ES2586057T3 - Comprimido de liberación sostenida que comprende pregabalina a través de un sistema de control de la liberación de dos fases - Google Patents

Comprimido de liberación sostenida que comprende pregabalina a través de un sistema de control de la liberación de dos fases Download PDF

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Publication number
ES2586057T3
ES2586057T3 ES12817601.3T ES12817601T ES2586057T3 ES 2586057 T3 ES2586057 T3 ES 2586057T3 ES 12817601 T ES12817601 T ES 12817601T ES 2586057 T3 ES2586057 T3 ES 2586057T3
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ES
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Prior art keywords
phase
fifty
release control
pregabalin
fifteen
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ES12817601.3T
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English (en)
Inventor
Jeong-Hoon WOO
Woon-Sook NA
Yang-Soo JEONG
Chang-Keun Hyun
Yoong-Sik Park
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Yuhan Corp
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Yuhan Corp
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    • 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
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • 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
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • 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
    • A61K9/0065—Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Un comprimido de liberación sostenida que tiene un sistema de control de la liberación de dos fases, que consiste en una primera fase de control de la liberación que comprende pregabalina o su sal e hidroxipropilmetilcelulosa y una segunda fase de control de la liberación que comprende óxido de polietileno como un polímero de hinchamiento, estando la primera fase de control de la liberación dispersa de forma homogénea en la segunda fase de control de la liberación.

