CN101172966B - 一种阿立哌唑微晶的制备方法 - Google Patents
一种阿立哌唑微晶的制备方法 Download PDFInfo
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- CN101172966B CN101172966B CN200710078367A CN200710078367A CN101172966B CN 101172966 B CN101172966 B CN 101172966B CN 200710078367 A CN200710078367 A CN 200710078367A CN 200710078367 A CN200710078367 A CN 200710078367A CN 101172966 B CN101172966 B CN 101172966B
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- Prior art keywords
- aripiprazole
- ethanol
- drying
- temperature
- water
- 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.)
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- CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 title claims abstract description 50
- 229960004372 aripiprazole Drugs 0.000 title claims abstract description 50
- 238000004519 manufacturing process Methods 0.000 title 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 66
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 26
- 239000002904 solvent Substances 0.000 claims abstract description 15
- 238000002360 preparation method Methods 0.000 claims abstract description 13
- 239000000126 substance Substances 0.000 claims abstract description 5
- 238000001035 drying Methods 0.000 claims description 33
- 238000000034 method Methods 0.000 claims description 25
- 239000002245 particle Substances 0.000 claims description 25
- 230000001476 alcoholic effect Effects 0.000 claims description 9
- 239000012046 mixed solvent Substances 0.000 claims description 9
- 238000009775 high-speed stirring Methods 0.000 claims description 7
- 238000010438 heat treatment Methods 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 238000003756 stirring Methods 0.000 claims description 4
- 230000006837 decompression Effects 0.000 claims description 3
- 238000010992 reflux Methods 0.000 claims description 3
- 238000001816 cooling Methods 0.000 claims description 2
- 240000007594 Oryza sativa Species 0.000 claims 1
- 235000007164 Oryza sativa Nutrition 0.000 claims 1
- 235000009566 rice Nutrition 0.000 claims 1
- 239000013078 crystal Substances 0.000 abstract description 11
- 238000004090 dissolution Methods 0.000 abstract description 2
- 239000007787 solid Substances 0.000 abstract description 2
- 239000000047 product Substances 0.000 abstract 1
- 235000019441 ethanol Nutrition 0.000 description 18
- 238000002425 crystallisation Methods 0.000 description 15
- 230000008025 crystallization Effects 0.000 description 12
- 239000000843 powder Substances 0.000 description 7
- 238000001228 spectrum Methods 0.000 description 5
- 238000005516 engineering process Methods 0.000 description 4
- 238000000227 grinding Methods 0.000 description 4
- 238000001953 recrystallisation Methods 0.000 description 4
- 230000015572 biosynthetic process Effects 0.000 description 3
- 238000000967 suction filtration Methods 0.000 description 3
- 238000005406 washing Methods 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
- 230000003068 static effect Effects 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- BUWPZNOVIHAWHW-UHFFFAOYSA-N 2,3-dihydro-1h-quinolin-4-one Chemical compound C1=CC=C2C(=O)CCNC2=C1 BUWPZNOVIHAWHW-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- ZPEIMTDSQAKGNT-UHFFFAOYSA-N chlorpromazine Chemical compound C1=C(Cl)C=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZPEIMTDSQAKGNT-UHFFFAOYSA-N 0.000 description 1
