公开(公告)号：US20120107232A1

公开(公告)日：2012-05-03

申请号：US13169268

申请日：2011-06-27

申请人： WEI-CHUAN HSU ,  Te-Wei Lee ,  Shu-Pei Chiu ,  Yi-Ting Tsai ,  Gann Ting

发明人： WEI-CHUAN HSU ,  Te-Wei Lee ,  Shu-Pei Chiu ,  Yi-Ting Tsai ,  Gann Ting

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。

公开(公告)号：US20110158903A1

公开(公告)日：2011-06-30

申请号：US12650793

申请日：2009-12-31

申请人： SHU-PEI CHIU ,  Te-Wei Lee ,  Chia-Yu Yu ,  Su-Jung Chen ,  Chung-Li Ho ,  Wei-Chuan Hsu ,  Ya-Jen Chang

发明人： SHU-PEI CHIU ,  Te-Wei Lee ,  Chia-Yu Yu ,  Su-Jung Chen ,  Chung-Li Ho ,  Wei-Chuan Hsu ,  Ya-Jen Chang

IPC分类号： A61K51/12 ,  A61P35/00

CPC分类号： A61K51/1234 ,  A61K47/543 ,  A61K47/60

摘要： One pot process of preparing multifunctional liposome drug is provided. In this one pot process, liposome reacted with radionuclide labeled solution, chemotherapy drug, and targeted ligand at appropriate temperature. The product in this invention for preparation multifunctional liposome drugs in for imaging, delivery and targeting in cancer diagnosis and therapy has proved to be more simple, convenient, effective and easier than the prior art is.

摘要翻译： 提供了制备多功能脂质体药物的一锅法。 在这一锅法中，脂质体与放射性核素标记溶液，化疗药物和靶向配体在合适的温度下反应。 本发明中用于制备用于癌症诊断和治疗中的成像，递送和靶向的多功能脂质体药物的产品被证明比现有技术更简单，方便，有效和更容易。

公开(公告)号：US20080226546A1

公开(公告)日：2008-09-18

申请号：US11687650

申请日：2007-03-18

申请人： Te-Wei Lee ,  Ya-Jen Chang ,  Liang-Cheng Chen ,  Chia-Yu Yu ,  Shu-Pei Chiu ,  Shu-Ling Chen ,  Tsai-Yueh Luo ,  Chih-Hsien Chang ,  Gann Ting

发明人： Te-Wei Lee ,  Ya-Jen Chang ,  Liang-Cheng Chen ,  Chia-Yu Yu ,  Shu-Pei Chiu ,  Shu-Ling Chen ,  Tsai-Yueh Luo ,  Chih-Hsien Chang ,  Gann Ting

IPC分类号： A61K51/12 ,  A61K51/00 ,  A61P35/00 ,  A61K51/04

CPC分类号： A61K31/704 ,  A61K47/6911 ,  A61K51/0478 ,  A61K51/1234 ,  A61K2300/00

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。}

公开(公告)号：US20080139703A1

公开(公告)日：2008-06-12

申请号：US12029324

申请日：2008-02-11

申请人： Te-Wei Lee ,  Shu-Pei Chiu ,  Chiu-Yu Yu ,  Tsui-Jung Chang ,  Chih-Hsien Chang

发明人： Te-Wei Lee ,  Shu-Pei Chiu ,  Chiu-Yu Yu ,  Tsui-Jung Chang ,  Chih-Hsien Chang

IPC分类号： C08L89/00

CPC分类号： A61K9/1271 ,  A61K9/1278 ,  A61K47/62 ,  A61K47/6911 ,  C07K14/6555 ,  Y02P20/55

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。

公开(公告)号：US20140377169A1

公开(公告)日：2014-12-25

申请号：US13921217

申请日：2013-06-19

申请人： Ming-Hsin Li ,  Shu-Pei Chiu ,  Chih-Hsien Chang ,  Te-Wei Lee

发明人： Ming-Hsin Li ,  Shu-Pei Chiu ,  Chih-Hsien Chang ,  Te-Wei Lee

IPC分类号： B01J19/00 ,  A61K51/12

CPC分类号： B01J19/004 ,  A61K51/1234 ,  C07B59/001

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。

公开(公告)号：US20150033828A1

公开(公告)日：2015-02-05

申请号：US13956375

申请日：2013-08-01

申请人： Ming-Hsin Li ,  Shu-Pei Chiu ,  Chih-Hsien Chang ,  Te-Wei Lee

发明人： Ming-Hsin Li ,  Shu-Pei Chiu ,  Chih-Hsien Chang ,  Te-Wei Lee

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。

公开(公告)号：US20080102110A1

公开(公告)日：2008-05-01

申请号：US11608836

申请日：2006-12-10

申请人： Te-Wei Lee ,  Shu-Pei Chiu ,  Chiu-Yu Yu ,  Tsui-Jung Chang ,  Chih-Hsien Chang

发明人： Te-Wei Lee ,  Shu-Pei Chiu ,  Chiu-Yu Yu ,  Tsui-Jung Chang ,  Chih-Hsien Chang

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

CPC分类号： A61K9/1271 ,  A61K9/1278 ,  A61K47/62 ,  A61K47/6911 ,  C07K14/6555 ,  Y02P20/55

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.

