CN101193652B - 包含肠降血糖素肽和非质子极性溶剂的药物制剂 - Google Patents
包含肠降血糖素肽和非质子极性溶剂的药物制剂 Download PDFInfo
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- CN101193652B CN101193652B CN200680019970XA CN200680019970A CN101193652B CN 101193652 B CN101193652 B CN 101193652B CN 200680019970X A CN200680019970X A CN 200680019970XA CN 200680019970 A CN200680019970 A CN 200680019970A CN 101193652 B CN101193652 B CN 101193652B
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- pharmaceutical preparation
- incretin
- peptide
- preparation
- stabilised pharmaceutical
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Abstract
Description
方法 | 温度(℃) | 体系 | 功效(mg/mL) | ||||
SEC-HPLC | 0个月 | 1个月 | 2个月 | 3个月 | 6个月 | ||
功效(mg/mL) | 5 | 纯DMSO | 24.5 | ||||
5 | 0.5%水/DMSO | 24.4 | |||||
25 | 纯DMSO | 23.4 | 24.8 | 24.5 | 24.4 | 24.3 | |
25 | 0.5%水/DMSO | 23.4 | 24.9 | 24.5 | 24.4 | 24.3 | |
40 | 纯DMSO | 24.8 | 24.6 | 24.7 | 23.6 | ||
40 | 0.5%水/DMSO | 24.9 | 24.7 | 24 4 | 23.1 |
方法 | 温度(℃) | 体系 | %纯度 | |||
RP-HPLC | 1个月 | 2个月 | 3个月 | 6个月 | ||
%纯度 | 5 | 纯DMSO | 99.7 | |||
5 | 0.5%水/DMSO | 99.6 | ||||
25 | 纯DMSO | 99.7 | 99.1 | 98.4 | 97.0 | |
25 | 0.5%水/DMSO | 99.5 | 99.2 | 98.3 | 96.6 | |
40 | 纯DMSO | 96.5 | 90.2 | 83.7 | 71.1 | |
40 | 0.5%水/DMSO | 96.3 | 90.3 | 83.8 | 71.7 |
方法 | 温度(℃) | 体系 | %纯度 | |||
SCX-HPLC | 1个月 | 2个月 | 3个月 | 6个月 | ||
%纯度 | 5 | 纯DMSO | 99.5 | |||
5 | 0.5%水/DMSO | 99.4 | ||||
25 | 纯DMSO | 99.0 | 98.4 | 96.7 | 95.8 | |
25 | 0.5%水/DMSO | 99.2 | 98.3 | 97.9 | 95.8 | |
40 | 纯DMSO | 95.8 | 90.2 | 85.0 | 72.2 | |
40 | 0.5%水/DMSO | 96.0 | 90.7 | 85.7 | 72.5 |
方法 | 温度(℃) | 体系 | %纯度 | ||||
SCX-HPLC | 0.25个月 | 0.5个月 | 1个月 | 2个月 | 3个月 | ||
%纯度 | 25 | 含水缓冲液(pH4.5) | 99.2 | 98.5 | 97.1 | 94.8 | 90.4 |
40 | 含水缓冲液(pH4.5) | 92.2 | 87.9 |
制剂号 | 溶剂体系 | 混合物%w/w溶剂/DMSO |
1 | 乙酸乙酯/DMSO | 33%w/w |
2 | 碳酸丙烯酯/DMSO | 30%w/w |
3 | N-甲基吡咯烷酮/DMSO | 26%w/w |
4 | 二甲基甲酰胺/DMSO | 25%w/w |
5 | 二甲基乙酰胺/DMSO | 30%w/w |
6 | 水/DMSO | 10%w/w |
7 | N-甲基吡咯烷酮 | (纯) |
8 | 二甲基甲酰胺 | (纯) |
9 | 二甲基乙酰胺 | (纯) |
10 | DMSO | (纯) |
初始值的百分比 | |||||||||
月数 | |||||||||
SCX-纯度 | 37℃ | 25℃ | |||||||
制剂号 | 初始值 | 1 | 2 | 3 | 6 | 1 | 2 | 3 | 6 |
1 | 98.8 | 64.0 | 32.9 | 85.1 | 71.3 | ||||
2 | 97.1 | 16.4 | 51.3 | ||||||
3 | 97.6 | 88.0 | 77.7 | 62.0 | 52.1 | 95.8 | 90.0 | 83.3 | 78.1 |
4 | 98.6 | 19.8 | 60.5 | ||||||
5 | 99.0 | 86.4 | 72.2 | 53.5 | 40.9 | 94.0 | 89.6 | 86.9 | 77.6 |
6 | 99.1 | 94.3 | 88.7 | 79.6 | 73.6 | 97.3 | 97.8 | 96.8 | 91.3 |
7 | 81.4 | 30.7 | 52.1 | ||||||
8 | 92.9 | 5.6 | 28.1 | ||||||
9 | 98.3 | 65.7 | 28.7 | 87.3 | 76.7 | ||||
10 | 99.1 | 95.9 | 93.1 | 85.4 | 74.7 | 99.0 | 97.8 | 96.1 | 92.3 |
初始值的百分比 | |||||||||
月数 | |||||||||
RP-纯度 | 37℃ | 25℃ | |||||||
制剂号 | 初始值 | 1 | 2 | 3 | 6 | 1 | 2 | 3 | 6 |
1 | 97.0 | 62.2 | 32.8 | 86.8 | 73.2 | ||||
2 | 95.4 | 14.2 | 49.6 | ||||||
3 | 96.2 | 90.4 | 77.2 | 62.5 | 47.3 | 95.5 | 91.3 | 83.7 | 76.5 |
