CR20190245A - FORMULACIÓN DE FÁRMACO DE LIBERACIÓN RETARDADA (Divisional del Expediente 2014-0486) - Google Patents
FORMULACIÓN DE FÁRMACO DE LIBERACIÓN RETARDADA (Divisional del Expediente 2014-0486)Info
- Publication number
- CR20190245A CR20190245A CR20190245A CR20190245A CR20190245A CR 20190245 A CR20190245 A CR 20190245A CR 20190245 A CR20190245 A CR 20190245A CR 20190245 A CR20190245 A CR 20190245A CR 20190245 A CR20190245 A CR 20190245A
- Authority
- CR
- Costa Rica
- Prior art keywords
- polymeric material
- core
- drug
- inner layer
- layer comprises
- Prior art date
Links
- 230000003111 delayed effect Effects 0.000 title abstract 4
- 239000013583 drug formulation Substances 0.000 title 1
- 239000000463 material Substances 0.000 abstract 13
- 239000003814 drug Substances 0.000 abstract 8
- 229940079593 drug Drugs 0.000 abstract 8
- 239000012530 fluid Substances 0.000 abstract 8
- 239000000203 mixture Substances 0.000 abstract 6
- 239000011248 coating agent Substances 0.000 abstract 5
- 238000000576 coating method Methods 0.000 abstract 5
- 229920000831 ionic polymer Polymers 0.000 abstract 5
- 230000000112 colonic effect Effects 0.000 abstract 4
- 238000009472 formulation Methods 0.000 abstract 4
- 230000002496 gastric effect Effects 0.000 abstract 4
- 230000000968 intestinal effect Effects 0.000 abstract 4
- 238000002955 isolation Methods 0.000 abstract 3
- 241000894006 Bacteria Species 0.000 abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 239000012736 aqueous medium Substances 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 210000001072 colon Anatomy 0.000 abstract 2
- 230000008030 elimination Effects 0.000 abstract 2
- 238000003379 elimination reaction Methods 0.000 abstract 2
- 239000002609 medium Substances 0.000 abstract 2
- 238000013016 damping Methods 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000009246 food effect Effects 0.000 abstract 1
- 238000009413 insulation Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K9/5073—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 having two or more different coatings optionally including drug-containing subcoatings
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- 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
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- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/606—Salicylic acid; Derivatives thereof having amino groups
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- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
- A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
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- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
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- A61K9/2833—Organic macromolecular compounds
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- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Inorganic Chemistry (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Botany (AREA)
- Zoology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Medicinal Preparation (AREA)
- Laminated Bodies (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- General Preparation And Processing Of Foods (AREA)
- Grain Derivatives (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
La liberación retardada de un fármaco al colon se logra de una fromulación de liberación retardada que comprende un núcleo y un recubrimiento para el núcleo. El núcleo comprende un fármaco y un recubrimiento que comprende una capa interior y al menos una capa entre el núcleo y la capa exterior seleccionada del grupo que consiste de una capa de aislamiento y una capa interior. La capa exterior comprende una mezcla de un primer material polimérico que es susceptible a ataques por parte de la bacteria colónica, y un segundo material polimérico que tiene un umbral de pH a aproximadamente pH 5 o más alto. La capa interior comprende un tercer material polimérico que es soluble en el fluido intestinal o en el fluido gastrointestinal, tal tercer material polimérico se selecciona de ácido policarboxílico al menos parcialente neutralizado y un polímero no iónico. En modalidades en donde el tercer material polimérico no iónico, la capa interior comprende al menos un agente amortiguador y una base. La capa de islamiento comprende un polímero no iónico que es soluble en el fluido intestinal o fluido gastrointestinal. El exterior es u medio acuoso con um segundo material polimérico es un medio orgánico. Las ventajas de las formulaciones de acuerdo con la presente invención incluyen la