JP5968300B2 - 高用量、水溶性及び吸湿性薬剤基質用の制御放出性剤形 - Google Patents
高用量、水溶性及び吸湿性薬剤基質用の制御放出性剤形 Download PDFInfo
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| US11400065B2 (en) | 2019-03-01 | 2022-08-02 | Flamel Ireland Limited | Gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state |
| US11504347B1 (en) | 2016-07-22 | 2022-11-22 | Flamel Ireland Limited | Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics |
| US11583510B1 (en) | 2022-02-07 | 2023-02-21 | Flamel Ireland Limited | Methods of administering gamma hydroxybutyrate formulations after a high-fat meal |
| US11602512B1 (en) | 2016-07-22 | 2023-03-14 | Flamel Ireland Limited | Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics |
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| US11839597B2 (en) | 2016-07-22 | 2023-12-12 | Flamel Ireland Limited | Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics |
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| AU2011232408B2 (en) | 2010-03-24 | 2015-07-30 | Jazz Pharmaceuticals, Inc. | Controlled release dosage forms for high dose, water soluble and hygroscopic drug substances |
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| EP2931261A1 (en) * | 2012-12-14 | 2015-10-21 | SI Group, Inc. | High content sodium ibuprofen granules, their preparation and their use in preparing non-effervescent solid dosage forms |
| WO2014127053A2 (en) | 2013-02-13 | 2014-08-21 | Metabolix, Inc. | Process for ultra pure chemical production from biobased raw starting materials |
| US9050302B2 (en) | 2013-03-01 | 2015-06-09 | Jazz Pharmaceuticals Ireland Limited | Method of administration of gamma hydroxybutyrate with monocarboxylate transporters |
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| US10398662B1 (en) | 2015-02-18 | 2019-09-03 | Jazz Pharma Ireland Limited | GHB formulation and method for its manufacture |
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| US11000498B2 (en) | 2016-07-22 | 2021-05-11 | Flamel Ireland Limited | Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics |
| US20180263936A1 (en) | 2017-03-17 | 2018-09-20 | Jazz Pharmaceuticals Ireland Limited | Gamma-hydroxybutyrate compositions and their use for the treatment of disorders |
| WO2019126214A1 (en) | 2017-12-18 | 2019-06-27 | Tris Pharma, Inc. | Pharmaceutical composition comprising ghb gastro-retentive raft forming systems having trigger pulse drug release |
| WO2019126215A1 (en) | 2017-12-18 | 2019-06-27 | Tris Pharma, Inc. | Ghb pharmaceutical compositions comprising a floating interpenetrating polymer network forming system |
| IL275444B2 (en) | 2017-12-18 | 2025-01-01 | Tris Pharma Inc | Modified release drug powder formulation containing gastric-retaining raft-forming systems with pulsed drug release |
| BR112020012417A2 (pt) * | 2017-12-20 | 2020-11-24 | Flamel Ireland Limited | formulações embaladas de gama-hidroxibutirato de liberação modificada tendo estabilidade melhorada |
| AU2019383389A1 (en) * | 2018-11-19 | 2021-05-06 | Jazz Pharmaceuticals Ireland Limited | Alcohol-resistant drug formulations |
| CN115244028A (zh) | 2019-12-20 | 2022-10-25 | 凯瑞康宁生物工程有限公司 | 4-缬氨酰氧基丁酸的合成方法 |
| TW202139986A (zh) | 2020-02-21 | 2021-11-01 | 愛爾蘭商爵士製藥愛爾蘭有限責任公司 | 治療原發性嗜睡症之方法 |
| JP7682215B2 (ja) | 2020-06-18 | 2025-05-23 | エックスダブリューファーマ リミテッド | 水溶性医薬品有効成分の制御放出造粒物 |
