CN101822674A - 一种伊潘立酮药物组合物及其制备方法 - Google Patents
一种伊潘立酮药物组合物及其制备方法 Download PDFInfo
- Publication number
- CN101822674A CN101822674A CN201010184547A CN201010184547A CN101822674A CN 101822674 A CN101822674 A CN 101822674A CN 201010184547 A CN201010184547 A CN 201010184547A CN 201010184547 A CN201010184547 A CN 201010184547A CN 101822674 A CN101822674 A CN 101822674A
- Authority
- CN
- China
- Prior art keywords
- iloperidone
- particle diameter
- diluent
- mixture
- lactose
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 229960003162 iloperidone Drugs 0.000 title claims abstract description 58
- XMXHEBAFVSFQEX-UHFFFAOYSA-N iloperidone Chemical compound COC1=CC(C(C)=O)=CC=C1OCCCN1CCC(C=2C3=CC=C(F)C=C3ON=2)CC1 XMXHEBAFVSFQEX-UHFFFAOYSA-N 0.000 title claims abstract description 57
- 239000000203 mixture Substances 0.000 title claims abstract description 47
- 238000002360 preparation method Methods 0.000 title claims description 16
- 229940079593 drug Drugs 0.000 title abstract description 3
- 239000003814 drug Substances 0.000 title abstract description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 26
- 239000002245 particle Substances 0.000 claims description 19
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 18
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 18
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 18
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 18
- 239000008101 lactose Substances 0.000 claims description 17
- 238000010298 pulverizing process Methods 0.000 claims description 15
- 238000005516 engineering process Methods 0.000 claims description 13
- 238000005303 weighing Methods 0.000 claims description 12
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 11
- 229930195725 Mannitol Natural products 0.000 claims description 11
- 239000003085 diluting agent Substances 0.000 claims description 11
- -1 hydroxypropyl Chemical group 0.000 claims description 11
- 239000000594 mannitol Substances 0.000 claims description 11
- 235000010355 mannitol Nutrition 0.000 claims description 11
- 239000008187 granular material Substances 0.000 claims description 10
- 229920002472 Starch Polymers 0.000 claims description 7
- 239000002671 adjuvant Substances 0.000 claims description 7
- 239000008107 starch Substances 0.000 claims description 7
- 235000019698 starch Nutrition 0.000 claims description 7
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 239000000314 lubricant Substances 0.000 claims description 6
- 239000004094 surface-active agent Substances 0.000 claims description 6
- 239000002775 capsule Substances 0.000 claims description 3
- 238000002203 pretreatment Methods 0.000 claims description 2
- 239000004480 active ingredient Substances 0.000 abstract description 2
- 230000000694 effects Effects 0.000 abstract description 2
- 238000004090 dissolution Methods 0.000 abstract 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 34
- 235000019359 magnesium stearate Nutrition 0.000 description 17
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 10
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 9