- 229960001076 chlorpromazine Drugs 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000005457 ice water Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
Images
Abstract
Description
粒度(um) | 0.367 | 0.412 | 0.512 | 0.578 | 0.796 | 0.847 | 0.996 | 1.000 | 1.332 |
体积超出% | 100.00 | 99.99 | 99.79 | 99.29 | 98.69 | 98.39 | 98.04 | 97.96 | 97.49 |
粒度(um) | 1.556 | 1.989 | 2.345 | 2.750 | 2.795 | 3.832 | 3.986 | 4.763 | 5.000 |
体积超出% | 97.38 | 97.28 | 96.95 | 96.78 | 96.45 | 95.92 | 95.55 | 94.93 | 94.82 |
粒度(um) | 5.783 | 7.386 | 8.793 | 9.968 | 10.000 | 12.470 | 14.241 | 15.000 | 17.803 |
体积超出% | 94.12 | 93.14 | 91.83 | 88.96 | 88.75 | 82.99 | 78.24 | 75.96 | 67.74 |
粒度(um) | 20.000 | 21.976 | 25.956 | 31.760 | 35.967 | 40.000 | 47.140 | 50.000 | 55.175 |
体积超出% | 60.43 | 56.48 | 42.66 | 30.97 | 29.45 | 14.98 | 9.88 | 6.45 | 3.74 |
粒度(um) | 61.786 | 65.783 | 94.327 | ||||||
体积超出% | 2.48 | 0.94 | 0.00 |
粒度(um) | 0.313 | 0.379 | 0.459 | 0.556 | 0.673 | 0.815 | 0.987 | 1.000 | 1.195 |
体积超出% | 100.00 | 99.94 | 99.62 | 99.13 | 98.58 | 98.06 | 97.64 | 97.62 | 97.36 |
粒度(um) | 1.447 | 1.752 | 2.121 | 2.500 | 2.569 | 3.110 | 3.766 | 4.560 | 5.000 |
体积超出% | 97.18 | 97.02 | 96.77 | 96.46 | 96.40 | 95.90 | 95.29 | 94.62 | 94.26 |
粒度(um) | 5.522 | 6.686 | 8.096 | 9.803 | 10.000 | 11.870 | 14.373 | 15.000 | 17.403 |
体积超出% | 93.84 | 92.81 | 91.19 | 88.42 | 88.05 | 83.87 | 76.94 | 75.03 | 67.39 |
粒度(um) | 20.000 | 21.073 | 25.516 | 30.600 | 30.897 | 40.000 | 45.300 | 50.000 | 54.852 |
体积超出% | 58.96 | 55.54 | 42.37 | 29.95 | 29.32 | 14.51 | 9.22 | 5.96 | 3.65 |
粒度(um) | 63.000 | 66.417 | 97.380 | ||||||
体积超出% | 1.38 | 0.84 | 0.00 |
粒度(um) | 0.325 | 0.398 | 0.478 | 0.565 | 0.687 | 0.826 | 0.998 | 1.000 | 1.295 |
体积超出% | 100.00 | 99.95 | 99.78 | 99.21 | 98.63 | 98.32 | 97.92 | 97.81 | 97.45 |
粒度(um) | 1.457 | 1.867 | 2.321 | 2.640 | 2.769 | 3.410 | 3.966 | 4.661 | 5.000 |
体积超出% | 97.32 | 97.21 | 96.87 | 96.66 | 96.40 | 95.95 | 95.39 | 94.82 | 94.46 |
粒度(um) | 5.622 | 6.786 | 8.194 | 9.923 | 10.000 | 11.970 | 14.478 | 15.000 | 17.603 |
体积超出% | 93.89 | 92.89 | 91.25 | 88.46 | 88.25 | 83.93 | 77.99 | 75.43 | 67.47 |
粒度(um) | 20.000 | 21.273 | 25.716 | 30.800 | 35.997 | 40.000 | 45.450 | 50.000 | 54.965 |
体积超出% | 59.88 | 55.66 | 42.43 | 29.97 | 29.11 | 14.63 | 9.33 | 5.86 | 3.69 |
粒度(um) | 62.000 | 65.132 | 90.980 | ||||||
体积超出% | 1.48 | 0.89 | 0.00 |
Claims (8)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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CN200710078367A CN101172966B (zh) | 2007-04-06 | 2007-04-06 | 一种阿立哌唑微晶的制备方法 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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CN200710078367A CN101172966B (zh) | 2007-04-06 | 2007-04-06 | 一种阿立哌唑微晶的制备方法 |
Publications (2)
Publication Number | Publication Date |
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CN101172966A CN101172966A (zh) | 2008-05-07 |
CN101172966B true CN101172966B (zh) | 2012-08-29 |
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CN200710078367A Active CN101172966B (zh) | 2007-04-06 | 2007-04-06 | 一种阿立哌唑微晶的制备方法 |
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Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2012077134A1 (en) * | 2010-12-07 | 2012-06-14 | Ind-Swift Laboratories Limted | Process for preparing aripiprazole polymorphs |
CN102846616B (zh) * | 2011-06-27 | 2015-05-06 | 上海中西制药有限公司 | 一种阿立哌唑制剂及其制备方法 |
CN102850268B (zh) * | 2011-06-27 | 2015-07-15 | 上海中西制药有限公司 | 阿立哌唑ⅰ型微晶、阿立哌唑固体制剂及制备方法 |
