DK2787974T3 - Robuste peptidformuleringer med kontrolleret frigivelse - Google Patents

Robuste peptidformuleringer med kontrolleret frigivelse Download PDF

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DK2787974T3
DK2787974T3 DK12791208.7T DK12791208T DK2787974T3 DK 2787974 T3 DK2787974 T3 DK 2787974T3 DK 12791208 T DK12791208 T DK 12791208T DK 2787974 T3 DK2787974 T3 DK 2787974T3
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Fredrik Tiberg
Markus Johnsson
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Camurus Ab
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Claims (25)

1. Præformulering omfattende en lav-viskositets, ikke-flydende krystallinsk, blanding af: a. 25-55 vægtprocent af mindst et diacylglycerol og/eller mindst et tocopherol; b. 25-55 vægtprocent af mindst en phospholipidkomponent omfattende phospholipider, der har i. polære hovedgrupper omfattende mere end 50 % phosphatidylethanolamin, og ii. to acylkæder, der hver uafhængigt har 16 til 20 kulstofatomer, hvor mindst en acylkæde har mindst en umættethed i kulstofkæden, og der er ikke mere end fire umættetheder over to kulstofkæder; hvor phospholipidkomponenten b) omfatter mere end 50 % phosphatidylethanolamin (PE); c. 5-25 vægtprocent af mindst et biokompatibelt, oxygenindeholdende, lavviskositet organisk solvent; hvor 0,1-10 vægtprocent af mindst et peptid aktivt middel omfattende mindst en somatostatin-receptoragonist er opløst eller dispergeret i lav-viskositet-blandingen; hvor præformuleringen har en viskositet på 0,1 til 5000 mPas ved 20 °C; og hvor præformuleringen danner, eller er i stand til at danne, mindst en ikke-lamellar, flydende krystallinsk fasestruktur ved kontakt med en vandig fluid.
2. Præformulering ifølge krav 1, hvor det mindst ene peptid aktive middel er et begrænset peptid på 6-30 α-aminosyrer, fortrinsvis 6-10 α-aminosyrer, mere fortrinsvis omfattende eller bestående af mindst en valgt fra gruppen bestående af SST-14, SST-28, octreotid, lanreotid, pasireotid og vapreotid eller salte deraf, fortrinsvis pasireotid og octreotid eller salte deraf, hvor det peptid aktive middel eventuelt omfatter eller består af det relevante chlorid-, acetat-, pamoat- eller tartratsalt.
3. Præformulering ifølge krav 1 eller krav 2, hvor præformuleringen leverer en dosis af peptid aktivt middel i området fra 5 til 150 mg/ml, for eksempel 10 til 100 mg/ml, fortrinsvis 10 til 70 mg/ml, såsom 20 til 60 mg/ml, mest fortrinsvis 30 til 60 mg/ml.
4. Præformulering ifølge et hvilket som helst af kravene 1 til 3, hvor den flydende krystallinske fasestruktur er en omvendt hexagonal fasestruktur eller en omvendt kubisk fasestruktur eller blandinger deraf, fortrinsvis hvor den flydende krystallinske fasestruktur er valgt fra H2, I2, eller blandinger deraf.
5. Præformulering ifølge et hvilket som helst af kravene 1 til 4, hvor de ikke-polære halegrupper af komponent a) hver uafhængigt består i alt væsentligt af umættede C18-grupper.
6. Præformulering ifølge et hvilket som helst af kravene 1 til 4, hvor komponent a) består i alt væsentligt af mindst et tocopherol, eller hvor komponent a) består i alt væsentligt af en blanding af glyceroldioleat (GDO) og tocopherol.
7. Præformulering ifølge et hvilket som helst af kravene 1 til 6, hvor komponent b) er valgt fra phosphatidylethanolaminer, eller blandinger af phosphatidylethanolaminer med mindst en valgt fra phosphatidylcholiner, phosphatidylinositoler, og sphingomyeliner, fortrinsvis phosphatidylcholiner såsom soja-phosphatidylcholin (SPC) og/eller dioleoylphosphatidylcholin (DOPC).
8. Præformulering ifølge et hvilket som helst af kravene 1 til 7, hvor phospholipid-komponenten b) omfatter mindst 75 % PE, for eksempel mindst 80 % PE eller mindst 90 % PE, og mest fortrinsvis i alt væsentligt 100 % PE.