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 9
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 9
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 9
- 239000000741 silica gel Substances 0.000 description 9
- 229910002027 silica gel Inorganic materials 0.000 description 9
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 8
- 238000000034 method Methods 0.000 description 8
- 239000008194 pharmaceutical composition Substances 0.000 description 5
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 4
- 239000002002 slurry Substances 0.000 description 4
- 239000011734 sodium Substances 0.000 description 4
- 229910052708 sodium Inorganic materials 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 239000007864 aqueous solution Substances 0.000 description 3
- 239000011230 binding agent Substances 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 239000004141 Sodium laurylsulphate Substances 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- FDPIMTJIUBPUKL-UHFFFAOYSA-N pentan-3-one Chemical compound CCC(=O)CC FDPIMTJIUBPUKL-UHFFFAOYSA-N 0.000 description 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 2
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 description 1
- 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 description 1
- 101150049660 DRD2 gene Proteins 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 238000007922 dissolution test Methods 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000012805 post-processing Methods 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
Abstract
Description
组分 | 百分比(%) |
伊潘立酮 | 10.0 |
组分 | 百分比(%) |
乳糖 | 63.0 |
微晶纤维素 | 15.0 |
羟丙基甲基纤维素 | 3.00 |
交联聚维酮 | 7.50 |
微粉硅胶 | 0.50 |
硬脂酸镁 | 1.00 |
Total | 100.0 |
组分 | 百分比(%) |
伊潘立酮 | 10.0 |
乳糖 | 63.0 |
微晶纤维素 | 15.0 |
羟丙基甲基纤维素 | 3.00 |
交联聚维酮 | 7.50 |
微粉硅胶 | 0.50 |
硬脂酸镁 | 1.00 |
Total | 100.0 |
组分 | 百分比(%) |
伊潘立酮 | 10.0 |
乳糖 | 63.0 |
微晶纤维素 | 15.0 |
羟丙基甲基纤维素 | 3.00 |
交联聚维酮 | 7.50 |
微粉硅胶 | 0.50 |
硬脂酸镁 | 1.00 |
Total | 100.0 |
组分 | 百分比(%) |
伊潘立酮 | 2.00 |
乳糖 | 75.0 |
微晶纤维素 | 12.0 |
低取代羟丙纤维素(内加) | 5.00 |
低取代羟丙纤维素(外加) | 5.00 |
硬脂酸镁 | 1.00 |
Total | 100.0 |
组分 | 百分比(%) |
伊潘立酮 | 7.50 |
甘露醇 | 25.0 |
乳糖 | 45.0 |
微晶纤维素 | 10.0 |
十二烷基磺酸钠 | 1.0 |
羧甲淀粉钠 | 10.0 |
硬脂酸镁 | 1.50 |
Total | 100.0 |
组分 | 百分比(%) |
伊潘立酮 | 5.00 |
甘露醇 | 70.0 |
微晶纤维素 | 13.0 |
十二烷基磺酸钠 | 1.0 |
低取代羟丙纤维素 | 10.0 |
硬脂酸镁 | 1.00 |
Total | 100.0 |
组分 | 百分比(%) |
伊潘立酮 | 10.0 |
乳糖 | 69.0 |
微晶纤维素 | 12.0 |
低取代羟丙纤维素 | 8.00 |
硬脂酸镁 | 1.00 |
Total | 100.0 |
Claims (10)
Priority Applications (1)
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CN201010184547.3A CN101822674B (zh) | 2010-05-27 | 2010-05-27 | 一种伊潘立酮药物组合物及其制备方法 |
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CN201010184547.3A CN101822674B (zh) | 2010-05-27 | 2010-05-27 | 一种伊潘立酮药物组合物及其制备方法 |
Publications (2)
Publication Number | Publication Date |
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CN101822674A true CN101822674A (zh) | 2010-09-08 |
CN101822674B CN101822674B (zh) | 2015-03-11 |
