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1. 发明授权

US08545808B2 Compositions for radiolabeling diethylenetriaminepentaacetic acid (DTPA)-dextran 有权
标题翻译：放射性标记二亚乙基三胺五乙酸（DTPA） - 葡聚糖的组合物
公开(公告)号：US08545808B2
公开(公告)日：2013-10-01
申请号：US13461306
申请日：2012-05-01
申请人： Gerald Ross Magneson , Richard Cushman Orahood
发明人： Gerald Ross Magneson , Richard Cushman Orahood
IPC分类号： A61K51/00 , A01N59/16
CPC分类号： C07B59/005 , A61K51/0491 , A61K51/065 , C07B59/001 , C07B59/004 , C07B63/04 , C07B2200/05 , G01N33/534 , G01N33/60
摘要： The subject invention relates to the compositions for radiolabeling Diethylenetriaminepentaacetic Acid (DTPA)-dextran with Technetium-99m and for stabilizing the DTPA-dextran Cold Kit. The composition contains Stannous Chloride ions to reduce 99mTc-pertechnetate, Ascorbic Acid to reduce stannic ions to stannous ions to maintain a reducing environment, α,α-Trehalose to add bulk and to stabilize the lyophilized composition without interfering with the radiochemical yield, and Glycine to transchelate Technetium-99m under highly acidic conditions to facilitate radiolabeling DTPA-dextran with high radiochemical purity. In addition, the invention pertains to methods for making and using the compositions. The reconstitution of the lyophilized composition by 99mTc-pertechnetate, resulting in radiolabeled 99mTc-DTPA-dextran in a composition between pH 3 to 4. This invention contains a Diluent vial, which when used will shift the pH to a moderately acidic pH, which would provide less pain on injection and ease-of-use to clinical practitioners for adjusting its potency.
摘要翻译：本发明涉及用锝-99m放射性标记二亚乙基三胺五乙酸（DTPA） - 葡聚糖并用于稳定DTPA-葡聚糖冷试剂盒的组合物。该组合物含有氯化亚锡离子以减少99mTc-高锝酸盐，抗坏血酸将亚锡离子还原成亚锡离子以保持还原环境，α，α-海藻糖增加体积并稳定冻干组合物而不干扰放射化学产率，甘氨酸在高度酸性条件下将锝-99m转移以便放射性标记具有高放射化学纯度的DTPA-葡聚糖。此外，本发明涉及制备和使用组合物的方法。通过99mTc-高锝酸盐重构冻干组合物，得到在pH3-4之间的组合物中放射性标记的99mTc-DTPA-葡聚糖。本发明含有稀释剂小瓶，其使用时将pH值移至中等酸性pH值，为临床医师提供更少的注射疼痛和易于使用的调节效力。

2. 发明申请

US20120213700A1 COMPOSITIONS FOR RADIOLABELING DIETHYLENETRIAMINEPENTAACETIC ACID (DTPA)-DEXTRAN 有权
标题翻译：用于放射性二甲基氨基苯甲酸（DTPA）-DEXTRAN的组合物
公开(公告)号：US20120213700A1
公开(公告)日：2012-08-23
申请号：US13461306
申请日：2012-05-01
申请人： Gerald Ross Magneson , Richard Cushman Orahood
发明人： Gerald Ross Magneson , Richard Cushman Orahood
IPC分类号： A61K51/00 , B65B1/04
CPC分类号： C07B59/005 , A61K51/0491 , A61K51/065 , C07B59/001 , C07B59/004 , C07B63/04 , C07B2200/05 , G01N33/534 , G01N33/60
摘要： The subject invention relates to the compositions for radiolabeling Diethylenetriaminepentaacetic Acid (DTPA)-dextran with Technetium-99m and for stabilizing the DTPA-dextran Cold Kit. The composition contains Stannous Chloride ions to reduce 99mTc-pertechnetate, Ascorbic Acid to reduce stannic ions to stannous ions to maintain a reducing environment, α,α-Trehalose to add bulk and to stabilize the lyophilized composition without interfering with the radiochemical yield, and Glycine to transchelate Technetium-99m under highly acidic conditions to facilitate radiolabeling DTPA-dextran with high radiochemical purity. In addition, the invention pertains to methods for making and using the compositions. The reconstitution of the lyophilized composition by 99mTc-pertechnetate, resulting in radiolabeled 99mTc-DTPA-dextran in a composition between pH 3 to 4. This invention contains a Diluent vial, which when used will shift the pH to a moderately acidic pH, which would provide less pain on injection and ease-of-use to clinical practitioners for adjusting its potency.
摘要翻译：本发明涉及用锝-99m放射性标记二亚乙基三胺五乙酸（DTPA） - 葡聚糖并用于稳定DTPA-葡聚糖冷试剂盒的组合物。该组合物含有氯化亚锡离子以减少99mTc-高锝酸盐，抗坏血酸将亚锡离子还原成亚锡离子以保持还原环境，α，α-海藻糖增加体积并稳定冻干组合物而不干扰放射化学产率，甘氨酸在高度酸性条件下将锝-99m转移以便放射性标记具有高放射化学纯度的DTPA-葡聚糖。此外，本发明涉及制备和使用组合物的方法。通过99mTc-高锝酸盐重构冻干组合物，得到在pH3-4之间的组合物中放射性标记的99mTc-DTPA-葡聚糖。本发明含有稀释剂小瓶，其使用时将pH值移至中等酸性pH值，为临床医师提供更少的注射疼痛和易于使用的调节效力。