9. Præformulering ifølge et hvilket som helst af kravene 1 til 8, hvor phospholipid-komponenten b) yderligere omfatter mindst et phospholipid, der har i. polære hovedgrupper omfattende mindst 90 % phosphatidylcholin, og ii. to acylkæder, der hver uafhængigt har 16 til 20 kulstofatomer, hvor mindst en acylkæde har mindst en umættethed i kulstofkæden, og der ikke er mere end fire umættetheder over to kulstofkæder.
10. Præformulering ifølge et hvilket som helst af kravene 1 til 9, hvor phospholipid-komponenten b) omfatter mindst 10 % PC, foreksempel mindst 20 % PC eller mindst 30 % PC, fortrinsvis SPC, DOPC eller blandinger deraf.
11. Præformulering ifølge et hvilket som helst af kravene 1 til 10, hvor phospholipid-komponenten b) danner en hexagonal fase i kontakt med overskydende vand ved temperaturer i området fra 36 til 40 °C.
12. Præformulering ifølge et hvilket som helst af kravene 1 til 11, der har mindst en af: (i) en molekyleopløsning, L· og/eller l_3 fasestruktur; (ii) et forhold mellem a) og b) på mellem 40:60 til 60:40 efter vægt; og/eller (iii) yderligere omfattende op til 10 vægtprocent af a)+b) af en ladet anionisk amfifil.
13. Præformulering ifølge et hvilket som helst af kravene 1 til 12, hvor komponent c) er valgt fra alkoholer, ketoner, estere, ethere, amider, sulphoxider og blandinger deraf.
14. Præformulering ifølge et hvilket som helst af kravene 1 til 13, yderligere omfattende: 1 til 20 vægtprocent af mindst et polært solvent d) efter vægt af komponenterne a) + b) + c) + d), fortrinsvis 1,2 til 20 vægtprocent, fortrinsvis 2 til 20 vægtprocent, mere fortrinsvis 5-18 vægtprocent, mest fortrinsvis 8-15 vægtprocent, fortrinsvis hvor det polære solvent har en dielektrisk konstant på mindst 28 målt ved 25 °C, mere fortrinsvis mindst 30 målt ved 25 °C.
15. Præformulering ifølge krav 14, hvor komponent d) omfatter eller består af vand eller propylenglycol eller blandinger deraf, såsom præformuleringer hvor komponent d) omfatter mindst 2 % vand.
16. Præformulering ifølge et hvilket som helst af kravene 14 eller 15, hvor komponent c) omfatter mindst et biokompatibelt, organisk, mono-alkoholisk solvent, fortrinsvis mindst en valgt fra gruppen bestående af ethanol, propanol, isopropanol eller blandinger deraf, mere fortrinsvis ethanol.
17. Præformulering ifølge et hvilket som helst af kravene 14 til 16, hvor komponent c) omfatter dimethylsulfoxid (DMSO), N-methylpyrrolidon (NMP) eller blandinger af NMP og ethanol.
18. Præformulering ifølge et hvilket som helst af kravene 14 til 17, hvor komponenterne c) og d) kombineret er til stede i et totalt niveau på mindre end eller lig med 30 vægtprocent, mere fortrinsvis 25 vægtprocent, for eksempel i området 15-20 vægtprocent.
19. Præformulering ifølge et hvilket som helst af kravene 1 til 18, hvilken kan administreres ved hjælp af injektion, sprøjtning, dypning, skylning, påføring fra et kompres eller kuglerulle, maling, nedtrængning, aerosolsprøjtning eller pumpesprøjtning.
20. Injicerbar præformulering ifølge et hvilket som helst af kravene 1 til 18, hvilken danner et depot, der tilvejebringer kontinuerlig frigivelse af aktivt middel i mindst to uger, hvor det aktive middel omfatter mindst et valgt fra a. octreotid; b. pasireotid.
21. Fremgangsmåde til dannelsen af en præformulering ifølge et hvilket som helst af kravene 1 til 20 egnet til administrationen af et peptid aktivt middel omfattende mindst en somatostatin-receptoragonist til et (fortrinsvis pattedyr) individ, hvilken fremgangsmåde omfatter at danne en ikke-flydende krystallinsk, lav-viskositet-blanding af a. 25-55 vægtprocent af mindst et diacylglycerol og/eller mindst et tocopherol; b. 25-55 vægtprocent af mindst en phospholipidkomponent omfattende phospholipider, der har i. polære hovedgrupper omfattende mere end 50 % phosphatidylethanolamin, og ii. to acylkæder, der hver uafhængigt har 15 til 20 kulstofatomer hvor mindst en acylkæde har mindst en umættethed i kulstofkæden, og der er ikke mere end fire umættetheder over to kulstofkæder; hvor phospholipidkomponenten b) omfatter mere end 50 % PE; c. 5-25 vægtprocent af mindst et biokompatibelt, oxygenindeholdende, lavviskositet organisk solvent; og at opløse eller dispergere 0,1-10 vægtprocent af mindst et peptid aktivt middel omfattende mindst en somatostatin-receptoragonist i lav-viskositet-blandingen, eller i mindst en af komponenter a, b eller c forud for at danne lav-viskositet-blandingen.
