applicant: Sonia J. Heiber , Charles D. Ebert , Sirish C. Dave
Inventor： Sonia J. Heiber , Charles D. Ebert , Sirish C. Dave
CPC classification number: A61K9/006 , Y10S514/953
Abstract: 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.
Abstract translation: 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。
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公开(公告)号：US5227169A
公开(公告)日：1993-07-13
申请号：US848110
申请日：1992-03-09
Applicant: Sonia Heiber , Dinesh Patel , Charles D. Ebert
Inventor： Sonia Heiber , Dinesh Patel , Charles D. Ebert
CPC classification number: A61K9/703 , A61K47/26 , A61K9/0014 , A61K9/7061
Abstract: 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.
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公开(公告)号：US5863555A
公开(公告)日：1999-01-26
申请号：US964731
申请日：1997-11-05
Applicant: Sonia J. Heiber , Charles D. Ebert , Mark K. Gutniak
Inventor： Sonia J. Heiber , Charles D. Ebert , Mark K. Gutniak
Abstract: Drug delivery systems and methods for administering a glucagon-like insulinotropic peptide to the buccal mucosa for transmucosal drug delivery are described. The drug delivery systems comprise a drug composition containing an effective amount of the glucagon-like insulinotropic peptide and an effective amount of a permeation enhancer for enhancing permeation of glucagon-like insulinotropic peptide through the buccal mucosa and means for maintaining the drug composition in a drug transferring relationship with buccal mucosa. These systems can be in free form, such as creams, gels, and ointments, or can comprise a device of determined physical form, such as tablets, patches, and troches. A preferred glucagon-like insulinotropic peptide is GLP-1(7-36)amide.
Abstract translation: 描述了用于向口腔粘膜施用胰高血糖素样促胰岛素肽用于经粘膜药物递送的药物递送系统和方法。 药物递送系统包含含有有效量的胰高血糖素样促胰岛素肽的药物组合物和有效量的用于增强胰高血糖素样促胰岛素肽通过颊粘膜的渗透的渗透促进剂和用于将药物组合物保持在药物中的方法 转移与颊粘膜的关系。 这些系统可以是游离形式，例如乳膏，凝胶和软膏，或者可以包括具有确定的物理形式的装置，例如片剂，补片和锭剂。 优选的胰高血糖素样促胰岛素肽是GLP-1（7-36）酰胺。
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