ES2584858T3 - Composiciones farmacéuticas acuosas que contienen complejos de borato-poliol - Google Patents

Composiciones farmacéuticas acuosas que contienen complejos de borato-poliol Download PDF

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ES2584858T3
ES2584858T3 ES14150805.1T ES14150805T ES2584858T3 ES 2584858 T3 ES2584858 T3 ES 2584858T3 ES 14150805 T ES14150805 T ES 14150805T ES 2584858 T3 ES2584858 T3 ES 2584858T3
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Bhagwati P. Kabra
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Novartis AG
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    • 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
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K47/08—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
    • 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
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/186—Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
    • 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
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2121/00—Preparations for use in therapy

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  • Ophthalmology & Optometry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract

Composición oftálmica de múltiples dosis que comprende: brinzolamida, brimonidina o una combinación de las mismas como agente terapéutico; un primer poliol, seleccionándose el primer poliol de manitol, sorbitol o una combinación de los mismos, siendo la concentración del primer poliol de al menos el 0,01% en p/v pero no mayor del 0,5% en p/v; un segundo poliol, seleccionándose el segundo poliol de propilenglicol, glicerina o una combinación de los mismos, siendo la concentración del segundo poliol de al menos el 0,1% en p/v pero menor del 5% en p/v de la composición; una cantidad eficaz de borato, siendo la cantidad eficaz de al menos el 0,05% en p/v y menor del 0,5% en p/v de la composición global; BAC como conservante antimicrobiano, siendo la concentración de BAC en la composición mayor del 0,00001% en p/v pero menor del 0,0035% en p/v; y agua.

Description

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pueden usarse para suspensiones oftálmicas de fármacos tales como brinzolamida, roscovitina, amfenac amida, dexametasona, inhibidor de bradicinina, acetato de anecortavo, tandospirona, combinaciones de los mismos y sus combinaciones con otros fármacos.

Tabla C: ejemplos A a C con el 0,002% de BAC
Composición
A COMPARATIVO B COMPARATIVO C
Carbómero 974 P
0,45 0,45 0,45
Tiloxapol
0,025 0,025 0,025
Ácido bórico
0,3 0,6 0,3
Manitol
0,3 2,0 2
Propilenglicol
0,75 1 0,75
Cloruro de sodio
0,3 Ninguno Ninguno
Cloruro de benzalconio
0,002 0,002 0,002
Edetato de disodio
Ninguno Ninguno Ninguno
Hidróxido de sodio/HCl
pH 7,0 pH 7,0 pH 7,0
Agua purificada
CS CS CS
Osmolalidad
279 324 259
Viscosidad (cps) a 120 s-1
49,6 68,2 127,9
Viscosidad (cps) a 12 s-1
144,4 210,4 480,7
Microorganismos, tiempo
Criterios de la Ph. Eur. A Criterios de la Ph. Eur. B Reducciones log
S. aureus 6 horas 24 horas 7 días 14 días 28 días
2,0 3,0 NRa -1,0 3,0 NIb 4,6 4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9 2,5 4,9 4,9 4,9 4,9
P. aeruginosa 6 horas 24 horas 7 días 14 días 28 días
2,0 3,0 NR -1,0 3,0 NI 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 4,8 4,8 4,8 4,8 4,8
E. colic 6 horas 24 horas 7 días 14 días 28 días
NAd NA 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 3,0 5,0 5,0 5,0 5,0
C. albicans 7 días 14 días 28 días
2,0 NI NI -1,0 NI 4,7 4,7 4,7 4,7 4,7 4,7 4,8 4,8 4,8
A. niger 7 días 14 días 28 días
2,0 NI NI -1,0 NI 3,1 3,6 5,2 3,1 4,2 5,2 3,7 4,3 5,1
aNR = Sin recuperación bNI = Sin aumento cLa Ph. Eur. No tiene requisito para E. Coli dNA = No aplicable
Ejemplo D
El ejemplo D presentado en la tabla 3 es una composición con el 0,002% de BAC, ácido bórico y dos polioles diferentes y se proyecta para cumplir con los criterios de PET de la Ph. Eur B y A.
Tabla D: Ejemplo D con el 0,002% de BAC
Composición
D
Ácido bórico
0,3
Sorbitol
0,25
Propilenglicol
1,6
10
imagen9
Cada una de las composiciones H-J, entre otros usos, puede usarse como vehículos de suspensión para suspender agentes terapéuticos.
Composición
H I J
Cloruro de sodio
0,15 0,3 Ninguno
Cloruro de benzalconio
0,001 0,001 0,001
Hidróxido de sodio/HCl
pH 7,0 pH 7,0 pH 7,0
Agua purificada
CS CS CS
Osmolalidad
278 274 278
Viscosidad (cps) a 120 s-1
63,1 53,8 59,1
Viscosidad (cps) a 12 s-1
169 149 172
S. aureus 6 horas 24 horas 7 días 14 días 28 días
0,2 2,6 5,0 5,0 5,0 0,0 1,4 5,0 5,0 5,0 0,2 3,0 5,0 5,0 5,0
P. aeruginosa 6 horas 24 horas 7 días 14 días 28 días
4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9 4,9
E. coli 6 horas 24 horas 7 días 14 días 28 días
1,4 3,1 5,0 5,0 5,0 1,4 3,4 5,0 5,0 5,0 3,1 5,0 5,0 5,0 5,0
C. albicans 7 días 14 días 28 días
3,0 4,3 4,8 3,5 4,8 4,8 4,8 4,8 4,8
A. niger 7 días 14 días 28 días
3,2 3,7 3,6 3,5 3,4 3,0 3,6 3,5 3,4

