AR090187A1 - Procedimiento de elaboracion de microcapsulas entericas de alginato por gelacion ionica que contienen diclofenac o una de sus sales y composicion farmaceutica multiparticulada que las contiene - Google Patents
Procedimiento de elaboracion de microcapsulas entericas de alginato por gelacion ionica que contienen diclofenac o una de sus sales y composicion farmaceutica multiparticulada que las contieneInfo
- Publication number
- AR090187A1 AR090187A1 ARP130100626A ARP130100626A AR090187A1 AR 090187 A1 AR090187 A1 AR 090187A1 AR P130100626 A ARP130100626 A AR P130100626A AR P130100626 A ARP130100626 A AR P130100626A AR 090187 A1 AR090187 A1 AR 090187A1
- Authority
- AR
- Argentina
- Prior art keywords
- microcapsules
- pharmaceutical composition
- diclofenac
- salts
- enteric
- Prior art date
Links
Classifications
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- 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
-
- 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
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- 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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
- A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5089—Processes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dispersion Chemistry (AREA)
- Nutrition Science (AREA)
- Zoology (AREA)
- Physiology (AREA)
- Inorganic Chemistry (AREA)
- Rheumatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pain & Pain Management (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un procedimiento que permite la elaboración de microcápsulas entéricas sin recubrimiento, que contienen diclofenac o una de sus sales de uso oral (sódica, potásica, epolamina) que poseen actividad antiinflamatoria satisfactoria y baja agresividad gástrica; y una composición farmacéutica que las contiene. El procedimiento comprende cuatro etapas que consisten en a) preparar una mezcla en agua-etanol que contiene alginato de sodio, incorporar diclofenac o una de sus sales previamente disuelto completamente en presencia de un tensioactivo y bicarbonato de sodio; b) incorporar lentamente la solución anterior sobre una solución formada por una sal de calcio soluble en agua para producir la gelificación; c) resuspender las microcápsulas obtenidas y aisladas en solución acuosa al 1/1000 de alginato de sodio; y d) las microcápsulas así obtenidas se aíslan y previo secado se tamizan por mallas de 1000 y 250 mm; y se selecciona específicamente la fracción comprendida entre ambas mallas para la elaboración de la composición farmacéutica de elección descartando el resto. La composición farmacéutica que contiene las microcápsulas entéricas mencionadas (que determinan mucoprotección local) se puede presentar bajo la forma de cápsulas de uso oral, comprimidos, comprimidos masticables, o polvo para suspensión en agua en forma previa a su administración al paciente. También se refiere a composiciones farmacéuticas que contienen las microcápsulas entéricas sin agregados de recubrimientos, de diclofenac asociadas a inhibidores de la bomba protónica (por ejemplo, omeprazol) industrialmente conocidos y disponibles bajo la forma de pellets entéricos en composición farmacéutica de uso oral que contiene ambos principios activos en la misma composición. Reivindicación 1: Procedimiento de elaboración de microcápsulas entéricas de alginato de calcio de composición homogénea que contienen diclofenac o una de sus sales, caracterizado por las siguientes etapas: A) preparar una solución de una sal de alginato seleccionada entre alginato de sodio, potasio o amonio y disolver bajo agitación diclofenac o una de sus sales en presencia de un tensioactivo seleccionado entre sorbitan monoestearato, sorbitan monooleato, polioxietilen sorbitan monoestearato, polioxietilen sorbitan monooleato; polioxietilen sorbitan monolaurato; y bicarbonato de sodio a temperatura inferior a 60ºC; B) incorporar la solución obtenida en A) a una solución de cloruro de calcio controlando la temperatura inferior a 60ºC, durante todo el proceso; C) resuspender las microcápsulas formadas y aisladas sin secado previo en solución de alginato de sodio entre 0,05 y 0,1%, en agitación durante 30 a 120 minutos a temperatura ambiente; D) separar por filtración, secar y tamizar sucesivamente por mallas 1000 y 250 mm, seleccionando para la elaboración de la composición farmacéutica solamente la fracción de microcápsulas obtenidas y de tamaño comprendido entre ambas mallas; en donde las microcápsulas obtenidas y seleccionadas tienen contenido de principio activo superior al 55%; E) y opcionalmente, convertir las microcápsulas así obtenidas en microcápsulas de liberación prolongada. Reivindicación 12: Composición farmacéutica multilparticulada de uso oral bajo la forma de cápsulas caracterizada porque comprende entre 25 a 100 mg de diclofenac o una de sus sales sódica, potásica o de epolamina bajo la forma de microcápsulas entéricas elaboradas de acuerdo a las reivindicaciones 1 a 11.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/EP2012/054904 WO2013139377A1 (en) | 2012-03-20 | 2012-03-20 | Method for producing enteric alginate microcapsules via ionic gelation containing diclofenac or one of the salts thereof and multiparticled pharmaceutical composition containing them |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR090187A1 true AR090187A1 (es) | 2014-10-22 |
