HRP20140158T1 - Formulacija paliperidon implantata - Google Patents
Formulacija paliperidon implantata Download PDFInfo
- Publication number
- HRP20140158T1 HRP20140158T1 HRP20140158AT HRP20140158T HRP20140158T1 HR P20140158 T1 HRP20140158 T1 HR P20140158T1 HR P20140158A T HRP20140158A T HR P20140158AT HR P20140158 T HRP20140158 T HR P20140158T HR P20140158 T1 HRP20140158 T1 HR P20140158T1
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- Prior art keywords
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Links
- 238000009472 formulation Methods 0.000 title claims 13
- 239000000203 mixture Substances 0.000 title claims 13
- 239000007943 implant Substances 0.000 title claims 3
- PMXMIIMHBWHSKN-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCC(O)C4=NC=3C)=NOC2=C1 PMXMIIMHBWHSKN-UHFFFAOYSA-N 0.000 title claims 2
- 229960001057 paliperidone Drugs 0.000 title claims 2
- 239000003814 drug Substances 0.000 claims 7
- 229940079593 drug Drugs 0.000 claims 7
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 6
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims 4
- 229920001577 copolymer Polymers 0.000 claims 4
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 229920000642 polymer Polymers 0.000 claims 4
- 229920000249 biocompatible polymer Polymers 0.000 claims 3
- 239000002245 particle Substances 0.000 claims 3
- 230000005855 radiation Effects 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 230000005250 beta ray Effects 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 230000005251 gamma ray Effects 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 238000010952 in-situ formation Methods 0.000 claims 1
- 238000011065 in-situ storage Methods 0.000 claims 1
- 238000007918 intramuscular administration Methods 0.000 claims 1
- 239000000178 monomer Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
Classifications
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- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/24—Antidepressants
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Inorganic Chemistry (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Materials For Medical Uses (AREA)
Claims (12)
1. Injektabilna depo formulacija prikladna za formiranje in situ krutog implantata u organizmu, a sastoji se od lijeka paliperidona i/ili kombinacije njegovih farmaceutski prihvatljivih soli, biokompatibilnog kopolimera koji se sastoji od mliječne i glikolne kiseline s omjerom monomera mliječne i glikolne kiseline u rasponu od 50:50 te otapalo DMSO; formulacija otpušta lijek s neposrednim nastupom djelovanja te u kontinuitetu tijekom najmanje 8 tjedana pri čemu je in vivo farmakokinetički profil formulacije prikladan za primjenu svakih 8 tjedana ili dulje, a karakterizira ga molekularna težina biokompatibilnog kopolimera u rasponu između kDa te pripadajuća viskoznost u rasponu od do dl/g.
2. Formulacija iz zahtjeva 1 kod koje je biokompatibilni kopolimer ozračen beta ili gama zrakama u rasponu doza od 10-30 KGy mjereno na temperaturi između – i + kako bi se prilagodila njegova molekularna težina rasponu između kDa te pripadajuća viskoznost rasponu od do dl/g.
3. Formulacija iz zahtjeva 1 ili 2 kod koje je veličina distribucije čestica lijeka:
- manja od 10% čestica manjih od 10 mikrona;
- manja od 10% čestica većih od 225 mikrona i
- polovica promjera je u rasponu vrijednosti od 40 do 130 mikrona.
4. Formulacija u skladu s jednim od zahtjeva 1 do 3 kod koje je maseni omjer lijeka/(polimer+lijek) približno 33%.
5. Formulacija u skladu s jednim od zahtjeva 1 do 4 kod koje je sadržaj lijeka otprilike 13% masenog omjera ukupne formulacije, a viskoznost otopine koja sadrži polimer i DMSO je u rasponu od 1,7 – 1,8 Pas.
6. Formulacija iz jednog od prethodnih zahtjeva za liječenje shizofrenije ili bipolarnih poremećaja kod ljudi.
7. Farmaceutski komplet za in situ formiranje biorazgradivog implantata u organizmu, koji se sastoji od formulacije iz zahtjeva 1 do 6 kod kojeg se lijek i biokompatibilni polimer nalaze u prvom spremniku, a otapalo se nalazi u drugom, zasebnom spremniku.
