AR011805A1 - PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION OF AN ACTIVE SUBSTANCE. - Google Patents

PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION OF AN ACTIVE SUBSTANCE.

Info

Publication number
AR011805A1
AR011805A1 ARP980100675A ARP980100675A AR011805A1 AR 011805 A1 AR011805 A1 AR 011805A1 AR P980100675 A ARP980100675 A AR P980100675A AR P980100675 A ARP980100675 A AR P980100675A AR 011805 A1 AR011805 A1 AR 011805A1
Authority
AR
Argentina
Prior art keywords
omega
alkylene
group
formula
weight
Prior art date
Application number
ARP980100675A
Other languages
Spanish (es)
Original Assignee
Wicke K
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 Wicke K filed Critical Wicke K
Publication of AR011805A1 publication Critical patent/AR011805A1/en

Links

Classifications

    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K47/08—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
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Una composicion farmacéutica para administracion oral de compuestos heterocíclicos en forma de amonio cuaternario, que contiene: principio activo0,1 a 15% en peso, solvente hidrofilo 0 a 60% en peso, tensioactivo ionico 0 a 5% de peso, polisorbato 80 0 a 5% de peso, macrogoglicérido Q.S. para 100% depeso, con la condicion de que esté presente al menos un constituyente elegido entre el solvente hidrofilo y el tensioactivo ionico. Esta composicionfarmacéutica permite mejorar la biodisponibilidad del principio activo. El principio activo responde a la formula I en la cual: -A(-) es un anionfarmacéuticamente aceptable; -Am(+) representa: i- o bien un grupo Am1(+) de formula II; ii- o bien un grupo Am2(+) de formula III, iii-o bien un grupoAm3(+) de formula IV ; iv- o bien un grupo Am4(+) de formula: V; v o bien un grupo Am5(+) de formula VI; Ar representa un fenilo no substituido osubstituido una o dos veces por un substituyente, un naftilo; un indolilo; Q e Y representan uno de los grupos de valores siguientes: a) Q1 e Y1; b) Q2 e Y2cuando Am(+) representa un grupo Am1(+), Am2(+), Am4(+) o Am5(+), c) Q3 e Y3 cuando Am (+) representa un grupo Am1(+, Am2(+), o un grupo Am4(+) en el cual Ar1 representa un fenilo y p es dos; d) Q4 e Y4 cuando Am(+) representa un grupo Am1(+), Am3(+), Am4(+) o Am5(+); Q1 representa al hidrogeno; Y1 representa alhidrogeno; un (C1-C4)alquilo; un omega-(C1-C4)alcoxi-(C2-C4)alquileno; un omega-(C1-C4)alquilcaboniloxi-(C2-C4)alquileno; un omega-benzoiloxi-(C2-C4)alquileno; un omega-hidroxi-(C2-C4)alquileno; un omega-(C1-C4)alquiltio- -(C2-C4)alquileno; un omega-(C1-C4)alquilcarbonil-(C2-C4)alquileno; un omega--carboxi-(C2-C4)alquileno; un omega-(C1-C4)alcoxicarbonil-(C2-C4)alquileno, un omega-benciloxi(C2-C4)alquileno; un omega-formiloxi-(C2-C4)alquileno; unA pharmaceutical composition for oral administration of heterocyclic compounds in quaternary ammonium form, containing: active ingredient 0.1 to 15% by weight, hydrophilic solvent 0 to 60% by weight, ionic surfactant 0 to 5% by weight, polysorbate 80 0 to 5% by weight, macrogoglyceride QS for 100% weight, provided that at least one constituent chosen from the hydrophilic solvent and the ionic surfactant is present. This pharmaceutical composition makes it possible to improve the bioavailability of the active ingredient. The active ingredient responds to formula I in which: -A (-) is an anionpharmaceutically acceptable; -Am (+) represents: i- or an Am1 (+) group of formula II; ii- or an Am2 (+) group of formula III, iii- or an Am3 (+) group of formula IV; iv- or an Am4 (+) group of formula: V; v or an Am5 (+) group of formula VI; Ar represents an unsubstituted phenyl or substituted once or twice by a substituent, a naphthyl; an indolyl; Q and Y represent one of the following groups of values: a) Q1 and Y1; b) Q2 and Y2 when Am (+) represents a group Am1 (+), Am2 (+), Am4 (+) or Am5 (+), c) Q3 and Y3 when Am (+) represents a group Am1 (+, Am2 (+), or a group Am4 (+) in which Ar1 represents a phenyl and p is two; d) Q4 and Y4 when Am (+) represents a group Am1 (+), Am3 (+), Am4 (+) or Am5 (+); Q1 represents hydrogen; Y1 represents alhydrogen; a (C1-C4) alkyl; an omega- (C1-C4) alkoxy- (C2-C4) alkylene; an omega- (C1-C4) alkylcabonyloxy- (C2-C4) alkylene; an omega-benzoyloxy- (C2-C4) alkylene; an omega-hydroxy- (C2-C4) alkylene; an omega- (C1-C4) alkylthio- - (C2-C4) alkylene; an omega- (C1-C4) alkylcarbonyl- (C2-C4) alkylene; an omega-carboxy- (C2-C4) alkylene; an omega- (C1-C4) alkoxycarbonyl- (C2-C4) alkylene, an omega-benzyloxy (C2-C4) alkylene; an omega-formyloxy- (C2-C4) alkylene; a