Tabla G: Formulaciones de roscovitina con baja cantidad de BAC, ácido bórico y dos polioles
Composición
K
Roscovitina (AL-39256)
1
Carbómero 974P
0,45
Tiloxapol
0,025
Ácido bórico
0,3
Manitol
0,3
Propilenglicol
0,75
Cloruro de sodio
0,28
Cloruro de benzalconio
0,003
Hidróxido de sodio/HCl
pH 7,2
Agua purificada
CS
Osmolalidad (mOsm/kg)
271
Viscosidad (cps) a 12 s-1
198,1
Viscosidad (cps) a 120 s-1
66,5
S. aureus
6 horas 24 horas 7 días 14 días 28 días 5,1 5,1 5,1 5,1 5,1
P. aeruginosa
6 horas 24 horas 7 días 14 días 28 días 4,9 4,9 4,9 4,9 4,9
E. colic
6 horas 4,9
12
Composición
K
24 horas
4,9
7 días
4,9
14 días
4,9
28 días
4,9
C. albicans
7 días 4,8
14 días
4,8
28 días
4,8
A. niger
7 días 5,1
14 días
5,1
28 días
5,1
La composición K presenta una resistencia a la normalización de lágrimas de aproximadamente 4,4.
Tabla H: Formulaciones de brinzolamida y brinzolamida/brimonidina con baja cantidad de BAC, ácido bórico y dos polioles
Composición
M N
Brinzolamida
1,0 1,0
Brimonidina
0,15 0,15
Carbopol 974P
0,4 0,4
Tiloxapol
0,025 0,025
Ácido bórico
0,3 0,3
Manitol
0,3 0,3
Propilenglicol
0,75 0,75
Cloruro de sodio
0,23 0,23
Cloruro de benzalconio
0,003 0,003
Hidróxido de sodio y/o ácido clorhídrico
CS para pH 6,5 ± 0,2 CS para pH 6,5 ± 0,2
Agua purificada
CS hasta el 100% CS hasta el 100%
S. aureus 6 horas 24 horas 7 días 14 días 28 días
5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0
P. aeruginosa 6 horas 24 horas 7 días 14 días 28 días
5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0
E. colic 6 horas 24 horas 7 días 14 días 28 días
5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0 5,0
C. albicans 7 días 14 días 28 días
4,8 4,8 4,8 4,8 4,8 4,8
A. niger 7 días 14 días 28 días
4,3 4,1 4,2 4,4 4,3 4,1

Tabla I: Ejemplo O a V
Las composiciones M y N presentan una resistencia a la normalización de lágrimas de aproximadamente 18.
Los ejemplos O a V muestran que tanto la osmolalidad como la viscosidad de formulaciones que contienen carbómero pueden obtenerse en el intervalo deseado usando cloruro de sodio al tiempo que se mantiene la concentración de sodio inferior al 0,4%.
13
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Claims (1)

  1. imagen1
    imagen2
ES14150805.1T 2009-06-19 2010-06-17 Composiciones farmacéuticas acuosas que contienen complejos de borato-poliol Active ES2584858T3 (es)

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US21847209P 2009-06-19 2009-06-19

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ES10727317.9T Active ES2461617T3 (es) 2009-06-19 2010-06-17 Composiciones farmacéuticas acuosas que contienen complejos borato-polioles

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EP (4) EP3437634A1 (es)
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DK (3) DK2722035T3 (es)
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TWI544922B (zh) 2011-05-19 2016-08-11 愛爾康研究有限公司 高濃度歐羅派特錠（ｏｌｏｐａｔａｄｉｎｅ）眼用組成物
WO2014121028A1 (en) 2013-02-01 2014-08-07 Ocularis Pharma, Llc Methods and compositions for daily ophthalmic administration of phentolamine to improve visual performance
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US9693563B2 (en) 2013-08-20 2017-07-04 3M Innovative Properties Company Boron-silane polyether complex
WO2017217450A1 (ja) * 2016-06-15 2017-12-21 千寿製薬株式会社 眼科用医薬製品
JP6247430B1 (ja) * 2016-06-15 2017-12-13 千寿製薬株式会社 眼科用医薬製品
CN106237337B (zh) * 2016-08-05 2019-11-08 河南中帅医药科技股份有限公司 一种液体药物制剂用防腐组合物
GR1009419B (el) * 2017-11-07 2018-12-14 Φαρματεν Αβεε Οφθαλμικο φαρμακευτικο σκευασμα που περιεχει εναν συνδυασμο βρινζολαμιδης και βριμονιδινης και μεθοδος για την παρασκευη αυτου
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