JP6608925B2 - 医用撮像および医学療法のためのリン酸ストロンチウム - Google Patents
医用撮像および医学療法のためのリン酸ストロンチウム Download PDFInfo
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- JP6608925B2 JP6608925B2 JP2017522545A JP2017522545A JP6608925B2 JP 6608925 B2 JP6608925 B2 JP 6608925B2 JP 2017522545 A JP2017522545 A JP 2017522545A JP 2017522545 A JP2017522545 A JP 2017522545A JP 6608925 B2 JP6608925 B2 JP 6608925B2
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Description
20±10mol%のNa2O(モル濃度基準でLi2OもしくはK2Oまたはその組合せを最大25%含有し得る)と、
20±5mol%のSrO(その最大4分の1が別の放射線不透過性の酸化物、例えば酸化バリウム、酸化マンガンカルシウムまたは酸化コバルトによって置換されていてもよい)と、
60±10mol%のB2O3と、
0〜5mol%のその他の酸化物と
を含む。
実施例1:リン酸ストロンチウムマイクロスフェアの調製
上に記載した通りに、20mol%のNa2Oと20mol%のSrOと60mol%のBa2O3とを含むバッチからストロンチウム含有ホウ酸塩ガラスマイクロスフェアを調製した。マイクロスフェアの大きさは44〜105ミクロンの範囲であった。
0.05N HC1 0.5ml中の塩化イットリウム(Y−90)5μgの溶液をマイクロスフェア15mgに加え、30分間インキュベートした。1分後、5分後および30分後、マイクロスフェア内に搭載されたイットリウムの量を5回反復で測定し、平均値を求めた。経時的なイットリウムの取込みを図1に示す。
Claims (32)
- 結晶リン酸ストロンチウムと、その表面に結合または吸着した放射線撮像および/または放射線療法に適する少なくとも1つの放射性同位元素とを含み、1グラム当たり約90平方メートル超の表面積を有する、
放射性微粒子。 - マイクロスフェアである、請求項1に記載の放射性微粒子。
- 5μm〜1000μmの直径を有する、請求項1または2に記載の放射性微粒子。
- 前記表面に結合または吸着した前記放射性同位元素が、治療用のアルファ放射放射性同位元素またはベータ放射放射性同位元素である、請求項1〜3のいずれかに記載の放射性微粒子。
- 前記表面に結合または吸着した前記放射性同位元素が、診断用の陽電子放出放射性同位元素またはガンマ放射放射性同位元素である、請求項1〜3のいずれかに記載の放射性微粒子。
- 前記表面に結合または吸着した前記放射性同位元素が、治療用のアルファ放射放射性同位元素またはベータ放射放射性同位元素と診断用のガンマ放射放射性同位元素または陽電子放出放射性同位元素との組合せを含む、請求項1〜3のいずれかに記載の放射性微粒子。
- 前記表面に結合または吸着した前記放射性同位元素が、テクネチウム−99mである、請求項1〜6のいずれかに記載の放射性微粒子。
- 前記表面に結合または吸着した前記放射性同位元素が、テクネチウム−99m、インジウム−111、ルテチウム−177、サマリウム−153、イットリウム−90、ホルミウム−166、ガリウム−68、フッ素−18およびその組合せからなる群より選択される、請求項1〜6のいずれかに記載の放射性微粒子。
- 前記表面に結合または吸着した少なくとも2種類の異なる放射性同位元素を有する、請求項1〜8のいずれかに記載の放射性微粒子。
- 前記結合した放射性同位体が、少なくとも3種類の異なる放射性同位元素を含む、請求項1〜9のいずれかに記載の放射性微粒子。
- 請求項1〜10のいずれかに記載の放射性微粒子と、薬学的に許容される担体または希釈剤とを含む、医薬組成物。
- 放射性微粒子の調製のための工程であって、
(i)ストロンチウム含有ホウ酸塩ガラスの少なくとも一部を結晶リン酸ストロンチウムに変換するように前記ストロンチウム含有ホウ酸塩ガラス微粒子をリン酸塩溶液と反応させることと、
(ii)放射線撮像および/または放射線療法に適する少なくとも1つの放射性同位元素を前記リン酸ストロンチウム微粒子に結合または吸着させることと
を含む、工程。 - 前記微粒子を前記放射性同位元素の溶液と接触させることによって前記放射性同位元素が前記微粒子の表面に結合または吸着される、請求項12に記載の工程。
- 前記結合させることが前記微粒子を少なくとも1つの放射性同位元素と混合させることを含む、請求項13に記載の工程。
- 前記結合させることが前記微粒子を少なくとも1つの放射性同位元素を含む溶液中で混合することを含む、請求項14に記載の工程。
- 前記ストロンチウム含有ホウ酸塩ガラスが、実質的に完全にリン酸ストロンチウムに変換する、請求項12〜15のいずれかに記載の工程。
- 前記リン酸ストロンチウム含有ホウ酸塩ガラスが、実質的に完全に結晶リン酸ストロンチウムに変換する、請求項12〜15のいずれかに記載の工程。
- 前記放射性同位元素が、テクネチウム−99m、ガリウム68、ホルミウム−166、フッ素−18、インジウム−111、イットリウム−90、ルテチウム−177、サマリウム−153、およびその組合せからなる群より選択される、請求項12〜17のいずれかに記載の工程。
- 前記少なくとも1つの放射性同位元素が、Y−90/In−111、Y−90/Tc−99m、Y−90/Ga−68、Y−90/F−18、Y−90/Cu−64、Cu−67/Cu−64、Y−90/Lu−177、P−32/In−111、P−32/Tc−99m、P−32/Ga−68、Ho−166/In−111、Ho−166/Tc−99m、Sm−153/In−111、およびSm−153/Tc−99mからなる群より選択される放射性同位元素の組合せである、請求項12〜18のいずれかに記載の工程。
- 患者の組織標的または臓器に局所的に送達する用の、請求項11に記載の組成物。
- 前記組成物が追加の放射線治療剤をさらに含む、請求項20に記載の組成物。
- 前記組織標的または臓器が、脳、心筋、甲状腺、肺、肝臓、脾臓、胆嚢、腎臓、骨、血液、頭頸部、前立腺、乳房、卵巣および子宮からなる群より選択される、請求項20または21に記載の組成物。
- 前記放射性微粒子が、患者への投与の時間に先立つ24時間以内に調製される、請求項20または21に記載の組成物。
- 患者の組織または臓器の放射線画像を得る用の、請求項11に記載の組成物。
- 放射線診断剤によって放射されたガンマ線を撮像することによって前記放射線画像が得られる、請求項24に記載の組成物。
- 前記放射線画像が、放射線診断剤により放出された陽電子線を撮像することによって得られる、請求項24または25に記載の組成物。
- 前記放射線診断剤が、テクネチウム−99m、インジウム−111、ルテチウム−177、ガリウム−68、フッ素−18およびその組合せからなる群より選択される、請求項25または26に記載の組成物。
- 組織標的または臓器が、脳、心筋、甲状腺、肺、肝臓、脾臓、胆嚢、腎臓、骨、血液、頭頸部、前立腺、乳房、および子宮からなる群より選択される、請求項24〜27のいずれかに記載の組成物。
- 前記放射線画像が単光子放射型コンピュータ断層撮影法(SPECT)によって得られる、請求項24〜28のいずれかに記載の組成物。
- 前記放射線画像がPETによって得られる、請求項24〜28のいずれかに記載の組成物。
- 放射線療法での使用のための、請求項11に記載の組成物。
- アテローム性動脈硬化症の治療または腫瘍の治療用の、請求項31に記載の組成物。
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