ES2574836T3 - Formulación de liberación prolongada de nevirapina - Google Patents
Formulación de liberación prolongada de nevirapina Download PDFInfo
- Publication number
- ES2574836T3 ES2574836T3 ES08756672.5T ES08756672T ES2574836T3 ES 2574836 T3 ES2574836 T3 ES 2574836T3 ES 08756672 T ES08756672 T ES 08756672T ES 2574836 T3 ES2574836 T3 ES 2574836T3
- Authority
- ES
- Spain
- Prior art keywords
- nevirapine
- release formulation
- prolonged release
- hpmc
- tablets
- 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.)
- Active
Links
- NQDJXKOVJZTUJA-UHFFFAOYSA-N nevirapine Chemical compound C12=NC=CC=C2C(=O)NC=2C(C)=CC=NC=2N1C1CC1 NQDJXKOVJZTUJA-UHFFFAOYSA-N 0.000 title abstract description 33
- 229960000689 nevirapine Drugs 0.000 title abstract description 16
- 239000000203 mixture Substances 0.000 title description 6
- 238000009472 formulation Methods 0.000 title description 5
- 230000002035 prolonged effect Effects 0.000 title description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 abstract description 4
- 235000019359 magnesium stearate Nutrition 0.000 abstract description 2
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 abstract 1
- 229920003130 hypromellose 2208 Polymers 0.000 abstract 1
- 229940031707 hypromellose 2208 Drugs 0.000 abstract 1
- 229960001021 lactose monohydrate Drugs 0.000 abstract 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 10
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 10
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 6
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 229940098802 viramune Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un comprimido farmacéutico, en donde cada uno de los comprimidos comprende: (a) 400 mg de nevirapina anhidra; (b) 270 mg de Hipromelosa 2208; (c) 400 mg de lactosa monohidrato; y (d) 10 mg de estearato de magnesio; en donde cada uno de los comprimido se comprime mediante una fuerza de 10-25 kN.
Description
(estearato de magnesio) y se mezcla para preparar la mezcla final para su compresión en comprimidos. Los comprimidos se comprimen mediante una fuerza de aproximadamente 10-25 kN para formar comprimidos de 9,3 x 19,0 mm.
Los parámetros farmacocinéticos de las formulaciones antes descritas se confirmaron en una población de personas sanas de N = 17 tras una administración de dosis única. Un resumen de los resultados aparece en la Tabla 1, que figura más abajo.
Tabla 1 -Resumen de parámetros farmacocinéticos de dosis única [media geométrica (% de CV geométrica)] para Formulaciones de Nevirapina en personas normales (N = 17)
- Formulación
- AUC0-∞ (ng·h/mL) Cmáx (ng/mL) tmáx (h)
- 400 mg de Nevirapina, HPMC al 20% E
- 182,000 (31%) 1,990 (28%) 30,4 (31%)
- 400 mg de Nevirapina, HPMC al 20% K
- 149,000 (32%) 1,990 (27%) 23,5 (18%)
- 400 mg de Nevirapina, HPMC al 25% K
- 155,000 (30%) 1,970 (32%) 22,7 (44%)
- 400 mg de Nevirapina, HPMC al 30% K
- 166,000 (28%) 2,110 (24,3%) 27,5 (44%)
- 400 mg de Nevirapina, HPMC al 40% K
- 145,000 (47%) 1,610 (43%) 25,7 (43%)
- 300 mg de Nevirapina, HPMC al 20% E
- 118,000 (31%) 1,660 (26%) 24,6 (18%)
- 300 mg de Nevirapina, HPMC al 20% K
- 137,000 (51%) 1,660 (42%) 23,9 (27%)
- 300 mg de Nevirapina, HPMC al 25% K
- 126,000 (34%) 1,770 (25%) 24,5 (29%)
- 300 mg de Nevirapina, HPMC al 30% K
- 109,000 (29%) 1,340 (27%) 24,2 (41%)
- 300 mg de Nevirapina, HPMC al 40% K
- 97,800 (64%) 1,350 (44%) 25,0 (44%)
- 400 mg de Nevirapina, IR
- 210,000 (22%) 3,130 (12%) 4,31 (117%)
- 200 mg de Nevirapina, IR
- 114,000 (30%) 1,740 (21%) 2,17 (147%)
10 Los parámetros farmacocinéticos de las formulaciones descritas antes también se confirmaron tras una administración de dosis múltiple (nevirapina XR una vez al día durante 17 días) en una población de pacientes infestados con VIH, previamente tratados con comprimidos Viramune® de liberación inmediata. Un resumen de los resultados aparece en la Tabla 2, que figura más abajo.