GB2505860B (en) | 2011-06-27 | 2018-10-31 | Shanghai Zhongxi Pharmaceutical Corp | Aripiprazole medicament formulation and preparation method therefor |
CN104230799A (zh) * | 2013-06-21 | 2014-12-24 | 江苏豪森药业股份有限公司 | 制备阿立哌唑晶型的方法 |
CN104151237A (zh) * | 2014-08-08 | 2014-11-19 | 广东东阳光药业有限公司 | 一种小粒径喹诺酮衍生物的制备方法 |
EP3294724A4 (en) * | 2015-05-08 | 2018-11-21 | Davuluri, Ramamohan Rao | Improved process for the preparation of aripiprazole with reduced particle size |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1772738A (zh) * | 2005-06-07 | 2006-05-17 | 上海医药工业研究院 | 阿立哌唑晶型及其制备方法 |
CN1871007A (zh) * | 2003-10-23 | 2006-11-29 | 布里斯托尔-迈尔斯.斯奎布公司 | 制备具有所需平均粒度的无菌阿立哌唑的方法 |
WO2007035348A2 (en) * | 2005-09-15 | 2007-03-29 | Elan Pharma International, Limited | Nanoparticulate aripiprazole formulations |
-
2007
- 2007-04-06 CN CN200710078367A patent/CN101172966B/zh active Active
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1871007A (zh) * | 2003-10-23 | 2006-11-29 | 布里斯托尔-迈尔斯.斯奎布公司 | 制备具有所需平均粒度的无菌阿立哌唑的方法 |
CN1772738A (zh) * | 2005-06-07 | 2006-05-17 | 上海医药工业研究院 | 阿立哌唑晶型及其制备方法 |
WO2007035348A2 (en) * | 2005-09-15 | 2007-03-29 | Elan Pharma International, Limited | Nanoparticulate aripiprazole formulations |
Non-Patent Citations (3)
Title |
---|
Goldberg,Israel.Crystal Structures of Aripiprazole, a New Anti-psychotic Drug, and of Its Inclusion Compounds with Methanol, Ethanol and Water.《Journal of Inclusion Phenomena and Macrocyclic Chemistry》.2006,第55卷(第3-4期),第255页-261页. |
Tessler,Limor |
Tessler,Limor;Goldberg,Israel.Crystal Structures of Aripiprazole, a New Anti-psychotic Drug, and of Its Inclusion Compounds with Methanol, Ethanol and Water.《Journal of Inclusion Phenomena and Macrocyclic Chemistry》.2006,第55卷(第3-4期),第255页-261页. * |
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CN101172966A (zh) | 2008-05-07 |
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Effective date of registration: 20181221 Address after: 400061 Tu Shan Road, South Bank district, Chongqing, No. 565 Co-patentee after: Chongqing Medical Institute Pharmaceutical Co., Ltd. Patentee after: Chongqing Pharmaceutical Research Institute Co., Ltd. Address before: 400061 Tu Shan Road, South Bank district, Chongqing, No. 565 Patentee before: Chongqing Pharmaceutical Research Institute Co., Ltd. |
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Effective date of registration: 20181226 Address after: 401221 No. 2 Yanjiahua South Third Branch Road, Changshou District, Chongqing Co-patentee after: Chongqing Pharmaceutical Research Institute Co., Ltd. Patentee after: Chongqing Medical Institute Pharmaceutical Co., Ltd. Address before: 400061 Tu Shan Road, South Bank district, Chongqing, No. 565 Patentee before: Chongqing Pharmaceutical Research Institute Co., Ltd. |
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Effective date of registration: 20200417 Address after: 401221 No.3, Huanan 1st branch road, Changshou chemical industry park, Chongqing Co-patentee after: CHONGQING PHARMACEUTICAL RESEARCH INSTITUTE Co.,Ltd. Patentee after: CHONGQING CARELIFE PHARMACEUTICAL Co.,Ltd. Address before: 401221 No. 2 Yanjiahua South Third Branch Road, Changshou District, Chongqing Co-patentee before: CHONGQING PHARMACEUTICAL RESEARCH INSTITUTE Co.,Ltd. Patentee before: Chongqing Medical Institute Pharmaceutical Co., Ltd. |
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