| KR20230008190A (ko) | 2020-06-18 | 2023-01-13 | 엑스더블유파마 리미티드 | 수용성 원료의약품의 약학적 과립화제 |
| US11896573B2 (en) | 2020-07-24 | 2024-02-13 | XWPharma Ltd. | Pharmaceutical compositions and pharmacokinetics of a gamma-hydroxybutyric acid derivative |
| TW202228665A (zh) | 2020-10-05 | 2022-08-01 | 凱瑞康寧生技股份有限公司 | γ－羥基丁酸衍生物之修飾釋放組合物 |
| WO2022082105A2 (en) | 2020-10-16 | 2022-04-21 | Jazz Pharmaceuticals Ireland Limited | Treatment methods using ghb |
| EP4588471A3 (en) | 2021-03-19 | 2025-09-24 | XWPharma Ltd. | Pharmacokinetics of combined release formulations of a gamma-hydroxybutyric acid derivative |
| EP4415701A1 (en) | 2021-10-11 | 2024-08-21 | Jazz Pharmaceuticals Ireland Limited | Method of administering oxybate |
| WO2023135150A1 (en) | 2022-01-11 | 2023-07-20 | Jazz Pharmaceuticals Ireland Limited | Method of administering oxybate |
| KR20250148613A (ko) | 2023-02-03 | 2025-10-14 | 트리스 파마 인코포레이티드 | 저 나트륨 옥시베이트 밤마다 1회 투여 조성물 |
Family Cites Families (129)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB922029A (en) | 1960-05-19 | 1963-03-27 | Equilibre Biolog L | Therapeutic composition |
| US3051619A (en) | 1960-05-19 | 1962-08-28 | Equilibre Biolog L | 4-hydroxy butyric acid therapeutic compositions and process of use for clinical sedation, hypnosis, or anaesthesia |
| DE1642902A1 (de) | 1965-09-30 | 1971-05-19 | Unilever Nv | Verfahren zur kontinuierlichen Entsaeuerung von Glyceridoelen |
| US4221778A (en) | 1979-01-08 | 1980-09-09 | Pennwalt Corporation | Prolonged release pharmaceutical preparations |
| US4374441A (en) | 1980-05-23 | 1983-02-22 | Book Covers, Inc. | Method of making a book cover and pocket element therefor |
| ZA814854B (en) | 1980-07-17 | 1982-07-28 | J Klosa | Nonhygroscopic salts of 4-hydroxybutryric acid, methods of their production and pharmaceutical preparations containing these salts |
| EP0044801B1 (de) | 1980-07-17 | 1984-02-15 | Josef Dr. Klosa | Nichthygroskopische Salze der 4-Hydroxybuttersäure, Verfahren zu ihrer Herstellung und ihre Verwendung zur Herstellung pharmazeutischer Mittel |
| CH655507B (enExample) | 1983-01-12 | 1986-04-30 | ||
| US4524217A (en) | 1984-06-08 | 1985-06-18 | Celanese Corporation | Process for producing N-acyl-hydroxy aromatic amines |
| EP0235408B1 (en) | 1984-08-06 | 1991-01-09 | The University Of Toronto Innovations Foundation | Pharmaceutical composition and treatment |
| IE59106B1 (en) | 1985-05-31 | 1994-01-12 | Warner Lambert Co | A therapeutic effervescent composition and a method of preparing the same |
| US4687662A (en) | 1985-08-30 | 1987-08-18 | Warner-Lambert Company | Therapeutic effervescent composition |
| US4738985A (en) | 1986-03-19 | 1988-04-19 | The University Of Toronto Innovations Foundations | Pharmaceutical composition and treatment |
| DE3804168A1 (de) | 1988-02-11 | 1989-08-24 | Gewerk Eisenhuette Westfalia | Planetenueberlagerungsgetriebe und ueberlagerungsantrieb fuer kettenbaender u. dgl., insbesondere fuer kettenfoerderer und kettengezogene bergbau-gewinnungsmaschinen |
| IT1217783B (it) | 1988-06-03 | 1990-03-30 | Farmaceutico Ct S R L Lab | Impiego di salo dell,acido gamma idrossi butirrico per la preparazione di composizioni farmaceutiche adatta ad essereimpiegate nella terapia dell,alcolismo e composizioni relative |
| US5294430A (en) | 1988-09-12 | 1994-03-15 | University Of Rochester | Use of dithiocarbamates to treat myelosuppression |
