CN100531717C - 含氨甲喋呤增效剂的抗癌缓释剂 - Google Patents
含氨甲喋呤增效剂的抗癌缓释剂 Download PDFInfo
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- CN100531717C CN100531717C CNB2006102000622A CN200610200062A CN100531717C CN 100531717 C CN100531717 C CN 100531717C CN B2006102000622 A CNB2006102000622 A CN B2006102000622A CN 200610200062 A CN200610200062 A CN 200610200062A CN 100531717 C CN100531717 C CN 100531717C
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- methotrexate
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- anticancer
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Abstract
Description
试验组(n) | 给药方式 | 第一天肿瘤内药物含量 | 第三大肿瘤内药物含量 | 第7天肿瘤内药物含量 |
1(3) | 尾静脉注射普通注射剂 | 0.65 | 0.35 | 0.12 |
2(3) | 腹腔注射普通注射剂 | 0.58 | 0.3 | 0.08 |
3(3) | 瘤周注射普通注射剂 | 2.8 | 1.2 | 0.3 |
4(3) | 瘤周注射缓释注射剂 | 10 | 18 | 20 |
5(3) | 瘤周放置缓释植入剂 | 20 | 30 | 32 |
6(3) | 瘤内注射普通注射剂 | 4 | 2 | 1 |
7(3) | 瘤内注射缓释注射剂 | 90 | 80 | 60 |
8(3) | 瘤内放置缓释植入剂 | 94 | 90 | 84 |
试验组(n) | 给约方式 | 肿瘤体积(cm<sup>3</sup>) | P值 |
1(6) | - | 70 | |
2(6) | 尾静脉注射普通注射剂 | 65 | 0.06 |
3(6) | 腹腔注射普通注射剂 | 66 | 0.06 |
4(6) | 瘤周注射普通注射剂 | 58 | 0.03 |
5(6) | 瘤周注射缓释注射剂 | 32 | <0.01 |
6(6) | 瘤周放置缓释植入剂 | 22 | <0.01 |
7(6) | 瘤内注射普通注射剂 | 54 | 0.04 |
8(6) | 瘤内注射缓释注射剂 | 22 | <0.001 |
9(6) | 瘤内放置缓释植入剂 | 16 | <0.001 |
组别 | 氨甲喋呤 | 增效剂 | 肿瘤抑制率(%) | P值 |
1 | + | - | 60 | * |
2 | - | 曲普瑞林 | 46 | * |
3 | - | 戈舍瑞林 | 42 | * |
4 | - | 亮丙瑞林 | 38 | * |
5 | - | 阿那曲唑 | 48 | * |
6 | - | 艾多昔芬 | 36 | * |
7 | + | 曲普瑞林 | 80 | ** |
8 | + | 戈舍瑞林 | 82 | ** |
9 | + | 亮丙瑞林 | 88 | ** |
10 | + | 阿那曲唑 | 88 | ** |
11 | + | 艾多昔芬 | 90 | ** |
瘤细胞 | 氨 | A | B | C | D | E | 氨+A | 氨+B | 氨+C | 氨+D | 氨+E |
CNS | 62 | 50 | 48 | 38 | 58 | 42 | 84 | 78 | 92 | 88 | 86 |
C6 | 64 | 52 | 46 | 36 | 64 | 40 | 90 | 84 | 94 | 84 | 94 |
SA | 58 | 58 | 36 | 42 | 62 | 48 | 86 | 82 | 88 | 92 | 92 |
BC | 54 | 54 | 40 | 42 | 64 | 54 | 84 | 84 | 94 | 84 | 82 |
BA | 58 | 46 | 38 | 48 | 60 | 56 | 82 | 90 | 98 | 92 | 90 |
LH | 60 | 56 | 40 | 52 | 58 | 60 | 92 | 88 | 90 | 88 | 84 |
PAT | 64 | 48 | 46 | 50 | 54 | 68 | 92 | 78 | 92 | 88 | 90 |
试验组(n) | 所受治疗 | 肿瘤抑制率(%) | P值 |
1(6) | 对照 | - | |
2(6) | 氨甲喋呤 | 42 | <0.05 |