8. Farmaceutski komplet u skladu sa zahtjevom 7 kod kojeg je barem jedan primarni ili sekundarni spremnik štrcaljka, bočica, uređaj ili uložak, bilo za jednokratnu ili višekratnu uporabu.
9. Metoda proizvodnje formulacije u skladu s bilo kojim od prethodnih zahtjeva 1-6 koja se sastoji od osiguravanja biokompatibilnog kopolimera koji ima početnu polimernu masu veću od one koja je potrebna za formulacije intramuskularnih depo preparata te prilagodbe njegove molekularne težine na vrijednosti između kDa kao i njegove pripadne viskoznosti u rasponu između i dl/g zračenjem beta ili gama zrakama u rasponu doza od 10 – 30 KGy mjereno na temperaturi između – i + .
10. Metoda u skladu sa zahtjevom 9 kod je doza zračenja isporučena polimeru u rasponu od 16 do 25 KGy mjereno na temperaturi od .
11. Metoda u skladu sa zahtjevom 9 ili 10 kod koje se biokompatibilni polimer s početnom molekularnom težinom od otprilike 50 kDa zrači dozom od približno 16 KGy kako bi se smanjila njegova molekularna težina na vrijednost između 35 i 38 kDa.
12. Metoda u skladu sa zahtjevima 9 ili 10 kod koje se biokompatibilni polimer molekularne težine od približno 63 kDa zrači dozom od približno 30 KGy kako bi se njegova molekularna težina smanjila na vrijednost između kDa.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2011/059001 WO2011151356A2 (en) | 2010-05-31 | 2011-05-31 | Methods for the preparation of injectable depot compositions |
| PCT/EP2011/059000 WO2011151355A1 (en) | 2010-05-31 | 2011-05-31 | Antipsychotic injectable depot composition |
| EP12170366.4A EP2529757B1 (en) | 2011-05-31 | 2012-05-31 | Paliperidone implant formulation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20140158T1 true HRP20140158T1 (hr) | 2014-04-25 |
Family
ID=47074463
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20140158AT HRP20140158T1 (hr) | 2011-05-31 | 2014-02-19 | Formulacija paliperidon implantata |
Country Status (29)
| Country | Link |
|---|---|
| EP (1) | EP2529757B1 (hr) |
| JP (1) | JP6430933B2 (hr) |
| KR (1) | KR101892496B1 (hr) |
| CN (2) | CN109966239A (hr) |
| AU (1) | AU2013269546B2 (hr) |
| BR (1) | BR112014029208B1 (hr) |
| CA (1) | CA2874702C (hr) |
| CL (1) | CL2014003215A1 (hr) |
| CO (1) | CO7160109A2 (hr) |
| CY (1) | CY1114975T1 (hr) |
| DK (1) | DK2529757T3 (hr) |
| EA (1) | EA029921B1 (hr) |
| ES (1) | ES2456917T3 (hr) |
| HR (1) | HRP20140158T1 (hr) |
| IL (1) | IL235850A0 (hr) |
| IN (1) | IN2014DN10673A (hr) |
| MA (1) | MA37661B1 (hr) |
| MX (1) | MX365097B (hr) |
| MY (1) | MY181549A (hr) |
| NZ (1) | NZ703319A (hr) |
| PH (1) | PH12014502668A1 (hr) |
| PL (1) | PL2529757T3 (hr) |
| PT (1) | PT2529757E (hr) |
| SG (1) | SG11201407971QA (hr) |
| SI (1) | SI2529757T1 (hr) |
| SM (1) | SMT201400044B (hr) |
| UA (1) | UA115987C2 (hr) |
| WO (1) | WO2013178811A1 (hr) |
| ZA (1) | ZA201409297B (hr) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10285936B2 (en) | 2010-05-31 | 2019-05-14 | Laboratorios Farmacéuticos Rovi, S.A. | Injectable composition with aromatase inhibitor |
