JP2008521932A5 - - Google Patents
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- Publication number
- JP2008521932A5 JP2008521932A5 JP2007544563A JP2007544563A JP2008521932A5 JP 2008521932 A5 JP2008521932 A5 JP 2008521932A5 JP 2007544563 A JP2007544563 A JP 2007544563A JP 2007544563 A JP2007544563 A JP 2007544563A JP 2008521932 A5 JP2008521932 A5 JP 2008521932A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- amount ranging
- weight
- lactose
- poloxamer
- 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
- 239000000203 mixture Substances 0.000 claims 18
- 229940126062 Compound A Drugs 0.000 claims 16
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 16
- 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 12
- 238000009472 formulation Methods 0.000 claims 12
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 12
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 12
- 239000008101 lactose Substances 0.000 claims 12
- 229910052751 metal Inorganic materials 0.000 claims 12
- 239000002184 metal Substances 0.000 claims 12
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 claims 12
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 11
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 9
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 9
- 239000000314 lubricant Substances 0.000 claims 9
- 239000003085 diluting agent Substances 0.000 claims 8
- 229920001983 poloxamer Polymers 0.000 claims 7
- 229960000502 poloxamer Drugs 0.000 claims 7
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 6
- MHQJUHSHQGQVTM-HNENSFHCSA-N Octadecyl fumarate Chemical compound CCCCCCCCCCCCCCCCCCOC(=O)\C=C/C(O)=O MHQJUHSHQGQVTM-HNENSFHCSA-N 0.000 claims 6
- 229910000389 calcium phosphate Inorganic materials 0.000 claims 6
- 239000001506 calcium phosphate Substances 0.000 claims 6
- 235000011010 calcium phosphates Nutrition 0.000 claims 6
- 239000003349 gelling agent Substances 0.000 claims 6
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 6
- 239000008108 microcrystalline cellulose Substances 0.000 claims 6
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 6
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 6
- 239000002904 solvent Substances 0.000 claims 6
- 229940071138 stearyl fumarate Drugs 0.000 claims 6
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 6
- 239000000945 filler Substances 0.000 claims 5
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 229920001992 poloxamer 407 Polymers 0.000 claims 4
- 229940044476 poloxamer 407 Drugs 0.000 claims 4
- 239000007891 compressed tablet Substances 0.000 claims 3
- 239000008187 granular material Substances 0.000 claims 3
- 239000002245 particle Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000007921 spray Substances 0.000 claims 3
- 239000003826 tablet Substances 0.000 claims 3
- 208000030507 AIDS Diseases 0.000 claims 2
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 208000037357 HIV infectious disease Diseases 0.000 claims 2
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical group [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims 2
- 235000019700 dicalcium phosphate Nutrition 0.000 claims 2
- 229940095079 dicalcium phosphate anhydrous Drugs 0.000 claims 2
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical group CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 2
- 235000019359 magnesium stearate Nutrition 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000002156 mixing Methods 0.000 claims 2
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 229920003084 Avicel® PH-102 Polymers 0.000 claims 1