Description

imagen1
imagen2
imagen3
imagen4
(continuación)
Componentes
Ejemplo (mg por un comprimido)
1
2 3 4 5 6 7 8 9
Segunda fase de control de la liberación
Óxido de polietileno (Polyox 301) 100 - 100 100 100 100 50 150 100
Óxido de polietileno (Polyox 303)
- 100 - - - - - - -
Crospovidona
- - 50 - 50 50 50 50 100
Almidón glicolato de sodio
- - - 50 - - - - -
Dióxido de silicio coloidal
15 15 15 15 15 15 15 15 15
Estearato de magnesio
5 5 5 5 5 5 5 5 5
Total
795 795 845 845 795 745 745 845 845
<Tabla 2>
Componentes
Ejemplo (mg por un comprimido)
10
11 12 13 14 15 16 17 18
Primera fase de control de la liberación
Pregabalina 300 300 300 300 300 300 300 300 300
Hidroxipropilmetilcelulosa
250 150 150 350 350 100 100 250 250
Hidroxipropilcelulosa
25 15 15 25 25 10 10 15 15
Segunda fase de control de la liberación
Óxido de polietileno (Polyox 301) 100 300 200 100 100 100 100 100 100
Hidroxipropilmetilcelulosa (100.000 cps)
100 - - - - - - - -
Hidroxipropilmetilcelulosa (400 cps)
- - 100 - - 300 - - -
Crospovidona
- 50 50 - - 50 50 - -
Almidón glicolato de sodio
- - - 50 - - - 100 200
Celulosa microcristalina
- - - 50 100 - - - -
Dióxido de silicio coloidal
15 15 15 15 15 15 15 15 15
Estearato de magnesio
5 5 5 5 5 5 5 5 5
Total
845 835 835 895 895 880 580 785 885
<Tabla 3>
Componentes
Ejemplo (mg por un comprimido)
19
20 21 22
Primera fase de control de la liberación
Pregabalina 300 300 300 300
Hidroxipropilmetilcelulosa
150 200 150 150
Hidroxipropilcelulosa
15 20 15 15
6
(continuación)
Componentes
Ejemplo (mg por un comprimido)
19
20 21 22
Óxido de polietileno (Polyox 301)
100 100 100 100
Hidroxipropilmetilcelulosa(100 cps)
- - 100 -
Segunda fase de control de la liberación
Crospovidona - - - 50
Dióxido de silicio coloidal
15 15 15 15
Estearato de magnesio
5 5 5 5
Total
585 640 685 635
<Tabla 4>
Componentes
Ejemplo (mg por un comprimido)
23
24 25 26 27 28 29 30 31
Primera fase de control de la liberación
Pregabalina 150 150 150 150 150 150 150 150 150
Hidroxipropilmetilcelulosa
300 300 450 350 350 500 200 350 400
Hidroxipropilcelulosa
25 25 25 25 25 25 20 20 20
Segunda fase de control de la liberación
Óxido de polietileno (Polyox 301) 100 100 100 100 100 100 100 100 100
Crospovidona
50 50 50 - - - - - -
Almidón glicolato de sodio
- - - 50 50 50 - - -
Celulosa microcristalina
- 150 - 50 200 50 - - -
Dióxido de silicio coloidal
10 10 10 10 10 10 10 10 10
Estearato de magnesio
5 5 5 5 5 5 5 5 5
Total
640 740 790 740 890 890 485 635 685
<Tabla 5>
Componentes
Ejemplo (mg por un comprimido)
32
33 34
Primera fase de control de la liberación
Pregabalina 75 75 75
Hidroxipropilmetilcelulosa
300 575 475
Hidroxipropilcelulosa
20 25 15
Segunda fase de control de la liberación
Óxido de polietileno (Polyox 301) 100 100 100
Crospovidona
50 50 -
Almidón glicolato de sodio
- 50 -
Celulosa microcristalina
- - -
Dióxido de silicio coloidal
10 10 10
Estearato de magnesio
5 5 5
Total
560 890 680
7
imagen5
(continuación)
Tiempo (h)
Ejemplo (Tasa de disolución, %)
19
20 21 22
4
40,7 39,7 38,7 43,2
6
54,1 52,8 52,2 56,9
8
66,1 64,4 63,5 69,1
12
84,1 80,3 81,5 87,0
16
95,3 92,3 93,0 98,0
24
102,8 101,0 103,4 106,5
<Tabla 9>
Tiempo (h)
Ejemplo (Tasa de disolución, %)
23
24 25 26 27 28 29 30 31
0,5
12,9 12,7 11,5 13,1 12,7 12,3 12,8 12,5 11,0
1
19,1 19,5 17,7 19,8 18,8 18,6 20,2 19,0 17,4
2
30,1 29,5 27,2 30,2 28,1 28,0 33,9 29,1 26,7
3
39,3 36,6 34,0 39,0 35,9 35,5 43,4 37,2 34,4
4
47,1 43,5 40,8 46,2 42,5 41,6 51,9 44,3 43,2
6
58,7 50,8 50,2 57,5 53,6 51,1 66,4 56,4 51,7
8
68,9 58,1 56,6 67,9 63,1 58,7 78,4 66,3 62,0
12
83,9 70,6 69,7 83,5 77,8 71,6 95,1 81,6 76,0
16
95,4 80,6 79,8 94,3 87,9 82,1 104,7 92,6 87,4
24
107,9 95,1 94,8 109,0 101,0 97,0 105,7 104,4 99,1
<Tabla 10>
Tiempo (h)
Ejemplo (Tasa de disolución, %)
32
33 34
0,5
11,0 10,7 11,6
1
18,9 16,3 17,8
2
30,5 24,7 27,6
3
38,3 31,1 36,7
4
45,9 36,3 43,2
6
58,3 44,2 53,4
8
66,6 51,3 60,5
12
79,2 63,1 75,4
16
88,3 73,1 85,3
24
96,4 86,7 97,1
Ejemplo Experimental 2: Medición de los tiempos de inicio de la flotación y los tiempos de mantenimiento de la flotación
Las pruebas de disolución de los comprimidos preparados en los Ejemplos anteriores se realizaron de acuerdo con la 'Prueba de Disolución 2 (Procedimiento de Pala)' de la Farmacopea Coreana. Como medio de disolución se
10 utilizaron 900 ml de una solución de HCl 0,06 N y la prueba de disolución se realizó a 37 ± 0,5 °C y a la velocidad de rotación de pala de 50 rpm. Se midieron los tiempos de demora de la flotación y después se midieron los tiempos de mantenimiento de la flotación hasta las 24 horas. Los resultados se presentan en las Tablas 11 a 13. Como se muestra en las Tablas 11 a 13, los comprimidos preparados de acuerdo con la presente invención iniciaron la flotación dentro de los 30 minutos y cada flotación se mantuvo durante por lo menos 24 horas.
9
imagen6
imagen7
imagen8
imagen9