4 | 96.5 | 20.1 | 64.1 | ||||||
5 | 97.5 | 88.3 | 74.1 | 50.8 | 39.0 | 96.2 | 92.5 | 86 8 | 78.7 |
6 | 97.7 | 97.7 | 94.7 | 87.3 | 81.5 | 99.5 | 98.7 | 97.6 | 96.9 |
7 | 86.6 | 32.5 | 59.9 | ||||||
8 | 91.8 | 0.4 | 26.5 | ||||||
9 | 96.8 | 68.4 | 28.6 | 89.4 | 80.7 | ||||
10 | 97.4 | 98.0 | 94.1 | 83.1 | 74.3 | 99.5 | 98.9 | 97.4 | 95.5 |
初始值的百分比 | |||||||||
月数 | |||||||||
SEC-功效 | 37℃ | 25℃ | |||||||
制剂号 | 初始值 | 1 | 2 | 3 | 6 | 1 | 2 | 3 | 6 |
1 | 9.05 | 107.0 | 107.5 | 103.3 | 102.5 | ||||
2 | 8.24 | 99.0 | 98.4 | ||||||
3 | 8.52 | 100.1 | 103.0 | 96.3 | 91.6 | 99.9 | 101.2 | 98.6 | 97.7 |
4 | 8.80 | 103.2 | 99.5 | ||||||
5 | 9.06 | 100.8 | 100.8 | 99.3 | 101.5 | 100.5 | 100.0 | 100.2 | 98.9 |
6 | 9.48 | 101.6 | 102.1 | 102.2 | 99.2 | 98.5 | 100.7 | 100.9 | 99.6 |
7 | 9.57 | 98.2 | 98.7 | ||||||
8 | 9.27 | 103.3 | 102.2 | ||||||
9 | 9.02 | 102.2 | 100.5 | 102.2 | 103.7 | ||||
10 | 9.42 | 102.7 | 102.1 | 102.7 | 98.9 | 100.9 | 101.9 | 101.5 | 101.9 |
Claims (49)
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US60/669,353 | 2005-04-08 | ||
PCT/US2006/013073 WO2006110551A2 (en) | 2005-04-08 | 2006-04-06 | Pharmaceutical formulations comprising incretin peptide and aprotic polar solvent |
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CN101193652A CN101193652A (zh) | 2008-06-04 |
CN101193652B true CN101193652B (zh) | 2011-11-02 |
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EP (1) | EP1909824B1 (zh) |
CN (1) | CN101193652B (zh) |
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AU (1) | AU2006235183B2 (zh) |
CA (1) | CA2602249C (zh) |
ES (1) | ES2365410T3 (zh) |
WO (1) | WO2006110551A2 (zh) |
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- 2006-04-06 CN CN200680019970XA patent/CN101193652B/zh not_active Expired - Fee Related
- 2006-04-06 AU AU2006235183A patent/AU2006235183B2/en not_active Ceased
- 2006-04-06 WO PCT/US2006/013073 patent/WO2006110551A2/en active Application Filing
- 2006-04-06 ES ES06740736T patent/ES2365410T3/es active Active
- 2006-04-06 EP EP06740736A patent/EP1909824B1/en not_active Revoked
- 2006-04-06 US US11/910,723 patent/US20080200383A1/en not_active Abandoned
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Also Published As
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CN101193652A (zh) | 2008-06-04 |
EP1909824B1 (en) | 2011-05-18 |
WO2006110551A3 (en) | 2007-05-18 |
US20150111824A1 (en) | 2015-04-23 |
EP1909824A2 (en) | 2008-04-16 |
AU2006235183B2 (en) | 2011-02-10 |
ES2365410T3 (es) | 2011-10-04 |
US20160120950A1 (en) | 2016-05-05 |
WO2006110551A2 (en) | 2006-10-19 |
ATE509634T1 (de) | 2011-06-15 |
CA2602249A1 (en) | 2006-10-19 |
US20080200383A1 (en) | 2008-08-21 |
CA2602249C (en) | 2012-07-10 |
AU2006235183A1 (en) | 2006-10-19 |
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