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Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102274162A (zh) * | 2011-08-02 | 2011-12-14 | 无锡万全医药技术有限公司 | 一种含有难溶性药物和亲水凝胶材料的固体组合物及其制备方法 |
CN102440971A (zh) * | 2010-10-15 | 2012-05-09 | 重庆市力扬医药开发有限公司 | 伊潘立酮口腔崩解片 |
CN102462679A (zh) * | 2010-11-15 | 2012-05-23 | 浙江九洲药物科技有限公司 | 一种伊潘立酮药物口服制剂及其制备方法 |
CN102670532A (zh) * | 2012-05-21 | 2012-09-19 | 上海医药工业研究院 | 伊潘立酮药物组合物及其制备方法 |
CN104013589A (zh) * | 2014-05-07 | 2014-09-03 | 万特制药(海南)有限公司 | 一种阿西替尼口腔崩解片及其制备方法 |
CN104069500A (zh) * | 2014-06-20 | 2014-10-01 | 湖南天地恒一制药有限公司 | 一种包含乐卡地平的药物组合物 |
CN104324008A (zh) * | 2014-09-18 | 2015-02-04 | 山东省药学科学院 | 一种工业化制备微粉化伊潘立酮的方法 |
CN104546770A (zh) * | 2015-01-07 | 2015-04-29 | 万特制药(海南)有限公司 | 一种阿齐沙坦的口腔崩解片及其制备方法 |
CN105796516A (zh) * | 2016-03-21 | 2016-07-27 | 山东省药学科学院 | 一种伊潘立酮片剂的制备方法 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004006886A2 (en) * | 2002-07-15 | 2004-01-22 | Novartis Ag | Injectable depot formulation comprising crystals of iloperidone |
CN101822673A (zh) * | 2009-03-04 | 2010-09-08 | 北京德众万全药物技术开发有限公司 | 一种含有伊潘立酮的固体药物组合物 |
CN102078320A (zh) * | 2009-12-01 | 2011-06-01 | 严洁 | 伊潘立酮药物组合物及其制备方法 |
-
2010
- 2010-05-27 CN CN201010184547.3A patent/CN101822674B/zh active Active
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004006886A2 (en) * | 2002-07-15 | 2004-01-22 | Novartis Ag | Injectable depot formulation comprising crystals of iloperidone |
CN101822673A (zh) * | 2009-03-04 | 2010-09-08 | 北京德众万全药物技术开发有限公司 | 一种含有伊潘立酮的固体药物组合物 |
CN102078320A (zh) * | 2009-12-01 | 2011-06-01 | 严洁 | 伊潘立酮药物组合物及其制备方法 |
Non-Patent Citations (2)
Title |
---|
AMY BARBARA MONTES ET AL: "Iloperidone (Fanapt): An FDA-Approved Treatment Option for Schizophrenia", 《P&T》, vol. 34, no. 11, 30 November 2009 (2009-11-30), pages 606 - 613 * |
雷同康: "分散片的处方和工艺", 《中国医药工业杂志》, vol. 30, no. 2, 31 December 1999 (1999-12-31), pages 87 - 90 * |
Cited By (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102440971A (zh) * | 2010-10-15 | 2012-05-09 | 重庆市力扬医药开发有限公司 | 伊潘立酮口腔崩解片 |
CN102462679A (zh) * | 2010-11-15 | 2012-05-23 | 浙江九洲药物科技有限公司 | 一种伊潘立酮药物口服制剂及其制备方法 |
CN102274162A (zh) * | 2011-08-02 | 2011-12-14 | 无锡万全医药技术有限公司 | 一种含有难溶性药物和亲水凝胶材料的固体组合物及其制备方法 |
CN102670532A (zh) * | 2012-05-21 | 2012-09-19 | 上海医药工业研究院 | 伊潘立酮药物组合物及其制备方法 |
CN102670532B (zh) * | 2012-05-21 | 2015-01-21 | 上海医药工业研究院 | 伊潘立酮药物组合物及其制备方法 |
CN104013589A (zh) * | 2014-05-07 | 2014-09-03 | 万特制药(海南)有限公司 | 一种阿西替尼口腔崩解片及其制备方法 |
CN104069500A (zh) * | 2014-06-20 | 2014-10-01 | 湖南天地恒一制药有限公司 | 一种包含乐卡地平的药物组合物 |
CN104324008A (zh) * | 2014-09-18 | 2015-02-04 | 山东省药学科学院 | 一种工业化制备微粉化伊潘立酮的方法 |
CN104546770A (zh) * | 2015-01-07 | 2015-04-29 | 万特制药(海南)有限公司 | 一种阿齐沙坦的口腔崩解片及其制备方法 |
CN105796516A (zh) * | 2016-03-21 | 2016-07-27 | 山东省药学科学院 | 一种伊潘立酮片剂的制备方法 |
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CN101822674B (zh) | 2015-03-11 |
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Denomination of invention: A drug combination of ipyridone and its preparation method Granted publication date: 20150311 Pledgee: Sanya Rural Commercial Bank Co.,Ltd. Pledgor: AVENTIS PHARMA (HAINAN) Co.,Ltd. Registration number: Y2024980014810 |