HRP20171402T4 - Priprava polilaktidno-poliglikolidnih mikročestica sa sigmoidnim profilom oslobađanja - Google Patents
Priprava polilaktidno-poliglikolidnih mikročestica sa sigmoidnim profilom oslobađanja Download PDFInfo
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- HRP20171402T4 HRP20171402T4 HRP20171402TT HRP20171402T HRP20171402T4 HR P20171402 T4 HRP20171402 T4 HR P20171402T4 HR P20171402T T HRP20171402T T HR P20171402TT HR P20171402 T HRP20171402 T HR P20171402T HR P20171402 T4 HRP20171402 T4 HR P20171402T4
- Authority
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- Croatia
- Prior art keywords
- phase
- microparticles
- organic solvent
- preparation
- risperidone
- Prior art date
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- 239000011859 microparticle Substances 0.000 title claims 16
- 238000002360 preparation method Methods 0.000 title claims 10
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 title 1
- 229920000954 Polyglycolide Polymers 0.000 title 1
- 239000012071 phase Substances 0.000 claims 22
- 239000003960 organic solvent Substances 0.000 claims 11
- 229920000642 polymer Polymers 0.000 claims 10
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims 9
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims 9
- 229960001534 risperidone Drugs 0.000 claims 9
- 238000000034 method Methods 0.000 claims 7
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 claims 7
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 6
- 238000001035 drying Methods 0.000 claims 6
- 229920002451 polyvinyl alcohol Polymers 0.000 claims 6
- 238000005406 washing Methods 0.000 claims 6
- 239000000243 solution Substances 0.000 claims 5
- 239000008346 aqueous phase Substances 0.000 claims 4
- 239000000839 emulsion Substances 0.000 claims 4
- JJTUDXZGHPGLLC-IMJSIDKUSA-N 4511-42-6 Chemical compound C[C@@H]1OC(=O)[C@H](C)OC1=O JJTUDXZGHPGLLC-IMJSIDKUSA-N 0.000 claims 3
- 239000012062 aqueous buffer Substances 0.000 claims 3
- 230000001804 emulsifying effect Effects 0.000 claims 3
- 238000000926 separation method Methods 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
- PXIPVTKHYLBLMZ-UHFFFAOYSA-N Sodium azide Chemical compound [Na+].[N-]=[N+]=[N-] PXIPVTKHYLBLMZ-UHFFFAOYSA-N 0.000 claims 2
- 238000010791 quenching Methods 0.000 claims 2
- 230000000171 quenching effect Effects 0.000 claims 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J3/00—Processes of treating or compounding macromolecular substances
- C08J3/12—Powdering or granulating
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J3/00—Processes of treating or compounding macromolecular substances
- C08J3/12—Powdering or granulating
- C08J3/14—Powdering or granulating by precipitation from solutions
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J2300/00—Characterised by the use of unspecified polymers
- C08J2300/16—Biodegradable polymers
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08J—WORKING-UP; GENERAL PROCESSES OF COMPOUNDING; AFTER-TREATMENT NOT COVERED BY SUBCLASSES C08B, C08C, C08F, C08G or C08H
- C08J2367/00—Characterised by the use of polyesters obtained by reactions forming a carboxylic ester link in the main chain; Derivatives of such polymers
- C08J2367/04—Polyesters derived from hydroxy carboxylic acids, e.g. lactones
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Polymers & Plastics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (7)
1. Postupak za pripravu biorazgradivih mikročestica poli (D,L-laktidkoglikolid) polimera (PLGA), koji ima sigmoidni profil oslobađanja risperidona koji se nalazi unutar mikročestica, naznačen time da obuhvaća slijedeće korake:
a. priprema unutarnje uljne faze otapanjem PLGA polimera i risperidona u organskom otapalu koje je diklorometan, pri čemu je koncentracija polimera u unutarnjoj uljnoj fazi u rasponu od 5-8% w/w;
b. priprema vanjske vodene faze koja se sastoji od vode, polivinil alkohola (PVA), po izboru vodene otopine pufera za podešavanje pH vrijednosti na vrijednost kod koje risperidon pokazuje nižu topljivost te istog organskog otapala koje se koristi u uljnoj fazi, pri čemu je količina organskog otapala dodana u vanjsku fazu dovoljna za zasićivanje vanjske faze;
c. emulgiranje unutarnje faze u vanjsku fazu ili mehaničkim miješanjem ili upotrebom homogenizatora s visokim smicanjem;
d. prijenos emulzije u medij za gašenje koji ima temperaturu postavljenu na 5°C a koji je termostatski kontroliran;
e. odvajanje dobivenih stvrdnutih mikročestica i po izboru pranje mikročestica, i
f. sušenje mikročestica u jednom koraku bez daljnjeg koraka pranja i / ili sušenja.