| US4916161A (en) | 1988-10-25 | 1990-04-10 | Bristol-Myers Squibb | Taste-masking pharmaceutical agents |
| JP2564690B2 (ja) | 1990-06-14 | 1996-12-18 | 三省製薬 株式会社 | メラニン生成抑制外用剤 |
| DE4113984C2 (de) | 1991-04-29 | 2002-05-08 | Koehler Chemie Dr Franz | Salze der 4-Hydroxy-Buttersäure |
| US5415870A (en) | 1991-07-01 | 1995-05-16 | Gerhard Gergely | Effervescent systems using reaction doping agents |
| IT1271403B (it) | 1993-03-26 | 1997-05-28 | Ct Lab Farm Srl | Sali dell'acido gamma-idrossibutirrico ad attivita' ansiolitica e per il trattamento degli stati depressivi |
| KR100337985B1 (ko) * | 1993-06-14 | 2002-11-23 | 얀센 파마슈티카 엔.브이. | 아스테미졸및슈도에페드린의서방성필름-코팅정제 |
| IT1266565B1 (it) * | 1993-07-22 | 1997-01-09 | Ct Lab Farm Srl | Composizioni farmaceutiche a rilascio controllato a base di uno o piu' sali farmaceuticamente accettabili dell'acido gamma-idrossi-butirrico. |
| US5833599A (en) | 1993-12-13 | 1998-11-10 | Multum Information Services | Providing patient-specific drug information |
| DE4432757A1 (de) * | 1994-09-14 | 1996-03-21 | Boehringer Mannheim Gmbh | Pharmazeutische Zubereitung enthaltend Metformin und Verfahren zu deren Herstellung |
| FR2725623A1 (fr) | 1994-10-18 | 1996-04-19 | Flamel Tech Sa | Microcapsules medicamenteuses et/ou nutritionnelles pour administration per os |
| US7072840B1 (en) | 1994-10-28 | 2006-07-04 | Cybear, L.L.C. | Prescription management system |
| US5845255A (en) | 1994-10-28 | 1998-12-01 | Advanced Health Med-E-Systems Corporation | Prescription management system |
| GB9423542D0 (en) | 1994-11-22 | 1995-01-11 | Marples Brian A | Pharmaceutical compounds |
| JP4072597B2 (ja) * | 1994-12-27 | 2008-04-09 | ナムローゼ・フェンノートシャップ・オルガノン | 持続性製剤 |
| US5758095A (en) | 1995-02-24 | 1998-05-26 | Albaum; David | Interactive medication ordering system |
| US5840331A (en) | 1995-06-07 | 1998-11-24 | Arch Development Corporation | Use of γ-hydroxybutyrate for the stimulation of sleep-related secretion growth hormone and prolactin |
| US6112182A (en) | 1996-01-16 | 2000-08-29 | Healthcare Computer Corporation | Method and apparatus for integrated management of pharmaceutical and healthcare services |
| IT1283782B1 (it) | 1996-08-09 | 1998-04-30 | Ct Lab Farm Srl | Uso di ammidi dell'acido gamma-idrossibutirrico nel trattamento di tossicodipendenze,ed in particolare sell'alcolismo |
| US20080292700A1 (en) * | 1997-04-21 | 2008-11-27 | Biovail Laboratories | Controlled release formulations using intelligent polymers |
| US5990162A (en) | 1997-08-29 | 1999-11-23 | Orphan Medical, Inc. | Method for treatment of fibromyalgia and chronic fatigue syndrome |
| US20060165606A1 (en) | 1997-09-29 | 2006-07-27 | Nektar Therapeutics | Pulmonary delivery particles comprising water insoluble or crystalline active agents |
| US6472432B1 (en) | 1997-11-17 | 2002-10-29 | Nicholas V. Perricone | Treatment of rosacea using lipoic acid |
| US6014631A (en) | 1998-04-02 | 2000-01-11 | Merck-Medco Managed Care, Llc | Computer implemented patient medication review system and process for the managed care, health care and/or pharmacy industry |
| US6322819B1 (en) | 1998-10-21 | 2001-11-27 | Shire Laboratories, Inc. | Oral pulsed dose drug delivery system |