公开(公告)号：US09707521B2

公开(公告)日：2017-07-18

申请号：US13956375

申请日：2013-08-01

申请人： Ming-Hsin Li ,  Shu-Pei Chiu ,  Chih-Hsien Chang ,  Te-Wei Lee

发明人： Ming-Hsin Li ,  Shu-Pei Chiu ,  Chih-Hsien Chang ,  Te-Wei Lee

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.

公开(公告)号：US07803350B2

公开(公告)日：2010-09-28

申请号：US11881901

申请日：2007-07-30

申请人： Te-Wei Lee ,  Chun-Ying Huang ,  Ming-Shiuan Wu ,  Te-Jung Chen ,  Kwo-Ping Chang ,  Shiang-Rong Chang ,  Shyh-Yi Chyi ,  Chih-Hsien Chang ,  Yin-Mao Hsu ,  Kuo-Hsien Fan ,  Wei-Chuan Hsu ,  Ying-Kai Fu ,  Charng-Feng Kao

发明人： Te-Wei Lee ,  Chun-Ying Huang ,  Ming-Shiuan Wu ,  Te-Jung Chen ,  Kwo-Ping Chang ,  Shiang-Rong Chang ,  Shyh-Yi Chyi ,  Chih-Hsien Chang ,  Yin-Mao Hsu ,  Kuo-Hsien Fan ,  Wei-Chuan Hsu ,  Ying-Kai Fu ,  Charng-Feng Kao

IPC分类号： A61K51/00 ,  A61K36/14

CPC分类号： A61K51/02 ,  A61K41/009 ,  A61K51/121

摘要： This invention provides a process for producing a radioactive arsenic-containing compound, comprising the steps of: (i) subjecting an arsenic-containing compound to a neutron irradiation treatment, said arsenic-containing compound being selected from a group consisting of As2O3, As2S3, As2S2, and a combination thereof, such that the arsenic element contained in the arsenic-containing compound is converted to a radioactive arsenic isotope; and (ii) recovering the resultant product from step (i).This invention also provides a pharmaceutical composition comprising a therapeutically effective amount of the radioactive arsenic-containing compound and a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the treatment of tumors/cancers such as hematological malignancies and solid tumors.

摘要翻译： 本发明提供一种放射性含砷化合物的制造方法，其特征在于，包括以下工序：（i）对含砷化合物进行中子照射处理，所述含砷化合物选自As2O3，As2S3， As2S2及其组合，使含砷化合物中所含的砷元素转化为放射性砷同位素; 和（ii）从步骤（i）中回收所得产物。 本发明还提供包含治疗有效量的放射性含砷化合物和药学上可接受的载体的药物组合物。 药物组合物可用于治疗肿瘤/癌症如血液恶性肿瘤和实体瘤。

公开(公告)号：US20080003177A1

公开(公告)日：2008-01-03

申请号：US11881901

申请日：2007-07-30

申请人： Chun-Ying Huang ,  Ming-Shiuan Wu ,  Te-Wei Lee ,  Te-Jung Chen ,  Kwo-Ping Chang ,  Shyh-Yi Chyi ,  Yin-Mao Hsu ,  Kuo-Hsien Fan ,  Wei-Chuan Hsu ,  Ying-Kai Fu ,  Charng-Feng Kao ,  Shiang-Rong Chang ,  Chih-Hsien Chang

发明人： Chun-Ying Huang ,  Ming-Shiuan Wu ,  Te-Wei Lee ,  Te-Jung Chen ,  Kwo-Ping Chang ,  Shyh-Yi Chyi ,  Yin-Mao Hsu ,  Kuo-Hsien Fan ,  Wei-Chuan Hsu ,  Ying-Kai Fu ,  Charng-Feng Kao ,  Shiang-Rong Chang ,  Chih-Hsien Chang

IPC分类号： A61K51/02 ,  A61P35/00

CPC分类号： A61K51/02 ,  A61K41/009 ,  A61K51/121

摘要： This invention provides a process for producing a radioactive arsenic-containing compound, comprising the steps of: (i) subjecting an arsenic-containing compound to a neutron irradiation treatment, said arsenic-containing compound being selected from a group consisting of As2O3, As2S3, As2S2, and a combination thereof, such that the arsenic element contained in the arsenic-containing compound is converted to a radioactive arsenic isotope; and (ii) recovering the resultant product from step (i). This invention also provides a pharmaceutical composition comprising a therapeutically effective amount of the radioactive arsenic-containing compound and a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the treatment of tumors/cancers such as hematological malignancies and solid tumors.

摘要翻译： 本发明提供了一种制备放射性含砷化合物的方法，包括以下步骤：（i）对含砷化合物进行中子照射处理，所述含砷化合物选自： 2 3 3 3 3 SUB>及其组合，使含砷化合物中所含的砷元素转化为放射性砷同位素; 和（ii）从步骤（i）中回收所得产物。 本发明还提供包含治疗有效量的放射性含砷化合物和药学上可接受的载体的药物组合物。 药物组合物可用于治疗肿瘤/癌症如血液恶性肿瘤和实体瘤。