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IL157477A - Pharmaceutical salts comprising a pharmaceutically active substance and a sugar substitute and medicaments comprising them - Google Patents

Pharmaceutical salts comprising a pharmaceutically active substance and a sugar substitute and medicaments comprising them

Info

Publication number
IL157477A
IL157477A IL157477A IL15747703A IL157477A IL 157477 A IL157477 A IL 157477A IL 157477 A IL157477 A IL 157477A IL 15747703 A IL15747703 A IL 15747703A IL 157477 A IL157477 A IL 157477A
Authority
IL
Israel
Prior art keywords
alkyl
meta
salt
medicament
pharmaceutical salt
Prior art date
Application number
IL157477A
Original Assignee
Gruenenthal Chemie
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 Gruenenthal Chemie filed Critical Gruenenthal Chemie
Publication of IL157477A publication Critical patent/IL157477A/en

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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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • 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
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A61K9/0058—Chewing gums
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/48—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups
    • C07C215/54—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups linked by carbon chains having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/56—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups
    • C07C215/58—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
    • C07C215/62—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by hydroxy groups with hydroxy groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain the chain having at least three carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/46—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C215/64—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/64—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms
    • C07C217/66—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain
    • C07C217/68—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains further substituted by singly-bound oxygen atoms with singly-bound oxygen atoms and six-membered aromatic rings bound to the same carbon atom of the carbon chain with singly-bound oxygen atoms, six-membered aromatic rings and amino groups bound to the same carbon atom of the carbon chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/74—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with rings other than six-membered aromatic rings being part of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D291/00—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms
    • C07D291/02—Heterocyclic compounds containing rings having nitrogen, oxygen and sulfur atoms as the only ring hetero atoms not condensed with other rings
    • C07D291/06—Six-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
    • C07D489/04—Salts; Organic complexes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Rheumatology (AREA)
  • Physiology (AREA)
  • Zoology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
  • Saccharide Compounds (AREA)

Claims (20)