22. Præformulering ifølge et hvilket som helst af kravene 1 til 20 til anvendelse i behandlingen eller profylaksen afen tilstand valgt fra Cushings sygdom, akromegali, type I eller type II diabetes mellitus, i særdeleshed komplikationer deraf, f.eks. angiopati, diabetisk proliferativ retinopati, diabetisk makulært ødem, nefropati, neuropati og Dawn-fænomen, og andre stofskiftesygdomme relateret til insulin- eller glucagon-frigivelse, f.eks. fedme, f.eks. sygelig fedme eller hypothalamisk eller hyperinsulinemisk fedme, enterokutan og pankreaskutan fistel, irritabelt tarmsyndrom, inflammatoriske sygdomme, f.eks. Graves sygdom, inflammatorisk tarmsygdom, psoriasis eller rheumatoid arthritis, polycystisk nyresygdom, dumping-syndrom, vandet diarrésyndrom, AI DS-relate ret diarré, kemoterapi-induceret diarré, akut eller kronisk bugspytkirtelbetændelse og gastrointestinal hormon-sekreterende tumorer (f.eks. GEP-tumorer, for eksempel vipomaer, glucagonomaer, insulinomaer, karcinoider og lignende), lymfocyt-ondartetheder, f.eks. lymfomer eller leukæmier, hepatocellulær karcinom samt gastrointestinal blødning, f.eks. variceal oesophagial blødning.
23. Forfyldt indgivelsesindretning indeholdende en præformulering ifølge et hvilket som helst af kravene 1 til 20, fortrinsvis hvor indretningen er en sprøjte eller sprøjtecylinder, en nåleløs injektor, en multi- eller engangsinjektor, en patron eller en ampul.
24. Indretningen ifølge krav 23, der indeholder en enkelt dosis på 1 til 200 mg, fortrinsvis 1 til 150 mg, af peptid aktivt middel omfattende mindst en somatostatin-receptoragonist, fortrinsvis pasireotidpamoat, fortrinsvis ved omkring 0,2 til 4 mg per dag mellem planlagte indgivelser, fortrinsvis omkring 0,6 til 3 mg per dag, i særdeleshed 1 til 2 mg/dag.
25. Indretningen ifølge et hvilket som helst af kravene 23 eller 24, der indeholder en total volumen til indgivelse på ikke mere end 5 ml, fortrinsvis ikke mere end 2 ml, mere fortrinsvis omkring 1,5 ml.
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Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2390331C2 (ru) * 2004-06-04 2010-05-27 Камурус Аб Жидкие депо-препараты
GB0711656D0 (en) * 2007-06-15 2007-07-25 Camurus Ab Formulations
WO2012160213A1 (en) * 2011-05-25 2012-11-29 Camurus Ab Controlled release peptide formulations
ES2834318T3 (es) * 2012-05-25 2021-06-17 Camurus Ab Formulaciones de agonistas de receptores de la somatostatina
SI2877155T1 (sl) 2012-07-26 2021-04-30 Camurus Ab Opioidne formulacije
EP2823808A1 (en) * 2013-07-09 2015-01-14 Ipsen Pharma S.A.S. Pharmaceutical composition for a sustained release of lanreotide
EP3060230A4 (en) 2013-10-22 2017-06-14 Prolynx LLC Conjugates of somatostatin and its analogs
WO2016092569A1 (en) * 2014-12-10 2016-06-16 Council Of Scientific & Industrial Research A discontinuous reverse micellar composition in cubic fd3m phase for sustained release of therapeutic drugs
CA2971642A1 (en) * 2014-12-23 2016-06-30 Camurus Ab Controlled-release formulations
GB201516554D0 (en) * 2015-09-18 2015-11-04 Camurus Ab Controlled-release formulations
ITUB20160416A1 (it) * 2016-01-28 2017-07-28 Italfarmaco Spa Uso di una formulazione a lento rilascio di octreotide per la prevenzione della formazione di seroma
CN108883157A (zh) * 2016-03-31 2018-11-23 太阳医药高级研发有限公司 适用于每周一次或每两周一次给药的利拉鲁肽的粘弹性凝胶