3(6) | 甲羟孕酮 | 36 | <0.01 |
4(6) | 托瑞米芬 | 40 | <0.01 |
5(6) | 阿那曲唑 | 44 | <0.01 |
6(6) | 依西美坦 | 46 | <0.01 |
7(6) | 氨甲喋呤+甲羟孕酮 | 86 | <0.001 |
8(6) | 氨甲喋呤+托瑞米芬 | 80 | <0.001 |
9(6) | 氨甲喋呤+阿那曲唑 | 82 | <0.001 |
10(6) | 氨甲喋呤+依西美坦 | 92 | <0.001 |
试验组(n) | 所受治疗 | 肿瘤抑制率(%) | P值 |
1(6) | 对照 | - | |
2(6) | 氨甲喋呤 | 58 | <0.05 |
3(6) | 吉非替尼 | 50 | <0.01 |
4(6) | 厄洛替尼 | 40 | <0.01 |
5(6) | 拉帕替尼 | 36 | <0.01 |
6(6) | 伏他拉尼 | 36 | <0.01 |
7(6) | 氨甲喋呤+吉非替尼 | 82 | <0.001 |
8(6) | 氨甲喋呤+厄洛替尼 | 84 | <0.001 |
9(6) | 氨甲喋呤+拉帕替尼 | 92 | <0.001 |
10(6) | 氨甲喋呤+伏他拉尼 | 94 | <0.001 |
试验组(n) | 所受治疗 | 肿瘤抑制率(%) | P值 |
1(6) | 对照 | - | |
2(6) | 氨甲喋呤 | 54 | <0.05 |
3(6) | 培立替尼 | 58 | <0.05 |
4(6) | 反应停 | 36 | <0.05 |
5(6) | 雷诺胺 | 46 | <0.05 |
6(6) | 血管抑素 | 36 | <0.01 |
7(6) | 氨甲喋呤+培立替尼 | 80 | <0.01 |
8(6) | 氨甲喋呤+反应停 | 82 | <0.01 |
9(6) | 氨甲喋呤+雷诺胺 | 90 | <0.01 |
10(6) | 氨甲喋呤+血管抑素 | 88 | <0.001 |
试验组(n) | 所受治疗 | 肿瘤抑制率(%) | P值 |
1(6) | 对照 | - | |
2(6) | 氨甲喋呤 | 58 | <0.05 |
3(6) | 内皮抑素 | 40 | <0.01 |
4(6) | 甲磺酸甲磺酸 | 50 | <0.01 |
5(6) | 司马斯尼 | 40 | <0.01 |
6(6) | 达萨替尼 | 42 | <0.01 |
7(6) | 氨甲喋呤+内皮抑素 | 86 | <0.001 |
8(6) | 氨甲喋呤+甲磺酸甲磺酸 | 88 | <0.001 |
9(6) | 氨甲喋呤+司马斯尼 | 92 | <0.001 |
10(6) | 氨甲喋呤+达萨替尼 | 94 | <0.001 |
试验组(n) | 所受治疗 | 肿瘤抑制率(%) | P值 |
1(6) | 对照 | - | |
2(6) | 氨甲喋呤 | 52 | <0.05 |
3(6) | 阿瓦斯丁 | 48 | <0.01 |
4(6) | 卡那替尼 | 38 | <0.01 |
5(6) | 索拉非尼 | 40 | <0.01 |
6(6) | 苏尼替尼 | 50 | <0.01 |
7(6) | 氨甲喋呤+阿瓦斯丁 | 80 | <0.001 |
8(6) | 氨甲喋呤+卡那替尼 | 78 | <0.001 |
9(6) | 氨甲喋呤+索拉非尼 | 86 | <0.001 |
10(6) | 氨甲喋呤+苏尼替尼 | 90 | <0.001 |
溶媒黏度(cp) | 注射成功次数 | 注射成功率(%) |
10 | 1 | 5 |
50 | 2 | 10 |
100 | 4 | 20 |
200 | 7 | 35 |
300 | 9 | 45 |
400 | 12 | 60 |
500 | 14 | 70 |
550 | 14 | 70 |
600 | 16 | 80 |
650 | 18 | 90 |
Claims (2)
- 【权利要求1】一种含氨甲喋呤增效剂的抗癌缓释剂,其特征在于抗癌缓释剂为抗癌缓释注射剂,由以下成分组成:(A)缓释微球,包括:抗癌有效成分缓释辅料和(B)溶媒;其中,抗癌有效成分为氨甲喋呤和选自激素类抗癌药的氨甲喋呤增效剂的组合;溶媒中的助悬剂为甘露醇;所述的抗癌缓释注射剂为下列组合:抗癌有效成分为10%氨甲喋呤和10%亮丙瑞林,缓释辅料为对羧苯基丙烷:癸二酸为20:80的聚苯丙生,溶媒为含15%甘露醇的生理盐水;抗癌有效成分的重量百分比基于微球,助悬剂为体积重量比基于溶媒。
- 【权利要求2】一种含氨甲喋呤增效剂的抗癌缓释剂,其特征在于抗癌缓释剂为缓释植入剂,经瘤内或瘤周注射或放置给药;所述的缓释植入剂的组成为下列组合:抗癌有效成分为10%阿那曲唑和20%氨甲喋呤,缓释辅料为对羧苯基丙烷:癸二酸为20:80的聚苯丙生;以上均为重量百分比。
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