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    Stabilized reverse micelle compositions and uses thereof
    1.
    发明授权
    Stabilized reverse micelle compositions and uses thereof 有权
    稳定的反胶束组合物及其用途

    公开(公告)号：US08535650B2

    公开(公告)日：2013-09-17

    申请号：US10497775

    申请日：2002-12-03

    申请人： Panayiotis P. Constantinides ,  Likan Liang ,  Eun-Hyun Jang

    发明人： Panayiotis P. Constantinides ,  Likan Liang ,  Eun-Hyun Jang

    IPC分类号： A61K9/107 ,  A61K31/727

    CPC分类号： A61K31/727 ,  A61K8/0291 ,  A61K9/107 ,  A61K9/1075 ,  A61K9/4891 ,  A61K38/09 ,  A61K38/23 ,  A61K38/27 ,  A61K38/28 ,  A61K38/29 ,  A61Q19/00

    摘要： The invention relates to compositions and methods for drug delivery suitable for promoting the transmucosal absorption of drugs, especially drugs with poor intrinsic bioavailability, such as peptides, proteins, vaccines, and nucleic acids. The delivery system of this invention preferably comprises fatty acid esters and their hydrophilic derivatives that associate with water and other polar solvents to form reverse micelles that are physically stabilized in the presence of gastrointestinal fluid, water, and other hydrophilic solvents. Such stable reverse micelles are formed by suitable mixtures of polymeric or non-polymeric compounds with amphiphiles. Micelles made using these methods undergo phase transformation more slowly resulting in delayed drug release profiles and sustained absorption. When administered as a pharmaceutical to mucosal surfaces following oral ingestion or intranasal administration, therapeutic molecules principally solubilized in the aqueous phase are protected from digestion by mucosal enzymes and other mucosal degradative processes and are taken up by absorptive cell mechanisms and reach appropriate body compartments. The reverse micelle compositions may comprise mono-, di-glycerides and/or their transesterified products containing C6-C12 fatty acids chains, wherein the transester groups consist of hydrophilic moieties.

    摘要翻译： 本发明涉及用于药物递送的组合物和方法，其适用于促进药物，特别是具有差的内在生物利用度的药物（例如肽，蛋白质，疫苗和核酸）的经粘膜吸收。 本发明的递送系统优选包括与水和其它极性溶剂缔合的脂肪酸酯及其亲水性衍生物，以形成在胃肠液，水和其它亲水溶剂存在下物理稳定的反胶束。 这种稳定的反胶束由聚合物或非聚合物与两亲物的合适混合物形成。 使用这些方法制备的胶束进行相变更慢，导致延迟的药物释放曲线和持续吸收。 当口服摄取或鼻内给药后作为药物施用于粘膜表面时，主要溶解在水相中的治疗分子被保护不被粘膜酶和其它粘膜降解过程消化，并被吸收细胞机制吸收并达到适当的身体隔室。 反胶束组合物可以包含含有C 6 -C 12脂肪酸链的单 - ，二 - 甘油酯和/或其酯交换产物，其中所述酯基组由亲水部分组成。

    Emulsion vehicle for poorly soluble drugs
    2.
    发明授权
    Emulsion vehicle for poorly soluble drugs 失效
    用于难溶性药物的乳剂

    公开(公告)号：US06458373B1

    公开(公告)日：2002-10-01

    申请号：US09003173

    申请日：1998-01-05

    申请人： Karel J. Lambert ,  Panayiotis P. Constantinides ,  Steven C. Quay

    发明人： Karel J. Lambert ,  Panayiotis P. Constantinides ,  Steven C. Quay

    IPC分类号： A01N2500

    CPC分类号： A61K47/22 ,  A61K9/0019 ,  A61K9/1075 ,  A61K9/4858 ,  Y10S514/938 ,  Y10S514/975 ,  Y10S977/775 ,  Y10S977/801 ,  Y10S977/907 ,  Y10S977/915

    摘要： An emulsion of &agr;-tocopherol, stabilized by biocompatible surfactants, as a vehicle or carrier for therapeutic drugs, which is substantially ethanol free and which can be administered to animals or humans various routes is disclosed. Also included in the emulsion is PEGylated vitamin E. PEGylated &agr;-tocopherol includes polyethylene glycol subunits attached by a succinic acid diester at the ring hydroxyl of vitamin E and serves as a primary surfactant, stabilizer and a secondary solvent in emulsions of &agr;-tocopherol.

    摘要翻译： 公开了通过生物相容性表面活性剂稳定的α-生育酚乳剂，作为治疗药物的载体或载体，其基本上不含有乙醇，并且可以施用于动物或人类各种途径。 乳液中还包含聚乙二醇化维生素E.聚乙二醇化α-生育酚包括在维生素E的环羟基处由琥珀酸二酯连接的聚乙二醇亚单位，并且用作α-生育酚乳液中的主要表面活性剂，稳定剂和第二溶剂。

    Method for treating colorectal carcinoma using a taxane/tocopherol formulation
    10.
    发明授权
    Method for treating colorectal carcinoma using a taxane/tocopherol formulation 失效
    使用紫杉烷/生育酚制剂治疗结直肠癌的方法

    公开(公告)号：US06727280B2

    公开(公告)日：2004-04-27

    申请号：US10188289

    申请日：2002-07-01

    申请人： Nagesh Palepu ,  Dean Kessler ,  Alexander K. Tustian ,  Steven C. Quay ,  Panayiotis P. Constantinides ,  Karel J. Lambert

    发明人： Nagesh Palepu ,  Dean Kessler ,  Alexander K. Tustian ,  Steven C. Quay ,  Panayiotis P. Constantinides ,  Karel J. Lambert

    IPC分类号： A61K3121

    CPC分类号： A61K9/1075 ,  A61K9/0019 ,  A61K9/4858 ,  A61K47/22

    摘要： The present invention provides methods for administering a taxane composition for the treatment of cancer. In one aspect, the compositions are not diluted prior to administration. Some embodiments provide methods for administering a taxane as a bolus injection or an intravenous infusion in less than about 30 minutes. In other aspects, the invention provides methods for administering a taxane to provide high concentrations of the taxane in blood or in tumors. Another aspect provides methods for administering a taxane to provide anti-tumor activities against solid tumors. In some embodiments, the methods provide anti-tumor activities against tumors that were resistant to conventional taxane administration methods. In some embodiments, the methods provide anti-tumor activities against colorectal tumors.

    摘要翻译： 本发明提供了用于治疗癌症的紫杉烷组合物的方法。 在一个方面，组合物在施用前不经稀释。 一些实施方案提供了在少于约30分钟内施用紫杉烷作为推注或静脉内输注的方法。 在其他方面，本发明提供了用于施用紫杉烷以在血液或肿瘤中提供高浓度紫杉烷的方法。 另一方面提供了用于施用紫杉烷以提供抵抗实体瘤的抗肿瘤活性的方法。 在一些实施方案中，所述方法提供对常规紫杉烷给药方法有抗性的针对肿瘤的抗肿瘤活性。 在一些实施方案中，所述方法提供针对结肠直肠肿瘤的抗肿瘤活性。