EP1677798A2 - Formes posologiques orales d'oxycodone en dose quotidienne unique et a liberation controlee - Google Patents
Formes posologiques orales d'oxycodone en dose quotidienne unique et a liberation controleeInfo
- Publication number
- EP1677798A2 EP1677798A2 EP04817492A EP04817492A EP1677798A2 EP 1677798 A2 EP1677798 A2 EP 1677798A2 EP 04817492 A EP04817492 A EP 04817492A EP 04817492 A EP04817492 A EP 04817492A EP 1677798 A2 EP1677798 A2 EP 1677798A2
- Authority
- EP
- European Patent Office
- Prior art keywords
- auc
- oxycodone
- formulation
- hours
- auco
- 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.)
- Withdrawn
Links
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- 229960002085 oxycodone Drugs 0.000 title claims abstract description 242
- 239000002552 dosage form Substances 0.000 title claims abstract description 223
- 238000013270 controlled release Methods 0.000 title claims description 49
- 239000000203 mixture Substances 0.000 claims abstract description 176
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- 238000000338 in vitro Methods 0.000 claims abstract description 36
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- 230000036470 plasma concentration Effects 0.000 claims description 42
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 29
- DQCKKXVULJGBQN-XFWGSAIBSA-N naltrexone Chemical compound N1([C@@H]2CC3=CC=C(C=4O[C@@H]5[C@](C3=4)([C@]2(CCC5=O)O)CC1)O)CC1CC1 DQCKKXVULJGBQN-XFWGSAIBSA-N 0.000 claims description 21
- 229960003086 naltrexone Drugs 0.000 claims description 21
- 238000013268 sustained release Methods 0.000 claims description 20
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- 229940105606 oxycontin Drugs 0.000 description 36
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 30
- 238000011282 treatment Methods 0.000 description 30
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- MUZQPDBAOYKNLO-RKXJKUSZSA-N oxycodone hydrochloride Chemical compound [H+].[Cl-].O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C MUZQPDBAOYKNLO-RKXJKUSZSA-N 0.000 description 27
- BQNSLJQRJAJITR-UHFFFAOYSA-N 1,1,2-trichloro-1,2-difluoroethane Chemical compound FC(Cl)C(F)(Cl)Cl BQNSLJQRJAJITR-UHFFFAOYSA-N 0.000 description 26
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- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 20
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- 229940068196 placebo Drugs 0.000 description 14
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- 229910052939 potassium sulfate Inorganic materials 0.000 description 1
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- CONVKSGEGAVTMB-RXSVEWSESA-M potassium-L-ascorbate Chemical compound [K+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] CONVKSGEGAVTMB-RXSVEWSESA-M 0.000 description 1
- MLICVSDCCDDWMD-KVVVOXFISA-M potassium;(z)-octadec-9-enoate Chemical compound [K+].CCCCCCCC\C=C/CCCCCCCC([O-])=O MLICVSDCCDDWMD-KVVVOXFISA-M 0.000 description 1
- ANBFRLKBEIFNQU-UHFFFAOYSA-M potassium;octadecanoate Chemical compound [K+].CCCCCCCCCCCCCCCCCC([O-])=O ANBFRLKBEIFNQU-UHFFFAOYSA-M 0.000 description 1
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- 229910052708 sodium Inorganic materials 0.000 description 1
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- OKUCEQDKBKYEJY-UHFFFAOYSA-N tert-butyl 3-(methylamino)pyrrolidine-1-carboxylate Chemical compound CNC1CCN(C(=O)OC(C)(C)C)C1 OKUCEQDKBKYEJY-UHFFFAOYSA-N 0.000 description 1
- RBTVSNLYYIMMKS-UHFFFAOYSA-N tert-butyl 3-aminoazetidine-1-carboxylate;hydrochloride Chemical compound Cl.CC(C)(C)OC(=O)N1CC(N)C1 RBTVSNLYYIMMKS-UHFFFAOYSA-N 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
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- 239000001069 triethyl citrate Substances 0.000 description 1
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
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- 125000005591 trimellitate group Chemical group 0.000 description 1
- PVNIQBQSYATKKL-UHFFFAOYSA-N tripalmitin Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCC PVNIQBQSYATKKL-UHFFFAOYSA-N 0.000 description 1
- YPDXSCXISVYHOB-UHFFFAOYSA-N tris(7-methyloctyl) benzene-1,2,4-tricarboxylate Chemical compound CC(C)CCCCCCOC(=O)C1=CC=C(C(=O)OCCCCCCC(C)C)C(C(=O)OCCCCCCC(C)C)=C1 YPDXSCXISVYHOB-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
Definitions
- FIG 1 is a perspective view of one embodiment of a controlled release osmotic dosage form.
