ES2467105T5 - Moxifloxacino compactado - Google Patents

Moxifloxacino compactado Download PDF

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Publication number
ES2467105T5
ES2467105T5 ES09765042.8T ES09765042T ES2467105T5 ES 2467105 T5 ES2467105 T5 ES 2467105T5 ES 09765042 T ES09765042 T ES 09765042T ES 2467105 T5 ES2467105 T5 ES 2467105T5
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Prior art keywords
moxifloxacin
compacted
tablets
film
coated
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ES09765042.8T
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ES2467105T3 (es
Inventor
Dieter Swatschek
Max Werner Scheiwe
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Ratiopharm GmbH
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Ratiopharm GmbH
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Application filed by Ratiopharm GmbH filed Critical Ratiopharm GmbH
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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
    • A61K9/14—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
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K9/14—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
    • 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
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2893—Tablet coating processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Glass Compositions (AREA)

Description

imagen1
imagen2
imagen3
imagen4
imagen5
imagen6
imagen7
imagen8
imagen9
imagen10
8.000), dióxido de titanio y pigmentos colorantes.
Ejemplos según la invención 4, 4a, 5 y 5a
5 De forma análoga a los ejemplos 1-3 y 1a-3a se prepararon los ejemplos 4-5 y 4a-5a, usándose moxifloxacino en forma de base libre en vez de la sal clorhidrato.
Las cantidades usadas se dan en la tabla 2.
10 Ejemplo comparativo 6
Se fabricó un núcleo de comprimido tal como se describe en el ejemplo 6 del documento EP 1 128 831 B1, mediante granulación en húmedo. Las cantidades usadas se dan en la tabla 3.
15 Comparación de las propiedades físicas
Se comparan las propiedades físicas de los comprimidos resultantes en la tabla 4.
Se muestra que los comprimidos fabricados mediante compactación (en seco) (tanto recubiertos con película como
20 también no recubiertos con película) muestran propiedades ventajosas con respecto a la resistencia a la rotura y la friabilidad. Además, los comprimidos según la invención se pueden barnizar mejor, se producen menos desprendimientos.
Además, se muestra que las formulaciones exentas de lactosa muestran una mejor uniformidad de contenido.
25 En conjunto, puede concluirse que con el procedimiento según la invención puede influirse positivamente en las propiedades físicas de los comprimidos resultantes. Además, el procedimiento según la invención es ventajoso en el aspecto de disminución de coste energético, que no es óptimo en el caso del procedimiento del estado de la técnica, ya que, en primer lugar, se introduce la humedad en forma de solución granulada y, después, debe eliminarse de
30 nuevo con un procedimiento de secado caro.
imagen11
Tabla 2
Ejemplo 4
Ejemplo 5
Núcleo
mg % en peso Mg % en peso
Moxifloxacino (base libre)
400,00 58,93 400,00 58,93
CMC (celulosa microcristalina)
231,80 34,15 230,80 34,00
Croscarmelosa Na
32,00 4,71 5,00 0,74
Aerosil
5,00 0,74 5,00 0,74
Kollidon VA 64
0,00 0,00 28,00 4,12
Estearato de Mg (E572)
10,00 1,47 10,00 1,47
678,80
100,00 678,80 100,00
Película
Ejemplo 4a Ejemplo 5a
Hipromelosa
10,80 10,80
Dióxido de titanio
3,24 3,24
Polietilenglicol
3,60 3,60
Oxido de hierro, rojo
0,36 0,36
18,00
18,00
Comprimido recubierto con película (CP)
696,80 696,80
Procedimiento de fabricación
Granulación en seco Granulación en seco
Tabla 3
Núcleo
Ejemplo 6 (comparativo) % en peso
Moxifloxacino-HCI
436,80 64,35
CMC (E460 (1))
136,00 20,04
Monohidrato de lactosa
68,00 10,02
Manitol
0,00 0,00
Croscarmelosa Na
32,00 4,71
Estearato de Mg (E572)
6,00 0,88
Aerosil
0,00 0,00
678,80
100,00
Película
No hay fabricación de comprimidos recubiertos con película
Procedimiento de fabricación
Granulación acuosa
Tabla 4
Ejemplo 6 comparativo
Ejemplo 1 Ejemplo 2 Ejemplo 3 Ejemplo 4 Ejemplo 5
Fuerza de compresión [kN] FCPrev FCPrin DT [%]
14 23 4,3 12 23 5,5 12 23 4,2-6,8 12 23 8,6 8 15 7,22 8 15 4,78
RR núcleos [N]/DT [%]
152,66 / 7,42 250,72 / 7,17 230,43 / 5,94 235,6 / 5,36 188 / 7,32 200 / 5,63
Abrasión núcleos [%]
Con cubierta; >1 % 0,26 0,25 0,31 0,55 0,41
Desprendimiento [%]
1 0 0 0 0 0
RR CP [NJ/DT [%]
No se puede barnizar 313,13/6,13 285,6/6,77 290,03/8,95 271,73 284
Disgregación CP [min]
No se ha fabricado ningún CR 1 '43" 2'29" 2'25" 1'25" 4'07"
RR = Resistencia a la rotura FCPrev = Fuerza de compresión previa FCPrin = Fuerza de compresión principal DT = Desviación típica