| CA2355293C (en) | 1998-12-23 | 2005-08-16 | Orphan Medical, Inc. | Microbiologically sound and stable solutions of gamma-hydroxybutyrate salt for the treatment of narcolepsy |
| EP1316309A1 (en) | 1998-12-23 | 2003-06-04 | Orphan Medical Inc. | Microbiologically sound and stable solutions of gamma-hydroxybutyrate salt for the treatment of narcolepsy |
| US6067524A (en) | 1999-01-07 | 2000-05-23 | Catalina Marketing International, Inc. | Method and system for automatically generating advisory information for pharmacy patients along with normally transmitted data |
| US6565872B2 (en) | 1999-02-16 | 2003-05-20 | Xiao Yu Wu | Polymeric system for drug delivery and solute separation |
| US6384020B1 (en) | 1999-07-14 | 2002-05-07 | Shire Laboratories, Inc. | Rapid immediate release oral dosage form |
| JP2004509900A (ja) | 2000-09-22 | 2004-04-02 | オーファン メディカル，インコーポレイティド | 炭水化物、脂質、またはアミノ酸キャリアを含むγ−ヒドロキシブチレート組成物 |
| WO2002045684A2 (en) | 2000-12-06 | 2002-06-13 | Pharmacia Corporation | Rapidly dispersing pharmaceutical composition comprising effervescent agents |
| FR2830447B1 (fr) | 2001-10-09 | 2004-04-16 | Flamel Tech Sa | Forme galenique orale microparticulaire pour la liberation retardee et controlee de principes actifs pharmaceutiques |
| US8101209B2 (en) | 2001-10-09 | 2012-01-24 | Flamel Technologies | Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles |
| US20030180249A1 (en) | 2002-03-18 | 2003-09-25 | Khanna Satish Chandra | Dosage forms for hygroscopic active ingredients |
| US7985422B2 (en) * | 2002-08-05 | 2011-07-26 | Torrent Pharmaceuticals Limited | Dosage form |
| US8216609B2 (en) * | 2002-08-05 | 2012-07-10 | Torrent Pharmaceuticals Limited | Modified release composition of highly soluble drugs |
| RU2210360C1 (ru) | 2002-09-19 | 2003-08-20 | Общество С Ограниченной Ответственностью "Консорциум-Пик" | Психотропное средство |
| US7668730B2 (en) | 2002-12-17 | 2010-02-23 | JPI Commercial, LLC. | Sensitive drug distribution system and method |
| CA2510289A1 (en) | 2002-12-23 | 2004-07-15 | Merck Frosst Canada & Co. | Pharmaceutical compositions and method of treating parkinson's disease |
| US20050031688A1 (en) | 2003-08-04 | 2005-02-10 | Ayala William J. | Positive wakeup pharmaceutical sleep system with compatible pre-bedtime administration |
| CA2524300C (en) * | 2003-08-08 | 2008-10-28 | Biovail Laboratories International Srl | Modified-release tablet of bupropion hydrochloride |
| EP1656117A1 (en) | 2003-08-11 | 2006-05-17 | Merck Frosst Canada Ltd. | Flavored taste-masked pharmaceutical formulation made using a one-step coating process |
| US20050142192A1 (en) | 2003-10-15 | 2005-06-30 | Wyeth | Oral administration of [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1(7)-en-2-yl)alkyl] phosphonic acid and derivatives |
| CA2579576A1 (en) | 2004-09-07 | 2006-03-16 | Orphan Medical, Inc. | Improved ghb compositions |
| US8193211B2 (en) * | 2004-09-30 | 2012-06-05 | Supernus Pharmaceuticals, Inc. | Controlled release compositions of gamma-hydroxybutyrate |
| PE20060935A1 (es) | 2004-10-21 | 2006-10-26 | Novartis Ag | Composicion farmaceutica que comprende diclofenaco |
| EP1809286A4 (en) | 2004-11-10 | 2010-09-01 | Univ Columbia | METHOD FOR TREATING MOTION TROUBLESHOOTING |
| EA014249B1 (ru) * | 2005-01-27 | 2010-10-29 | Алембик Лимитед | Формуляция леветирацетама длительного высвобождения |
