Method for Preparing Lipid-Spacer-Reactive Functional Group-Peptide
    1.
    发明申请
    Method for Preparing Lipid-Spacer-Reactive Functional Group-Peptide 审中-公开
    脂质间隔反应性功能团肽的制备方法

    公开(公告)号:US20080139703A1

    公开(公告)日:2008-06-12

    申请号:US12029324

    申请日:2008-02-11

    IPC分类号: C08L89/00

    摘要: The present invention discloses a method for preparing lipid-spacer-reactive functional group-peptide, wherein the peptide consists of 3 to 16 amino acid residues in which at least one amino acid residue is lysine (Lys), the reactive functional group is a formula of —X—CO—Y—CO—, wherein X represents an oxygen atom or a nitrogen atom, and Y represents C1-6 alkylene which may be interrupted by one or two oxygen or nitrogen atom(s), the spacer is a hydrophilic polymer, and the lipid is phosphatidylethanoaminecarbonyl represented by the formula (I): R1 and R2 are the same or different and individually represent linear or branch C7-30 alkyl or linear or branch C7-30 alkenyl; which is characterized in that the reaction is carried out in a liquid phase and comprises the following steps of (a) firstly protecting Lys amino acid residue in the peptide through a protection group; (b) subsequently reacting the peptide with the lipid-spacer-reactive functional group; and (c) finally removing the protection group from Lys amino acid residue in the peptide.

    摘要翻译: 本发明公开了一种制备脂质 - 间隔物反应性官能团肽的方法,其中肽由3至16个氨基酸残基组成,其中至少一个氨基酸残基为赖氨酸(Lys),反应性官能团为式 的-X-CO-Y-CO-,其中X表示氧原子或氮原子,Y表示可被一个或两个氧或氮原子间隔的C 1-6亚烷基( s),间隔基是亲水性聚合物,并且脂质是由式(I)表示的磷脂酰硫代氨基羰基:R 1和R 2都相同或不同,并且各自代表 直链或支链C 7-30烷基或直链或支链C 7-30链烯基; 其特征在于反应在液相中进行,并包括以下步骤:(a)首先通过保护基保护肽中的Lys氨基酸残基; (b)随后使肽与脂质 - 间隔物反应性官能团反应; 和(c)最后从肽中的Lys氨基酸残基中除去保护基团。

    Method for Preparing Lipid-Spacer-Reactive Functional Group-Peptide

    公开(公告)号:US20080102110A1

    公开(公告)日:2008-05-01

    申请号:US11608836

    申请日:2006-12-10

    IPC分类号: A61K9/127 C07K7/08 C07K7/06

    摘要: The present invention discloses a method for preparing lipid-spacer-reactive functional group-peptide, whereinthe peptide consists of 3 to 16 amino acid residues in which at least one amino acid residue is lysine (Lys), the reactive functional group is a formula of —X—CO—Y—CO—, wherein X represents an oxygen atom or a nitrogen atom, and Y represents C1-6 alkylene which may be interrupted by one or two oxygen or nitrogen atom(s), the spacer is a hydrophilic polymer, and the lipid is phosphatidylethanoaminecarbonyl represented by the formula (I): R1 and R2 are the same or different and individually represent linear or branch C7-30 alkyl or linear or branch C7-30 alkenyl; which is characterized in that the reaction is carried out in a liquid phase and comprises the following steps of (a) firstly protecting Lys amino acid residue in the peptide through a protection group; (b) subsequently reacting the peptide with the lipid-spacer-reactive functional group; and (c) finally removing the protection group from Lys amino acid residue in the peptide.

    Automated synthesis device to produce Re-188-Liposome and method thereof
    3.
    发明申请
    Automated synthesis device to produce Re-188-Liposome and method thereof 审中-公开
    自动合成装置生产Re-188-脂质体及其方法

    公开(公告)号:US20140377169A1

    公开(公告)日:2014-12-25

    申请号:US13921217

    申请日:2013-06-19

    IPC分类号: B01J19/00 A61K51/12

    摘要: An automated synthesis device to produce Re-188-BMEDA solution including: a plurality of reagent vials, three-way solenoid valves, gel filtration columns and micro pumps, and a reaction vial, a product vial, a temporary storage vial, a filter membrane, and a waste vial, wherein the plurality of reagent vials include first reagent vial and second reagent vials being connected to the reaction vial through first micro pump, the third reagent vial and fourth reagent vial being connected to the reaction vial through second micro pump, fifth reagent vial being connected to the reaction vial through third micro pump, and sixth reagent vial being connected to the temporary storage vial through fourth micro pump, wherein the reaction vial is connected to the plurality of gel filtration columns through the micro-pump, respectively. The automated synthesis device is operable with program to upgrade yield and avoid contamination.

