Process for preparing a pharmaceutical formulation of contrast agents
    82.
    发明申请
    Process for preparing a pharmaceutical formulation of contrast agents 审中-公开
    制备造影剂药物制剂的方法

    公开(公告)号:US20090208421A1

    公开(公告)日:2009-08-20

    申请号:US12155997

    申请日:2008-06-12

    IPC分类号: A61K49/10

    摘要: The invention relates to a process for preparing a liquid pharmaceutical formulation containing a complex of macrocyclic chelate with a lanthanide and a mol/mol amount of free macrocyclic chelate of between 0.002% and 0.4%, advantageously between 0.02% and 0.3% and very advantageously between 0.025% and 0.25%, the macrocyclic chelate advantageously being chosen from DOTA, NOTA, DOTAGA, DO3A, BT-DO3A, HP-DO3A and PCTA, and is preferably DOTA, the said process comprising the following successive steps: a) determination of a theoretical target concentration of free macrocyclic chelate Ctcl in the final liquid pharmaceutical formulation; b) preparation of a liquid pharmaceutical composition containing, firstly, the complex of macrocyclic chelate with a lanthanide, and, secondly, free macrocyclic chelate and/or free lanthanide; c) measurement in the pharmaceutical formulation obtained in step b) of the concentration of free macrocyclic chelate Ccl and/or of free lanthanide Cll; d) adjustment of Ccl and/or of Cll so as to obtain Ccl=Ctcl and Cll=0.

    摘要翻译: 本发明涉及制备含有大环螯合物与镧系元素络合物和摩尔/摩尔量的游离大环螯合物的液体药物制剂的方法,其含量为0.002%至0.4%,有利地为0.02%至0.3%,非常有利地介于 0.025%和0.25%,大环螯合物有利地选自DOTA,NOTA,DOTAGA,DO3A,BT-DO3A,HP-DO3A和PCTA,并且优选为DOTA,所述方法包括以下连续步骤:a) 最终液体药物制剂中游离大环螯合物Ctcl的理论目标浓度; b)制备液体药物组合物,其首先包含大环螯合物与镧系元素的复合物,其次,游离的大环螯合物和/或游离的镧系元素; c)在步骤b)中获得的药物制剂中游离大环螯合物Ccl和/或游离镧​​系元素C11的浓度的测量; d)调整Ccl和/或Cll,以获得Ccl = Ctcl和Cll = 0。

    Therapeutic use of methionine to reduce the toxicity of platinum-containing anti-tumor compounds
    84.
    发明授权
    Therapeutic use of methionine to reduce the toxicity of platinum-containing anti-tumor compounds 失效
    治疗用甲硫氨酸降低含铂抗肿瘤化合物的毒性

    公开(公告)号:US07557142B2

    公开(公告)日:2009-07-07

    申请号:US10694448

    申请日:2003-10-27

    IPC分类号: A61K31/195

    摘要: Methods of preventing or reducing ototoxicity in patients undergoing treatment with therapeutically effective amounts of platinum-containing chemotherapeutic agents such as cisplatin or aminoglycoside antibiotics are provided. The methods comprise administering an effective amount of an otoprotective agent comprising methionine or a methionine-like moiety to said patient prior to, simultaneously with, or subsequently to administration of the platinum-containing chemotherapeutic agent or aminoglycoside antibiotic. Combinations of these time periods can also be employed.