- Dosage form 10 comprises wall 20 that surrounds and encloses an internal compartment (not seen in Figure 1).
- the internal compartment contains a composition comprising oxycodone, and/or one or more of its pharmaceutically acceptable acid addition salts.
- Wall 20 is provided with at least one drug delivery exit 60 for connecting the internal compartment with the exterior environment of use. Accordingly, following oral ingestion of dosage form 10, fluid is imbibed through wall 20 and oxycodone and/or one or more of its pharmaceutically acceptable acid addition salts is released through exit 60.
- the preferred geometrical embodiment in Figure 1 illustrates a standard biconvex shaped tablet, the geometry may embrace a capsule shaped caplet and other oral dosage forms.
- the final dosage form contained a color overcoat and a wax coat and had a mean release rate of 3.94 mg oxycodone hydrochloride, USP per hour (4.93 %/hr).
- the formulation of this example is summarized in Table 5 and is referred to hereinafter as the "Example 3 SZO-24 dosage form.”
- Example 4 Pharmacokinetics and Pharmacodynamics of Osmotic Oxycodone Hydrochloride (Fast and Slow) and Immediate Release Oxycodone Hydrochloride in Healthy Volunteers
- This study investigated the pharmacokinetics and pharmacodynamics of the "fast” and “slow” osmotic oxycodone HCl systems of Example 1 and immediate release (IR) oxycodone HCl in healthy male volunteers.
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Polysaccharides And Polysaccharide Derivatives (AREA)
Abstract
L'invention porte sur des préparations d'oxycodone produisant in vivo des profils plasmatiques sensiblement constants. Les niveaux de tolérance associés à ces profils et ceux associés aux profils biphasés se sont avérés statistiquement identiques. Ces profils plasmatiques sensiblement constants in vivo sont produits par des formes posologiques présentant des profils in vitro d'ordre sensiblement nul. De tels profils de libération produisent in vivo pour une faible dose unique des niveaux de Cmax pouvant réduire la probabilité d'effets secondaires adverses.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US51588003P | 2003-10-29 | 2003-10-29 | |
| PCT/US2004/036132 WO2005041968A2 (fr) | 2003-10-29 | 2004-10-28 | Formes posologiques orales d'oxycodone en dose quotidienne unique et a liberation controlee |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| EP1677798A2 true EP1677798A2 (fr) | 2006-07-12 |
Family
ID=34549453
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP04817492A Withdrawn EP1677798A2 (fr) | 2003-10-29 | 2004-10-28 | Formes posologiques orales d'oxycodone en dose quotidienne unique et a liberation controlee |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1677798A2 (fr) |
| JP (1) | JP2007509979A (fr) |
| KR (1) | KR20060108690A (fr) |
| CN (1) | CN1933837A (fr) |
| AU (1) | AU2004285547A1 (fr) |
| BR (1) | BRPI0415639A (fr) |
| CA (1) | CA2546691A1 (fr) |
| EC (1) | ECSP066534A (fr) |
| IL (1) | IL175193A0 (fr) |
| MA (1) | MA28215A1 (fr) |
| NO (1) | NO20062398L (fr) |
| RU (1) | RU2006118323A (fr) |
| WO (1) | WO2005041968A2 (fr) |
| ZA (1) | ZA200604310B (fr) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE526950T1 (de) | 1999-10-29 | 2011-10-15 | Euro Celtique Sa | Hydrocodon-formulierungen mit gesteuerter freisetzung |
| US10179130B2 (en) | 1999-10-29 | 2019-01-15 | Purdue Pharma L.P. | Controlled release hydrocodone formulations |
