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    Vivo agents comprising metal-ion chelates with acidic saccharides and glycosaminoglycans, giving improved site-selective localization, uptake mechanism, sensitivity and kinetic-spatial profiles
    5.
    发明授权
    Vivo agents comprising metal-ion chelates with acidic saccharides and glycosaminoglycans, giving improved site-selective localization, uptake mechanism, sensitivity and kinetic-spatial profiles 失效
    包含金属离子螯合物与酸性糖和糖胺聚糖的体内药物，提供改善的位点选择性定位，摄取机制，灵敏度和动力学空间分布

    公开(公告)号：US5707604A

    公开(公告)日：1998-01-13

    申请号：US472634

    申请日：1995-06-07

    申请人： David F. Ranney

    发明人： David F. Ranney

    IPC分类号： C08B37/00 ,  A61B5/055

    CPC分类号： B82Y5/00 ,  C08B37/0063 ,  Y10S514/836 ,  Y10T436/24

    摘要： This application concerns novel agents comprising cationic or chemically basic metal chelators in association with hydrophilic carriers of anionic or chemically acidic saccharides, sulfatoids and glycosaminoglycans. In certain embodiments, the agents comprise metals and metal ions. Covalent and non-covalent chemical and physical means are described for stabilizing the binding of the metal chelators to the carriers. Novel non-covalently bound compositions are described which give uniquely high payloads and ratio of metal chelator to carrier, ranging from a low of about 15% metal chelator by weight, to a characteristic range of 70% to 90% metal chelator by weight. Specific embodiments are described comprising deferoxamine, ferrioxamine, iron-basic porphine, iron-triethylenetetraamine, gadolinium DTPA-lysine, gadolinium DOTA-lysine and gadolinium with basic derivatives of porphyrins, porphines, expanded porphyrins, Texaphyrins and sapphyrins as the basic or cationic metal chelators, which are in turn, bound to acidic or anionic carriers, including one or more of acidic or anionic saccharides, and including sulfated sucrose, pentosan polysulfate, dermatan sulfate, essentially purified dermatan sulfate with a sulfur content of up to 9% and with selective oligosaccharide oversulfation, chondroitin sulfate, oversulfated chondroitin sulfate, heparan sulfate, beef heparin, porcine heparin, non-anticoagulant heparins, and other native and modified acidic saccharides and glycosaminoglycans.

    摘要翻译： 本申请涉及包含阳离子或化学碱性金属螯合剂与阴离子或化学酸性糖，硫酸酯和糖胺聚糖的亲水载体相关的新型试剂。 在某些实施方案中，试剂包含金属和金属离子。 描述了用于稳定金属螯合剂与载体的结合的共价和非共价化学和物理手段。 描述了新的非共价结合的组合物，其赋予独特的高有效载荷和金属螯合剂与载体的比例，范围从约15重量％的金属螯合剂的低至特征范围为70重量％至90重量％的金属螯合剂。 描述了具体的实施方案，其包括去铁胺，铁草胺，铁 - 碱性卟吩，铁三亚乙基四胺，钆DTPA-赖氨酸，钆DOTA-赖氨酸和钆与卟啉，卟吩，扩增的卟啉，Texaphyrins和sap with的碱性衍生物作为碱性或阳离子金属螯合剂 ，它们依次与酸性或阴离子载体结合，包括一种或多种酸性或阴离子糖，并且包括硫酸化蔗糖，戊聚糖多硫酸盐，硫酸皮肤素，硫酸含量高达9％的基本上纯化的硫酸皮肤素，并具有选择性 寡糖过硫酸盐，硫酸软骨素，硫酸硫酸软骨素，硫酸乙酰肝素，牛肝素，猪肝素，非抗凝血素肝素等天然和改性酸性糖和糖胺聚糖。

    In vivo agents comprising cationic drugs, peptides and metal chelators with acidic saccharides and glycosaminoglycans, giving improved site-selective localization, uptake mechanism, sensitivity and kinetic-spatial profiles, including tumor sites
    9.
    发明授权
    In vivo agents comprising cationic drugs, peptides and metal chelators with acidic saccharides and glycosaminoglycans, giving improved site-selective localization, uptake mechanism, sensitivity and kinetic-spatial profiles, including tumor sites 失效
    包含阳离子药物，肽和具有酸性糖和糖胺聚糖的金属螯合剂的体内试剂，提供改善的位点选择性定位，摄取机制，灵敏度和动力学空间分布，包括肿瘤部位