46 157477/3 CLAIMS:
1. A pharmaceutical salt of a pharmaceutical active compound and at least one sugar substitute, wherein the salt- forming active compound is a salt-forming 1-phenyl-3-dimethylairiinopropane compound of the general formula in which X is OH, F, CI, H or an OCOR6 group, R1 is a Ci-4-alkyl group, R2 is H or a C1-4 -alkyl group and R3 is H or a straight-chain C -alkyl group or the radicals R2 and R3 together form a C -7-cycloalkyl radical, and if R5 is H, R4 is meta-O-Z where Z is H, Ci-3 -alkyl, PO (O-C CO (OC1-5 -alkyl), CONH-CeH - d -alkyl), CO-CeFLrR7, where R7 is ortho-OCOCi-3 -alkyl or meta- or para-CH2N(R8)2 where R8 is Ci-4-alkyl or 4-morpholino, or R4 is meta-S-C1-3- 10 , 11 alkyl, meta-Cl, meta-F, meta-CR9R10Rn where R*, R1U, R11 are H or F, ortho-OH ortho-0-C2-3 -alkyl, para-F or para-CRyRluR" where Ry, R10, Ru are H or F, or if R3 is para-Cl, -F, -OH or -0-C1-3 -alkyl, R4 is meta-Cl, -F, -OH or -0-C,.3 -alkyl, or R4 and R together are 3,4-OCH=CH- or 3,4-OCH=CHO- R6 is C]-3 -alkyl, 47 157477/3 in the form of their possible stereoisomers as racemates or diastereomencally pure enantiomers or in the form of mixtures of enantiomers, in which the respective enantiomers are present in nonequimolar amounts, or wherein the salt-forming active compound is a salt-forming 6-dimethylaminomethyl-1-phenylcyclohexane compound of the general formula II, in which R1' is H, OH, CI or F, R2' and R3' are identical or different and are H, C1-4-alkyl, benzyl, CF3, OH, OCH2-C6H5, O-Ci-4-alkyl, CI or F with the proviso that at least one of the radicals R2' or R3' is H, R4' is H, CH3, PO (O-C -alkyl)2, CO(0- C1-5-alkyl), CO-C6H4-R5', CO-C1-5 -alkyl, CO-CHR6'-NHR7 or an unsubstituted or substituted pyridyl, tbienyl, thiazoyl or phenyl group, R5' is OC(0)C1-3 -alkyl in the ortho-position or CH2-N(R8')2 in the meta- or para-position, where R8 is C -alkyl or both radicals R8 ' together with N are the 4-morpholino radical, and R6 and R7' are identical or different and are H or Ci-6 -alkyl, 48 157477/3 with the proviso that if both radicals R2' and R3' are H, R4 is not CH3 if R1' is H, OH or CI or R4' is not H if r is OH, in the form of their possible stereoisomers as racemates or diastereomerically pure enantiomers or in the form of mixtures of enantiomers, in which the respective enantiomers are present in nonequimolar amounts.
2. The pharmaceutical salt as claimed in claim 1, characterized in that the solubility of the salt in water is < 250 mg/ml, preferably < 200 mg/ml, more preferably < 150 mg/ml, most preferably < 100 mg/ml.
3. The pharmaceutical salt as claimed in claim 1 or 2, characterized in that the salt-forming sugar substitute is saccharin, cyclamate or acesulfam, preferably saccharin.
4. The pharmaceutical salt as claimed in one of claims 1 to 3, characterized in that X is OH, F, CI or H, R1 is a C1-4-alkyl group, R2 is H or CH3 and R3 is H or CH3, and if R5 is H, R4 is meta-O-C!-3 -alkyl, meta-OH, meta-S-Ci.3 -alkyl, meta-F, meta-Cl, meta-C¾, meta-CF2-H, meta-CF3 or para-CF3 or if R5 is a para-Cl or -F, R4 is meta-Cl or -F, or R4and R5 together are 3,4-OCH=CH-.
5. The pharmaceutical salt as claimed in one of claims 1 to 4, characterized in that the radicals R2 and R3 have different meanings and the compounds of the general formula I as claimed in claim 1 are present in the form of their diastereomers having the configuration la 49 157477/4
6. The pharmaceutical salt as claimed in one of claims 1 to 5, characterized in that the salt-forming l-phenyl-3-dimethylaminopropane compound is selected from the group consisting of : ( 1 RS ,2RS)-3 -(3 -dimethy lamino- 1 -hydroxy- 1 ,2-di-methylpropyl) phenol, (-)-(l R,2R)-3-(3-dimethylamino- 1 -ethyl-2-methylpropyl) phenol, (+)-( 1 S ,2S)-3 -(3 -dimethylamino- 1 -ethyl-2-methyl-propyl) phenol, (2RS,3RS)- 1 -dimethylamino-3 -(3 -methoxyphenyl)-2-methylpentan-3 -ol, (-)-(l S,2S)-3-(3-dimethylamino-l-ethyl-l-fluoro-2-methylpropyl)phenol, (+)-(l R,2r)-3 -(3 -dimethylamino- 1 -hydroxy- 1 ,2-dimethylpropyl) phenol, (+)-(2R,3R)- 1 -dimethylamino-3 -(3 -methoxyphenyl)-2-methylpentan-3 -ol and (-)-(2S,3 S)- 1 -dimethylamino-3 -(3 -methoxyphenyl)-2-methylpentan-3 -ol.
7. The pharmaceutical salt as claimed in one of claims 1 to 3, characterized in that Rr is H, OH or F.
8. The pharmaceutical salt as claimed in claims 1 to 3 or 7, characterized in that the compounds of the general formula II have a configuration in which the phenyl ring and the dimethylaminomethyl group are in each case arranged in an equatorial position to one another.
9. The pharmaceutical salt as claimed in one of claims 1 to 3 7 or 8, characterized in that the salt-forming 6-dimethylaminomethyl-l-phenylcyclohexane compound is selected from the group consisting of: (-)-(lR,2R)-3-(2-dimethylaminomethylcyclohexyl)-phenol,(lRS,3RS,6RS)-6-(dimethylaminomethyl)-l-(3-methoxyphenyl)cyclohexane-l,3-diol and (lRS,3RS,6RS)-6-(dimethylaminomethyl)-l-(3-hydroxyphenyl)cyclohexane-l,3-diol.
10. A medicament comprising at least one pharmaceutical salt as claimed in one of claims 1 to 9 and, optionally, physiologically tolerable excipients.
11. A medicament comprising at least one pharmaceutical salt as claimed in one of claims 1 to 9 for the control of pain.
12. A medicament comprising at least one pharmaceutical salt as claimed in one of claims 1 to 9 for the control of urinary incontinence. 50 157477/2
13. The medicament as claimed in one of claims 10 to 12, characterized in that it is present in the form of gels, chewing gums, juices, sprays, tablets, chewable tablets, coated tablets, powders, optionally filled into capsules, easily reconstitutable dry preparations, preferably in the form of gels, aqueous or oily juices, sublingual sprays, tablets or chewable tablets.
14. The medicament as claimed in one of claims 10 to 12, characterized in that it is present formulated in multiparticulate form, preferably in form of microtablets, microcapsules, granules, active compound crystals or pellets, more preferably in form of microtablets, granules or pellets, optionally filled into capsules or compressed to give tablets.
15. The medicament as claimed in one of claims 10 to 14, characterized in that the salt is present at least partially in delayed-release form.
16. The medicament as claimed in claim 15, characterized in that delaying of the release is carried out by applying a release-delaying coating, embedding in a release-delaying matrix, binding to an ion-exchange resin or by a combination of at least two of these methods.
17. The medicament as claimed in claim 16, characterized in that the release-delaying coating is based on a water-insoluble, optionally modified natural or synthetic polymer, optionally in combination with a customary plasticizer, or on a natural, semisynthetic or synthetic wax or fat or fatty alcohol or a mixture of at least two of these components.
18. The medicament as claimed in claim 16, characterized in that the matrix is based on a hydrophilic matrix material, preferably hydrophilic polymers, more preferably cellulose ethers, cellulose esters and/or acrylic resins, yet more preferably ethylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, hydroxymethyl-cellulose, poly(meth)acrylic acid and/or their salts, amides and/or esters.
19. The medicament as claimed in claim 16, characterized in that the matrix is based on a hydrophobic matrix material, preferably hydrophobic polymers, waxes, fats, long-chain fatty acids, fatty alcohols or appropriate esters or ethers or their mixtures, more preferably on mono- or diglycerides of Ci2-C3o fatty acids and/or Ci2-C30 -fatty alcohols and/or waxes or their mixtures. 51 157477/2
20. The medicament as claimed in one of claims 10 to 19, characterized in that it has a protective coating, preferably an enteric protective coating. For the Applicants, REINHOLD COHN AND PARTNERS By:
IL157477A 2001-02-28 2003-08-19 Pharmaceutical salts comprising a pharmaceutically active substance and a sugar substitute and medicaments comprising them IL157477A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10109763A DE10109763A1 (en) 2001-02-28 2001-02-28 Pharmaceutical salts
PCT/EP2002/002169 WO2002067916A2 (en) 2001-02-28 2002-02-28 Pharmaceutical salts

