IN VIVO STIMULATION OF INTESTINAL TRANSPORTERS FOR EXCRETION OF NITROGENOUS WASTES
    11.
    发明申请
    IN VIVO STIMULATION OF INTESTINAL TRANSPORTERS FOR EXCRETION OF NITROGENOUS WASTES 审中-公开
    用于放出氮气的INTESTINAL TRANSPORTER的VIVO刺激

    公开(公告)号:WO2005105068A1

    公开(公告)日:2005-11-10

    申请号:PCT/US2005/012237

    申请日:2005-04-12

    CPC classification number: A61K31/00 A61K31/715 A61K31/724 A61K31/738 A61K31/78

    Abstract: A method for stimulating active transporters of metabolic waste, in particular urea and creatinine, in the GI tract of a mammal, comprising the step of administering an effective amount of a concentrator activation agent to the intestinal tract of the mammal, is disclosed. Methods for concentrating metabolic wastes in the intestinal tract to be above those achieved through passive diffusion alone, are also disclosed.

    Abstract translation: 公开了一种用于刺激哺乳动物胃肠道中代谢废物,特别是尿素和肌酸酐的活性转运蛋白的方法,包括向哺乳动物的肠道施用有效量的浓缩器活化剂的步骤。 将肠道中代谢废物浓缩至单独通过被动扩散获得的代谢废物的方法也被公开。

    CRYSTALLINE DRUG PARTICLES PREPARED USING A CONTROLLED PRECIPITATION (RECRYSTALLIZATION) PROCESS
    12.
    发明申请
    CRYSTALLINE DRUG PARTICLES PREPARED USING A CONTROLLED PRECIPITATION (RECRYSTALLIZATION) PROCESS 审中-公开
    使用控制退化(再结晶)工艺制备的晶体药物颗粒

    公开(公告)号:WO2004012710A1

    公开(公告)日:2004-02-12

    申请号:PCT/US2003/021882

    申请日:2003-07-14

    CPC classification number: A61K9/146 A61K9/145

    Abstract: Particles having a plurality of crystalline domains are described. Each crystalline domain is oriented differently than any of the adjacent domains and comprises a drug substance. A plurality of interfacial regions surround the crystalline domains, each interfacial region comprising at least one stabilizer. A process used to prepare the particles of the present invention is also described. The particles of the present invention exhibit relatively fast dissolution times as compared to particles prepared by processes described in the prior art.

    Abstract translation: 描述具有多个结晶域的颗粒。 每个结晶结构域的取向与任何相邻的结构域不同,并且包含药物物质。 多个界面区域围绕结晶域,每个界面区域包括至少一个稳定剂。 还描述了用于制备本发明的颗粒的方法。 与通过现有技术中描述的方法制备的颗粒相比,本发明的颗粒表现出相对较快的溶解时间。

    DRUG NANOPARTICLES FROM TEMPLATE EMULSIONS
    13.
    发明申请
    DRUG NANOPARTICLES FROM TEMPLATE EMULSIONS 审中-公开
    来自模板乳剂的药物纳米颗粒

    公开(公告)号:WO2003059319A1

    公开(公告)日:2003-07-24

    申请号:PCT/US2003/000726

    申请日:2003-01-10

    CPC classification number: A61K9/14

    Abstract: A method for producing micron-sized or submicron-sized drugs is disclosed, which comprises preparing a template emulsion comprising water and a templating agent; preparing a drug-containing mixture comprising a drug substance; and combining the template emulsion with the drug-containing mixture to form a template emulsion loaded with drug particles. Drug particles prepared from this process are also disclosed. The resulting drug particles demonstrate faster dissolution rates and enhanced bioavailability as compared to unprocessed drug particles and particles prepared using other processes.

