HRP20140158T1 - Formulacija paliperidon implantata - Google Patents

Formulacija paliperidon implantata Download PDF

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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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HR
Croatia
Prior art keywords
formulation
range
kda
molecular weight
drug
Prior art date
Application number
HRP20140158AT
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English (en)
Inventor
Aduriz Ibon Gutierro
Rodriguez Guillermo Franco
Original Assignee
Laboratorios Farmaceuticos Rovi, S.A.
Priority date (The priority date 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 date listed.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47074463&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20140158(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from PCT/EP2011/059000 external-priority patent/WO2011151355A1/en
Priority claimed from PCT/EP2011/059001 external-priority patent/WO2011151356A2/en
Application filed by Laboratorios Farmaceuticos Rovi, S.A. filed Critical Laboratorios Farmaceuticos Rovi, S.A.
Publication of HRP20140158T1 publication Critical patent/HRP20140158T1/hr

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants

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  • 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)
  • Dermatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (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.
HRP20140158AT 2011-05-31 2014-02-19 Formulacija paliperidon implantata HRP20140158T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/EP2011/059000 WO2011151355A1 (en) 2010-05-31 2011-05-31 Antipsychotic injectable depot composition
PCT/EP2011/059001 WO2011151356A2 (en) 2010-05-31 2011-05-31 Methods for the preparation of injectable depot compositions
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) CN104349792A (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)

* Cited by examiner, † Cited by third party
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
ES2589106T3 (es) 2010-05-31 2016-11-10 Laboratorios Farmaceuticos Rovi, S.A. Composición inyectable antipsicótica de liberación controlada
PT2394663T (pt) 2010-05-31 2021-11-26 Farm Rovi Lab Sa Composições para implantes biodegradáveis injectáveis
US10463607B2 (en) 2010-05-31 2019-11-05 Laboratorios Farmaceutics Rofi S.A. Antipsychotic Injectable Depot Composition
US10881605B2 (en) 2010-05-31 2021-01-05 Laboratorios Farmaceuticos Rovi, S.A. Methods for the preparation of injectable depot compositions
ES2456917T3 (es) * 2011-05-31 2014-04-24 Laboratorios Farmacéuticos Rovi, S.A. Formulación de implante de paliperidona
LT2529756T (lt) * 2011-05-31 2021-07-26 Laboratorios Farmaceuticos Rovi, S.A. Risperidono ir (arba) paliperidono implantų kompozicija
HUE049485T2 (hu) 2015-04-07 2020-09-28 Janssen Pharmaceuticals Inc Adagolási rend hosszan ható, injektálható paliperidon-észterek beadásának elmaradása esetén
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
AU2017319728A1 (en) * 2016-08-31 2019-02-07 Mapi Pharma Ltd Depot systems comprising glatiramer acetate
AU2018354431B2 (en) * 2017-10-27 2024-01-18 Geneora Pharma (Shijiazhuang) Co., Ltd. Dosage regimen of paliperidone palmitate extended-release injectable suspension
WO2019226516A1 (en) 2018-05-24 2019-11-28 Celanese EVA Performance Polymers Corporation Implantable device for sustained release of a macromolecular drug compound
JP2021524840A (ja) 2018-05-24 2021-09-16 セラニーズ・イーブイエイ・パフォーマンス・ポリマーズ・エルエルシー 高分子薬剤化合物の持続放出用の埋め込み型デバイス
SI4025187T1 (sl) 2020-11-30 2024-03-29 Janssen Pharmaceutica Nv Režimi odmerjanja, povezani s formulacijami paliperidona za injiciranje s podaljšanim sproščanjem
AU2021389587A1 (en) 2020-11-30 2023-07-13 Janssen Pharmaceutica Nv Dosing regimens associated with extended release paliperidone injectable formulations
HRP20240074T1 (hr) 2020-11-30 2024-03-29 Janssen Pharmaceutica Nv Režimi za doziranje povezani s injektibilnim formulacijama paliperidona s produljenim oslobađanjem
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)

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Publication number Priority date Publication date Assignee Title
CA2915574C (en) * 2003-07-18 2017-02-07 Oakwood Laboratories, L.L.C. Prevention of molecular weight reduction of the polymer, impurity formation and gelling in polymer compositions
NZ552841A (en) 2004-08-04 2009-07-31 Alza Corp Controlled release dosage form comprising two layers, wherein the delay layer is substanially free of non-microencapsulated drug
US8852638B2 (en) * 2005-09-30 2014-10-07 Durect Corporation Sustained release small molecule drug formulation
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ES2562878T3 (es) * 2007-05-25 2016-03-08 Indivior Uk Limited Formulaciones de liberación sostenida de compuestos de risperidona
EP2178872A1 (en) 2007-07-27 2010-04-28 Synthon B.V. Paliperidone derivatives
BRPI0821408A2 (pt) 2007-12-19 2015-06-16 Janssen Pharmaceutica Nv Regime de dosagem associado a ésteres de paliperidona injetáveis de longa ação
US8758780B2 (en) 2009-10-06 2014-06-24 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
PT2394663T (pt) * 2010-05-31 2021-11-26 Farm Rovi Lab Sa Composições para implantes biodegradáveis injectáveis
ES2456917T3 (es) * 2011-05-31 2014-04-24 Laboratorios Farmacéuticos Rovi, S.A. Formulación de implante de paliperidona
LT2529756T (lt) * 2011-05-31 2021-07-26 Laboratorios Farmaceuticos Rovi, S.A. Risperidono ir (arba) paliperidono implantų kompozicija

Also Published As

Publication number Publication date
CA2874702A1 (en) 2013-12-05
PH12014502668B1 (en) 2015-02-02
WO2013178811A1 (en) 2013-12-05
EA029921B1 (ru) 2018-05-31
EP2529757A1 (en) 2012-12-05
MX2014014484A (es) 2015-02-24
ZA201409297B (en) 2015-12-23
SG11201407971QA (en) 2014-12-30
AU2013269546A1 (en) 2015-01-22
PL2529757T3 (pl) 2014-04-30
KR20150015020A (ko) 2015-02-09
IL235850A0 (en) 2015-01-29
BR112014029208A2 (pt) 2017-06-27
EA201401348A1 (ru) 2015-04-30
KR101892496B1 (ko) 2018-10-04
MA37661B1 (fr) 2016-12-30
EP2529757B1 (en) 2014-01-08
CL2014003215A1 (es) 2015-07-10
AU2013269546B2 (en) 2017-12-14
CN104349792A (zh) 2015-02-11
CA2874702C (en) 2021-05-11
CN109966239A (zh) 2019-07-05
BR112014029208B1 (pt) 2020-04-07
UA115987C2 (uk) 2018-01-25
NZ703319A (en) 2016-12-23
MY181549A (en) 2020-12-28
DK2529757T3 (en) 2014-02-24
PT2529757E (pt) 2014-02-27
MX365097B (es) 2019-05-22
JP6430933B2 (ja) 2018-11-28
SMT201400044B (it) 2014-05-07
JP2015518035A (ja) 2015-06-25
ES2456917T3 (es) 2014-04-24
PH12014502668A1 (en) 2015-02-02
MA37661A1 (fr) 2016-03-31
IN2014DN10673A (hr) 2015-08-28
SI2529757T1 (sl) 2014-05-30
CO7160109A2 (es) 2015-01-15
CY1114975T1 (el) 2016-12-14

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