CN102885774B - 普拉格雷组合物及其制备方法 - Google Patents
普拉格雷组合物及其制备方法 Download PDFInfo
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- CN102885774B CN102885774B CN201110200680.8A CN201110200680A CN102885774B CN 102885774 B CN102885774 B CN 102885774B CN 201110200680 A CN201110200680 A CN 201110200680A CN 102885774 B CN102885774 B CN 102885774B
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- prasugrel
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- 239000005465 B01AC22 - Prasugrel Substances 0.000 title claims abstract description 97
- 229960004197 prasugrel Drugs 0.000 title claims abstract description 97
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- 238000002360 preparation method Methods 0.000 title claims abstract description 31
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- 230000002421 anti-septic effect Effects 0.000 claims abstract description 9
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- 230000002378 acidificating effect Effects 0.000 claims abstract description 8
- 239000003086 colorant Substances 0.000 claims abstract description 7
- 239000000314 lubricant Substances 0.000 claims abstract description 6
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 54
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 36
- 239000002671 adjuvant Substances 0.000 claims description 25
- 239000003513 alkali Substances 0.000 claims description 25
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- 239000011230 binding agent Substances 0.000 claims description 16
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 16
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- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 9
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- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 6
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- -1 correctives Substances 0.000 claims description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 4
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 4
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- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims description 4
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- 229920001223 polyethylene glycol Polymers 0.000 claims description 4
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims description 4
- 229920001353 Dextrin Polymers 0.000 claims description 3
- 239000004375 Dextrin Substances 0.000 claims description 3
- 239000001329 FEMA 3811 Substances 0.000 claims description 3
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 3
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 3
- 235000003704 aspartic acid Nutrition 0.000 claims description 3
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims description 3
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- ITVGXXMINPYUHD-CUVHLRMHSA-N neohesperidin dihydrochalcone Chemical compound C1=C(O)C(OC)=CC=C1CCC(=O)C(C(=C1)O)=C(O)C=C1O[C@H]1[C@H](O[C@H]2[C@@H]([C@H](O)[C@@H](O)[C@H](C)O2)O)[C@@H](O)[C@H](O)[C@@H](CO)O1 ITVGXXMINPYUHD-CUVHLRMHSA-N 0.000 claims description 3
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- 238000012216 screening Methods 0.000 claims description 3
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- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims description 2
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 claims description 2
- CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 claims description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 2
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- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
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Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