    Abstract translation: 公开了一种制备微米级或亚微米级药物的方法,其包括制备包含水的模板乳液和制备包含药物物质的药物混合物的模板剂,并将模板乳剂与含药物混合物组合以形成 装载有药物颗粒的模板乳液。 还公开了从该方法制备的药物颗粒。 与未处理的药物颗粒和使用其它方法制备的颗粒相比,所得药物颗粒显示更快的溶解速率和增强的生物利用度。

    ACTINIUM-225 COMPLEXES AND CONJUGATES FOR TARGETED RADIOTHERAPY
    16.
    发明申请
    ACTINIUM-225 COMPLEXES AND CONJUGATES FOR TARGETED RADIOTHERAPY 审中-公开
    ACTINIUM-225复合物和靶向放射治疗的结合

    公开(公告)号:WO2002067999A2

    公开(公告)日:2002-09-06

    申请号:PCT/US2002/005872

    申请日:2002-02-28

    CPC classification number: A61K51/0497 A61K51/0482

    Abstract: 225 Ac complexes comprising a functionalized polyazamacrocyclic chelant compound of the formula I hereinbelow: (I) wherein T is (II), G is independently hydrogen or (III); each Q is independently hydrogen, (CHR 5 ) p CO 2 R or (CHR 5 ) p PO 3 R 6 R 7 or (IV); Q 1 is hydrogen, (CHR 5 ) w CO 2 R or (CHR 5 ) w PO 3 R 6 R 7 ; each R is independently hydrogen, benzyl or C 1 -C 4 alkyl; R 6 and R 7 are independently H, C 1 -C 6 alkyl or (C 1 -C 2 ) phenyl; each R 5 is independently hydrogen; C 1 -C 4 alkyl or (C 1 -C 2 alkyl) phenyl; with the proviso that at least two of the sum of Q and Q 1 must be other than hydrogen; A is CH, N, C-Br, C-C1, C-SO 3 H, C-OR 8 , C-OR 9 N + -R 10 X - , OR (V); Z and Z 1 independently are CH, N, C-SO 3 H, N + -R 10 X - , C-CH 2 - OR 8 or C-C(0) R 11 ; R 8 is H, C 1 -C 5 alkyl, benzyl, or benzyl substituted with at least one R 12 ; R 9 is C 1 -C 16 alkylamino; R 10 is C 1 -C 16 alkyl, benzyl, or benzyl substituted with at least one R 12 ; R 11 is O- (C 1 -C 3 alkyl), OH or NHR 13 ; R 12 is H, NO 2 , NH 2 , isothiocyanato, semicarbazido, thiosemicarbazido, maleimido, bromoacetamido or carboxyl; R 13 is C 1 -C 5 alkyl; X and Y are each independently hydrogen or may be taken with an adjacent X and Y to form an additional carbon-carbon bond; n is 0 or 1; m is an integer from 0 to 10 inclusive; p is 1 or 2; r is O or 1; w is O or 1; with the proviso that n is only 1 when X and/or Y form an additional carbon-carbon bond, and the sum of r and w is 0 or 1; L is a linker/spacer group covalently bonded to, and replaces one hydrogen atom of one of the carbon atoms to which it is joined, said linker/spacer group being represented by the formula (VI) wherein; s is an integer of 0 or 1; t is an integer of 0 to 20 inclusive; R 1 is H or an electrophilic or nucleophilic moiety which allows for covalent attachment to a biological carrier, or synthetic linker which can be attached to a biological carrier, or precursor thereof; and Cys represents a cyclic aliphatic moiety, or aromatic moiety, aliphatic heterocyclic moiety, or aromatic heterocyclic moiety, each of said moieties optionally substituted with one or more groups which do not interfere with binding to a biological carrier; with the proviso that when R 1 is H, the linkage to the biological carrier is through one of Q or Q 1 ; and with the proviso that when R 1 is other than H, at least one of Q and Q 1 must be ((CHR 5 ) p PO 3 R 6 R 7 ; and with further proviso that when Q is CHR 5 ) p CO 2 R, Q 1 is (CHR 5 ) w CO 2 R, R is H, R 5 is H, and R 1 is H, then the sum of m, n, p, r, s, t, and w is greater than 1; or pharmaceutically acceptable salts thereof; complexed with 225 AC.