| FR2881652B1 (fr) | 2005-02-08 | 2007-05-25 | Flamel Technologies Sa | Forme pharmaceutique orale microparticulaire anti-mesuage |
| US20080293698A1 (en) | 2005-05-16 | 2008-11-27 | Joseph Johnson | Methods and Compositions for Treating Arg |
| US7645802B2 (en) * | 2005-06-27 | 2010-01-12 | Biovail Laboratories International Srl. | Bupropion hydrobromide and therapeutic applications |
| EP1909769A2 (en) | 2005-08-01 | 2008-04-16 | Alpharma, Inc. | Alcohol resistant pharmaceutical formulations |
| PL116330U1 (en) | 2005-10-31 | 2007-04-02 | Alza Corp | Method for the reduction of alcohol provoked rapid increase in the released dose of the orally administered opioide with prolonged liberation |
| US20090317355A1 (en) | 2006-01-21 | 2009-12-24 | Abbott Gmbh & Co. Kg, | Abuse resistant melt extruded formulation having reduced alcohol interaction |
| US20070264346A1 (en) | 2006-02-16 | 2007-11-15 | Flamel Technologies | Multimicroparticulate pharmaceutical forms for oral administration |
| US8309104B2 (en) | 2006-03-02 | 2012-11-13 | Watson Pharmaceuticals, Inc. | Oral controlled release formulation for sedative and hypnotic agents |
| ES2396039T3 (es) | 2006-03-16 | 2013-02-18 | Tris Pharma, Inc. | Formulaciones de liberación modificada que contienen complejos de fármaco-resina de intercambio iónico |
| US9023400B2 (en) | 2006-05-24 | 2015-05-05 | Flamel Technologies | Prolonged-release multimicroparticulate oral pharmaceutical form |
| AU2007275034A1 (en) * | 2006-07-21 | 2008-01-24 | Lab International Srl | Hydrophilic abuse deterrent delivery system |
| US20080085304A1 (en) | 2006-10-10 | 2008-04-10 | Penwest Pharmaceuticals Co. | Robust sustained release formulations |
| US8394845B2 (en) | 2006-10-30 | 2013-03-12 | Hanall Biopharma Co., Ltd. | Method of using combination preparation comprising angiotensin-II-receptor blocker and HMG-CoA reductase inhibitor |
| MX2009005339A (es) | 2006-11-21 | 2009-06-01 | Mcneil Ppc Inc | Suspensiones analgesicas de liberacion modificada. |
| CA2930487A1 (en) | 2007-01-16 | 2008-07-24 | Egalet Ltd. | Use of i) a polyglycol and ii) an active drug substance for the preparation of a pharmaceutical composition for i)mitigating the risk of alcohol induced dose dumping and/or ii) reducing the risk of drug abuse |
| US7568822B2 (en) | 2007-03-28 | 2009-08-04 | Visteon Global Technologies, Inc. | Predictive adaptive front lighting algorithm for branching road geometry |
| US8202542B1 (en) | 2007-05-31 | 2012-06-19 | Tris Pharma | Abuse resistant opioid drug-ion exchange resin complexes having hybrid coatings |
| GB2462611A (en) * | 2008-08-12 | 2010-02-17 | Cambridge Lab | Pharmaceutical composition comprising tetrabenazine |
| US8778398B2 (en) | 2008-11-04 | 2014-07-15 | Jazz Pharmaceuticals, Inc. | Immediate release formulations and dosage forms of gamma-hydroxybutyrate |
| US8771735B2 (en) | 2008-11-04 | 2014-07-08 | Jazz Pharmaceuticals, Inc. | Immediate release dosage forms of sodium oxybate |
| FR2938431B1 (fr) | 2008-11-14 | 2013-12-20 | Debregeas Et Associes Pharma | Nouvelle composition a base d'acide gamma-hydroxybutyrique |
| SI2421808T1 (sl) | 2009-04-23 | 2013-12-31 | Concert Pharmaceuticals Inc. | Analogi 4-hidroksi maslene kisline |
| FR2951378B1 (fr) | 2009-10-16 | 2012-06-01 | Flamel Tech Sa | Forme pharmaceutique orale solide anti-mesusage et dotee d'un profil specifique de liberation modifiee |