| EP2283829A1 (fr) | 2000-10-30 | 2011-02-16 | Euro-Celtique S.A. | Formulations d'hydrocodone à liberation lente |
| US20110104214A1 (en) | 2004-04-15 | 2011-05-05 | Purdue Pharma L.P. | Once-a-day oxycodone formulations |
| UA81224C2 (uk) * | 2001-05-02 | 2007-12-25 | Euro Celtic S A | Дозована форма оксикодону та її застосування |
| US7776314B2 (en) | 2002-06-17 | 2010-08-17 | Grunenthal Gmbh | Abuse-proofed dosage system |
| DE10336400A1 (de) | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| DE10361596A1 (de) | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| US8075872B2 (en) | 2003-08-06 | 2011-12-13 | Gruenenthal Gmbh | Abuse-proofed dosage form |
| US20070048228A1 (en) | 2003-08-06 | 2007-03-01 | Elisabeth Arkenau-Maric | Abuse-proofed dosage form |
| DE102004032051A1 (de) | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten, festen Darreichungsform |
| DE102005005446A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Bruchfeste Darreichungsformen mit retardierter Freisetzung |
| DE102004032049A1 (de) | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Gegen Missbrauch gesicherte, orale Darreichungsform |
| DE102005005449A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| SA07280459B1 (ar) | 2006-08-25 | 2011-07-20 | بيورديو فارما إل. بي. | أشكال جرعة صيدلانية للتناول عن طريق الفم مقاومة للعبث تشتمل على مسكن شبه أفيوني |
| DE102007011485A1 (de) | 2007-03-07 | 2008-09-11 | Grünenthal GmbH | Darreichungsform mit erschwertem Missbrauch |
| CA2713128C (fr) | 2008-01-25 | 2016-04-05 | Gruenenthal Gmbh | Forme posologique pharmaceutique |
| JP2011511782A (ja) | 2008-02-12 | 2011-04-14 | アボット・ラボラトリーズ | 長期放出性ヒドロコドンアセトアミノフェンならびにその関連方法および用途 |
| BRPI0912014A2 (pt) | 2008-05-09 | 2019-03-06 | Grünenthal GmbH | processo para a preparação de uma formulação em pó intermediária e uma forma de dosagem sólida final sob uso de uma etapa de congelamento por atomização |
| RU2015138422A (ru) | 2009-07-22 | 2018-12-25 | Грюненталь Гмбх | Стабильная при окислении, прочная на излом лекарственная форма |
| CN102573805A (zh) | 2009-07-22 | 2012-07-11 | 格吕伦塔尔有限公司 | 热熔挤出的控制释放剂型 |
| US20110150989A1 (en) * | 2009-12-22 | 2011-06-23 | Mallinkckrodt Inc. | Methods of Producing Stabilized Solid Dosage Pharmaceutical Compositions Containing Morphinans |
| EP2555756B1 (fr) * | 2010-04-07 | 2018-08-22 | Lupin Limited | Compositions pharmaceutiques à libération contrôlée de tapentadol |
| NZ607392A (en) | 2010-09-02 | 2015-03-27 | Gruenenthal Chemie | Tamper resistant dosage form comprising inorganic salt |
| BR112013005234A2 (pt) | 2010-09-02 | 2016-05-03 | Gruenenthal Gmbh | forma de dosagem resistente à violação compreendendo um polímero aniônico. |
| PE20141638A1 (es) | 2011-07-29 | 2014-11-22 | Gruenenthal Chemie | Tableta a prueba de manipulacion que proporciona liberacion de farmaco inmediato |
| RS56527B1 (sr) | 2011-07-29 | 2018-02-28 | Gruenenthal Gmbh | Tableta za trenutno oslobađanje leka rezistentna na zloupotrebu |
| MX356421B (es) | 2012-02-28 | 2018-05-29 | Gruenenthal Gmbh | Forma de dosificacion resistente a la manipulacion indebida que comprende un compuesto farmacologicamente activo y un polimero anionico. |
| DK2838512T3 (en) | 2012-04-18 | 2018-11-19 | Gruenenthal Gmbh | MANIPULATED AND DOSAGE DUMPED PHARMACEUTICAL DOSAGE FORM |
| US10064945B2 (en) | 2012-05-11 | 2018-09-04 | Gruenenthal Gmbh | Thermoformed, tamper-resistant pharmaceutical dosage form containing zinc |