    摘要翻译: 提供了用治疗有效量的含铂化学治疗剂如顺铂或氨基糖苷类抗生素预防或减少接受治疗的患者的耳毒性的方法。 所述方法包括在施用含铂化学治疗剂或氨基糖苷类抗生素之前,同时或随后施用有效量的包含甲硫氨酸或甲硫氨酸样部分的保护剂。 也可以使用这些时间段的组合。

    Metallofullerols and their Applications for Preparation of Medicine for Inhibition of Tumor Growth
    86.
    发明申请
    Metallofullerols and their Applications for Preparation of Medicine for Inhibition of Tumor Growth 有权
    金属富勒烯及其在制备抑制肿瘤生长的药物中的应用

    公开(公告)号:US20090076171A1

    公开(公告)日:2009-03-19

    申请号:US11992249

    申请日:2006-09-15

    IPC分类号: A61K31/045 C07C31/28

    摘要: This invention provides a composition of polyhydroxylated metallofullerene compound and its application in the preparation of antitumor pharmaceutical. In one embodiment, metallofullerol comprising the formula, M@C2m(OH)x, wherein M is selected from rare earth elements such as La or Gd; m is carbon atoms of 41 or 30; x is a number of hydroxyl group of from 10 to about 50. Actually, due to the reset of the neighboring hydroxyl, the numbers of O and H in Carbon cage are different, formula are thus written as M@C2mOxHy. Comparing to the clinical anticancer drugs such as Paclitaxel, Cyclophosphamide, and Cisplatin, metallofullerol of M@C2m(OH)x or M@C2mOxHy has superior advantages of higher antitumor efficiency, low dosage, low toxicity, and better biocompatibility.

    摘要翻译: 本发明提供多羟基化金属富勒烯化合物的组合物及其在制备抗肿瘤药物中的应用。 在一个实施方案中,包含式M 2 C 2m(OH)x的金属富勒烯,其中M选自稀土元素如La或Gd; m为41或30的碳原子; x是10〜50左右的羟基数。实际上,由于相邻羟基的复位,碳笼中O和H的数目不同,所以公式被写为M @ C2mOxHy。 与紫杉醇,环磷酰胺和顺铂等临床抗癌药物相比,M @ C2m(OH)x或M @ C2mOxHy的金属富勒醇具有较高的抗肿瘤效率,低剂量,低毒性,更好的生物相容性等优点。

    COCHLEATES WITHOUT METAL CATIONS AS BRIDGING AGENTS
    87.
    发明申请
    COCHLEATES WITHOUT METAL CATIONS AS BRIDGING AGENTS 审中-公开
    没有金属作为桥梁代理商的COCHLEATES

    公开(公告)号:US20090036417A1

    公开(公告)日:2009-02-05

    申请号:US12239847

    申请日:2008-09-29

    申请人: Tuo JIN

    发明人: Tuo JIN

    摘要: This invention provides a cochleate and nano-cochleate systems wherein the agents bridging lipid bilayer are organic multi-valent cations. This invention also provides a method for preparing the cochleate system comprising direct cochleation and hydrogel-isolated procedure. The preparation method comprises using the charge ration between the bridging agents and lipids to control the particle sizes. This cochleate or nano-cochleate system may be used for microencapsulation and delivery of therapeutics wherein the therapeutic agents are loaded in the cochleate structure as the bridging agents between lipid bilayers. Finally, this invention provides other uses of these new cochleate and nano- cochleate systems.

    摘要翻译: 本发明提供了一种耳蜗和纳耳耳蜗系统,其中桥接脂质双层的试剂是有机多价阳离子。 本发明还提供了一种制备耳蜗系统的方法,其包括直接的耳蜗和水凝胶分离过程。 制备方法包括使用桥联剂和脂质之间的电荷比来控制颗粒尺寸。 该耳蜗或纳耳耳蜗系统可用于微囊化和递送治疗剂,其中治疗剂作为脂质双层之间的桥连剂加载在耳蜗结构中。 最后,本发明提供了这些新的耳蜗和纳耳耳蜗系统的其它用途。

    Method of Improving Treatments in Rheumatic and Arthritic Diseases
    88.
    发明申请
    Method of Improving Treatments in Rheumatic and Arthritic Diseases 审中-公开
    改善风湿性关节炎疾病治疗方法

