AR054226A1 - PHARMACEUTICAL COMPOSITION IN THE FORM OF A COMPRESSED FORM, INCLUDING THE COMPOUND 4-METHYL-2OXO-2H-1-BENZOPIRAN-7-IL-TIO-B-D-XYLOPYRANOSIDE, USE OF DERMATAN SULFATE AND SUCH COMPOUND TO PREPARE IT AND METHOD - Google Patents

PHARMACEUTICAL COMPOSITION IN THE FORM OF A COMPRESSED FORM, INCLUDING THE COMPOUND 4-METHYL-2OXO-2H-1-BENZOPIRAN-7-IL-TIO-B-D-XYLOPYRANOSIDE, USE OF DERMATAN SULFATE AND SUCH COMPOUND TO PREPARE IT AND METHOD

Info

Publication number
AR054226A1
AR054226A1 AR20060100564A ARP060100564A AR054226A1 AR 054226 A1 AR054226 A1 AR 054226A1 AR 20060100564 A AR20060100564 A AR 20060100564A AR P060100564 A ARP060100564 A AR P060100564A AR 054226 A1 AR054226 A1 AR 054226A1
Authority
AR
Argentina
Prior art keywords
compound
hours
tablet
composition
dermatan sulfate
Prior art date
Application number
AR20060100564A
Other languages
Spanish (es)
Original Assignee
Smithkline Beecham Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of AR054226A1 publication Critical patent/AR054226A1/en

Links

Classifications

    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K9/2022—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
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

Landscapes

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

Abstract

Composicion farmacéutica en forma de comprimido que comprende una cantidad eficaz del compuesto 4-metil-2-oxo-qH-1-benzopiran-7-il-5-tio-beta-D-xilopiran'sidoque tiene la formula (1) y se denomina aquí alternativamente ôCompuesto Aö, dicha composicion posee una o más de las siguientes propiedades: a) un nivel de actividad anti-lla en estado de equilibrio, de al menos 1 microgramo (incluyendo, por ejemplo, al menos 2 microgramos) de unidades de sulfato de dermatán por ml de plasma durante un largo período de tiempo después de la administracion oral; y/o b) un nivel de Compuesto A en situacion de equilibrio de al menos 0,25-4 microgramos (incluyendo, por ejemplo, al menos 0,5-8 microgramos) de Compuesto A por ml de plasma durante un largo período de tiempo después de la administracion oral; y/o c) un perfil de disolucion in-vitro en el que: desde 5 hasta 65% del compuesto A se libera después de 2 horas; desde 35 hasta 85% del compuesto A se libera después de 4 horas; y no menos de 75% del compuesto A se libera después de 8 horas; en el que la disolucion se mide utilizando un aparato de disolucion tipo 2 (paletas) en las siguientes condiciones: a 100 +/- 4 rpm, a una temperatura de 37 +/- 0,5 degree C, en 1 litro +/- 5 ml de tampon de acetato 0,05 M en dodecilsulfato de sodio 0,05 M, pH 4,9 +/- 0,05, durante al menos 8 horas. El nivel antilla y/o el nivel plasmático de Compuesto A en estado de equilibrio se presenta durante al menos 8 horas, o al menos 10 horas, o al menos 12 horas, después de la administracion oral. Dicha composicion puede comprender además polímero hinchable, polímero matriz y agente flotante, y opcionalmente diluyente, aglutinante, deslizante y/o un lubricante. Uso de sulfato de dermatán y uso del Compuesto A para preparar dicha composicion farmacéutica, y método de preparacion de dicho comprimido,. Se aplica para tratar o prevenir trastornos tromboembolicos, incluyendo trombosis o hipercoagulabilidad. Reivindicacion 21: Uso de sulfato de dermatán caracterizado porque es para preparar una composicion segun cualquiera de las reivindicaciones precedentes, util para proporcionar un nivel anti-lla medio en estado de equilibrio de al menos 1 microgramo, incluyendo, por ejemplo, al menos 2 microgramos de unidades de sulfato de dermatán por ml de plasma en un mamífero que los necesite, que comprende administrar dicha composicion al mamífero. Reivindicacion 28: Un método para preparar una composicion farmacéutica en la forma de un comprimido que comprende una cantidad eficaz de Compuesto A, caracterizado porque comprende: a) formar una mezcla seca de Compuesto A, un diluyente, y un aglutinante; b) granular en humedo la mezcla seca con un fluido de granulacion adecuado; c) secar los gránulos humedos para eliminar sustancialmente el fluido de granulacion; d) formar una mezcla de compresion mezclando los gránulos secos con un polímero matriz, un polímero hinchable, un agente flotante y, opcionalmente, un diluyente, lubricante y/o deslizante; e) comprimir la mezcla para formar un comprimido; y f) opcionalmente,. recubrir el comprimido. Reivindicacion 33: Un comprimido farmacéutico caracterizado porque es preparado mediante el método de cualquiera de las reivindicaciones 28-32.Pharmaceutical tablet composition comprising an effective amount of the compound 4-methyl-2-oxo-qH-1-benzopyran-7-yl-5-thio-beta-D-xylopyran'sido which has the formula (1) and is alternatively referred to herein as "Compound Aö," said composition has one or more of the following properties: a) a level of anti-flame activity at steady state, of at least 1 microgram (including, for example, at least 2 micrograms) of units of dermatan sulfate per ml of plasma for a long period of time after oral administration; and / or b) a level of Compound A in equilibrium situation of at least 0.25-4 micrograms (including, for example, at least 0.5-8 micrograms) of Compound A per ml of plasma for a long period of time after oral administration; and / or c) an in-vitro dissolution profile in which: from 5 to 65% of compound A is released after 2 hours; from 35 to 85% of compound A is released after 4 hours; and not less than 75% of compound A is released after 8 hours; in which the solution is measured using a type 2 dissolution apparatus (vanes) under the following conditions: at 100 +/- 4 rpm, at a temperature of 37 +/- 0.5 degree C, in 1 liter +/- 5 ml of 0.05 M acetate buffer in 0.05 M sodium dodecyl sulfate, pH 4.9 +/- 0.05, for at least 8 hours. The antilla level and / or the plasma level of Compound A in steady state is presented for at least 8 hours, or at least 10 hours, or at least 12 hours, after oral administration. Said composition may further comprise swellable polymer, matrix polymer and floating agent, and optionally diluent, binder, slider and / or a lubricant. Use of dermatan sulfate and use of Compound A to prepare said pharmaceutical composition, and method of preparing said tablet. It is applied to treat or prevent thromboembolic disorders, including thrombosis or hypercoagulability. Claim 21: Use of dermatan sulfate characterized in that it is for preparing a composition according to any of the preceding claims, useful for providing an average anti-flame level in equilibrium state of at least 1 microgram, including, for example, at least 2 micrograms of units of dermatan sulfate per ml of plasma in a mammal that needs them, which comprises administering said composition to the mammal. Claim 28: A method for preparing a pharmaceutical composition in the form of a tablet comprising an effective amount of Compound A, characterized in that it comprises: a) forming a dry mixture of Compound A, a diluent, and a binder; b) wet granulate the dry mixture with a suitable granulation fluid; c) drying the wet granules to substantially remove the granulation fluid; d) forming a compression mixture by mixing the dried granules with a matrix polymer, an inflatable polymer, a floating agent and, optionally, a diluent, lubricant and / or slider; e) compress the mixture to form a tablet; and f) optionally. coat the tablet. Claim 33: A pharmaceutical tablet characterized in that it is prepared by the method of any of claims 28-32.

