CN1778301A - 布地奈德靶向微丸及其制备方法 - Google Patents
布地奈德靶向微丸及其制备方法 Download PDFInfo
- Publication number
- CN1778301A CN1778301A CN 200410072871 CN200410072871A CN1778301A CN 1778301 A CN1778301 A CN 1778301A CN 200410072871 CN200410072871 CN 200410072871 CN 200410072871 A CN200410072871 A CN 200410072871A CN 1778301 A CN1778301 A CN 1778301A
- Authority
- CN
- China
- Prior art keywords
- budesonide
- coating layer
- acrylate copolymer
- methyl acrylate
- coat layer
- 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
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 title claims abstract description 43
- 229960004436 budesonide Drugs 0.000 title claims abstract description 42
- 238000002360 preparation method Methods 0.000 title claims description 29
- 239000011806 microball Substances 0.000 title description 3
- 238000000576 coating method Methods 0.000 claims abstract description 41
- 239000011248 coating agent Substances 0.000 claims abstract description 28
- 239000000725 suspension Substances 0.000 claims description 54
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 31
- 238000005303 weighing Methods 0.000 claims description 30
- BAPJBEWLBFYGME-UHFFFAOYSA-N acrylic acid methyl ester Natural products COC(=O)C=C BAPJBEWLBFYGME-UHFFFAOYSA-N 0.000 claims description 28
- 239000011247 coating layer Substances 0.000 claims description 27
- 239000000463 material Substances 0.000 claims description 27
- 229920001577 copolymer Polymers 0.000 claims description 25
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 claims description 23
- 238000013019 agitation Methods 0.000 claims description 23
- 239000010410 layer Substances 0.000 claims description 22
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical group O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 20
- 239000006185 dispersion Substances 0.000 claims description 19
- 239000008188 pellet Substances 0.000 claims description 17
- 239000002904 solvent Substances 0.000 claims description 16
- 239000004014 plasticizer Substances 0.000 claims description 14
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical group CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims description 13
- 239000001069 triethyl citrate Substances 0.000 claims description 12
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims description 12
- 235000013769 triethyl citrate Nutrition 0.000 claims description 12
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Substances CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 5
- 238000001035 drying Methods 0.000 claims description 4
- 239000012530 fluid Substances 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 235000010603 pastilles Nutrition 0.000 claims description 4
- 229940093429 polyethylene glycol 6000 Drugs 0.000 claims description 4
- ONKUXPIBXRRIDU-UHFFFAOYSA-N Diethyl decanedioate Chemical compound CCOC(=O)CCCCCCCCC(=O)OCC ONKUXPIBXRRIDU-UHFFFAOYSA-N 0.000 claims description 3
- 239000007921 spray Substances 0.000 claims description 3
- 229930006000 Sucrose Natural products 0.000 claims description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 2
- MOVRNJGDXREIBM-UHFFFAOYSA-N aid-1 Chemical compound O=C1NC(=O)C(C)=CN1C1OC(COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=O)OC2C(OC(C2)N2C3=C(C(NC(N)=N3)=O)N=C2)CO)C(O)C1 MOVRNJGDXREIBM-UHFFFAOYSA-N 0.000 claims description 2
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 claims description 2
- 229960004793 sucrose Drugs 0.000 claims description 2
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 abstract description 8
- 229920000858 Cyclodextrin Polymers 0.000 abstract description 2
- 235000011175 beta-cyclodextrine Nutrition 0.000 abstract description 2
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical class OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
- 239000007788 liquid Substances 0.000 description 23
- 229920003134 Eudragit® polymer Polymers 0.000 description 21
- 210000001072 colon Anatomy 0.000 description 10
- 239000003814 drug Substances 0.000 description 10
- 239000007787 solid Substances 0.000 description 10
- 238000002156 mixing Methods 0.000 description 8
- 239000000047 product Substances 0.000 description 7
- 238000004519 manufacturing process Methods 0.000 description 6
- 229920000642 polymer Polymers 0.000 description 6
- 239000002202 Polyethylene glycol Substances 0.000 description 5
- 239000003960 organic solvent Substances 0.000 description 5
- 229920001223 polyethylene glycol Polymers 0.000 description 5
- 238000005516 engineering process Methods 0.000 description 4
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- 239000000470 constituent Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 229960003511 macrogol Drugs 0.000 description 3
- FELGMEQIXOGIFQ-CYBMUJFWSA-N (3r)-9-methyl-3-[(2-methylimidazol-1-yl)methyl]-2,3-dihydro-1h-carbazol-4-one Chemical compound CC1=NC=CN1C[C@@H]1C(=O)C(C=2C(=CC=CC=2)N2C)=C2CC1 FELGMEQIXOGIFQ-CYBMUJFWSA-N 0.000 description 2
- FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 description 2
