AR127101A1 - INJECTABLE EXTENDED-RELEASE ANTIPSYCHOTIC COMPOSITION - Google Patents
INJECTABLE EXTENDED-RELEASE ANTIPSYCHOTIC COMPOSITIONInfo
- Publication number
- AR127101A1 AR127101A1 ARP220102531A ARP220102531A AR127101A1 AR 127101 A1 AR127101 A1 AR 127101A1 AR P220102531 A ARP220102531 A AR P220102531A AR P220102531 A ARP220102531 A AR P220102531A AR 127101 A1 AR127101 A1 AR 127101A1
- Authority
- AR
- Argentina
- Prior art keywords
- micrometers
- particle size
- measured
- exceeding
- distribution
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 5
- 230000000561 anti-psychotic effect Effects 0.000 title 1
- 238000013265 extended release Methods 0.000 title 1
- 239000002245 particle Substances 0.000 abstract 16
- 238000002050 diffraction method Methods 0.000 abstract 4
- 229920001606 poly(lactic acid-co-glycolic acid) Polymers 0.000 abstract 4
- 229940079593 drug Drugs 0.000 abstract 3
- 239000003814 drug Substances 0.000 abstract 3
- 239000000843 powder Substances 0.000 abstract 3
- 238000007873 sieving Methods 0.000 abstract 3
- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 abstract 1
- 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 abstract 1
- JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 abstract 1
- 239000000178 monomer Substances 0.000 abstract 1
- 229960001057 paliperidone Drugs 0.000 abstract 1
- 229920000642 polymer Polymers 0.000 abstract 1
- 229960001534 risperidone Drugs 0.000 abstract 1
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 238000013268 sustained release Methods 0.000 abstract 1
- 239000012730 sustained-release form Substances 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L11/00—Pulses, i.e. fruits of leguminous plants, for production of food; Products from legumes; Preparation or treatment thereof
- A23L11/05—Mashed or comminuted pulses or legumes; Products made therefrom
-
- 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
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L3/00—Preservation of foods or foodstuffs, in general, e.g. pasteurising, sterilising, specially adapted for foods or foodstuffs
- A23L3/40—Preservation of foods or foodstuffs, in general, e.g. pasteurising, sterilising, specially adapted for foods or foodstuffs by drying or kilning; Subsequent reconstitution
- A23L3/44—Freeze-drying
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- 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
Abstract
Se proporciona una composición de liberación sostenida inyectable de acción prolongada que tiene al menos fármaco, disolvente y copolímero PLGA. La composición muestra un rendimiento farmacéutico mejorado debido al empleo de clases ventajosas de polímero PLGA con una distribución mejorada del tamaño de partícula. Reivindicación 1: Una mezcla en polvo que comprende fármaco en polvo y copolímero PLGA en polvo, caracterizado porque: a) el fármaco se selecciona del grupo que consiste en risperidona, paliperidona o una mezcla de las mismas; y b) el copolímero PLGA tiene una proporción de monómeros entre láctido (L) y glicólido (G) de 50:50 ± 10% a 75:25 ± 10%, 50:50 ± 10% o 75:25 ± 10% y tiene una distribución de tamaño de partícula seleccionada del grupo que consiste en: i) distribución de masa de tamaño de partícula con no más del 10% superior a 300 micrómetros, preferiblemente no superior a 250 micrómetros, según medida por tamizado analítico de acuerdo con USP<786>; ii) distribución de volumen de tamaño de partícula con un D₉₀ no superior a 300 micrómetros, preferiblemente no superior a 280 micrómetros según medida por análisis de difracción láser; iii) una distribución de masa de tamaño de partícula con no más del 10% superior a 300 micrómetros, preferiblemente no superior a 250 micrómetros, y en donde no más del 70% de las partículas tienen un tamaño de partícula inferior a 150 micrómetros, según medida por tamizado analítico de acuerdo con USP<786>; iv) una distribución de masa de tamaño de partícula en donde no más del 70% de las partículas tienen un tamaño de partícula inferior a 150 micrómetros, según medida por tamizado analítico de acuerdo con USP<786>; v) una distribución de volumen de tamaño de partícula con un D₉₀ no superior a 300 micrómetros, preferiblemente no superior a 280 micrómetros según medida por análisis de difracción