ARP980100675A 1997-02-17 1998-02-16 PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION OF AN ACTIVE SUBSTANCE. AR011805A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR9701825A FR2759584B1 (en) 1997-02-17 1997-02-17 PHARMACEUTICAL COMPOSITION FOR THE ORAL ADMINISTRATION OF HETEROCYCLIC COMPOUNDS IN QUATERNARY AMMONIUM FORM

Publications (1)

Publication Number Publication Date
AR011805A1 true AR011805A1 (en) 2000-09-13

Family

ID=9503804

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980100675A AR011805A1 (en) 1997-02-17 1998-02-16 PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION OF AN ACTIVE SUBSTANCE.

Country Status (11)

Country Link
EP (1) EP0969825A1 (en)
JP (1) JP2001511795A (en)
AR (1) AR011805A1 (en)
AU (1) AU6404998A (en)
BR (1) BR9807694A (en)
CA (1) CA2281560A1 (en)
FR (1) FR2759584B1 (en)
HR (1) HRP980075A2 (en)
NO (1) NO993928L (en)
WO (1) WO1998035662A1 (en)
ZA (1) ZA981289B (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102188424B (en) * 2011-03-23 2013-03-27 浙江理工大学 Anti-leukemia effects of SR140333

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2676055B1 (en) * 1991-05-03 1993-09-03 Sanofi Elf AMINO POLYCYCLIC COMPOUNDS AND THEIR ENANTIOMERS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.
FR2676054B1 (en) * 1991-05-03 1993-09-03 Sanofi Elf NOVEL N-ALKYLENEPIPERIDINO COMPOUNDS AND THEIR ENANTIOMERS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.
FR2688219B1 (en) * 1992-03-03 1994-07-08 Sanofi Elf AMATONIUM QUATERNARY SALTS OF AMINO AROMATIC COMPOUNDS, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.
FR2696178B1 (en) * 1992-09-30 1994-12-30 Sanofi Elf Quaternary basic amides, process for their preparation and pharmaceutical compositions containing them.
FR2717804B1 (en) * 1994-03-25 1996-06-21 Sanofi Sa Salts of substituted nitrogen heteroaromatic compounds, process for their preparation and pharmaceutical compositions containing them.
MX9701305A (en) * 1994-08-25 1998-05-31 Merrell Pharma Inc Novel substituted piperidines useful for the treatment of allergic diseases.
FR2725986B1 (en) * 1994-10-21 1996-11-29 Adir NOVEL PIPERIDINE DERIVATIVES, THEIR PREPARATION PROCESS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
FR2725900B1 (en) * 1994-10-21 1997-07-18 Sanofi Sa USE OF NK1 RECEPTOR ANTAGONISTS FOR THE PREPARATION OF DRUGS WITH CARDIOREGULATORY ACTION
FR2729954B1 (en) * 1995-01-30 1997-08-01 Sanofi Sa SUBSTITUTED HETEROCYCLIC COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
FR2729951B1 (en) * 1995-01-30 1997-04-18 Sanofi Sa NOVEL HETEROCYCLIC COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

Also Published As

Publication number Publication date
FR2759584A1 (en) 1998-08-21
CA2281560A1 (en) 1998-08-20
WO1998035662A1 (en) 1998-08-20
ZA981289B (en) 1998-08-26
EP0969825A1 (en) 2000-01-12
NO993928D0 (en) 1999-08-16
AU6404998A (en) 1998-09-08
BR9807694A (en) 2000-03-21
JP2001511795A (en) 2001-08-14
NO993928L (en) 1999-08-16
FR2759584B1 (en) 1999-06-11
HRP980075A2 (en) 1998-10-31

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