Family
ID=45855800
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130100626A AR090187A1 (es) | 2012-03-20 | 2013-02-27 | Procedimiento de elaboracion de microcapsulas entericas de alginato por gelacion ionica que contienen diclofenac o una de sus sales y composicion farmaceutica multiparticulada que las contiene |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US9668978B2 (es) |
| EP (1) | EP2827843B1 (es) |
| CN (1) | CN104244927B (es) |
| AR (1) | AR090187A1 (es) |
| CA (1) | CA2899664C (es) |
| CL (2) | CL2014002465A1 (es) |
| ES (1) | ES2584403T3 (es) |
| MX (1) | MX354454B (es) |
| PH (1) | PH12014501981B1 (es) |
| PL (1) | PL2827843T3 (es) |
| SG (1) | SG11201505320TA (es) |
| UA (1) | UA112345C2 (es) |
| WO (1) | WO2013139377A1 (es) |
| ZA (1) | ZA201406886B (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2017012643A (es) * | 2015-03-31 | 2018-08-01 | Laboratorios Bago S A | Procedimiento de elaboracion de pellets entericos que contienen un inhibidor de la bomba protonica y composiciones farmaceuticas multiparticuladas que los contienen. |
| WO2017084680A1 (en) * | 2015-11-17 | 2017-05-26 | Rontis Hellas S.A. | Pharmaceutical composition containing a non-steroidal antiinflammatory drug and a proton pump inhibitor |
| CN109498571B (zh) * | 2018-11-19 | 2019-09-10 | 朗天药业(湖北)有限公司 | 一种艾司奥美拉唑钠缓释微球及其制备方法 |
| TW202126301A (zh) | 2019-10-04 | 2021-07-16 | 愛爾蘭商席歐拉斯製藥有限公司 | 小兒懸浮調配物 |
| CN112494450A (zh) * | 2020-12-12 | 2021-03-16 | 海南海神同洲制药有限公司 | 化学药专用口腔崩解片包覆结构及其制备方法 |
| CN115317464B (zh) * | 2022-09-01 | 2023-08-08 | 苏州弘森药业股份有限公司 | 一种双氯芬酸钾微胶囊及其制备方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0520119A1 (de) | 1991-06-17 | 1992-12-30 | Spirig Ag Pharmazeutische Präparate | Neue orale Diclofenaczubereitung |
| NZ253999A (en) | 1992-08-05 | 1996-07-26 | Faulding F H & Co Ltd | Pelletised substained release medicament |
| ES2068762B1 (es) | 1993-07-21 | 1995-12-01 | Lipotec Sa | Un nuevo preparado farmaceutico para mejorar la biodisponibilidad de drogas de dificil absorcion y procedimiento para su obtencion. |
| US6096344A (en) * | 1995-07-28 | 2000-08-01 | Advanced Polymer Systems, Inc. | Bioerodible porous compositions |
| SE9600070D0 (sv) * | 1996-01-08 | 1996-01-08 | Astra Ab | New oral pharmaceutical dosage forms |
| US7687542B2 (en) * | 1996-05-17 | 2010-03-30 | Kowa Pharmaeuticals America, Inc. | Rapidly bioavailable tablet and capsule formulations of diclofenac |
| US6544556B1 (en) * | 2000-09-11 | 2003-04-08 | Andrx Corporation | Pharmaceutical formulations containing a non-steroidal antiinflammatory drug and a proton pump inhibitor |
| AR044398A1 (es) | 2004-05-19 | 2005-09-14 | Bago Sa Labor | Procedimiento para la elaboracion de microcapsulas recubiertas que contienen agentes farmacologicamente activos y composiciones farmaceuticas conteniendo dichas microcapsulas". |
-
2012
- 2012-03-20 CN CN201280071655.7A patent/CN104244927B/zh not_active Expired - Fee Related
- 2012-03-20 PL PL12709640.2T patent/PL2827843T3/pl unknown
- 2012-03-20 EP EP12709640.2A patent/EP2827843B1/en active Active
- 2012-03-20 WO PCT/EP2012/054904 patent/WO2013139377A1/en active Application Filing
- 2012-03-20 US US14/386,377 patent/US9668978B2/en active Active
- 2012-03-20 UA UAA201410294A patent/UA112345C2/uk unknown
- 2012-03-20 MX MX2014011289A patent/MX354454B/es active IP Right Grant
- 2012-03-20 ES ES12709640.2T patent/ES2584403T3/es active Active
- 2012-03-20 SG SG11201505320TA patent/SG11201505320TA/en unknown
- 2012-03-20 CA CA2899664A patent/CA2899664C/en active Active
-
2013
- 2013-02-27 AR ARP130100626A patent/AR090187A1/es not_active Application Discontinuation
-
2014
- 2014-09-05 PH PH12014501981A patent/PH12014501981B1/en unknown
- 2014-09-17 CL CL2014002465A patent/CL2014002465A1/es unknown
- 2014-09-19 ZA ZA2014/06886A patent/ZA201406886B/en unknown
-
2016
- 2016-12-27 CL CL2016003348A patent/CL2016003348A1/es unknown
-
2017
- 2017-03-09 US US15/454,127 patent/US9918941B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| PH12014501981A1 (en) | 2014-11-24 |
| MX354454B (es) | 2018-03-06 |
| PL2827843T3 (pl) | 2016-11-30 |
| EP2827843B1 (en) | 2016-05-25 |
| US9668978B2 (en) | 2017-06-06 |
| CA2899664A1 (en) | 2013-09-26 |
| ZA201406886B (en) | 2015-06-24 |
| ES2584403T3 (es) | 2016-09-27 |
| EP2827843A1 (en) | 2015-01-28 |
| US20150072000A1 (en) | 2015-03-12 |
| CN104244927A (zh) | 2014-12-24 |
| SG11201505320TA (en) | 2015-08-28 |
| CA2899664C (en) | 2019-07-09 |
| US9918941B2 (en) | 2018-03-20 |
| WO2013139377A1 (en) | 2013-09-26 |
| CL2014002465A1 (es) | 2015-05-08 |
| CN104244927B (zh) | 2017-03-15 |
| UA112345C2 (uk) | 2016-08-25 |
| PH12014501981B1 (en) | 2014-11-24 |
| MX2014011289A (es) | 2015-02-17 |
| US20170172934A1 (en) | 2017-06-22 |
| CL2016003348A1 (es) | 2018-03-23 |
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Legal Events
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| FC | Refusal |