Claims (1)

  1. imagen1
ES09765042.8T 2008-12-08 2009-12-04 Moxifloxacino compactado Active ES2467105T5 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102008061083 2008-12-08
DE102008061083 2008-12-08
PCT/EP2009/008692 WO2010066385A1 (de) 2008-12-08 2009-12-04 Kompaktiertes moxifloxacin

Publications (2)

Publication Number Publication Date
ES2467105T3 ES2467105T3 (es) 2014-06-11
ES2467105T5 true ES2467105T5 (es) 2017-12-05

Family

ID=41600617

Family Applications (1)

Application Number Title Priority Date Filing Date
ES09765042.8T Active ES2467105T5 (es) 2008-12-08 2009-12-04 Moxifloxacino compactado

Country Status (6)

Country Link
US (2) US20110293717A1 (es)
EP (3) EP2364141B2 (es)
EA (1) EA028676B1 (es)
ES (1) ES2467105T5 (es)
PL (1) PL2364141T5 (es)
WO (1) WO2010066385A1 (es)

Families Citing this family (12)

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CN102204911B (zh) * 2011-03-25 2013-04-17 华润赛科药业有限责任公司 一种盐酸莫西沙星药物组合物及其制备方法
KR101435244B1 (ko) * 2011-04-12 2014-08-29 씨제이헬스케어 주식회사 목시플록사신 수성 제형 및 이의 제조방법
CN103284962B (zh) * 2012-02-23 2015-09-16 重庆圣华曦药业股份有限公司 莫西沙星分散片及制备方法
CN103301080B (zh) * 2012-03-15 2014-12-10 成都国为医药科技有限公司 一种含有盐酸莫西沙星的药物组合物及其制备方法
CN103768063B (zh) * 2012-10-19 2016-04-20 深圳信立泰药业股份有限公司 一种盐酸莫西沙星药物组合物及其制备方法
GR1008169B (el) * 2013-03-19 2014-04-08 "Φαρματεν Α.Β.Ε.Ε.", Φαρμακευτικο σκευασμα περιεχον εναν αντιβακτηριακο παραγοντα φθοριοκινολονης και μεθοδος για την παρασκευη αυτου
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BR112017000515A2 (pt) * 2014-07-18 2017-11-14 Msd Wellcome Trust Hilleman Laboratories Pvt Ltd formulação de vacina contra rotavírus termoestável seca por liofilização e processo para preparação da mesma
CN106074413A (zh) * 2016-07-20 2016-11-09 南通雅本化学有限公司 一种含有莫西沙星的药物组合物
CN108969497A (zh) * 2018-10-12 2018-12-11 沈阳华泰药物研究有限公司 一种碳酸镧片剂组合物及其制备方法

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Also Published As

Publication number Publication date
EP2364141B1 (de) 2014-03-05
PL2364141T3 (pl) 2014-07-31
US20150133489A1 (en) 2015-05-14
EA028676B1 (ru) 2017-12-29
EP2735307A1 (de) 2014-05-28
US20110293717A1 (en) 2011-12-01
ES2467105T3 (es) 2014-06-11
EP2364141B2 (de) 2017-08-02
EA201170777A1 (ru) 2011-12-30
EP2364141A1 (de) 2011-09-14
EP2837376A3 (de) 2015-03-25
EP2837376A2 (de) 2015-02-18
WO2010066385A1 (de) 2010-06-17
PL2364141T5 (pl) 2018-02-28

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