- 108010002459 HIV Integrase Proteins 0.000 claims 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000011248 coating agent Substances 0.000 claims 1
- 238000000576 coating method Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000000227 grinding Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000005096 rolling process Methods 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 239000007909 solid dosage form Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63294404P | 2004-12-03 | 2004-12-03 | |
| US60/632,944 | 2004-12-03 | ||
| PCT/US2005/043727 WO2006060711A2 (en) | 2004-12-03 | 2005-12-02 | Pharmaceutical formulation of carboxamide hiv integrase inhibitors containing a release rate controlling composition |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008521932A JP2008521932A (ja) | 2008-06-26 |
| JP2008521932A5 true JP2008521932A5 (cg-RX-API-DMAC7.html) | 2009-01-15 |
| JP5228488B2 JP5228488B2 (ja) | 2013-07-03 |
Family
ID=36118082
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007544563A Expired - Fee Related JP5228488B2 (ja) | 2004-12-03 | 2005-12-02 | 放出速度調節組成物を含有しているカルボキサミドｈｉｖインテグラーゼ阻害薬の医薬配合物 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US8852632B2 (cg-RX-API-DMAC7.html) |
| EP (2) | EP2586444B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5228488B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR101351059B1 (cg-RX-API-DMAC7.html) |
| CN (1) | CN101068550B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2005311652B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BRPI0518781A2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2588445C (cg-RX-API-DMAC7.html) |
| ES (1) | ES2755273T3 (cg-RX-API-DMAC7.html) |
| IL (1) | IL183615A (cg-RX-API-DMAC7.html) |
| MX (1) | MX2007006635A (cg-RX-API-DMAC7.html) |
| NO (1) | NO20073405L (cg-RX-API-DMAC7.html) |
| NZ (1) | NZ555120A (cg-RX-API-DMAC7.html) |
| RU (1) | RU2382648C2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2006060711A2 (cg-RX-API-DMAC7.html) |
| ZA (1) | ZA200703866B (cg-RX-API-DMAC7.html) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101068533B (zh) * | 2004-12-03 | 2011-04-27 | 默沙东公司 | 含有抗成核剂的药物组合物 |
| UA87884C2 (uk) * | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| CA2588466A1 (en) * | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Use of atazanavir for improving the pharmacokinetics of drugs metabolized by ugt1a1 |
| WO2009009531A2 (en) * | 2007-07-09 | 2009-01-15 | Concert Pharmaceuticals Inc. | Pyrimidinecarboxamide derivatives for the treatment of hiv infections |
| JP6122639B2 (ja) * | 2009-10-26 | 2017-04-26 | メルク・シャープ・エンド・ドーム・コーポレイション | インテグラーゼ阻害剤を含有する固形医薬組成物 |
| US8987272B2 (en) * | 2010-04-01 | 2015-03-24 | Critical Outcome Technologies Inc. | Compounds and method for treatment of HIV |
| US9107922B2 (en) | 2010-07-16 | 2015-08-18 | Concert Pharmaceuticals, Inc. | Pyrimidinecarboxamide derivatives |
| US9968607B2 (en) | 2011-04-25 | 2018-05-15 | Hetero Research Foundation | Pharmaceutical compositions of raltegravir, methods of preparation and methods of use therof |
| ES2450944T3 (es) * | 2011-06-01 | 2014-03-25 | Ratiopharm Gmbh | Composición y comprimido que comprenden raltegravir |
| EP2827845B1 (en) | 2012-03-22 | 2018-12-26 | Novo Nordisk A/S | Compositions comprising a delivery agent and preparation thereof |
| WO2014030172A2 (en) * | 2012-08-23 | 2014-02-27 | Hetero Research Foundation | Pharmaceutical formulations of rufinamide |
| US9763934B2 (en) * | 2014-03-05 | 2017-09-19 | Professional Compounding Centers Of America | Synergistic effect of poloxamer-based composition and itraconazole on fungus and yeast |