| AR096439A1 (es) | 2013-05-29 | 2015-12-30 | Gruenenthal Gmbh | Forma de dosificación resistente al uso indebido que contiene una o más partículas |
| JP6445537B2 (ja) | 2013-05-29 | 2018-12-26 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | １個または複数の粒子を含有する改変防止（ｔａｍｐｅｒ−ｒｅｓｉｓｔａｎｔ）剤形 |
| US10624862B2 (en) | 2013-07-12 | 2020-04-21 | Grünenthal GmbH | Tamper-resistant dosage form containing ethylene-vinyl acetate polymer |
| AU2014356581C1 (en) | 2013-11-26 | 2020-05-28 | Grunenthal Gmbh | Preparation of a powdery pharmaceutical composition by means of cryo-milling |
| MX2016014738A (es) | 2014-05-12 | 2017-03-06 | Gruenenthal Gmbh | Formulacion en capsula de liberacion inmediata resistente a alteraciones que comprende tapentadol. |
| MX2016015417A (es) | 2014-05-26 | 2017-02-22 | Gruenenthal Gmbh | Multiparticulas protegidas contra vertido de dosis etanolico. |
| JP2018517676A (ja) | 2015-04-24 | 2018-07-05 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 即時放出および溶媒抽出に対する耐性を有する改変防止製剤 |
| AU2016319203A1 (en) | 2015-09-10 | 2018-02-22 | Grünenthal GmbH | Protecting oral overdose with abuse deterrent immediate release formulations |
| CA3032233C (fr) | 2016-08-10 | 2021-09-14 | F. Hoffmann-La Roche Ag | Compositions pharmaceutiques comprenant des inhibiteurs de la proteine kinase akt |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5914131A (en) * | 1994-07-07 | 1999-06-22 | Alza Corporation | Hydromorphone therapy |
| UA81224C2 (uk) * | 2001-05-02 | 2007-12-25 | Euro Celtic S A | Дозована форма оксикодону та її застосування |
| DE60325715D1 (de) * | 2002-04-29 | 2009-02-26 | Alza Corp | Methoden und darreichungsformen zur kontrollierten freisetzung von oxykodon |
| RU2004134728A (ru) * | 2002-05-31 | 2005-06-10 | Алза Корпорейшн (Us) | Дозированные формы и композиции для осмотической доставки различных дозировок оксикодона |
-
2004
- 2004-10-28 AU AU2004285547A patent/AU2004285547A1/en not_active Abandoned
- 2004-10-28 EP EP04817492A patent/EP1677798A2/fr not_active Withdrawn
- 2004-10-28 CA CA002546691A patent/CA2546691A1/fr not_active Abandoned
- 2004-10-28 JP JP2006538357A patent/JP2007509979A/ja not_active Withdrawn
- 2004-10-28 KR KR1020067010336A patent/KR20060108690A/ko not_active Withdrawn
- 2004-10-28 BR BRPI0415639-0A patent/BRPI0415639A/pt not_active IP Right Cessation
- 2004-10-28 RU RU2006118323/15A patent/RU2006118323A/ru unknown
- 2004-10-28 WO PCT/US2004/036132 patent/WO2005041968A2/fr not_active Ceased
- 2004-10-28 CN CNA2004800394188A patent/CN1933837A/zh active Pending
-
2006
- 2006-04-25 IL IL175193A patent/IL175193A0/en unknown
- 2006-04-28 MA MA28979A patent/MA28215A1/fr unknown
- 2006-04-28 EC EC2006006534A patent/ECSP066534A/es unknown
- 2006-05-26 NO NO20062398A patent/NO20062398L/no not_active Application Discontinuation
- 2006-05-26 ZA ZA200604310A patent/ZA200604310B/en unknown
Non-Patent Citations (1)
| Title |
|---|
| See references of WO2005041968A2 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2007509979A (ja) | 2007-04-19 |
| RU2006118323A (ru) | 2007-12-10 |
| KR20060108690A (ko) | 2006-10-18 |
| NO20062398L (no) | 2006-07-27 |
| ECSP066534A (es) | 2006-11-24 |
| AU2004285547A1 (en) | 2005-05-12 |
| IL175193A0 (en) | 2008-04-13 |
| CN1933837A (zh) | 2007-03-21 |
| BRPI0415639A (pt) | 2006-12-12 |
| MA28215A1 (fr) | 2006-10-02 |
| CA2546691A1 (fr) | 2005-05-12 |
| WO2005041968A2 (fr) | 2005-05-12 |
| WO2005041968A3 (fr) | 2006-06-22 |
| ZA200604310B (en) | 2007-11-28 |
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