| AU2011232408B2 (en) | 2010-03-24 | 2015-07-30 | Jazz Pharmaceuticals, Inc. | Controlled release dosage forms for high dose, water soluble and hygroscopic drug substances |
| KR20130086131A (ko) | 2010-04-06 | 2013-07-31 | 알러간, 인코포레이티드 | 전방내 약물 송달을 위한 서-방출 저장소 임플란트 |
| SG10201502720VA (en) | 2010-04-07 | 2015-05-28 | Proteus Digital Health Inc | Miniature ingestible device |
| EP2386289A1 (en) | 2010-04-29 | 2011-11-16 | Ipsen Pharma S.A.S. | Clay compositions |
| CN102946869B (zh) | 2010-05-04 | 2016-08-03 | 爵士制药有限公司 | γ-羟基丁酸的速释制剂及剂型 |
| WO2011140310A2 (en) | 2010-05-07 | 2011-11-10 | Microdermis Corporation | Povidone-iodine topical composition |
| US8791113B2 (en) | 2010-06-28 | 2014-07-29 | Merck Patent Gmbh | 2,4-diaryl-substituted [1,8] naphthyridines as kinase inhibitors for use against cancer |
| GB201014633D0 (en) | 2010-09-02 | 2010-10-13 | Avexxin As | Rheumatoid arthritis treatment |
| US8617602B2 (en) | 2010-09-03 | 2013-12-31 | William Wayne Howard | Immediate release compositions and methods for delivering drug formulations using weak acid ion exchange resins in abnormally high pH environments |
| EP2623497B1 (en) | 2010-09-30 | 2016-01-20 | Toyama Chemical Co., Ltd. | Meglumine salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide |
| MY161429A (en) | 2010-09-30 | 2017-04-14 | Toyama Chemical Co Ltd | Sodium salt of 6-fluoro-3-hydroxy-2-pyrazine carboxamide |
| US8623409B1 (en) | 2010-10-20 | 2014-01-07 | Tris Pharma Inc. | Clonidine formulation |
| US20130230587A1 (en) | 2010-11-10 | 2013-09-05 | Rubicon Research Private Limited | Sustained release compositions |
| US20140141090A1 (en) | 2011-02-02 | 2014-05-22 | Edward S. Wilson | Pharmaceutical Composition Comprising Opioid Agonist And Sequestered Antagonist |
| FR2971422B1 (fr) | 2011-02-11 | 2016-05-20 | Debregeas Et Associes Pharma | Granules d'acide gamma-hydroxybutyrique |
| WO2012112492A1 (en) | 2011-02-14 | 2012-08-23 | Concert Pharmaceuticals Inc. | 4-hydroxybutyric acid deuterated analogs |
| WO2012142520A2 (en) | 2011-04-15 | 2012-10-18 | Threshold Pharmaceuticals, Inc. | Unit dose form for oral administration |
| EP2760911B1 (en) | 2011-09-27 | 2017-11-22 | Tepha, Inc. | Controlled hydrolysis of poly-4-hydroxybutyrate and copolymers |
| WO2014078014A2 (en) | 2012-11-14 | 2014-05-22 | Metabolix, Inc. | Production of salts of 4-hydroxybutyrate using biobased raw materials |
| FR2999426B1 (fr) | 2012-12-13 | 2015-01-02 | Flamel Tech Sa | Forme orale multiparticulaire a liberation immediate d'au moins un compose actif, comprenant des particules enrobees resistantes au broyage. |
| US8591922B1 (en) | 2012-12-14 | 2013-11-26 | Jazz Pharmacuticals, Inc. | Gamma-hydroxybutyrate compositions and their use for the treatment of disorders |
| US9050302B2 (en) | 2013-03-01 | 2015-06-09 | Jazz Pharmaceuticals Ireland Limited | Method of administration of gamma hydroxybutyrate with monocarboxylate transporters |
| US20150005334A1 (en) | 2013-03-15 | 2015-01-01 | Inspirion Delivery Technologies, Llc | Abuse deterrent compositions and methods of use |
| US10751287B2 (en) | 2013-03-15 | 2020-08-25 | Purdue Pharma L.P. | Tamper resistant pharmaceutical formulations |
| US9801852B2 (en) | 2013-08-30 | 2017-10-31 | Jazz Pharmaceuticals, Inc. | Devices and methods for facilitating and controlling use of a medication |