2. Postupak za pripravu biorazgradivih mikročestica poli (D,L-laktidkoglikolid) polimera (PLGA), koji ima sigmoidni profil oslobađanja risperidona koji se nalazi unutar mikročestica, koji obuhvaća slijedeće korake:
a. priprema unutarnje uljne faze koja ima viskoznost od 10-1000 cP otapanjem PLGA polimera i risperidona u organskom otapalu koje je diklorometan, pri čemu je koncentracija polimera u unutarnjoj uljnoj fazi u rasponu od 5-40% w/w;
b. priprema vanjske vodene faze koja se sastoji od vode, polivinil alkohola (PVA), po izboru vodene otopine pufera za podešavanje pH vrijednosti na vrijednost kod koje risperidon pokazuje nižu topljivost te istog organskog otapala koje se koristi u uljnoj fazi, pri čemu je količina organskog otapala dodana u vanjsku fazu dovoljna za zasićenje vanjske faze;
c. emulgiranje unutarnje faze u vanjsku fazu ili mehaničkim miješanjem ili upotrebom homogenizatora s visokim smicanjem;
d. prijenos emulzije u medij za gašenje koji ima temperaturu postavljenu na 30-40°C a koji je termostatski kontroliran;
e. odvajanje dobivenih stvrdnutih mikročestica i po izboru pranje mikročestica, i
f. sušenje mikročestica u jednom koraku bez daljnjeg koraka pranja i / ili sušenja.
3. Postupak za pripravu biorazgradivih mikročestica poli (D,L-laktidkoglikolid) polimera (PLGA), koji ima sigmoidni profil oslobađanja risperidona koji se nalazi unutar mikročestica, koji obuhvaća slijedeće korake:
a. priprema unutarnje uljne faze koja ima viskoznost od 10-1000 cP otapanjem PLGA polimera i risperidona u organskom otapalu koje je diklorometan, pri čemu je koncentracija polimera u unutarnjoj uljnoj fazi u rasponu od 5-40% w/w;
b. priprema vanjske vodene faze koja se sastoji od vode, polivinil alkohola (PVA), po izboru vodene otopine pufera za podešavanje pH vrijednosti na vrijednost kod koje risperidon pokazuje nižu topljivost te istog organskog otapala koje se koristi u uljnoj fazi, pri čemu se organsko otapalo dodaje u količini 2-10 puta iznad točke zasićenja;
c. emulgiranje unutarnje faze u vanjsku fazu ili mehaničkim miješanjem ili upotrebom homogenizatora s visokim smicanjem;
d. prijenos emulzije u medij za gašenje koji ima temperaturu postavljenu na 5°C a koji je termostatski kontroliran;
e. odvajanje dobivenih stvrdnutih mikročestica i po izboru pranje mikročestica, i
f. sušenje mikročestica u jednom koraku bez daljnjeg koraka pranja i / ili sušenja.
4. Postupak prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time da je volumen medija za gašenje od 0,7 do 3 puta volumena potrebnog za otapanje cijelog organskog otapala iz uljnih mikrokapi emulzije.