láser y con un D₈₀ no inferior a 135 micrómetros según medida por análisis de difracción láser; vi) una distribución de volumen de tamaño de partícula con un D₈₀ no inferior a 135 micrómetros según medida por análisis de difracción láser; vii) una distribución de volumen de tamaño de partícula con un D₅₀ de aproximadamente 50 - 150 micrómetros; viii) una distribución de volumen de tamaño de partícula con un D₁₀ de aproximadamente 10 - 50 micrómetros; ix) una distribución de volumen de tamaño de partícula con un D₉₀ de aproximadamente 170 - 300 micrómetros; x) una distribución de volumen de tamaño de partícula con un D₅₀ de aproximadamente 50 - 150 micrómetros, un D₁₀ de aproximadamente 10 - 50 micrómetros y un D₉₀ de aproximadamente 170 - 300 micrómetros, y xi) una combinación de cualquiera de lo anterior.A long-acting injectable sustained release composition is provided having at least drug, solvent and PLGA copolymer. The composition shows improved pharmaceutical performance due to the employment of advantageous classes of PLGA polymer with improved particle size distribution. Claim 1: A powder mixture comprising powder drug and powder PLGA copolymer, characterized in that: a) the drug is selected from the group consisting of risperidone, paliperidone or a mixture thereof; and b) the PLGA copolymer has a monomer ratio between lactide (L) and glycolide (G) of 50:50 ± 10% to 75:25 ± 10%, 50:50 ± 10% or 75:25 ± 10% and has a particle size distribution selected from the group consisting of: i) particle size mass distribution with not more than 10% exceeding 300 micrometers, preferably not exceeding 250 micrometers, as measured by analytical sieving in accordance with USP 786>; ii) particle size volume distribution with a D₉₀ not exceeding 300 micrometers, preferably not exceeding 280 micrometers as measured by laser diffraction analysis; iii) a particle size mass distribution with no more than 10% greater than 300 micrometers, preferably no greater than 250 micrometers, and wherein no more than 70% of the particles have a particle size less than 150 micrometers, according to measured by analytical sieving in accordance with USP<786>; iv) a particle size mass distribution where no more than 70% of the particles have a particle size less than 150 micrometers, as measured by analytical sieving in accordance with USP<786>; v) a particle size volume distribution with a D₉₀ not exceeding 300 micrometers, preferably not exceeding 280 micrometers as measured by laser diffraction analysis and with a D₈₀ not less than 135 micrometers as measured by laser diffraction analysis; vi) a particle size volume distribution with a D₈₀ of not less than 135 micrometers as measured by laser diffraction analysis; vii) a particle size volume distribution with a D₅₀ of approximately 50 - 150 micrometers; viii) a particle size volume distribution with a D₁₀ of approximately 10 - 50 micrometers; ix) a particle size volume distribution with a D₉₀ of approximately 170 - 300 micrometers; x) a particle size volume distribution with a D₅₀ of approximately 50 - 150 micrometers, a D₁₀ of approximately 10 - 50 micrometers and a D₉₀ of approximately 170 - 300 micrometers, and xi) a combination of any of the above.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163246446P | 2021-09-21 | 2021-09-21 | |
| US202263310884P | 2021-09-21 | 2021-09-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR127101A1 true AR127101A1 (en) | 2023-12-20 |
Family
ID=83995229
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220102531A AR127101A1 (en) | 2021-09-21 | 2022-09-20 | INJECTABLE EXTENDED-RELEASE ANTIPSYCHOTIC COMPOSITION |
Country Status (5)
| Country | Link |
|---|---|
| AR (1) | AR127101A1 (en) |
| AU (1) | AU2022351480A1 (en) |
| CA (1) | CA3230338A1 (en) |
| TW (1) | TW202313047A (en) |
| WO (1) | WO2023046731A1 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20230372331A1 (en) * | 2022-05-18 | 2023-11-23 | Anxo Pharmaceutical Co., Ltd. | Pharmaceutical composition |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4389330A (en) | 1980-10-06 | 1983-06-21 | Stolle Research And Development Corporation | Microencapsulation process |
| US4530840A (en) | 1982-07-29 | 1985-07-23 | The Stolle Research And Development Corporation | Injectable, long-acting microparticle formulation for the delivery of anti-inflammatory agents |