| US10350159B2 (en) | 2010-05-31 | 2019-07-16 | Laboratories Farmacéuticos Rovi, S.A. | Paliperidone implant formulation |
| US10335366B2 (en) | 2010-05-31 | 2019-07-02 | Laboratorios Farmacéuticos Rovi, S.A. | Risperidone or paliperidone implant formulation |
| US10881605B2 (en) | 2010-05-31 | 2021-01-05 | Laboratorios Farmaceuticos Rovi, S.A. | Methods for the preparation of injectable depot compositions |
| ES2589106T3 (es) | 2010-05-31 | 2016-11-10 | Laboratorios Farmaceuticos Rovi, S.A. | Composición inyectable antipsicótica de liberación controlada |
| LT2394663T (lt) | 2010-05-31 | 2022-02-10 | Laboratorios Farmaceuticos Rovi, S.A. | Kompozicijos, skirtos įšvirkščiamiems in situ biologiškai skaidiems implantams |
| US10463607B2 (en) | 2010-05-31 | 2019-11-05 | Laboratorios Farmaceutics Rofi S.A. | Antipsychotic Injectable Depot Composition |
| SI2529756T1 (sl) * | 2011-05-31 | 2021-09-30 | Laboratorios Farmaceuticos Rovi, S.A. | Formulacija vsadka z risperidonom in/ali paliperidonom |
| ES2456917T3 (es) * | 2011-05-31 | 2014-04-24 | Laboratorios Farmacéuticos Rovi, S.A. | Formulación de implante de paliperidona |
| ES2802299T3 (es) * | 2015-04-07 | 2021-01-18 | Janssen Pharmaceuticals Inc | Régimen de dosificación para dosis olvidadas para ésteres de paliperidona inyectables de acción prolongada |
| CN106038569A (zh) * | 2016-05-26 | 2016-10-26 | 湖南赛沃药业有限公司 | 一种帕利哌酮植入剂及其制备方法 |
| SI3506921T1 (sl) * | 2016-08-31 | 2023-10-30 | Mapi Pharma Ltd. | Depojski sistemi, ki vsebujejo glatiramer acetat |
| JP7337080B2 (ja) * | 2017-10-27 | 2023-09-01 | 嘉奥制薬（石家庄）有限公司 | パリペリドンパルミチン酸エステル徐放性懸濁注射液の投薬レジメン |
| CN111989068A (zh) | 2018-05-24 | 2020-11-24 | 塞拉尼斯伊娃高性能聚合物公司 | 用于持续释放大分子药物化合物的可植入器件 |
| WO2019226516A1 (en) | 2018-05-24 | 2019-11-28 | Celanese EVA Performance Polymers Corporation | Implantable device for sustained release of a macromolecular drug compound |
| JP2023552149A (ja) | 2020-11-30 | 2023-12-14 | ヤンセン ファーマシューティカ エヌ．ベー． | 持続放出パリペリドン注射可能製剤に関連する投与レジメン |
| US11439647B2 (en) | 2020-11-30 | 2022-09-13 | Janssen Pharmaceutica Nv | Dosing regimens associated with extended release paliperidone injectable formulations |
| FI4025188T3 (fi) | 2020-11-30 | 2024-02-21 | Janssen Pharmaceutica Nv | Pitkävaikutteisiin injektoitaviin paliperidoniformulaatioihin liittyviä annosteluohjelmia |
| TW202313047A (zh) | 2021-09-21 | 2023-04-01 | 西班牙商禾霏藥品實驗室有限公司 | 抗精神病可注射儲積型組合物 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2819769C (en) * | 2003-07-18 | 2016-06-28 | Oakwood Laboratories, L.L.C. | Prevention of molecular weight reduction of the polymer, impurity formation and gelling in polymer compositions |
| ATE401868T1 (de) | 2004-08-04 | 2008-08-15 | Alza Corp | ZUSAMMENSETZUNG MIT VERZÖGERTER ARZNEIMITTELFREISETZUNG MIT EINEM AUFSTEIGENDEN NULLORDNUNG-FREIGABE-MUSTER; VERFAHREN ZUR HERSTELLUNG EINER SOLCHEN ZUSAMMENSETZUNGß |
| US8852638B2 (en) * | 2005-09-30 | 2014-10-07 | Durect Corporation | Sustained release small molecule drug formulation |
| US8314110B2 (en) | 2007-04-19 | 2012-11-20 | Youxin Li | Compounds for treating mental disorders, and preparation and uses thereof |
