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 (https=) | 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 (https=) |
| EP (2) | EP1904067B2 (https=) |
| JP (1) | JP5228488B2 (https=) |
| KR (1) | KR101351059B1 (https=) |
| CN (1) | CN101068550B (https=) |
| AU (1) | AU2005311652B2 (https=) |
| BR (1) | BRPI0518781A2 (https=) |
| CA (1) | CA2588445C (https=) |
| ES (1) | ES2755273T3 (https=) |
| IL (1) | IL183615A (https=) |
| MX (1) | MX2007006635A (https=) |
| NO (1) | NO20073405L (https=) |
| NZ (1) | NZ555120A (https=) |
| RU (1) | RU2382648C2 (https=) |
| WO (1) | WO2006060711A2 (https=) |
| ZA (1) | ZA200703866B (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA87884C2 (uk) | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| EP1819323B2 (en) | 2004-12-03 | 2023-03-22 | Merck Sharp & Dohme Corp. | Pharmaceutical composition containing an anti-nucleating agent |
| BRPI0518741A2 (pt) * | 2004-12-03 | 2008-12-02 | Merck & Co Inc | uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero |
| US7687509B2 (en) | 2007-07-09 | 2010-03-30 | Concert Pharmaceuticals Inc. | Pyrimidinecarboxamide derivatives |
| US9649311B2 (en) * | 2009-10-26 | 2017-05-16 | Merck Sharp & Dohme Corp. | Solid pharmaceutical compositions containing an integrase inhibitor |
| EP2552915B1 (en) * | 2010-04-01 | 2017-07-19 | Critical Outcome Technologies Inc. | Compounds for the treatment of hiv |
| WO2012009446A1 (en) | 2010-07-16 | 2012-01-19 | Concert Pharmaceuticals Inc. | Novel 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 |
| ES2965469T3 (es) | 2012-03-22 | 2024-04-15 | Novo Nordisk As | Composiciones que comprenden un agente de suministro y preparación de estas |
| US20150224086A1 (en) * | 2012-08-23 | 2015-08-13 | 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 |
| EP3801532B1 (en) * | 2018-06-06 | 2025-11-05 | Merck Sharp & Dohme LLC | 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 |
| EP1512403A1 (en) * | 1999-12-03 | 2005-03-09 | Polichem S.A. | Methods for making sustained-release pharmaceutical compositions of ergot alkaloids having improved bioavailability and compositions thereof |
| CN1255185C (zh) * | 2001-05-03 | 2006-05-10 | 弗·哈夫曼-拉罗切有限公司 | 无定形甲磺酸奈非那韦的药物剂型 |
| SE0102887D0 (sv) * | 2001-08-29 | 2001-08-29 | Astrazeneca Ab | New formulation |
| WO2003017981A1 (en) * | 2001-08-29 | 2003-03-06 | Ranbaxy Laboratories Limited | Controlled release formulation of clarithromycin or tinidazol |
| ATE355064T1 (de) * | 2001-10-26 | 2006-03-15 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase |
| IL161337A0 (en) * | 2001-10-26 | 2004-09-27 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone 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 |
| NZ540729A (en) * | 2002-12-27 | 2008-03-28 | Angeletti P Ist Richerche Bio | Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds useful as HIV integrase inhibitors |
| ATE500819T1 (de) * | 2003-12-31 | 2011-03-15 | Bend Res Inc | Stabilisierte pharmazeutische feste zusammensetzungen von arzneimitteln mit geringer löslichkeit, poloxameren und stabilisierenden polymeren |
| BRPI0518741A2 (pt) | 2004-12-03 | 2008-12-02 | Merck & Co Inc | uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero |
| EP1819323B2 (en) * | 2004-12-03 | 2023-03-22 | Merck Sharp & Dohme Corp. | Pharmaceutical composition containing an anti-nucleating agent |
| UA87884C2 (uk) * | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
-
2005
- 2005-12-02 EP EP05852839.9A patent/EP1904067B2/en not_active Expired - Lifetime
- 2005-12-02 JP JP2007544563A patent/JP5228488B2/ja not_active Expired - Fee Related
- 2005-12-02 EP EP12198385.2A patent/EP2586444B1/en not_active Expired - Lifetime
- 2005-12-02 RU RU2007125122/15A patent/RU2382648C2/ru not_active IP Right Cessation
- 2005-12-02 WO PCT/US2005/043727 patent/WO2006060711A2/en not_active Ceased
- 2005-12-02 BR BRPI0518781-8A patent/BRPI0518781A2/pt not_active IP Right Cessation
- 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 NZ NZ555120A patent/NZ555120A/en not_active IP Right Cessation
- 2005-12-02 CA CA2588445A patent/CA2588445C/en not_active Expired - Fee Related
- 2005-12-02 ES ES12198385T patent/ES2755273T3/es not_active Expired - Lifetime
- 2005-12-02 AU AU2005311652A patent/AU2005311652B2/en not_active Ceased
- 2005-12-02 MX MX2007006635A patent/MX2007006635A/es active IP Right Grant
- 2005-12-02 US US11/792,118 patent/US8852632B2/en active Active
-
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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