Tabla 2 – Resumen de parámetros farmacocinéticos de estado estacionario para comprimidos de liberación 15 inmediata (IR) y 400 mg de liberación prolongada (XR) en pacientes infestados con el VIH
- Tratamiento
- tmáx (h) Cmáx (ng/mL) Cmin (ng/mL) AUC0-24 (h·ng/mL)
- IR (N = 19)
- g media 1,8 5,576 2,976 96,137
- g CV%
- 130 26 31 26
- ER 25% K (N =18)
- g media 4,3 3,911 2,622 75,544
- g CV%
- 134 26 35 29
- ER 20% K (N =9)
- g media 5,8 3,904 2,609 79,308
- g CV%
- 92 37 45 38
7
Claims (1)
-
imagen1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94276507P | 2007-06-08 | 2007-06-08 | |
| US942765P | 2007-06-08 | ||
| PCT/US2008/065705 WO2008154234A2 (en) | 2007-06-08 | 2008-06-04 | Extended release formulation of nevirapine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2574836T3 true ES2574836T3 (es) | 2016-06-22 |
Family
ID=39739795
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES08756672.5T Active ES2574836T3 (es) | 2007-06-08 | 2008-06-04 | Formulación de liberación prolongada de nevirapina |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US8460704B2 (es) |
| EP (1) | EP2155169B1 (es) |
| JP (1) | JP5417662B2 (es) |
| KR (1) | KR101017862B1 (es) |
| CN (1) | CN101784263B (es) |
| AR (1) | AR066924A1 (es) |
| AU (1) | AU2008262031B2 (es) |
| BR (1) | BRPI0811732A2 (es) |
| CA (1) | CA2687491C (es) |
| CL (1) | CL2008001678A1 (es) |
| CO (1) | CO6150128A2 (es) |
| DK (1) | DK2155169T3 (es) |
| EA (1) | EA018377B1 (es) |
| EC (1) | ECSP099561A (es) |
| ES (1) | ES2574836T3 (es) |
| HU (1) | HUE028598T2 (es) |
| IL (1) | IL199924A0 (es) |
| MA (1) | MA31430B1 (es) |
| MX (1) | MX2009007764A (es) |
| NZ (1) | NZ578664A (es) |
| PE (2) | PE20090371A1 (es) |
| PL (1) | PL2155169T3 (es) |
| TN (1) | TN2009000510A1 (es) |
| TW (1) | TWI419716B (es) |
| UA (1) | UA97971C2 (es) |
| UY (1) | UY31128A1 (es) |
| WO (1) | WO2008154234A2 (es) |
| ZA (1) | ZA200904939B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY149159A (en) | 2005-11-15 | 2013-07-31 | Hoffmann La Roche | Method for treating joint damage |
| US20130172274A1 (en) | 2005-12-20 | 2013-07-04 | Duke University | Methods and compositions for delivering active agents with enhanced pharmacological properties |
| AU2008262031B2 (en) | 2007-06-08 | 2011-08-25 | Boehringer Ingelheim International Gmbh | Extended release formulation of nevirapine |
| CN105727261A (zh) | 2008-06-27 | 2016-07-06 | 杜克大学 | 包含弹性蛋白样肽的治疗剂 |
| US20140193491A1 (en) | 2011-05-30 | 2014-07-10 | Cipla Limited | Pharmaceutical antiretroviral composition |
| US20130084277A1 (en) * | 2011-08-24 | 2013-04-04 | Phasebio Pharmaceuticals, Inc. | Formulations of active agents for sustained release |
| CA2866133A1 (en) * | 2012-03-05 | 2013-09-12 | Cipla Limited | Pharmaceutical antiretroviral combinations comprising lamivudine, festinavir and nevirapine |