AR20060100564A 2005-02-18 2006-02-16 PHARMACEUTICAL COMPOSITION IN THE FORM OF A COMPRESSED FORM, INCLUDING THE COMPOUND 4-METHYL-2OXO-2H-1-BENZOPIRAN-7-IL-TIO-B-D-XYLOPYRANOSIDE, USE OF DERMATAN SULFATE AND SUCH COMPOUND TO PREPARE IT AND METHOD AR054226A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US65427905P 2005-02-18 2005-02-18
US69612105P 2005-07-01 2005-07-01

Publications (1)

Publication Number Publication Date
AR054226A1 true AR054226A1 (en) 2007-06-13

Family

ID=36917125

Family Applications (1)

Application Number Title Priority Date Filing Date
AR20060100564A AR054226A1 (en) 2005-02-18 2006-02-16 PHARMACEUTICAL COMPOSITION IN THE FORM OF A COMPRESSED FORM, INCLUDING THE COMPOUND 4-METHYL-2OXO-2H-1-BENZOPIRAN-7-IL-TIO-B-D-XYLOPYRANOSIDE, USE OF DERMATAN SULFATE AND SUCH COMPOUND TO PREPARE IT AND METHOD

Country Status (4)

Country Link
AR (1) AR054226A1 (en)
PE (1) PE20061010A1 (en)
TW (1) TW200640449A (en)
WO (1) WO2006089215A2 (en)

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69014064T2 (en) * 1989-09-22 1995-05-18 Fournier Ind & Sante Benzopyranone beta-D-thioxyloside, process for its preparation and its therapeutic use.
FR2801055B1 (en) * 1999-11-17 2002-02-08 Fournier Ind & Sante BETA-D-5-THIOXYLOSE DERIVATIVES, PREPARATION METHOD AND THERAPEUTIC USE

Also Published As

Publication number Publication date
TW200640449A (en) 2006-12-01
PE20061010A1 (en) 2006-11-11
WO2006089215A2 (en) 2006-08-24
WO2006089215A3 (en) 2006-11-23

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