CN101862326A - Medicine compound containing febuxostat - Google Patents
Medicine compound containing febuxostat Download PDFInfo
- Publication number
- CN101862326A CN101862326A CN200910082252A CN200910082252A CN101862326A CN 101862326 A CN101862326 A CN 101862326A CN 200910082252 A CN200910082252 A CN 200910082252A CN 200910082252 A CN200910082252 A CN 200910082252A CN 101862326 A CN101862326 A CN 101862326A
- Authority
- CN
- China
- Prior art keywords
- febuxostat
- pharmaceutical composition
- preparation
- binding agent
- surfactant
- 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
- BQSJTQLCZDPROO-UHFFFAOYSA-N febuxostat Chemical compound C1=C(C#N)C(OCC(C)C)=CC=C1C1=NC(C)=C(C(O)=O)S1 BQSJTQLCZDPROO-UHFFFAOYSA-N 0.000 title claims abstract description 31
- 229960005101 febuxostat Drugs 0.000 title claims abstract description 30
- 239000003814 drug Substances 0.000 title abstract description 10
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 229940079593 drug Drugs 0.000 title description 4
- 239000004094 surface-active agent Substances 0.000 claims abstract description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 239000011230 binding agent Substances 0.000 claims description 13
- 239000013078 crystal Substances 0.000 claims description 6
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 5
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 5
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 claims description 3
- HSRJKNPTNIJEKV-UHFFFAOYSA-N Guaifenesin Chemical compound COC1=CC=CC=C1OCC(O)CO HSRJKNPTNIJEKV-UHFFFAOYSA-N 0.000 claims description 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 3
- 239000004359 castor oil Substances 0.000 claims description 3
- 235000019438 castor oil Nutrition 0.000 claims description 3
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 3
- 239000002245 particle Substances 0.000 claims description 3
- -1 polyoxyethylene Polymers 0.000 claims description 3
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 3
- 229920000053 polysorbate 80 Polymers 0.000 claims description 3
- 239000004141 Sodium laurylsulphate Substances 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 229940063451 febuxostat 80 mg Drugs 0.000 claims description 2
- 239000000945 filler Substances 0.000 claims description 2
- 239000000314 lubricant Substances 0.000 claims description 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 2
- 239000008187 granular material Substances 0.000 description 24
- 238000002360 preparation method Methods 0.000 description 19
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 14
- 239000000203 mixture Substances 0.000 description 9
- 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 description 7
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 7
- 239000011248 coating agent Substances 0.000 description 7
- 238000000576 coating method Methods 0.000 description 7
- 239000006185 dispersion Substances 0.000 description 7
- 239000008101 lactose Substances 0.000 description 7
- 235000019359 magnesium stearate Nutrition 0.000 description 7
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 7
- 239000008108 microcrystalline cellulose Substances 0.000 description 7
- 229940016286 microcrystalline cellulose Drugs 0.000 description 7
- 238000012856 packing Methods 0.000 description 7
- 238000003756 stirring Methods 0.000 description 7
- 229920002472 Starch Polymers 0.000 description 6
- LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 description 6
- 239000008107 starch Substances 0.000 description 6
- 235000019698 starch Nutrition 0.000 description 6
- 201000005569 Gout Diseases 0.000 description 5
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 5
- 238000004090 dissolution Methods 0.000 description 5
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 5
- 229950005770 hyprolose Drugs 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 239000000080 wetting agent Substances 0.000 description 5
- TVWHNULVHGKJHS-UHFFFAOYSA-N Uric acid Natural products N1C(=O)NC(=O)C2NC(=O)NC21 TVWHNULVHGKJHS-UHFFFAOYSA-N 0.000 description 4
- 230000000052 comparative effect Effects 0.000 description 4
- 229960001375 lactose Drugs 0.000 description 4
- 239000002002 slurry Substances 0.000 description 4
- 229940116269 uric acid Drugs 0.000 description 4
- 229920002785 Croscarmellose sodium Polymers 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 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 description 2
- 229960003459 allopurinol Drugs 0.000 description 2
- OFCNXPDARWKPPY-UHFFFAOYSA-N allopurinol Chemical compound OC1=NC=NC2=C1C=NN2 OFCNXPDARWKPPY-UHFFFAOYSA-N 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 238000005453 pelletization Methods 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 201000001431 Hyperuricemia Diseases 0.000 description 1
- NIPNSKYNPDTRPC-UHFFFAOYSA-N N-[2-oxo-2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridin-5-yl)ethyl]-2-[[3-(trifluoromethoxy)phenyl]methylamino]pyrimidine-5-carboxamide Chemical compound O=C(CNC(=O)C=1C=NC(=NC=1)NCC1=CC(=CC=C1)OC(F)(F)F)N1CC2=C(CC1)NN=N2 NIPNSKYNPDTRPC-UHFFFAOYSA-N 0.000 description 1
- 229920003081 Povidone K 30 Polymers 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000000378 dietary effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229940125532 enzyme inhibitor Drugs 0.000 description 1