Publications (1)

Publication Number Publication Date
IL157477A true IL157477A (en) 2009-12-24

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IL15747702A IL157477A0 (en) 2001-02-28 2002-02-28 Pharmaceutical salts comprising a pharmaceutically active substance and a sugar substitute
IL157477A IL157477A (en) 2001-02-28 2003-08-19 Pharmaceutical salts comprising a pharmaceutically active substance and a sugar substitute and medicaments comprising them

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Country Status (24)

Country Link
EP (1) EP1390023B1 (en)
JP (2) JP4737583B2 (en)
KR (1) KR20030078943A (en)
CN (2) CN101125137A (en)
AR (1) AR033423A1 (en)
AT (1) ATE395053T1 (en)
BR (1) BR0207726A (en)
CA (2) CA2725635A1 (en)
CZ (1) CZ306998B6 (en)
DE (2) DE10109763A1 (en)
ES (1) ES2307739T3 (en)
HU (1) HU229048B1 (en)
IL (2) IL157477A0 (en)
MX (1) MXPA03007712A (en)
NO (1) NO333986B1 (en)
NZ (2) NZ551440A (en)
PE (1) PE20020973A1 (en)
PL (1) PL218187B1 (en)
PT (1) PT1390023E (en)
RU (1) RU2309942C2 (en)
SI (1) SI1390023T1 (en)
SK (1) SK287574B6 (en)
WO (2) WO2002067651A2 (en)
ZA (2) ZA200410015B (en)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20030527A1 (en) 2001-10-24 2003-07-26 Gruenenthal Chemie DELAYED-RELEASE PHARMACEUTICAL FORMULATION CONTAINING 3- (3-DIMETHYLAMINO-1-ETHYL-2-METHYL-PROPYL) PHENOL OR A PHARMACEUTICALLY ACCEPTABLE SALT OF THE SAME AND ORAL TABLETS CONTAINING IT
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