| US9770514B2 (en) | 2013-09-03 | 2017-09-26 | ExxPharma Therapeutics LLC | Tamper-resistant pharmaceutical dosage forms |
| BR112016017742A2 (pt) | 2014-02-06 | 2018-06-26 | Sequential Medicine Limited | composição e método auxiliares do sono |
| KR20160117596A (ko) | 2014-02-07 | 2016-10-10 | 오스펙스 파마슈티칼스, 인코포레이티드 | 신규 제약 제제 |
| US20160317388A1 (en) | 2014-05-01 | 2016-11-03 | Sun Pharmaceutical Industries Limited | Dual-chamber pack for extended release suspension compositions |
| RU2016147009A (ru) | 2014-05-01 | 2018-06-04 | Сан Фармасьютикал Индастриз Лимитед | Композиции с пролонгированным высвобождением в виде суспензии |
| US9962336B2 (en) | 2014-05-01 | 2018-05-08 | Sun Pharmaceutical Industries Limited | Extended release suspension compositions |
| WO2016178132A1 (en) | 2015-05-01 | 2016-11-10 | Sun Pharmaceutical Industries Limited | Dual-chamber pack for extended release suspension compositions |
| MA41124A (fr) | 2014-12-05 | 2017-10-10 | Sun Pharmaceutical Ind Ltd | Compositions en suspension à libération prolongée à rétention gastrique |
| US10398662B1 (en) | 2015-02-18 | 2019-09-03 | Jazz Pharma Ireland Limited | GHB formulation and method for its manufacture |
| CA3207586A1 (en) | 2016-02-24 | 2017-08-31 | Chemapotheca, Llc | Amphetamine controlled release, prodrug, and abuse-deterrent dosage forms |
| US11000498B2 (en) | 2016-07-22 | 2021-05-11 | Flamel Ireland Limited | Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics |
| UY37341A (es) | 2016-07-22 | 2017-11-30 | Flamel Ireland Ltd | Formulaciones de gamma-hidroxibutirato de liberación modificada con farmacocinética mejorada |
| US20180263936A1 (en) | 2017-03-17 | 2018-09-20 | Jazz Pharmaceuticals Ireland Limited | Gamma-hydroxybutyrate compositions and their use for the treatment of disorders |
| BR112020012417A2 (pt) | 2017-12-20 | 2020-11-24 | Flamel Ireland Limited | formulações embaladas de gama-hidroxibutirato de liberação modificada tendo estabilidade melhorada |
| AU2019383389A1 (en) | 2018-11-19 | 2021-05-06 | Jazz Pharmaceuticals Ireland Limited | Alcohol-resistant drug formulations |
| EP3930702A1 (en) | 2019-03-01 | 2022-01-05 | Flamel Ireland Limited | Gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state |
| MX2022007968A (es) | 2019-12-24 | 2022-09-02 | Jazz Pharmaceuticals Ireland Ltd | Dosificacion de gamma-hidroxibutirato (ghb). |
-
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- 2011-03-24 CN CN201180025543.3A patent/CN102917697B/zh active Active
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- 2020-09-04 US US17/012,831 patent/US10966931B2/en active Active
- 2020-09-04 US US17/012,823 patent/US10959956B2/en active Active
-
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- 2021-04-07 US US17/224,781 patent/US11090269B1/en active Active
- 2021-07-20 US US17/380,509 patent/US11207270B2/en active Active
- 2021-12-13 US US17/549,151 patent/US20220096384A1/en not_active Abandoned
Cited By (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12115145B2 (en) | 2016-07-22 | 2024-10-15 | Flamel Ireland Limited | Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics |
| US12115143B2 (en) | 2016-07-22 | 2024-10-15 | Flamel Ireland Limited | Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics |
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