CN100531718C - 含氨甲喋呤增效剂的缓释注射剂 - Google Patents
含氨甲喋呤增效剂的缓释注射剂 Download PDFInfo
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- CN100531718C CN100531718C CNB2006102000637A CN200610200063A CN100531718C CN 100531718 C CN100531718 C CN 100531718C CN B2006102000637 A CNB2006102000637 A CN B2006102000637A CN 200610200063 A CN200610200063 A CN 200610200063A CN 100531718 C CN100531718 C CN 100531718C
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- methotrexate
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Abstract
Description
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 |
试验组(n) | 所受治疗 | 肿瘤体积(cm<sup>3</sup>) | P值 |
1(6) | 对照 | 72±10 | |
2(6) | 氨甲喋呤 | 48±5.4 | <0.05 |
3(6) | 阿霉素 | 46±2.2 | <0.01 |
4(6) | 表柔比星 | 46±2.2 | <0.01 |
5(6) | 依达比星 | 48±3.2 | <0.01 |
6(6) | 戊柔比星 | 42±3.0 | <0.01 |
7(6) | 氨甲喋呤+阿霉素 | 22±2.0 | <0.001 |
8(6) | 氨甲喋呤+表柔比星 | 30±3.4 | <0.001 |
9(6) | 氨甲喋呤+依达比星 | 32±3.4 | <0.001 |
10(6) | 氨甲喋呤+戊柔比星 | 18±2.0 | <0.001 |
试验组(n) | 所受治疗 | 肿瘤体积(cm<sup>3</sup>) | P值 |
1(6) | 对照 | 80±10 | |
2(6) | 氨甲喋呤 | 48±5.3 | <0.05 |
3(6) | 06-BG | 60±6.3 | <0.01 |
4(6) | 06-BuG | 62±3.6 | <0.001 |
5(6) | O6-MG | 68±5.0 | <0.01 |
6(6) | O6-AG | 62±4.0 | <0.001 |
7(6) | 氨甲喋呤+O6-BG | 38±3.8 | <0.01 |
8(6) | 氨甲喋呤+O6-BuG | 20±2.6 | <0.001 |
9(6) | 氨甲喋呤+O6-MG | 26±3.8 | <0.01 |
10(6) | 氨甲喋呤+O6-AG | 22±2.4 | <0.001 |
试验组(n) | 所受治疗 | 肿瘤体积(cm<sup>3</sup>) | P值 |
1(6) | 对照 | 70±10 | |
2(6) | 氨甲喋呤 | 46±5.0 | <0.05 |
3(6) | 尼莫司汀 | 50±2.0 | <0.01 |
4(6) | 氨甲喋呤+尼莫司汀 | 30±2.2 | <0.001 |
5(6) | 卡莫司汀 | 48±3.2 | <0.01 |
6(6) | 卡莫司汀+氨甲喋呤 | 32±3.0 | <0.001 |
7(6) | 福莫司汀 | 32±2.6 | <0.01 |
8(6) | 福莫司汀+氨甲喋呤 | 22±2.6 | <0.001 |
9(6) | 萨莫司汀 | 46±4.8 | <0.01 |
10(6) | 萨莫司汀+氨甲喋呤 | 20±2.0 | <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 | 42 | <0.05 |
3(6) | 司莫司汀 | 48 | <0.01 |
4(6) | 洛莫司汀 | 42 | <0.01 |
5(6) | 甲基洛莫司汀 | 52 | <0.01 |
6(6) | 链佐星 | 40 | <0.01 |
7(6) | 氨甲喋呤+司莫司汀 | 86 | <0.001 |
8(6) | 氨甲喋呤+洛莫司汀 | 88 | <0.001 |
9(6) | 氨甲喋呤+甲基洛莫司汀 | 92 | <0.001 |
10(6) | 氨甲喋呤+链佐星 | 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 | 56 | <0.05 |
3(6) | 加莫司汀 | 54 | <0.01 |
4(6) | 雷莫司汀 | 46 | <0.01 |
5(6) | 环磷酰胺 | 48 | <0.01 |
6(6) | 美法仑 | 46 | <0.01 |
7(6) | 氨甲喋呤+加莫司汀 | 86 | <0.001 |
8(6) | 氨甲喋呤+雷莫司汀 | 88 | <0.001 |
9(6) | 氨甲喋呤+环磷酰胺 | 94 | <0.001 |
10(6) | 氨甲喋呤+美法仑 | 90 | <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) | 长春新碱 | 48 | <0.01 |
4(6) | 长春花碱 | 56 | <0.01 |
5(6) | 长春瑞滨 | 48 | <0.01 |
6(6) | 长春地辛 | 48 | <0.01 |
7(6) | 氨甲喋呤+长春新碱 | 88 | <0.001 |
8(6) | 氨甲喋呤+长春花碱 | 86 | <0.001 |
9(6) | 氨甲喋呤+长春瑞滨 | 94 | <0.001 |
10(6) | 氨甲喋呤+长春地辛 | 96 | <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 (1)
- 【权利要求1】一种含氨甲喋呤的抗癌药物缓释注射剂,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鸟嘌呤类似物的氨甲喋呤增效剂的组合;溶媒中的助悬剂为甘露醇;所述的抗癌药物缓释注射剂为下列组合:抗癌有效成分为10%氨甲喋呤和10%O6-苄基鸟嘌呤,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。
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