    摘要翻译: 一种用于生产Re-188-BMEDA溶液的自动化合成装置,包括:多个试剂瓶,三通电磁阀,凝胶过滤柱和微型泵,以及反应瓶,产品小瓶,临时储存小瓶,过滤膜 以及废物小瓶,其中所述多个试剂小瓶包括通过第一微泵连接到所述反应小瓶的第一试剂小瓶和第二试剂小瓶,所述第三试剂小瓶和第四试剂小瓶通过第二微泵连接到所述反应小瓶, 第五试剂小瓶通过第三微泵连接到反应小瓶,第六试剂小瓶通过第四微泵连接到临时存储小瓶,其中反应小瓶分别通过微型泵连接到多个凝胶过滤柱 。 自动合成装置可与程序一起操作,以提高产量并避免污染。

    Kit for preparation of nano-targeted liposome drug in combined radionuclide therapy and chemotherapy
    4.
    发明申请
    Kit for preparation of nano-targeted liposome drug in combined radionuclide therapy and chemotherapy 审中-公开
    用于在联合放射​​性核素治疗和化疗中制备纳米靶向脂质体药物的试剂盒

    公开(公告)号:US20080226546A1

    公开(公告)日:2008-09-18

    申请号:US11687650

    申请日:2007-03-18

    摘要: This invention is to manufacture a kit for preparation of nano-targeted liposome drugs in combined chemotherapy and radionuclide therapy. It is a kit consisting of three components: (1) A 10 ml vial A which contains BMEDA, gluconate acetate, SnCl2. (2) A 10 ml vial B which contains DSPC, cholesterol, DSPE-PEG, and Doxorubicin(DXR) (or Daunorubicin, Vinolbine). (3) A 10 ml vial C which contains 188ReO4− (or 186ReO4−) solution. The procedure of using the kit is as follows: (1) Remove the contents of the 188ReO4− (or 186ReO4−) solution from vial C. (2) Inject the 188ReO4− (or 186ReO4−) solution into the vial A, and the mixtures react in appropriate temperature. (3) Remove the contents of the 188Re-BMEDA (or 186Re-BMEDA) solution from vial A. (4) Inject the 188Re-BMEDA (or 186Re-BMEDA) solution into the vial B, and the mixtures react in appropriate temperature. The reconstituted solution in the vial B is applied to combine bimodality radiochemotherapy for treatment of tumor and ascites.

    摘要翻译: 本发明是在联合化疗和放射性核素治疗中制备用于制备纳米靶向脂质体药物的试剂盒。 它是由三个组分组成的试剂盒:(1)含有BMEDA,葡萄糖酸乙酯,SnCl 2 2的10ml小瓶A. (2)含有DSPC,胆固醇,DSPE-PEG和多柔比星(DXR)(或柔红霉素,维罗非因)的10ml小瓶B。 (3)将含有<! - SIPO - >反应物(或<! - SIPO - > - )解决方案。 使用试剂盒的步骤如下:(1)除去 188 - (或 186 < 来自小瓶C的溶液。(2)注射<! - SIPO - >反应物 > - (或 186 )溶液加入到小瓶A中,并且混合物在合适的温度下反应。 (3)从小瓶A中取出 188 Re-BMEDA(或<186> 重BMEDA)溶液的内容物。(4)注入 188 Re-BMEDA)溶液加入小瓶B中,混合物在合适的温度下反应。 将小瓶B中的重构溶液应用于结合双功能放射化学疗法治疗肿瘤和腹水。

    Automated test apparatus for testing risk and integrity of pharmaceutical filtration membranes and method thereof
    5.
    发明申请
    Automated test apparatus for testing risk and integrity of pharmaceutical filtration membranes and method thereof 有权
    用于测试药物过滤膜的风险和完整性的自动化试验装置及其方法

    公开(公告)号:US20150033828A1

    公开(公告)日:2015-02-05

    申请号:US13956375

    申请日:2013-08-01

    IPC分类号: G01N15/08

    CPC分类号: B01D65/102 B01D65/10 G01M3/06

    摘要: An automated test apparatus for risk and integrity testing for pharmaceutical filtration membranes, including at least the following components: a liquid injection inlet, a pump, a fluid pressure gauge, a gas pressure gauge, a plurality of solenoid valves, a plurality of membranes, a gas pressure regulator valve, a pharmaceutical product bottle, and a bubble generation bottle. The automated test apparatus of the present invention is controlled by computer software in connection with an automatic pharmaceutical synthesis apparatus for automated testing. In use of the automated test apparatus of the present invention, it needs only to start the operating system of the automated test apparatus for membrane risk and integrity test after the completion of the automatic pharmaceutical synthesis. The membrane risk and integrity test can be accomplished in a short time by measuring pressures of gas and liquid with pressure gauges deposed online concurrently.