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000001856 Ethyl cellulose Substances 0.000 description 2
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 238000003556 assay Methods 0.000 description 2
- 239000002702 enteric coating Substances 0.000 description 2
- 238000009505 enteric coating Methods 0.000 description 2
- 229920001249 ethyl cellulose Polymers 0.000 description 2
- 235000019325 ethyl cellulose Nutrition 0.000 description 2
- 239000000835 fiber Substances 0.000 description 2
- 229940050549 fiber Drugs 0.000 description 2
- 229960005343 ondansetron Drugs 0.000 description 2
- 239000013558 reference substance Substances 0.000 description 2
- 230000008685 targeting Effects 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 208000011231 Crohn disease Diseases 0.000 description 1
- 239000011805 ball Substances 0.000 description 1
- 230000002902 bimodal effect Effects 0.000 description 1
- 239000007795 chemical reaction product Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 206010009887 colitis Diseases 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- 238000004880 explosion Methods 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229920003145 methacrylic acid copolymer Polymers 0.000 description 1
- 238000005457 optimization Methods 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 230000003637 steroidlike Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000000185 sucrose group Chemical group 0.000 description 1
Images
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- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims (9)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNB2004100728710A CN100333727C (zh) | 2004-11-25 | 2004-11-25 | 布地奈德靶向微丸及其制备方法 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNB2004100728710A CN100333727C (zh) | 2004-11-25 | 2004-11-25 | 布地奈德靶向微丸及其制备方法 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN1778301A true CN1778301A (zh) | 2006-05-31 |
CN100333727C CN100333727C (zh) | 2007-08-29 |
Family
ID=36768839
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CNB2004100728710A Expired - Fee Related CN100333727C (zh) | 2004-11-25 | 2004-11-25 | 布地奈德靶向微丸及其制备方法 |
Country Status (1)
Country | Link |
---|---|
CN (1) | CN100333727C (zh) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101926805A (zh) * | 2009-06-24 | 2010-12-29 | 天津金耀集团有限公司 | 一种含有16,17异恶唑烷类甾体化合物的药物组合物 |
CN101744725B (zh) * | 2008-12-09 | 2013-04-17 | 北京华素制药股份有限公司 | 缓释微丸包衣生产工艺参数的优化方法 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE4332394A1 (de) * | 1993-09-23 | 1995-03-30 | Falk Pharma Gmbh | Budesonid-Pellets mit kontrolliertem Freigabeprofil und Verfahren zu ihrer Herstellung |
SE9700133D0 (sv) * | 1997-01-20 | 1997-01-20 | Astra Ab | New formulation |
JP2002502812A (ja) * | 1998-02-09 | 2002-01-29 | ジョエル・ボロニック | 胃腸管の慢性炎症疾患の治療 |
-
2004
- 2004-11-25 CN CNB2004100728710A patent/CN100333727C/zh not_active Expired - Fee Related
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN101744725B (zh) * | 2008-12-09 | 2013-04-17 | 北京华素制药股份有限公司 | 缓释微丸包衣生产工艺参数的优化方法 |
CN101926805A (zh) * | 2009-06-24 | 2010-12-29 | 天津金耀集团有限公司 | 一种含有16,17异恶唑烷类甾体化合物的药物组合物 |
Also Published As
Publication number | Publication date |
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CN100333727C (zh) | 2007-08-29 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
C06 | Publication | ||
PB01 | Publication | ||
C10 | Entry into substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
C14 | Grant of patent or utility model | ||
GR01 | Patent grant | ||
CP01 | Change in the name or title of a patent holder |
Address after: Cheng linzhuan Hedong District of Tianjin City Road 300161 No. 91 Patentee after: Tianjin Pharmaceutical Research Institute Co.,Ltd. Address before: Cheng linzhuan Hedong District of Tianjin City Road 300161 No. 91 Patentee before: TIANJIN PHARMACEUTICALS Group Corp. |
|
CP01 | Change in the name or title of a patent holder | ||
CP02 | Change in the address of a patent holder | ||
CP02 | Change in the address of a patent holder |
Address after: 300457 Tianjin Binhai New Area Tianjin Development Zone West District Xinye Jiujie north, Xinhuan West Road East Patentee after: Tianjin Pharmaceutical Research Institute Co.,Ltd. Address before: Cheng linzhuan Hedong District of Tianjin City Road 300161 No. 91 Patentee before: Tianjin Pharmaceutical Research Institute Co.,Ltd. |
|
CP02 | Change in the address of a patent holder | ||
CP02 | Change in the address of a patent holder |
Address after: 300457 North Xinye 9th Street and East Xinhuan West Road, West District, Binhai New Area, Tianjin Patentee after: Tianjin Pharmaceutical Research Institute Co.,Ltd. Address before: 300457 Tianjin Binhai New Area Tianjin Development Zone West District Xinye Jiujie north, Xinhuan West Road East Patentee before: Tianjin Pharmaceutical Research Institute Co.,Ltd. |
|
CF01 | Termination of patent right due to non-payment of annual fee | ||
CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20070829 Termination date: 20211125 |