| CN104523630B (zh) * | 2015-01-22 | 2017-08-25 | 山东新时代药业有限公司 | 一种奈韦拉平片剂 |
| EP3153157A1 (en) | 2015-10-09 | 2017-04-12 | Teva Pharmaceutical Works Private Limited Company | Pharmaceutical composition for prolonged release of nevirapine |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5366972A (en) | 1989-04-20 | 1994-11-22 | Boehringer Ingelheim Pharmaceuticals, Inc. | 5,11-dihydro-6H-dipyrido(3,2-B:2',3'-E)(1,4)diazepines and their use in the prevention or treatment of HIV infection |
| US5133974A (en) | 1989-05-05 | 1992-07-28 | Kv Pharmaceutical Company | Extended release pharmaceutical formulations |
| CA2030056C (en) | 1989-11-17 | 1995-10-17 | Karl D. Hargrave | 5,11-dihydro-6h-dipyrido[3,2-b:2',3'-e][1,4]diazepines and their use in the prevention or treatment of hiv infection |
| US5419917A (en) * | 1994-02-14 | 1995-05-30 | Andrx Pharmaceuticals, Inc. | Controlled release hydrogel formulation |
| US6514530B2 (en) * | 1997-09-09 | 2003-02-04 | Alza Corporation | Dosage form comprising means for changing drug delivery shape |
| ES2172944T3 (es) | 1997-12-05 | 2002-10-01 | Alza Corp | Forma de dosificacion osmotica que comprende un primer y un segundo revestimiento. |
| DE69915346T2 (de) * | 1998-12-17 | 2004-07-22 | Alza Corp., Mountain View | Umwandlung von flüssigkeitsgefüllten gelatinkapseln in systeme mit gesteuerter wirkstoffabgabe durch mehrfache beschichtungen |
| MX339071B (es) * | 1999-03-31 | 2016-05-09 | Janssen Pharmaceutica Nv | Almidon pregelatinizado en una formulacion de liberacion controlada. |
| TR200200763T2 (tr) * | 1999-09-24 | 2003-09-22 | Janssen Pharmaceutica N.V. | Antiviral bileşimler |
| AU2084801A (en) | 1999-12-09 | 2001-06-18 | Alza Corporation | Antiviral medication |
| US6541014B2 (en) * | 2000-10-13 | 2003-04-01 | Advancis Pharmaceutical Corp. | Antiviral product, use and formulation thereof |
| WO2002092095A1 (en) | 2001-05-11 | 2002-11-21 | Boehringer Ingelheim International Gmbh | Use of nevirapine to treat or prevent lipid pathology in patients with hiv that is resistant to nevirapine |
| US20030050620A1 (en) | 2001-09-07 | 2003-03-13 | Isa Odidi | Combinatorial type controlled release drug delivery device |
| AU2003287666A1 (en) | 2002-11-13 | 2004-06-03 | Control Delivery Systems, Inc. | Systemic delivery of antiviral agents |
| WO2004112724A2 (en) | 2003-06-20 | 2004-12-29 | Viral Genomix, Inc. | Compositions for and methods for treating hiv |
| CN1863512A (zh) | 2003-10-01 | 2006-11-15 | 鲁宾有限公司 | 控释药物组合物及其制备方法 |
| PL1696822T3 (pl) | 2003-11-13 | 2010-08-31 | Psivida Inc | Wstrzykiwane implanty o opóźnionym wydzielaniu mające matrycę rdzenia i powłokę podatne na erozję biologiczną |
| CA2577288C (en) * | 2004-09-02 | 2010-11-30 | Janssen Pharmaceutica N.V. | Hydrochloride of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile |
| WO2006114709A1 (en) * | 2005-04-25 | 2006-11-02 | Aurobindo Pharma Limited | Pharmaceutical compositions of antiretrovirals |
| RS20070512A (sr) | 2005-06-29 | 2009-01-22 | Panacea Biotec Ltd., | Farmaceutske kompozicije sa zadržanim otpuštanjem i postupci za njihovo dobijanje |
| EP1906937B1 (en) | 2005-07-22 | 2016-10-19 | Rubicon Research Pvt Ltd. | Novel dispersible tablet composition |
| FR2891459B1 (fr) | 2005-09-30 | 2007-12-28 | Flamel Technologies Sa | Microparticules a liberation modifiee d'au moins un principe actif et forme galenique orale en comprenant |
| EP1933815A2 (en) * | 2005-10-14 | 2008-06-25 | Microdose Technologies Inc. | Pharmaceutical packaging of an oral dosage combination |
| AU2008262031B2 (en) | 2007-06-08 | 2011-08-25 | Boehringer Ingelheim International Gmbh | Extended release formulation of nevirapine |
-
2008
- 2008-06-04 AU AU2008262031A patent/AU2008262031B2/en not_active Ceased
- 2008-06-04 CA CA2687491A patent/CA2687491C/en active Active
- 2008-06-04 DK DK08756672.5T patent/DK2155169T3/en active
- 2008-06-04 MX MX2009007764A patent/MX2009007764A/es active IP Right Grant
- 2008-06-04 EA EA200900958A patent/EA018377B1/ru not_active IP Right Cessation
- 2008-06-04 PL PL08756672.5T patent/PL2155169T3/pl unknown
- 2008-06-04 UA UAA200908230A patent/UA97971C2/ru unknown
- 2008-06-04 EP EP08756672.5A patent/EP2155169B1/en not_active Revoked
- 2008-06-04 CN CN2008800193577A patent/CN101784263B/zh active Active
- 2008-06-04 US US12/523,226 patent/US8460704B2/en active Active
- 2008-06-04 BR BRPI0811732-2A2A patent/BRPI0811732A2/pt not_active IP Right Cessation
- 2008-06-04 NZ NZ578664A patent/NZ578664A/en not_active IP Right Cessation
- 2008-06-04 JP JP2009552940A patent/JP5417662B2/ja active Active
- 2008-06-04 WO PCT/US2008/065705 patent/WO2008154234A2/en not_active Ceased
- 2008-06-04 ES ES08756672.5T patent/ES2574836T3/es active Active
- 2008-06-04 KR KR1020097016610A patent/KR101017862B1/ko active Active
- 2008-06-04 HU HUE08756672A patent/HUE028598T2/en unknown
- 2008-06-06 CL CL2008001678A patent/CL2008001678A1/es unknown
- 2008-06-06 TW TW097121294A patent/TWI419716B/zh active
- 2008-06-06 PE PE2008000969A patent/PE20090371A1/es not_active Application Discontinuation
- 2008-06-06 PE PE2013000070A patent/PE20131035A1/es not_active Application Discontinuation
- 2008-06-06 AR ARP080102446A patent/AR066924A1/es unknown
- 2008-06-06 UY UY31128A patent/UY31128A1/es not_active Application Discontinuation
-
2009
- 2009-07-15 ZA ZA200904939A patent/ZA200904939B/xx unknown
- 2009-07-16 IL IL199924A patent/IL199924A0/en unknown
- 2009-07-21 CO CO09075419A patent/CO6150128A2/es unknown
- 2009-08-05 EC EC2009009561A patent/ECSP099561A/es unknown
- 2009-12-04 TN TNP2009000510A patent/TN2009000510A1/fr unknown
- 2009-12-07 MA MA32400A patent/MA31430B1/fr unknown
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