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    Stabilized reverse micelle compositions and uses thereof
    1.
    发明申请
    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：US20050079145A1

    公开(公告)日：2005-04-14

    申请号：US10497775

    申请日：2002-12-03

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

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

    IPC分类号： A61K8/14 ,  A61K9/107 ,  A61K9/48 ,  A61K31/727 ,  A61K47/10 ,  A61K47/14 ,  A61K47/32 ,  A61K47/34 ,  A61K47/48 ,  A61Q19/00 ,  A61K7/06 ,  A61K7/075 ,  A61K7/08 ,  A61K7/11

    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 tha 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 transesterifed products containing C6-C12 fatty acids chains, wherein the transester groups consist of hydrohilic 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含与水和其它极性溶剂缔合以形成反胶束的脂肪酸酯及其亲水性衍生物，其在胃肠液，水和其它亲水溶剂存在下物理稳定。 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C6-C12脂肪酸链的单 - ，二 - 甘油酯和/或其酯交换产物，其中酯基组由亲水部分组成。

    Monoterpene compositions and uses thereof
    2.
    发明申请
    Monoterpene compositions and uses thereof 审中-公开
    单萜组合物及其用途

    公开(公告)号：US20060104997A1

    公开(公告)日：2006-05-18

    申请号：US10498566

    申请日：2002-12-11

    申请人： Panayiotis Constantinides ,  Reena Patil ,  Elijah Bolotin ,  Likan Liang

    发明人： Panayiotis Constantinides ,  Reena Patil ,  Elijah Bolotin ,  Likan Liang

    IPC分类号： A61K9/00 ,  A61K9/127 ,  A61K31/337 ,  A61K31/11 ,  A61K31/045

    CPC分类号： A61K9/4858 ,  A61K9/1075 ,  A61K31/045 ,  A61K31/11 ,  A61K31/337 ,  A61K47/10 ,  A61K47/22

    摘要： The present invention relates to pharmaceutical compositions and methods for the mucosal and oral administration of monoterpenes and derivatives thereof. The compositions of this invention further comprise one or more surfactants and cosolvents and are in the form of self-emulsifying compositions. The compositions of the invention may further comprise water-insoluble therapeutic agents, vaccines and diagnostics. Such agents include but are not limited to taxanes, steroids, topoisomerase inhibitors such as etoposide and other water-insoluble or lipophilic drugs.

    摘要翻译： 本发明涉及用于粘膜和口服单萜及其衍生物的药物组合物和方法。 本发明的组合物还包含一种或多种表面活性剂和助溶剂，并且是自乳化组合物的形式。 本发明的组合物还可包含水不溶性治疗剂，疫苗和诊断。 这些试剂包括但不限于紫杉烷类，类固醇类，拓扑异构酶抑制剂如依托泊苷和其他水不溶性或亲脂性药物。

    Lipid particles and suspensions and uses thereof
    3.
    发明申请
    Lipid particles and suspensions and uses thereof 审中-公开
    脂质颗粒和悬浮液及其用途

    公开(公告)号：US20060078618A1

    公开(公告)日：2006-04-13

    申请号：US10498572

    申请日：2002-12-11

    申请人： Panayiotis Constantinides ,  Reena Patil ,  Likan Liang

    发明人： Panayiotis Constantinides ,  Reena Patil ,  Likan Liang

    IPC分类号： A61K9/14

    CPC分类号： A61K9/1075 ,  A61K9/0019 ,  A61K9/127

    摘要： The present invention relates to formulations and methods for the mucosal and parenteral administration of lipid particles an suspensions. The formulations of this invention are stable lipid particles useful for oral delivery of water-insoluble therapeutic agents, vaccines and diagnostics. The compositions of this invention promote the mucosal absorption of biologically active molecules across mucosal epithelial barriers. Stabilization of lipid particles is achieved by coating the hydrophobic central core with a polymer shell. The polymer shell can include bioadhesive agents, ligands, and absorption promoting agents. This invention relates to oral drug delivery systems for hydrophobic drugs, and in particular is concerned with improving the bioavailability of hydrophobic drugs from such systems. Using this system, anticancer drugs such as taxanes are orally effective.

    摘要翻译： 本发明涉及用于粘膜和肠胃外给予脂质颗粒悬浮液的制剂和方法。 本发明的制剂是用于口服递送水不溶性治疗剂，疫苗和诊断的稳定的脂质颗粒。 本发明的组合物促进生物活性分子穿过粘膜上皮屏障的粘膜吸收。 脂质颗粒的稳定通过用聚合物壳涂覆疏水性中心核来实现。 聚合物壳可以包括生物粘附剂，配体和吸收促进剂。 本发明涉及用于疏水药物的口服药物递送系统，并且特别涉及提高来自这种系统的疏水性药物的生物利用度。 使用该系统，抗癌药如紫杉烷是口服有效的。

    Stabilized reverse micelle compositions and uses thereof
    4.
    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。

    Self-emulsifying formulations of fenofibrate and/or fenofibrate derivatives with improved oral bioavailability and/or reduced food effect
    10.
    发明授权
    Self-emulsifying formulations of fenofibrate and/or fenofibrate derivatives with improved oral bioavailability and/or reduced food effect 失效
    非诺贝特和/或非诺贝特衍生物的自乳化制剂具有改善的口服生物利用度和/或降低的食物效应

    公开(公告)号：US07022337B2

    公开(公告)日：2006-04-04

    申请号：US10607719

    申请日：2003-06-27

    申请人： Likan Liang ,  Amir H. Shojaei ,  Scott A. Ibrahim ,  Beth A. Burnside

    发明人： Likan Liang ,  Amir H. Shojaei ,  Scott A. Ibrahim ,  Beth A. Burnside

    IPC分类号： A61K9/48

    CPC分类号： A61K9/4866 ,  A61K9/1075 ,  A61K9/4858 ,  A61K31/216 ,  Y02A50/393

    摘要： A fibrate self-emulsifying oral formulation with improved bioavailability when compared to commercially available formulations containing a therapeutically effective dose of fenofibrate, derivative of fenofibrate or mixtures thereof dissolved in a fibrate solubilizer selected from N-alkyl derivative of 2-pyrrolidone, mono- or di- or polyethylene glycol monoethers, C8-12 fatty acid mono- or di-esters of propylene glycol, or combinations thereof, one or more surfactants and optionally one or more stabilizers useful in the treatment of hypercholesterolaemia or hypertriglyceridaemia in mammals in the fed or fasted state.

    摘要翻译： 与可商购获得的制剂相比，具有改善的生物利用度的贝特类自乳化口服制剂与含有治疗有效剂量的非诺贝特，非诺贝特衍生物或其混合物的溶解在选自2-吡咯烷酮N-烷基衍生物，单 - 或二 - 或聚乙二醇单醚，C 8-12脂肪酸丙二醇的单酯或二酯或其组合，一种或多种表面活性剂和任选的一种或多种稳定剂，其可用于治疗高胆固醇血症或 哺乳动物在喂食或禁食状态下的高甘油三酯血症。