Claims (1)

  1. imagen1
ES12817601.3T 2011-07-26 2012-07-20 Comprimido de liberación sostenida que comprende pregabalina a través de un sistema de control de la liberación de dos fases Active ES2586057T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
KR20110074011 2011-07-26
KR20110074011 2011-07-26
PCT/KR2012/005831 WO2013015578A1 (en) 2011-07-26 2012-07-20 Sustained release tablet comprising pregabalin through two-phase release-controlling system

Publications (1)

Publication Number Publication Date
ES2586057T3 true ES2586057T3 (es) 2016-10-11

Family

ID=47601326

Family Applications (1)

Application Number Title Priority Date Filing Date
ES12817601.3T Active ES2586057T3 (es) 2011-07-26 2012-07-20 Comprimido de liberación sostenida que comprende pregabalina a través de un sistema de control de la liberación de dos fases

Country Status (7)

Country Link
US (1) US20140161880A1 (es)
EP (1) EP2736499B1 (es)
JP (1) JP6170918B2 (es)
KR (1) KR101724024B1 (es)
CN (1) CN103702664B (es)
ES (1) ES2586057T3 (es)
WO (1) WO2013015578A1 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2415460A1 (de) * 2010-08-03 2012-02-08 ratiopharm GmbH Orale Darreichungsform von Pregabalin
KR102221846B1 (ko) * 2014-04-07 2021-02-26 영진약품 주식회사 안정성이 개선된 프레가발린을 함유하는 약제학적 조성물 및 이의 제조방법
CN111840239B (zh) 2014-10-24 2022-11-18 江苏恒瑞医药股份有限公司 一种普瑞巴林缓释制剂
CN104906064B (zh) * 2015-05-15 2017-12-22 中国药科大学 一种普瑞巴林胃漂浮缓释片剂及其制备方法
CN104840443B (zh) * 2015-05-27 2018-04-27 齐鲁制药有限公司 含活性成分普瑞巴林的药物组合物
CA3030105A1 (en) * 2016-07-17 2018-01-25 Mapi Pharma Ltd. Extended release dosage forms of pregabalin
JP6919119B2 (ja) * 2017-01-23 2021-08-18 日新製薬株式会社 ３位が置換されたγ−アミノ酪酸誘導体を含有する圧縮固形医薬組成物。
KR102039344B1 (ko) 2017-02-01 2019-11-01 지엘팜텍주식회사 프레가발린 함유 경구용 서방성 삼중정제
KR102039345B1 (ko) * 2017-02-01 2019-11-01 지엘팜텍주식회사 프레가발린 함유 고팽윤성 서방성 삼중정제
TW202002958A (zh) * 2018-03-22 2020-01-16 日商日東電工股份有限公司 含普瑞巴林（ｐｒｅｇａｂａｌｉｎ）之組成物的製造方法及含普瑞巴林之組成物
WO2019238068A1 (zh) * 2018-06-13 2019-12-19 北京泰德制药股份有限公司 一种普瑞巴林缓释组合物及其制备方法
CN109044981B (zh) * 2018-08-07 2021-02-19 广州帝奇医药技术有限公司 一种普瑞巴林胃漂浮型缓释片及其制备方法
KR20220048341A (ko) * 2020-10-12 2022-04-19 뉴지랩테라퓨틱스 주식회사 나파모스타트 또는 이의 약제학적으로 허용가능한 염을 함유하는 방출 조절 제형 및 이의 제조방법

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Publication number Publication date
EP2736499A4 (en) 2015-04-01
JP2014521639A (ja) 2014-08-28
EP2736499B1 (en) 2016-05-11
US20140161880A1 (en) 2014-06-12
EP2736499A1 (en) 2014-06-04
WO2013015578A1 (en) 2013-01-31
JP6170918B2 (ja) 2017-07-26
CN103702664B (zh) 2016-10-19
KR20130012923A (ko) 2013-02-05
KR101724024B1 (ko) 2017-04-06
CN103702664A (zh) 2014-04-02

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