    公开(公告)号：US6106866A

    公开(公告)日：2000-08-22

    申请号：US509338

    申请日：1995-07-31

    申请人： David F. Ranney

    发明人： David F. Ranney

    IPC分类号： A61K47/48 ,  A61K49/12 ,  A61K31/726

    CPC分类号： A61K49/189 ,  A61K47/4823 ,  A61K49/12 ,  B82Y5/00

    摘要： A drug carrier composition comprising a drug complexed with dermatan sulfate is disclosed. The drug is preferably an anti tumor drug and may be taxol, a peptide onco-agent or vincristine. The most preferred antitumor drug is doxorubicin. The dermatan sulfate is essentially purified dermatan sulfate with a sulfur content of up to 9% (w/w) and with selective oligosaccharide oversulfation. The compositions are administered in a fashion that allows efficient vascular access and induces the following in vivo effects: 1) rapid, partial or total endothelial envelopment of the drug (diagnostic) carrier; 2) sequestration of the carrier and protection of the entrapped agent from blood vascular clearance at an early time (2 minutes) when the endothelial pocket which envelops the carrier still invaginates into the vascular compartment; 3) acceleration of the carrier's transport across and/or through the vascular endothelium or subendothelial structures into the tissue compartment (interstitium); and 4) improvement of the efficiency with which the drug migrates across the endothelium, or epi-endothelial or subendothelial barriers, such that a lower total drug dose is required to obtain the desired effect relative to that required for standard agents. Analogous tissue uptake is described for transepithelial migration into the lungs, bladder and bowel.

    摘要翻译： 公开了包含与硫酸皮肤素复合的药物的药物载体组合物。 药物优选为抗肿瘤药物，并且可以是紫杉醇，肽原剂或长春新碱。 最优选的抗肿瘤药物是多柔比星。 硫酸皮肤素基本上是硫酸含量高达9％（w / w）和选择性寡糖过硫酸盐的硫酸皮肤素。 组合物以允许有效血管通路并诱导以下体内效应的方式施用：1）药物（诊断）载体的快速，部分或全部内皮包膜; 2）当包围载体的内皮袋仍然陷入血管隔室时，早期（2分钟），载体的螯合和夹带的药物保护被血管清除; 3）加速载体穿过和/或通过血管内皮或内皮下结构进入组织隔室（间质）; 和4）提高药物通过内皮或外膜 - 内皮或内皮下屏障迁移的效率，使得需要较低的总药物剂量以获得相对于标准试剂所需的效果。 描述类似组织摄取用于跨上皮移植到肺，膀胱和肠中。

    Lipid-coated condensed-phase microparticle composition
    10.
    发明授权
    Lipid-coated condensed-phase microparticle composition 失效
    脂质包被的凝聚相微粒组合物

    公开(公告)号：US5753261A

    公开(公告)日：1998-05-19

    申请号：US443402

    申请日：1995-05-17

    申请人： Julio M. Fernandez ,  Mark B. Knudson

    发明人： Julio M. Fernandez ,  Mark B. Knudson

    IPC分类号： A61K8/14 ,  A61K8/64 ,  A61K9/127 ,  A61K9/16 ,  A61K9/51 ,  A61Q7/00 ,  G01N33/58

    CPC分类号： A61K9/0009 ,  A61K8/14 ,  A61K8/64 ,  A61K9/127 ,  A61K9/51 ,  A61Q7/00 ,  G01N33/586

    摘要： A microparticle composition for use in compound delivery, when the composition is exposed to a selected target stimulus related to pH, temperature, radiation, or the presence of a selected ligand or ion-channel activator, is disclosed. The composition includes a condensed-phase particle matrix containing the compound to be delivered in entrapped form, and a stimulus-responsive lipid bilayer membrane formed around the matrix. Localized perturbation of the lipid membrane, and influx of monovalent counterions into the polymer matrix, in response to the selected target stimulus, causes matrix swelling and compound release from the particles.

    摘要翻译： 公开了当组合物暴露于与pH，温度，辐射或选定的配体或离子通道活化剂的存在相关的所选靶刺激物时用于化合物递送的微粒组合物。 该组合物包括含有以截留形式递送的化合物的冷凝相颗粒基质，以及形成于该基质周围的刺激响应脂质双层膜。 响应于所选择的靶刺激，脂质膜的局部扰动和单价抗衡离子流入聚合物基质中导致基质溶胀和化合物从颗粒中释放。