5. Postupak prema bilo kojem od patentnih zahtjeva 2 ili 3, naznačen time da koncentracija PLGA polimera iznosi 5-15%, osiguravajući viskoznost otopine od 10-100 cP.
6. Postupak prema patentnom zahtjevu 3, naznačen time da je količina organskog otapala 4 do 6 puta veća od količine otapala koja se može otopiti u volumenu vodene faze.
7. Postupak prema bilo kojem od prethodnih patentnih zahtjeva, pri čemu je sigmoidno oslobađanje in vitro profil oslobađanja naznačen početnom usporenom fazom, strmom srednjom fazom oslobađanja i ravnom fazom krajnjeg oslobađanja kako je određeno u USP-II aparatu koristeći kao sredstvo za otpuštanje 1000 ml fiziološke otopine pH 7.4 koja sadrži 0.03% natrijevog azida, temperatura se kontrolira na 37°C, a brzina lopatice se namjesti na 100 okretaja u minuti.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2013001821 | 2013-06-20 | ||
| PCT/EP2014/001652 WO2014202214A1 (en) | 2013-06-20 | 2014-06-18 | Preparation of polylactide-polyglycolide microparticles having a sigmoidal release profile |
| EP14733524.4A EP3010962B2 (en) | 2013-06-20 | 2014-06-18 | Preparation of polylactide-polyglycolide microparticles having a sigmoidal release profile |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20171402T1 HRP20171402T1 (hr) | 2017-11-03 |
| HRP20171402T4 true HRP20171402T4 (hr) | 2023-07-21 |
Family
ID=55532293
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20171402TT HRP20171402T4 (hr) | 2013-06-20 | 2014-06-18 | Priprava polilaktidno-poliglikolidnih mikročestica sa sigmoidnim profilom oslobađanja |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP3010962B2 (hr) |
| CY (1) | CY1119397T1 (hr) |
| HR (1) | HRP20171402T4 (hr) |
| PL (1) | PL3010962T5 (hr) |
| RS (1) | RS56427B2 (hr) |
| SI (1) | SI3010962T2 (hr) |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5792477A (en) | 1996-05-07 | 1998-08-11 | Alkermes Controlled Therapeutics, Inc. Ii | Preparation of extended shelf-life biodegradable, biocompatible microparticles containing a biologically active agent |
| US6194006B1 (en) | 1998-12-30 | 2001-02-27 | Alkermes Controlled Therapeutics Inc. Ii | Preparation of microparticles having a selected release profile |
| US6331317B1 (en) | 1999-11-12 | 2001-12-18 | Alkermes Controlled Therapeutics Ii Inc. | Apparatus and method for preparing microparticles |
| US6264987B1 (en) | 2000-05-19 | 2001-07-24 | Alkermes Controlled Therapeutics Inc. Ii | Method for preparing microparticles having a selected polymer molecular weight |
-
2014
- 2014-06-18 PL PL14733524.4T patent/PL3010962T5/pl unknown
- 2014-06-18 RS RS20171034A patent/RS56427B2/sr unknown
- 2014-06-18 SI SI201430366T patent/SI3010962T2/sl unknown
- 2014-06-18 HR HRP20171402TT patent/HRP20171402T4/hr unknown
- 2014-06-18 EP EP14733524.4A patent/EP3010962B2/en active Active
-
2017
- 2017-09-27 CY CY20171101018T patent/CY1119397T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SI3010962T1 (sl) | 2017-10-30 |
| EP3010962A1 (en) | 2016-04-27 |
| HRP20171402T1 (hr) | 2017-11-03 |
| EP3010962B2 (en) | 2023-02-08 |
| PL3010962T5 (pl) | 2023-05-15 |
| CY1119397T1 (el) | 2018-02-14 |
| SI3010962T2 (sl) | 2023-04-28 |
| EP3010962B1 (en) | 2017-07-26 |
| RS56427B2 (sr) | 2023-04-28 |
| RS56427B1 (sr) | 2018-01-31 |
| PL3010962T3 (pl) | 2018-01-31 |
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