普拉格雷游离碱 | 5g |
微晶纤维素 | 100g |
聚维酮 | 1g |
微粉硅胶 | 2g |
制成 | 1000粒 |
普拉格雷游离碱 | 5g |
乳糖 | 70g |
低取代羟丙基纤维素 | 15g |
枸橼酸 | 20g |
聚维酮 | 1g |
微粉硅胶 | 3g |
硬脂酸镁 | 1g |
制成 | 1000粒 |
普拉格雷游离碱 | 5g |
微晶纤维素 | 70g |
乳糖 | 20g |
聚维酮 | 1g |
硬脂酸镁 | 1g |
制成 | 1000片 |
普拉格雷游离碱 | 5g |
乳糖 | 70g |
地取代羟丙基纤维素 | 15g |
枸橼酸 | 20g |
聚维酮 | 1g |
微粉硅胶 | 3g |
硬脂酸镁 | 1g |
制成 | 1000片 |
普拉格雷游离碱 | 5g |
甘露醇 | 1500g |
阿斯巴坦 | 200g |
聚维酮 | 20g |
制成 | 1000袋 |
普拉格雷游离碱 | 5g |
甘露醇 | 850g |
马来酸 | 50g |
阿斯巴坦 | 95g |
聚维酮 | 30g |
孔雀香精 | 2g |
制成 | 1000袋 |
普拉格雷游离碱 | 10g |
甘露醇 | 700g |
枸橼酸 | 100g |
预交化淀粉 | 100g |
阿斯巴坦 | 90g |
孔雀香精 | 2g |
制成 | 1000袋 |
普拉格雷游离碱 | 15g |
蔗糖 | 350g |
淀粉 | 500g |
枸橼酸 | 50g |
阿斯巴坦 | 50g |
羧甲基纤维素 | 20g |
柠檬香精 | 2g |
制成 | 1000袋 |
普拉格雷游离碱 | 5g |
甘露醇 | 500g |
枸橼酸 | 200g |
微晶纤维素 | 150g |
羟丙甲基纤维素 | 10g |
阿斯巴坦 | 95g |
香蕉香精 | 2g |
制成 | 1000袋 |
普拉格雷游离碱 | 5g |
乳糖 | 400g |
酒石酸 | 200g |
微晶纤维素 | 400g |
阿斯巴坦 | 95g |
羟丙甲基纤维素(5cps) | 20g |
橘子香精 | 2g |
制成 | 1000袋 |
普拉格雷游离碱 | 5g |
糊精 | 285g |
微晶纤维素 | 400g |
门冬氨酸 | 300g |
新橙皮甙二氢查耳酮 | 10g |
羟丙甲基纤维素(5cps) | 20g |
制成 | 1000袋 |
普拉格雷游离碱 | 5g |
微晶纤维素 | 250g |
甘露醇 | 1000g |
阿斯巴坦 | 200g |
羟丙甲基纤维素 | 50 |
制成 | 1000袋 |
普拉格雷游离碱 | 5g |
枸橼酸 | 500g |
预交化淀粉 | 100g |
甘露醇 | 200g |
阿斯巴坦 | 100g |
孔雀香精 | 0.1g |
制成 | 1000粒 |
普拉格雷游离碱 | 5g |
枸橼酸 | 500g |
蔗糖 | 450g |
阿斯巴坦 | 50g |
羧甲基纤维素 | 30g |
柠檬香精 | 0.1g |
制成 | 1000粒 |
普拉格雷游离碱 | 5g |
枸橼酸 | 200g |
甘露醇 | 500g |
微晶纤维素 | 250g |
羟丙甲基纤维素 | 50g |
阿斯巴坦 | 100g |
香蕉香精 | 0.1g |
制成 | 1000粒 |
时间(min) | A(%) | B(%) |
0-2 | 40 | 60 |
2-13 | 40→90 | 60→10 |
13-25 | 90 | 10 |
1 | 2 | 3 | 4 | 5 | 6 | 平均 | |
按照实施例17制备的胶囊 | 47 | 51 | 48 | 55 | 49 | 52 | 50 |
按照实施例18制备的片剂 | 44 | 46 | 50 | 47 | 45 | 46 | 46 |
按照实施例19制备的颗粒剂 | 50 | 48 | 45 | 47 | 46 | 47 | 47 |
按照实施例20制备的干混悬 | 45 | 47 | 43 | 47 | 45 | 45 | 45 |
EFFIENT Tablets | 98 | 95 | 98 | 99 | 101 | 97 | 98 |
Claims (8)
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CN104688695B (zh) * | 2013-12-04 | 2017-11-10 | 长春海悦药业股份有限公司 | 一种含有伏立康唑的药物组合物 |
CN106310229A (zh) * | 2015-06-30 | 2017-01-11 | 深圳翰宇药业股份有限公司 | 一种马昔瑞林薄膜衣片及其制备方法 |
CN107961221B (zh) * | 2016-10-20 | 2020-06-05 | 长春海悦药业股份有限公司 | 一种含有盐酸普拉格雷的药物组合物及其制备方法 |
Citations (6)
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EP1005864A1 (en) * | 1998-11-30 | 2000-06-07 | Tecnimede-Sociedade Tecnico-Medicinal, S.A. | Antioxidant free stable pharmaceutical compositions containing thienopyridine derivatives |
US20080214599A1 (en) * | 2005-08-19 | 2008-09-04 | John Thomas Brandt | Use of Par-1/Par-4 Inhibitors for Treating or Preventing Vascular Diseases |
CN101472929A (zh) * | 2006-04-06 | 2009-07-01 | 第一三共株式会社 | 制备高纯度的普拉格雷或其酸加成盐的方法 |
CN101600430A (zh) * | 2006-12-07 | 2009-12-09 | 第一三共株式会社 | 含有甘露糖醇或乳糖的固体药物制剂 |
WO2010137613A1 (ja) * | 2009-05-28 | 2010-12-02 | 第一三共株式会社 | 貯蔵安定性が改善された固形製剤 |
EP2377520A1 (de) * | 2010-03-24 | 2011-10-19 | Ratiopharm GmbH | Pharmazeutische Zusammensetzung des Prasugrels |
-
2011
- 2011-07-18 CN CN201110200680.8A patent/CN102885774B/zh active Active
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1005864A1 (en) * | 1998-11-30 | 2000-06-07 | Tecnimede-Sociedade Tecnico-Medicinal, S.A. | Antioxidant free stable pharmaceutical compositions containing thienopyridine derivatives |
US20080214599A1 (en) * | 2005-08-19 | 2008-09-04 | John Thomas Brandt | Use of Par-1/Par-4 Inhibitors for Treating or Preventing Vascular Diseases |
CN101472929A (zh) * | 2006-04-06 | 2009-07-01 | 第一三共株式会社 | 制备高纯度的普拉格雷或其酸加成盐的方法 |
CN101600430A (zh) * | 2006-12-07 | 2009-12-09 | 第一三共株式会社 | 含有甘露糖醇或乳糖的固体药物制剂 |
WO2010137613A1 (ja) * | 2009-05-28 | 2010-12-02 | 第一三共株式会社 | 貯蔵安定性が改善された固形製剤 |
EP2377520A1 (de) * | 2010-03-24 | 2011-10-19 | Ratiopharm GmbH | Pharmazeutische Zusammensetzung des Prasugrels |
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