liberación acelerada del fármaco cuando se expone a condiciones colónicas y la reducción o eliminación del efecto de los alimentos y/o alcohol en la liberación del fármaco después e la administración.Delayed release of a drug to the colon is achieved from a delayed release formulation comprising a core and a coating for the core. The core comprises a drug and the coating comprises an outer layer and at least one layer between the core and the outer layer selected from the group consisting of an isolation layer and an inner layer. The outer layer comprises a mixture of a first polymeric material which is susceptible to attack by colonic bacteria, and a second polymeric material which has a pH threshold at about pH 5 or above. The inner layer comprises a third polymeric material which is soluble in intestinal fluid or gastrointestinal fluid, said third polymeric material being selected from an at least partially neutralised polycarboxylic acid and a non-ionic polymer. In embodiments in which the third polymeric material is a non-ionic polymer, the inner layer comprises at least one of a buffer agent and a base. The isolation layer comprises a non-ionic polymer which is soluble in intestinal fluid or gastrointestinal fluid. The outer is applied directly to the inner layer or the isolation layer using a coating preparation formed by combining the first polymeric material in an aqueous medium with a second polymeric material in an organic medium. Advantages of formulations according to the present invention include accelerated release of the drug when exposed to colonic conditions and reduction or elimination of a food and/or alcohol effect on drug release after administration.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261640217P | 2012-04-30 | 2012-04-30 | |
| EP12166110.2A EP2659881B1 (en) | 2012-04-30 | 2012-04-30 | A delayed release drug formulation |
| PCT/EP2013/058923 WO2013164316A1 (en) | 2012-04-30 | 2013-04-29 | A delayed release drug formulation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20190245A true CR20190245A (es) | 2019-07-29 |
Family
ID=46025554
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20190245A CR20190245A (es) | 2012-04-30 | 2013-04-29 | FORMULACIÓN DE FÁRMACO DE LIBERACIÓN RETARDADA (Divisional del Expediente 2014-0486) |
| CR20190246A CR20190246A (es) | 2012-04-30 | 2013-04-29 | Formulación de fármaco de liberación retardada |
| CR20140485A CR20140485A (es) | 2012-04-30 | 2014-10-21 | Formulacion de farmaco de liberacion retardada |
| CR20140486A CR20140486A (es) | 2012-04-30 | 2014-10-21 | Formulacion de farmaco de liberacion retardada |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20190246A CR20190246A (es) | 2012-04-30 | 2013-04-29 | Formulación de fármaco de liberación retardada |
| CR20140485A CR20140485A (es) | 2012-04-30 | 2014-10-21 | Formulacion de farmaco de liberacion retardada |
| CR20140486A CR20140486A (es) | 2012-04-30 | 2014-10-21 | Formulacion de farmaco de liberacion retardada |
Country Status (41)
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2655622T3 (es) * | 2012-04-30 | 2018-02-20 | Tillotts Pharma Ag | Una formulación de fármaco de liberación retardada |
| CU24343B1 (es) * | 2012-04-30 | 2018-05-08 | Tillotts Pharma Ag | Formulación de fármaco de liberación retardada |
| US20140141075A1 (en) * | 2012-11-21 | 2014-05-22 | Warner Chilcott Company, Llc | 5-aminosalicylic acid capsule formulation |
| KR102167265B1 (ko) * | 2013-02-22 | 2020-10-19 | 제리아 신야쿠 고교 가부시키 가이샤 | 장용정 |
| AU2013404367B2 (en) | 2013-10-29 | 2020-02-27 | Tillotts Pharma Ag | A delayed release drug formulation |
| WO2015097600A2 (en) | 2013-12-24 | 2015-07-02 | Sentiss Pharma Private Limited | Topical brimonidine tartrate ophthalmic solution |
| WO2016196440A1 (en) | 2015-06-01 | 2016-12-08 | Xeno Biosciences Inc. | Methods and compositions to modulate the gut microbiota and to manage weight |
| KR102279993B1 (ko) | 2015-09-23 | 2021-07-21 | 엑스더블유파마 리미티드 | 감마-하이드록시부티르산의 전구체 및 이의 조성물 및 용도 |
| CN105816883B (zh) * | 2016-02-03 | 2018-12-14 | 华南师范大学 | 一种负载抗癌药物姜黄素的益生菌叶酸靶向载体及其制备方法 |
| EP3257501A1 (en) | 2016-06-14 | 2017-12-20 | Tillotts Pharma AG | Multiple unit dosage form comprising a core with individual core units covered by a mucoadhesive material, and an enteric core coating |
| CN110520111B (zh) * | 2016-11-30 | 2023-12-19 | 塞诺生物科学股份有限公司 | 用以管理体重和调节肠道微生物群的药物制剂和方法 |
| ES3032290T3 (en) | 2018-03-20 | 2025-07-16 | Theriva Biologics Inc | Intestinal alkaline phosphatase formulations |
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