| US4938763B1 (en) | 1988-10-03 | 1995-07-04 | Atrix Lab Inc | Biodegradable in-situ forming implants and method of producing the same |
| US5656297A (en) | 1992-03-12 | 1997-08-12 | Alkermes Controlled Therapeutics, Incorporated | Modulated release from biocompatible polymers |
| HU219487B (en) | 1993-11-19 | 2001-04-28 | Janssen Pharmaceutica Nv. | Microparticles containing risperidone, process for producing them, their use, medicaments containing the same and their production |
| US6331311B1 (en) | 1996-12-20 | 2001-12-18 | Alza Corporation | Injectable depot gel composition and method of preparing the composition |
| US6143314A (en) | 1998-10-28 | 2000-11-07 | Atrix Laboratories, Inc. | Controlled release liquid delivery compositions with low initial drug burst |
| US6194006B1 (en) | 1998-12-30 | 2001-02-27 | Alkermes Controlled Therapeutics Inc. Ii | Preparation of microparticles having a selected release profile |
| US6461631B1 (en) | 1999-11-16 | 2002-10-08 | Atrix Laboratories, Inc. | Biodegradable polymer composition |
| WO2001051024A2 (en) | 2000-01-11 | 2001-07-19 | Roland Bodmeier | Implantation kit comprising a support phase and a solvent |
| WO2002038185A2 (en) | 2000-11-13 | 2002-05-16 | Atrix Laboratories, Inc. | Injectable sustained release delivery system with loperamide |
| CN101057824A (en) | 2002-07-31 | 2007-10-24 | 阿尔萨公司 | Injectable multimodal polymer depot compositions and uses thereof |
| WO2004081196A2 (en) | 2003-03-11 | 2004-09-23 | Qlt Usa Inc. | Formulations for cell- schedule dependent anticancer agents |
| WO2004094415A1 (en) | 2003-04-22 | 2004-11-04 | Synthon B.V. | Risperidone monohydrochloride |
| US8221778B2 (en) | 2005-01-12 | 2012-07-17 | The Trustees Of The University Of Pennsylvania | Drug-containing implants and methods of use thereof |
| CA2553254C (en) | 2004-01-12 | 2013-12-17 | The Trustees Of The University Of Pennsylvania | Long-term delivery formulations and methods of use thereof |
| US8313763B2 (en) | 2004-10-04 | 2012-11-20 | Tolmar Therapeutics, Inc. | Sustained delivery formulations of rapamycin compounds |
| US8852638B2 (en) | 2005-09-30 | 2014-10-07 | Durect Corporation | Sustained release small molecule drug formulation |
| AU2007303793A1 (en) | 2006-10-05 | 2008-04-10 | Panacea Biotec Ltd. | Injectable depot composition and it's process of preparation |
| FR2908775B1 (en) | 2006-11-17 | 2012-08-31 | Biomatlante | HYDROGEL AND ITS BIOMEDICAL APPLICATIONS |
| HUE030789T2 (en) | 2007-05-18 | 2017-06-28 | Durect Corp | Improved depot formulations |
| NZ581862A (en) | 2007-05-25 | 2012-06-29 | Tolmar Therapeutics Inc | Injectable subcutaneous formulation comprising risperidone capable of forming a solid, microporous implant in a patient |
| US8629172B2 (en) | 2008-04-18 | 2014-01-14 | Warsaw Orthopedic, Inc. | Methods and compositions for treating post-operative pain comprising clonidine |
| ES2600797T3 (en) | 2008-08-12 | 2017-02-10 | Novartis Ag | Pharmaceutical compositions |
| WO2011042453A1 (en) | 2009-10-06 | 2011-04-14 | Ascendis Pharma As | Subcutaneous paliperidone composition |
| 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 |
| ES2897976T3 (en) | 2010-05-31 | 2022-03-03 | Farm Rovi Lab Sa | Injectable Biodegradable In Situ Implant Compositions |
| 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 |
| PL2394664T3 (en) | 2010-05-31 | 2016-12-30 | Antipsychotic injectable depot composition | |
| PL2529756T3 (en) | 2011-05-31 | 2021-11-15 | Laboratorios Farmaceuticos Rovi, S.A. | Risperidone and/or Paliperidone implant formulation |
| DK2529757T3 (en) | 2011-05-31 | 2014-02-24 | Rovi Lab Farmaceut Sa | Paliperidonimplantatformulering |
-
2022
- 2022-02-08 TW TW111104608A patent/TW202313047A/en unknown
- 2022-09-20 AR ARP220102531A patent/AR127101A1/en unknown
- 2022-09-21 WO PCT/EP2022/076186 patent/WO2023046731A1/en active Application Filing
- 2022-09-21 AU AU2022351480A patent/AU2022351480A1/en active Pending
- 2022-09-21 CA CA3230338A patent/CA3230338A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2022351480A1 (en) | 2024-03-28 |
| CA3230338A1 (en) | 2023-03-30 |
| TW202313047A (en) | 2023-04-01 |
| WO2023046731A1 (en) | 2023-03-30 |
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