| KR102293907B1 (ko) | 2015-06-30 | 2021-08-26 | 한미약품 주식회사 | 이리노테칸 함유 경구용 고형제제 및 그 제조방법 |
| CN108610338A (zh) * | 2016-12-12 | 2018-10-02 | 天津国际生物医药联合研究院 | 一种嘧啶酮酰胺类化合物的制备方法 |
| US20210290548A1 (en) * | 2018-06-06 | 2021-09-23 | Merck Sharp & Dohme Corp. | Formulations of raltegravir |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA56992C2 (uk) * | 1995-05-08 | 2003-06-16 | Фармація Енд Апджон Компані | <font face="Symbol">a</font>-ПІРИМІДИНТІОАЛКІЛЗАМІЩЕНІ ТА <font face="Symbol">a</font>-ПІРИМІДИНОКСОАЛКІЛЗАМІЩЕНІ СПОЛУКИ |
| IE970588A1 (en) * | 1997-08-01 | 2000-08-23 | Elan Corp Plc | Controlled release pharmaceutical compositions containing tiagabine |
| CN100400042C (zh) * | 1999-12-03 | 2008-07-09 | 聚合化学股份公司 | 制备生物利用度改善的麦角生物碱持续释放药物组合物的方法及其组合物 |
| PL366998A1 (en) * | 2001-05-03 | 2005-02-07 | F.Hoffmann-La Roche Ag | Pharmaceutical dosage form of amorphous nelfinavir mesylate |
| WO2003017981A1 (en) * | 2001-08-29 | 2003-03-06 | Ranbaxy Laboratories Limited | Controlled release formulation of clarithromycin or tinidazol |
| SE0102887D0 (sv) * | 2001-08-29 | 2001-08-29 | Astrazeneca Ab | New formulation |
| CN1700918B (zh) * | 2001-10-26 | 2011-06-08 | P·安杰莱蒂分子生物学研究所 | 关于hiv整合酶的n-取代的羟基嘧啶酮甲酰胺抑制剂 |
| CA2463975A1 (en) * | 2001-10-26 | 2003-05-01 | Maria Emilia Di Francesco | Dihydroxypyrimidine carboxamide inhibitors of hiv integrase |
| AU2003220186A1 (en) * | 2002-04-10 | 2003-10-27 | Merck And Co., Inc. | Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant |
| BR0317749A (pt) * | 2002-12-27 | 2005-11-22 | Angeletti P Ist Richerche Bio | Composto, composição farmacêutica, e, uso de um composto |
| DE602004031767D1 (de) | 2003-12-31 | 2011-04-21 | Bend Res Inc | Stabilisierte pharmazeutische feste zusammensetzungen von arzneimitteln mit geringer löslichkeit, poloxameren und stabilisierenden polymeren |
| UA87884C2 (uk) * | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| CA2588466A1 (en) | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Use of atazanavir for improving the pharmacokinetics of drugs metabolized by ugt1a1 |
| CN101068533B (zh) * | 2004-12-03 | 2011-04-27 | 默沙东公司 | 含有抗成核剂的药物组合物 |
-
2005
- 2005-12-02 NZ NZ555120A patent/NZ555120A/en not_active IP Right Cessation
- 2005-12-02 EP EP12198385.2A patent/EP2586444B1/en not_active Expired - Lifetime
- 2005-12-02 MX MX2007006635A patent/MX2007006635A/es active IP Right Grant
- 2005-12-02 BR BRPI0518781-8A patent/BRPI0518781A2/pt not_active IP Right Cessation
- 2005-12-02 ES ES12198385T patent/ES2755273T3/es not_active Expired - Lifetime
- 2005-12-02 JP JP2007544563A patent/JP5228488B2/ja not_active Expired - Fee Related
- 2005-12-02 CN CN2005800412301A patent/CN101068550B/zh not_active Expired - Fee Related
- 2005-12-02 KR KR1020077012535A patent/KR101351059B1/ko not_active Expired - Fee Related
- 2005-12-02 AU AU2005311652A patent/AU2005311652B2/en not_active Ceased
- 2005-12-02 CA CA2588445A patent/CA2588445C/en not_active Expired - Fee Related
- 2005-12-02 US US11/792,118 patent/US8852632B2/en active Active
- 2005-12-02 WO PCT/US2005/043727 patent/WO2006060711A2/en not_active Ceased
- 2005-12-02 RU RU2007125122/15A patent/RU2382648C2/ru not_active IP Right Cessation
- 2005-12-02 EP EP05852839.9A patent/EP1904067B2/en not_active Expired - Lifetime
-
2007
- 2007-05-14 ZA ZA2007/03866A patent/ZA200703866B/en unknown
- 2007-05-31 IL IL183615A patent/IL183615A/en not_active IP Right Cessation
- 2007-07-02 NO NO20073405A patent/NO20073405L/no not_active Application Discontinuation
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