3. 发明申请

US20100196272A1 COMPOSITIONS FOR RADIOLABELING DIETHYLENETRIAMINEPENTAACETIC ACID (DTPA)-DEXTRAN 审中-公开
标题翻译：用于放射性二甲基氨基苯甲酸（DTPA）-DEXTRAN的组合物
公开(公告)号：US20100196272A1
公开(公告)日：2010-08-05
申请号：US12362778
申请日：2009-01-30
申请人： Gerald Ross Magneson , Richard Cushman Orahood
发明人： Gerald Ross Magneson , Richard Cushman Orahood
IPC分类号： A61K51/04
CPC分类号： C07B59/005 , A61K51/0491 , A61K51/065 , C07B59/001 , C07B59/004 , C07B63/04 , C07B2200/05 , G01N33/534 , G01N33/60
摘要： The subject invention relates to the compositions for radiolabeling Diethylenetriaminepentaacetic Acid (DTPA)-dextran with Technetium-99m and for stabilizing the DTPA-dextran Cold Kit. The composition contains Stannous Chloride ions to reduce 99mTc-pertechnetate, Ascorbic Acid to reduce stannic ions to stannous ions to maintain a reducing environment, α,α-Trehalose to add bulk and to stabilize the lyophilized composition without interfering with the radiochemical yield, and Glycine to transchelate Technetium-99m under highly acidic conditions to facilitate radiolabeling DTPA-dextran with high radiochemical purity. In addition, the invention pertains to methods for making and using the compositions. The reconstitution of the lyophilized composition by 99mTc-pertechnetate, resulting in radiolabeled 99mTc-DTPA-dextran in a composition between pH 3 to 4. This invention contains a Diluent vial, which when used will shift the pH to a moderately acidic pH, which would provide less pain on injection and ease-of-use to clinical practioners for adjusting its potency.
摘要翻译：本发明涉及用锝-99m放射性标记二亚乙基三胺五乙酸（DTPA） - 葡聚糖并用于稳定DTPA-葡聚糖冷试剂盒的组合物。该组合物含有氯化亚锡离子以减少99mTc-高锝酸盐，抗坏血酸将亚锡离子还原成亚锡离子以保持还原环境，α，α-海藻糖增加体积并稳定冻干组合物而不干扰放射化学产率，甘氨酸在高度酸性条件下将锝-99m转移以便放射性标记具有高放射化学纯度的DTPA-葡聚糖。此外，本发明涉及制备和使用组合物的方法。通过99mTc-高锝酸盐重构冻干组合物，得到在pH3-4之间的组合物中放射性标记的99mTc-DTPA-葡聚糖。本发明含有稀释剂小瓶，其使用时将pH值移至中等酸性pH值，为临床工作者提供更少的注射痛苦和易用性，以调整其效力。

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