    摘要翻译: 一种用于药物过滤膜的风险和完整性测试的自动测试装置,包括至少以下组件:液体注射入口,泵,流体压力计,气体压力计,多个电磁阀,多个膜, 气体压力调节阀,药品瓶和气泡生成瓶。 本发明的自动测试装置由计算机软件与用于自动化测试的自动药物合成装置有关。 在使用本发明的自动测试装置时,仅需要在自动药物合成完成之后启动用于膜风险和完整性测试的自动测试装置的操作系统。 薄膜风险和完整性测试可以在短时间内通过测量气体和液体的压力同时在线排出的压力计来完成。

    Automated test apparatus for testing risk and integrity of pharmaceutical filtration membranes and method thereof

    公开(公告)号:US09707521B2

    公开(公告)日:2017-07-18

    申请号:US13956375

    申请日:2013-08-01

    IPC分类号: B01D65/10 G01M3/06

    CPC分类号: B01D65/102 B01D65/10 G01M3/06

    摘要: An automated test apparatus for risk and integrity testing for pharmaceutical filtration membranes, including at least the following components: a liquid injection inlet, a pump, a fluid pressure gauge, a gas pressure gauge, a plurality of solenoid valves, a plurality of membranes, a gas pressure regulator valve, a pharmaceutical product bottle, and a bubble generation bottle. The automated test apparatus of the present invention is controlled by computer software in connection with an automatic pharmaceutical synthesis apparatus for automated testing. In use of the automated test apparatus of the present invention, it needs only to start the operating system of the automated test apparatus for membrane risk and integrity test after the completion of the automatic pharmaceutical synthesis. The membrane risk and integrity test can be accomplished in a short time by measuring pressures of gas and liquid with pressure gauges deposed online concurrently.

    MAMMAL DEDICATED CELL LINE FROM HUMAN HEPATOCELLULAR CARCINOMA CELL
    7.
    发明申请
    MAMMAL DEDICATED CELL LINE FROM HUMAN HEPATOCELLULAR CARCINOMA CELL 审中-公开
    来自人肝细胞癌细胞的MAMMAL专用细胞系

    公开(公告)号:US20120295349A1

    公开(公告)日:2012-11-22

    申请号:US13555495

    申请日:2012-07-23

    IPC分类号: C12N5/10

    CPC分类号: G01N33/5008

    摘要: A mammal dedicated cell line is provided, which is a HepG2 hepatocellular carcinoma cell line (HepG2/NF-kB/Luc/sr39tk)1_18 obtained by co-transformation with NF-kB/Luc and NF-kB/sr39tk. Firstly, a successfully transformed pNF-kB/Luc HepG2 cell is obtained. Then, a dedicated cell line sensitive to TPA and MTX is generated by experimental screening Next, a plasmid construct carrying pNF-kB/sr39tk genome is introduced into the dedicated cell line by means of Superfect protocol. Finally, a HepG2 cell line co-expressing NF-kB/Luc and NF-kB/sr39tk is screened with G418 and ZEOCIN, and transformation result is confirmed by luminescence and radio activity. The (HepG2/NF-kB/Luc/sr39tk)1_18 obtained is suitable to screen drug for treating liver cancer and examine these cells by bioluminescence imaging and nuclear medicine imaging.

    摘要翻译: 提供哺乳动物专用细胞系,其是通过与NF-kB / Luc和NF-kB / sr39tk共转化获得的HepG2肝细胞癌细胞系(HepG2 / NF-kB / Luc / sr39tk)1-18。 首先,获得成功转化的pNF-kB / Luc HepG2细胞。 然后,通过实验筛选产生对TPA和MTX敏感的专用细胞系。接下来,通过Superfect方案将携带pNF-kB / sr39tk基因组的质粒构建体导入专用细胞系。 最后,用G418和ZEOCIN筛选共表达NF-kB / Luc和NF-kB / sr39tk的HepG2细胞株,通过发光和放射活性证实转化结果。 获得的(HepG2 / NF-kB / Luc / sr39tk)1_18适用于筛选药物治疗肝癌,并通过生物发光成像和核医学成像检查这些细胞。

    KIT FOR PREPARING A RADIOLABELED LIPOSOME AND A METHOD USING THE SAME
    8.
    发明申请
    KIT FOR PREPARING A RADIOLABELED LIPOSOME AND A METHOD USING THE SAME 审中-公开
    用于制备放射性脂质体的试剂盒和使用其的方法

    公开(公告)号:US20120107232A1

    公开(公告)日:2012-05-03

    申请号:US13169268

    申请日:2011-06-27

    IPC分类号: A61K51/12 A61P35/00

    CPC分类号: A61K51/1234

    摘要: A kit for preparing a radiolabeled liposome is provided, the kit including a liposome suspension and a radionuclide, wherein the liposome suspension includes a conjugate with a structure of [chelator-hydrophilic polymer-lipid]. A method for preparing a radiolabeled liposome using the kit is also disclosed herein, thereby the radiolabeled liposome being produced with the conjugate connected to the surface therein. The advantages of the present disclose such as simple, convenient and without purifying for the produced radiolabeled liposome are thus achieved. Further, the produced radiolabeled liposome has a high specific activity and a high sensitivity and suits for the clinical use.

    摘要翻译: 提供了用于制备放射性标记的脂质体的试剂盒,该试剂盒包括脂质体悬浮液和放射性核素,其中脂质体悬浮液包括具有[螯合剂 - 亲水性聚合物 - 脂质]结构的缀合物。 本文还公开了使用试剂盒制备放射性标记的脂质体的方法,由此产生放射性标记的脂质体,其中缀合物连接到其表面。 因此实现了本发明公开的优点,例如简单,方便和不需要纯化用于所制备的放射性标记的脂质体。 此外,所制备的放射性标记的脂质体具有高比活度和高灵敏度,适用于临床应用。