| CA2687979C (en) * | 2007-05-25 | 2017-07-04 | Tolmar Therapeutics, Inc. | Sustained delivery formulations of risperidone compounds |
| US20090036470A1 (en) | 2007-07-27 | 2009-02-05 | Jiri Bartl | Paliperidone derivatives |
| ES2868353T3 (es) | 2007-12-19 | 2021-10-21 | Janssen Pharmaceutica Nv | Régimen de dosificación asociado a ésteres de paliperidona inyectables de larga acción |
| WO2011042453A1 (en) | 2009-10-06 | 2011-04-14 | Ascendis Pharma As | Subcutaneous paliperidone composition |
| ES2589106T3 (es) | 2010-05-31 | 2016-11-10 | Laboratorios Farmaceuticos Rovi, S.A. | Composición inyectable antipsicótica de liberación controlada |
| LT2394663T (lt) * | 2010-05-31 | 2022-02-10 | Laboratorios Farmaceuticos Rovi, S.A. | Kompozicijos, skirtos įšvirkščiamiems in situ biologiškai skaidiems implantams |
| SI2529756T1 (sl) * | 2011-05-31 | 2021-09-30 | Laboratorios Farmaceuticos Rovi, S.A. | Formulacija vsadka z risperidonom in/ali paliperidonom |
| ES2456917T3 (es) * | 2011-05-31 | 2014-04-24 | Laboratorios Farmacéuticos Rovi, S.A. | Formulación de implante de paliperidona |
-
2012
- 2012-05-31 ES ES12170366.4T patent/ES2456917T3/es active Active
- 2012-05-31 SI SI201230022T patent/SI2529757T1/sl unknown
- 2012-05-31 EP EP12170366.4A patent/EP2529757B1/en active Active
- 2012-05-31 PT PT121703664T patent/PT2529757E/pt unknown
- 2012-05-31 DK DK12170366.4T patent/DK2529757T3/en active
- 2012-05-31 PL PL12170366T patent/PL2529757T3/pl unknown
-
2013
- 2013-05-31 BR BR112014029208A patent/BR112014029208B1/pt active IP Right Grant
- 2013-05-31 EA EA201401348A patent/EA029921B1/ru unknown
- 2013-05-31 CN CN201910004281.0A patent/CN109966239A/zh active Pending
- 2013-05-31 MX MX2014014484A patent/MX365097B/es active IP Right Grant
- 2013-05-31 KR KR1020147036778A patent/KR101892496B1/ko active IP Right Grant
- 2013-05-31 IN IN10673DEN2014 patent/IN2014DN10673A/en unknown
- 2013-05-31 NZ NZ703319A patent/NZ703319A/en unknown
- 2013-05-31 UA UAA201414185A patent/UA115987C2/uk unknown
- 2013-05-31 MY MYPI2014703550A patent/MY181549A/en unknown
- 2013-05-31 WO PCT/EP2013/061319 patent/WO2013178811A1/en active Application Filing
- 2013-05-31 AU AU2013269546A patent/AU2013269546B2/en active Active
- 2013-05-31 JP JP2015514532A patent/JP6430933B2/ja active Active
- 2013-05-31 CA CA2874702A patent/CA2874702C/en active Active
- 2013-05-31 SG SG11201407971QA patent/SG11201407971QA/en unknown
- 2013-05-31 CN CN201380028041.5A patent/CN104349792A/zh active Pending
-
2014
- 2014-02-19 HR HRP20140158AT patent/HRP20140158T1/hr unknown
- 2014-02-26 CY CY20141100156T patent/CY1114975T1/el unknown
- 2014-04-03 SM SM201400044T patent/SMT201400044B/xx unknown
- 2014-11-23 IL IL235850A patent/IL235850A0/en active IP Right Grant
- 2014-11-26 CL CL2014003215A patent/CL2014003215A1/es unknown
- 2014-11-28 PH PH12014502668A patent/PH12014502668A1/en unknown
- 2014-12-16 MA MA37661A patent/MA37661B1/fr unknown
- 2014-12-17 ZA ZA2014/09297A patent/ZA201409297B/en unknown
- 2014-12-30 CO CO14285846A patent/CO7160109A2/es unknown
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