    公开(公告)号:US20090035315A1

    公开(公告)日:2009-02-05

    申请号:US11629613

    申请日:2005-06-17

    摘要: Improved treatments of joint diseases, such as, e.g. osteoarthritis and rheumatoid arthritis, and pain, wherein a strontium-containing compound is administered alone or in combination with one or more second therapeutically and/or prophylactically active substances, selected from the group consisting of bisphosphonates, glucosamine, pallitative agents, analgesic agents, disease modifying anti-rheumatic compounds (DMARDs), selective estrogen receptor modulators (SERMs), aromatase inhibitors, non-steroidal anti-inflammatory agents (NSAIDs), COX-2 inhibitors, COX-3 inhibitors, opioids, inhibitors/antagonists of IL-1, inhibitors/antagonists of TNF-alpha, inhibitors of matrix metallo-proteinases (MMPs), cathepsin K inhibitors, inhibitors/antagonists of RANK-ligand, statins, glucocorticoids, chondroitin sulphate, NMDA receptor antagonists, inhibitors of interleukin-I converting enzyme, Calcitonin gene related peptide antagonists, glycine antagonists, vanilloid receptor antagonists, inhibitors of inducible nitric oxide synthetase (iNOS), N-acetylcholine receptor agonists, neurokinin antagonists, neuroleptic agents, PAR2 receptor antagonists and anabolic growth factors acting on joint tissue components. Pharmaceutical compositions comprising a strontium-containing compound and a second therapeutically and/or prophylactically active substance as defined above.

    摘要翻译: 改善关节疾病的治疗,例如, 骨关节炎和类风湿性关节炎以及疼痛,其中单独施用含锶化合物或与一种或多种第二治疗和/或预防活性物质组合施用,所述第二治疗和/或预防活性物质选自二膦酸盐,葡糖胺,扑灭剂,止痛剂,疾病 修饰抗风湿化合物(DMARD),选择性雌激素受体调节剂(SERM),芳香酶抑制剂,非甾体抗炎药(NSAID),COX-2抑制剂,COX-3抑制剂,阿片样物质,IL-1抑制剂/拮抗剂 ,TNF-α的抑制剂/拮抗剂,基质金属蛋白酶(MMPs)的抑制剂,组织蛋白酶K抑制剂,RANK-配体的抑制剂/拮抗剂,他汀类,糖皮质激素,硫酸软骨素,NMDA受体拮抗剂,白细胞介素-I转化酶抑制剂, 降钙素基因相关肽拮抗剂,甘氨酸拮抗剂,香草素受体拮抗剂,诱导型一氧化氮合成酶抑制剂(iNOS),N-乙酰 胆碱受体激动剂,神经激肽拮抗剂,精神抑制剂,PAR2受体拮抗剂和作用于关节组织成分的合成代谢生长因子。 包含含锶化合物和如上定义的第二治疗和/或预防活性物质的药物组合物。

    OPHTHALMIC GALLIUM COMPOSITIONS AND METHODS OF THEIR USE
    90.
    发明申请
    OPHTHALMIC GALLIUM COMPOSITIONS AND METHODS OF THEIR USE 审中-公开
    OPHTHALMIC GALLIUM组合物及其使用方法

    公开(公告)号:US20080292726A1

    公开(公告)日:2008-11-27

    申请号:US12177591

    申请日:2008-07-22

    摘要: Provided are ophthalmic pharmaceutical compositions comprising gallium. These compositions are designed primarily for topical ocular and intraocular administration. Also provided are methods of use for the compositions in the treatment of human and veterinary diseases and disorders. Treatable diseases and disorders include adverse conditions of the eye and adnexal tissues of the eye. These adverse conditions comprise inflammatory conditions, infections, cancers, and other pathological conditions.

    摘要翻译: 提供了包含镓的眼用药物组合物。 这些组合物主要用于局部眼和眼内给药。 还提供了用于治疗人和兽医疾病和病症的组合物的方法。 可治疗的疾病和病症包括眼睛的不利条件和眼睛的附属组织。 这些不利条件包括炎症状况,感染,癌症和其他病理状况。