    Abstract translation: 包含官能化的多氮杂环丁基螯合剂或其药学上可接受的盐与225缀合的Ac络合物,其包含共价连接到生物载体上的所述络合物,包含225缀合物和药学上可接受的载体的药物制剂 以及对具有癌症的哺乳动物进行治疗性治疗的方法,包括向所述哺乳动物施用治疗有效量的所述药物制剂。

    ORAL DRUG COMPLIANCE MONITORING USING MAGNETIC-FIELD SENSORS
    17.
    发明申请
    ORAL DRUG COMPLIANCE MONITORING USING MAGNETIC-FIELD SENSORS 审中-公开
    使用磁场传感器进行口服药物监测

    公开(公告)号:WO2007127316A2

    公开(公告)日:2007-11-08

    申请号:PCT/US2007/010154

    申请日:2007-04-24

    Abstract: A method to measure compliance with a pharmaceutical regimen, by the steps of: (a) ingesting a dose of a medication into the gastrointestinal tract of a person, the dose of medication comprising a drug formulation and a permanent magnet; (b) as a result of the ingestion of step (a), detecting passage of the permanent magnet past at least two magnetic field sensors positioned apart from each other and adjacent to the gastrointestinal tract; and (c) measuring compliance with the pharmaceutical regimen by way of the detection of step (b). And, apparatus useful to measure compliance with a pharmaceutical regimen by detecting ingestion of a dose of medication comprising a drug formulation and a permanent magnet, the apparatus including at least two magnetic field sensors positioned apart from each other on a necklace, each magnetic field sensor being in electronic communication with a microprocessor for receiving signals from the magnetic field sensors to determine the passage of a permanent magnet between the magnetic field sensors.

    Abstract translation: 通过以下步骤测量药物制剂的顺应性的方法:(a)将一剂药物摄入人的胃肠道,包括药物制剂和永久磁铁的药物剂量; (b)作为摄取步骤(a)的结果,检测永磁体经过位于彼此分开并邻近胃肠道的至少两个磁场传感器的通过; 和(c)通过检测步骤(b)测量药物方案的顺应性。 另外,通过检测摄入药物制剂和永久磁铁剂量的药物来测量药物方案的依从性的装置,该装置包括在项链上彼此分开定位的至少两个磁场传感器,每个磁场传感器 与微处理器电子通信,用于接收来自磁场传感器的信号,以确定永磁体在磁场传感器之间的通过。

    RADIOABLATION OF HEMOLYMPHOPOIETIC CELL POPULATIONS
    20.
    发明申请
    RADIOABLATION OF HEMOLYMPHOPOIETIC CELL POPULATIONS 审中-公开
    HEMOLYMPHOPOIETIC细胞群体的放射生物学

    公开(公告)号:WO2004052408A1

    公开(公告)日:2004-06-24

    申请号:PCT/US2002/039595

    申请日:2002-12-10

    CPC classification number: A61K51/0478 A61K51/0489

    Abstract: A method for achieving hemolymphopoietic chimerism is disclosed. The method involves the steps of administering to a recipient a bone seeking radiopharmaceutical; transplanting bone marrow-derived cells into the recipient; and transiently suppressing lymphocyte response so as to induce hemolymphopoietic chimerism. The method is useful for decreasing rejection of transplanted organs, tissues or cells and for treating autoimmune diseases. The present invention has the advantage of inducing hemolymphopoietic chimerism without the need for external radiation or harsh cytotoxic drugs. The present invention has the additional advantage of significantly prolonging tolerance to an organ, cell, or tissue transplant.

    Abstract translation: 公开了一种实现血液造血嵌合体的方法。 该方法包括向接受者施用寻骨放射性药物的步骤; 将骨髓来源的细胞移植到受体中; 并瞬时抑制淋巴细胞反应,以诱导血型兴奋性嵌合体。 该方法可用于减少移植器官,组织或细胞的排斥反应,并用于治疗自身免疫性疾病。 本发明具有诱导血型兴奋性嵌合体而不需要外部放射或刺激性细胞毒性药物的优点。 本发明具有显着延长对器官,细胞或组织移植的耐受性的额外优点。

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