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    Pharmaceutical formulations and systems for improved absorption and multistage release of active agents
    33.
    发明授权
    Pharmaceutical formulations and systems for improved absorption and multistage release of active agents 失效
    用于改善活性剂的吸收和多级释放的药物制剂和系统

    公开(公告)号：US07374779B2

    公开(公告)日：2008-05-20

    申请号：US10074687

    申请日：2002-02-11

    Applicant: Feng-Jing Chen ,  Srinivasan Venkateshwaran ,  Steven L. Krill ,  Mahesh V. Patel

    Inventor： Feng-Jing Chen ,  Srinivasan Venkateshwaran ,  Steven L. Krill ,  Mahesh V. Patel

    IPC: A61K9/48 ,  A61K9/40 ,  A61K9/14 ,  A61K9/66 ,  A61K9/52

    CPC classification number: B82Y5/00 ,  A61K9/1617 ,  A61K9/4808 ,  A61K9/4858 ,  A61K9/5015 ,  A61K9/5026 ,  A61K9/5084 ,  A61K31/57 ,  A61K38/13

    Abstract: The present invention pertains to pharmaceutical formulations and systems for delivery of active agents, wherein a first fraction of an active agent is suspended in a vehicle and a second fraction of active agent is solubilized in the vehicle, with the suspended fraction representing about 5 wt. % to about 80 wt. % of the active agent and the second fraction representing about 20 wt. % to about 95 wt. % of the active agent. One or more additional active agents, which may be fully solubilized, partially solubilized, or suspended, may also be present. The first and second fractions of the active agent may or may not have different release profiles. Generally, a significant fraction of the solubilized drug will release rapidly, providing for rapid onset, while the suspended drug may be formulated for delayed and/or sustained release.

    Abstract translation: 本发明涉及用于递送活性剂的药物制剂和系统，其中活性剂的第一部分悬浮在载体中，第二部分活性剂溶解在载体中，悬浮的分数代表约5wt。 ％至约80wt。 ％的活性剂和第二级分代表约20wt。 ％至约95wt。 ％的活性剂。 还可以存在可以完全溶解，部分溶解或悬浮的一种或多种另外的活性剂。 活性剂的第一和第二部分可以具有或可以不具有不同的释放曲线。 通常，大部分的溶解药物将快速释放，提供快速发作，而悬浮药物可以配制用于延迟和/或持续释放。

    Fatty acid esters of glycolic acid and its salts
    35.
    发明授权
    Fatty acid esters of glycolic acid and its salts 失效
    乙醇酸及其盐的脂肪酸酯

    公开(公告)号：US5912009A

    公开(公告)日：1999-06-15

    申请号：US959944

    申请日：1997-10-29

    Applicant: Srinivasan Venkateshwaran ,  David Fikstad ,  Sonal R. Patel

    Inventor： Srinivasan Venkateshwaran ,  David Fikstad ,  Sonal R. Patel

    IPC: A61F13/02 ,  A61K9/00 ,  A61K9/70 ,  A61K31/196 ,  A61K31/506 ,  A61K31/522 ,  A61K31/565 ,  A61K31/568 ,  A61K47/14

    CPC classification number: A61K9/7061 ,  A61K47/14 ,  A61K9/0014 ,  Y10S514/946 ,  Y10S514/947

    Abstract: A transdermal drug delivery system which enhances the delivery of the drug comprises a composition containing, as an enhancer, one or more C.sub.6 to C.sub.22 fatty acid esters of glycolic acid and its salts. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant contained in a penetration-enhancing vehicle comprising, 0.25 to 50% w. of the fatty acid glycolic acid ester enhancer in a suitable carrier vehicle. These fatty acid glycolic acid ester enhancers may be used in various carrier vehicles to enhance the transdermal delivery of active permeants in either free form or used in an occlusive device, particularly in a transdermal patch in matrix or reservoir form. When used in matrix patch form, the fatty acid glycolic acid ester enhancers and permeants are incorporated into a biocompatible adhesive. When used in a reservoir type patch, the permeant and fatty acid glycolic acid ester enhancers are incorporated into a carrier fluid of controlled viscosity such as a gel or ointment preferably containing a lower alkanol and water. In free form, the enhancer and permeant may be incorporated into an ointment, lotion, cream, or similar formulation.

    Abstract translation: 增强药物递送的透皮药物递送系统包含含有一种或多种乙醇酸及其盐的一种或多种C 6至C 22脂肪酸酯作为增强剂的组合物。 这些组合物由安全有效量的包含在穿透增强载体中的活性药物渗透剂组成，其包含0.25至50重量％的w。 的脂肪酸乙醇酸酯增强剂在合适的载体载体中。 这些脂肪酸乙醇酸酯增强剂可用于各种载体载体中，以增强游离形式的活性渗透物的透皮递送或用于闭塞装置，特别是基质或储液器形式的透皮贴剂。 当以基质斑块形式使用时，将脂肪酸乙醇酸酯增强剂和渗透剂掺入生物相容性粘合剂中。 当用于储层型贴片时，将渗透剂和脂肪酸乙醇酸酯增强剂掺入到受控粘度的载体流体中，例如优选含有低级链烷醇和水的凝胶或软膏剂。 以游离形式，增强剂和渗透剂可以掺入软膏，洗剂，霜剂或类似制剂中。

    Transdermal propentofylline compositions for the treatment of Alzheimers disease
    37.
    发明授权
    Transdermal propentofylline compositions for the treatment of Alzheimers disease 失效
    用于治疗阿尔茨海默病的经皮支持基线组合物

    公开(公告)号：US5762953A

    公开(公告)日：1998-06-09

    申请号：US701711

    申请日：1996-08-22

    Applicant: Srinivasan Venkateshwaran

    Inventor： Srinivasan Venkateshwaran

    IPC: C07D473/06 ,  A61K9/70 ,  A61K31/522 ,  A61L15/58 ,  A61P25/28 ,  A61F13/02

    CPC classification number: A61K9/7061 ,  A61K31/522 ,  A61K9/7084

    Abstract: Patients suffering from Alzheimer's disease are treated by transdermally administering an effective amount of propentofylline in the form of an occulsive device containing a delivery composition comprising a carrier vehicle having uniformly distributed therein effective amounts of propentofylline and, optionally, a penetration enhancer. The occulsive device may be a matrix type patch in which the carrier vehicle is a pressure sensitive adhesive or a reservoir type patch in which the carrier vehicle is a liquid of controlled viscosity, i.e. a gel, wherein the reservoir system contains means for maintaining it in a propentofylline transferring relationship with the derma when applied. Daily dosages of between about 5 and 49 mg/day are sufficient to maintain adequate plasma propentofylline levels.

    Abstract translation: 患有阿尔茨海默氏病的患者通过经皮施用有效量的含有含有载体载体的递送组合物的递送装置形式的丙烯酰线进行治疗，所述载体载体具有均匀分布有效量的丙内酰线和任选的渗透增强剂。 所述吸引装置可以是载体载体是其中载体载体是受控粘度的液体（即凝胶）的压敏粘合剂或储液器型补片的基质型补丁，其中储存系统包含用于将其保持在 丙诺啡线在应用时转移与皮肤的关系。 约5至49毫克/天的日剂量足以维持足够的血浆丙素酰胆碱水平。

    Drug-containing adhesive composite transdermal delivery device
    38.
    发明授权
    Drug-containing adhesive composite transdermal delivery device 失效
    含药物粘合剂复合透皮递送装置

    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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