- 239000002532 enzyme inhibitor Substances 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 description 1
- 239000010931 gold Substances 0.000 description 1
- 229910052737 gold Inorganic materials 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 150000003212 purines Chemical class 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 230000006641 stabilisation Effects 0.000 description 1
- 238000011105 stabilization Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 210000001835 viscera Anatomy 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
Dissolution % | 0 day | Quicken January | Quicken February | Quicken March | Quicken June |
Embodiment 1 | ??96.23±1.04 | ??97.96±2.00 | ??98.08±1.35 | ??99.25±1.43 | ??99.07±1.96 |
Embodiment 2 | ??98.93±1.10 | ??98.51±1.27 | ??98.93±1.70 | ??99.54±1.29 | ??98.53±1.07 |
Embodiment 3 | ??97.85±1.38 | ??100.3±1.47 | ??98.27±1.66 | ??98.35±1.89 | ??98.12±1.23 |
Embodiment 4 | ??99.02±1.57 | ??98.44±2.08 | ??100.0±1.09 | ??98.69±1.76 | ??97.99±1.64 |
The comparative example 1 | ??78.36±3.06 | ??76.48±5.32 | ??71.65±5.35 | ??68.56±4.14 | ??64.34±5.06 |
The comparative example 2 | ??73.89±2.88 | ??72.36±3.93 | ??70.84±6.36 | ??63.30±6.26 | ??55.89±4.88 |
The comparative example 3 | ??65.56±3.62 | ??63.15±4.29 | ??60.97±4.42 | ??54.56±4.61 | ??52.56±5.62 |
Claims (7)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2009100822522A CN101862326B (en) | 2009-04-20 | 2009-04-20 | Medicine compound containing febuxostat |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2009100822522A CN101862326B (en) | 2009-04-20 | 2009-04-20 | Medicine compound containing febuxostat |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101862326A true CN101862326A (en) | 2010-10-20 |
CN101862326B CN101862326B (en) | 2013-12-04 |
Family
ID=42954387
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2009100822522A Active CN101862326B (en) | 2009-04-20 | 2009-04-20 | Medicine compound containing febuxostat |
Country Status (1)
Country | Link |
---|---|
CN (1) | CN101862326B (en) |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102488665A (en) * | 2011-12-15 | 2012-06-13 | 宁夏康亚药业有限公司 | Febuxostat tablet and preparation method thereof |
CN102614145A (en) * | 2012-04-28 | 2012-08-01 | 杭州朱养心药业有限公司 | Stable febuxostat tablet and preparation method thereof |
CN102614146A (en) * | 2012-04-28 | 2012-08-01 | 杭州朱养心药业有限公司 | Method for preparing febuxostat tablet and febuxostat tablet |
CN102895210A (en) * | 2011-12-15 | 2013-01-30 | 宁夏康亚药业有限公司 | Febuxostat tablet with improved dissolution rate |
CN102895209A (en) * | 2011-12-15 | 2013-01-30 | 宁夏康亚药业有限公司 | Febuxostat tablet |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1954814A (en) * | 2005-10-26 | 2007-05-02 | 重庆医药工业研究院有限责任公司 | Medical composite with co-action for treating gout and its preparation method |
CN1970547B (en) * | 2006-12-07 | 2011-04-06 | 重庆医药工业研究院有限责任公司 | Novel febuxostat crystal form and its preparation method |
CN101780073B (en) * | 2009-01-21 | 2013-07-03 | 重庆圣华曦药业股份有限公司 | Febuxostat dispersible tablet drug and preparing method thereof |
-
2009
- 2009-04-20 CN CN2009100822522A patent/CN101862326B/en active Active
Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102488665A (en) * | 2011-12-15 | 2012-06-13 | 宁夏康亚药业有限公司 | Febuxostat tablet and preparation method thereof |
CN102895210A (en) * | 2011-12-15 | 2013-01-30 | 宁夏康亚药业有限公司 | Febuxostat tablet with improved dissolution rate |
CN102895209A (en) * | 2011-12-15 | 2013-01-30 | 宁夏康亚药业有限公司 | Febuxostat tablet |
CN102895209B (en) * | 2011-12-15 | 2013-12-25 | 宁夏康亚药业有限公司 | Febuxostat tablet |
CN102895210B (en) * | 2011-12-15 | 2014-08-06 | 宁夏康亚药业有限公司 | Febuxostat tablet with improved dissolution rate |
CN102614145A (en) * | 2012-04-28 | 2012-08-01 | 杭州朱养心药业有限公司 | Stable febuxostat tablet and preparation method thereof |
CN102614146A (en) * | 2012-04-28 | 2012-08-01 | 杭州朱养心药业有限公司 | Method for preparing febuxostat tablet and febuxostat tablet |
CN102614145B (en) * | 2012-04-28 | 2013-05-01 | 杭州朱养心药业有限公司 | Stable febuxostat tablet and preparation method thereof |
Also Published As
Publication number | Publication date |
---|---|
CN101862326B (en) | 2013-12-04 |
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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 | ||
TR01 | Transfer of patent right | ||
TR01 | Transfer of patent right |
Effective date of registration: 20210119 Address after: 570314 no.279 Nanhai Avenue, Xiuying District, Haikou City, Hainan Province Patentee after: AVENTIS PHARMA (HAINAN) Co.,Ltd. Address before: 100097, Wanquan mansion, 3 Jin Zhuang, Haidian District, Beijing, Sijiqing Patentee before: BEIJING D-VENTUREPHARM TECHNOLOGY DEVELOPMENT Co.,Ltd. |
|
DD01 | Delivery of document by public notice | ||
DD01 | Delivery of document by public notice |
Addressee: Song Xuemei Document name: Notice of conformity |
|
PE01 | Entry into force of the registration of the contract for pledge of patent right |
Denomination of invention: A drug combination containing febuxostat Granted publication date: 20131204 Pledgee: Sanya Rural Commercial Bank Co.,Ltd. Pledgor: AVENTIS PHARMA (HAINAN) Co.,Ltd. Registration number: Y2024980014810 |