WO2018060212A1 (en) 2016-09-27 2018-04-05 Camurus Ab Mixtures and formulations comprising an alkyl ammonium edta salt
DK3512495T3 (da) * 2016-09-15 2022-12-05 Camurus Ab Formuleringer af prostacyklinanaloger
WO2018217926A1 (en) 2017-05-24 2018-11-29 Vmr Products Llc Flavor disk
WO2019182745A1 (en) 2018-03-19 2019-09-26 Bryn Pharma, LLC Epinephrine spray formulations
WO2019213326A1 (en) * 2018-05-01 2019-11-07 Idrop, Inc. Eye drop formulation and method for sustained delivery of medicament to the retina
CA3097927A1 (en) 2018-05-01 2019-11-07 Chibi, Inc. Liquid depot for non-invasive sustained delivery of agents to the eye
CN108498849B (zh) * 2018-05-08 2021-04-30 武汉百纳礼康生物制药有限公司 一种液晶凝胶肝动脉栓塞剂及其制备方法
CN109091451B (zh) * 2018-09-10 2021-08-13 武汉百纳礼康生物制药有限公司 亲水性药物的油相液晶凝胶前体制剂及其制备方法
AU2020282018A1 (en) 2019-05-29 2022-01-06 Camurus Ab Lipid-controlled release compositions
EP4103587A1 (en) 2020-02-14 2022-12-21 Immunor AS Corona virus vaccine
WO2022093722A1 (en) * 2020-10-27 2022-05-05 Pts Consulting, Llc A liquid injectable composition of donepezil
CN113081954A (zh) * 2021-05-25 2021-07-09 南昌大学第二附属医院 一种凝胶载药贴剂药物输送系统
WO2023008498A1 (ja) * 2021-07-27 2023-02-02 株式会社ファルネックス 非ラメラ液晶形成性組成物及びその用途

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE8206744D0 (sv) 1982-11-26 1982-11-26 Fluidcarbon International Ab Preparat for kontrollerad avgivning av substanser
US4938763B1 (en) 1988-10-03 1995-07-04 Atrix Lab Inc Biodegradable in-situ forming implants and method of producing the same
US5538739A (en) 1989-07-07 1996-07-23 Sandoz Ltd. Sustained release formulations of water soluble peptides
MY107937A (en) 1990-02-13 1996-06-29 Takeda Chemical Industries Ltd Prolonged release microcapsules.
DK0752855T3 (da) * 1994-03-30 2000-01-03 Gs Dev Ab Anvendelse af fedtsyreestere som bioadhæsive substanser
SE518578C2 (sv) * 1994-06-15 2002-10-29 Gs Dev Ab Lipidbaserad komposition
EP0839525B1 (en) 1996-10-31 2004-08-04 Takeda Chemical Industries, Ltd. Sustained-release preparation
BE1011899A6 (fr) * 1998-04-30 2000-02-01 Ucb Sa Compositions pharmaceutiques gelifiables utilisables.
JP3952617B2 (ja) 1998-12-11 2007-08-01 株式会社日立製作所 内燃機関の排ガス浄化装置，排ガス浄化方法及び排ガス浄化触媒
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
US20080112915A1 (en) 2003-10-24 2008-05-15 Marianna Foldvari Dna Delivery with Gemini Cationic Surfactants
EP1682091B1 (en) * 2003-11-07 2017-03-29 Camurus Ab Compositions of lipids and cationic peptides
EP1713446B1 (en) 2004-01-23 2010-12-01 Camurus Ab Ternary non-lamellar lipid compositions
GB0401513D0 (en) 2004-01-23 2004-02-25 Camurus Ab Compositions
RU2390331C2 (ru) * 2004-06-04 2010-05-27 Камурус Аб Жидкие депо-препараты
CA2612006A1 (en) * 2004-06-15 2006-01-05 Encore Therapeutics, Inc. Phospholipid compositions and methods for their preparation and use
WO2006075125A1 (en) 2005-01-14 2006-07-20 Camurus Ab GnRH ANALOGUE FORMULATIONS
JP5171262B2 (ja) * 2005-01-14 2013-03-27 カムルス エービー ソマトスタチン類似体製剤
US9060935B2 (en) 2005-01-21 2015-06-23 Camurus Ab Pharmaceutical lipid compositions
ES2399645T3 (es) 2005-06-06 2013-04-02 Camurus Ab Formulaciones de análogos de GLP-1
GB0711656D0 (en) 2007-06-15 2007-07-25 Camurus Ab Formulations
GB0716385D0 (en) * 2007-08-22 2007-10-03 Camurus Ab Formulations

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