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EP0609589A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Compositions of alkylbenzenes in film-forming materials for visualization of the gastrointestinal tract

Assignee: GE Healthcare AS
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Filing: 1993-12-24
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Granted: —
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Expires: 2013-12-24
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Abstract

Abstract Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract, said polymeric material having atoms containing polarizable electrons thereon, in combination with a divalent cation, and an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof, and methods for their use in diagnostic radiology of the gastrointestinal tract wherein R= C 1 -C 25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxycarbonyl or lower-alkoxycarbonyloxy, (CRi R 2 )p-(CR 3 =CR 4 ) m Q, or (CR 1 R 2 )p-C=C-Q; Ri, R 2 , R 3 and R 4 are independently H, lower-alkyl, optionally substituted with halo; n is 1-5; m is 1-5; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.

Inventors

  • 👤 Kurt A. C/O Sterling Winthrop Inc. Josef
  • 👤 Edward R. C/O Sterling Winthrop Inc. Bacon
  • 👤 Kimberley G. C/O Sterling Winthrop Inc. Estep
  • 👤 Carl C/O Sterling Winthrop Inc. Illig
  • 👤 Brent D. C/O Sterling Winthrop Inc. Douty

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-02 15:04
CPC Classifications
C; C07; C07C; C07C17/00; C07C17/093; C07C17/10; C07C17/12; A; A61; A61K; A61K49/00; A61K49/04; A61K49/0433; A61K49/0447; A61K49/0461; A61K51/00; A61K51/12; A61K51/1217; C07C17/26; C07C17/263; C07C17/2635; C07C17/35; C07C17/354; C07C25/00; C07C25/02; C07C69/00; C07C69/62; C07C69/65

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 135 words
An x-ray contrast composition for oral or retrograde examination comprising: a polymeric material capable of forming a coating on the gastrointestinal tract, said polymeric material having atoms containing polarizable electrons thereon, in combination with a divalent cation: and an x-ray contrast producing agent having the formula, or a pharmaceutically acceptable salt thereof wherein R = Ci-C 25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxycarbonyl or lower-alkoxy-carbonyloxy, (CR 1 R 2 )p-(CR 3 =CR 4 ) m ,Q, or (CR 1 R 2 )p-C=C-Q; Ri, R 2 , R 3 and R 4 are independently H, lower-alkyl, optionally substituted with halo; n is 1-5; m is 1-5; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl in a pharmaceutically acceptable carrier.
Claim 2
Dependent Claim 135 words
An x-ray contrast composition for oral or retrograde examination comprising: a polymeric material capable of forming a coating on the gastrointestinal tract, said polymeric material having atoms containing polarizable electrons thereon, in combination with a divalent cation: and an x-ray contrast producing agent having the formula, or a pharmaceutically acceptable salt thereof wherein R = Ci-C 25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxycarbonyl or lower-alkoxy-carbonyloxy, (CR 1 R 2 )p-(CR 3 =CR 4 ) m ,Q, or (CR 1 R 2 )p-C=C-Q; Ri, R 2 , R 3 and R 4 are independently H, lower-alkyl, optionally substituted with halo; n is 1-5; m is 1-5; p is 1-10; and Q is H, lower-alkyl, lower-alkenyl lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl in a pharmaceutically acceptable carrier.
Claim 3
Dependent Claim 36 words
A composition as claimed in claim 1 wherein said contrast agent is selected from the group consisting of: 1,3,5-tri-N-hexyl-2,4,6-triiodobenzene, 1,3,5-triethyl-2,4,6-triiodobenzene, 1,3,5-tri-N-butyl-2,4,6-triiodobenzene, 1,3,5-tri-(4-methylpentyl)-2,4,6-triiodobenzene, 1,3,5-tri-N-pentyl-2,4,6-triiodobenzene, 1,3,5-tri-(3-methylbutyl)-2,4,6-triiodobenzene. 1,3,5-tri-N-propyl-2,4,6-triiodobenzene, 1,3,5-tri-N-heptyl-2,4,6-triiodobenzene, 2-(4-iodophenyl)nonane, 9-(p-iodophenyl)-10-undecenoic acid ethyl ester and (E)-11-(p-iodophenyl)-9-undecenoic acid ethyl ester.
Claim 4
Dependent Claim 33 words
A composition as claimed in claim 1 wherein said divalent cation is selected from the group consisting of Ca ++ , Mg ++ , Zn ++ , Ba ++ and a mixture thereof.
Claim 5
Dependent Claim 32 words
A composition as claimed in claim 1 wherein said polymeric material is anionic having the formula: wherein R is the polymeric chain; are anionic ligands; and M ++ is a divalent cation.
Claim 6
Dependent Claim 22 words
A composition as claimed in claim 4 wherein said anionic polymeric material is a sulfated polysaccharide having the formula: wherein R is
Claim 7
Dependent Claim 27 words
A composition as claimed in claim 1 wherein said polymeric material is cationic selected from the group consisting of: dermatan sulfate, keratosulfate, hyaluronic acid, heparin and chitin.
Claim 8
Dependent Claim 14 words
A composition as claimed in claim 1 wherein said polymeric material is a polysaccharide.
Claim 9
Dependent Claim 15 words
A composition as claimed in claim 1 wherein said polymeric material is a cellulose derivative.
Claim 10
Dependent Claim 20 words
A composition as claimed in claim 1 wherein said polymeric material is polyvinylpyrrolidone, polyvinyl alcohol or an ethylene oxide polymer.
Claim 11
Dependent Claim 16 words
A composition as claimed in claim 1 wherein said pharmaceutical carrier contains at least one surfactant.
Claim 12
Dependent Claim 12 words
A composition as claimed in claim 10 wherein said surfactant is cationic.
Claim 13
Dependent Claim 12 words
A composition as claimed in claim 10 wherein said surfactant is anionic.
Claim 14
Dependent Claim 12 words
A composition as claimed in claim 10 wherein said surfactant is zwitterionic.
Claim 15
Dependent Claim 12 words
A composition as claimed in claim 10 wherein said surfactant is nonionic.
Claim 16
Independent Claim 45 words
A method of carrying out x-ray examination of the gastrointestinal tract of a patient, said method comprises the oral or rectal administration to the patient of an effective contrast producing amount of a x-ray contrast composition as defined in any one of the preceding claims.
Claim 17
Dependent Claim 40 words
A method as claimed in claim 15 wherein the amount of contrast agent administered to said patient is in the range of from about 0.1 to about 16.0 g iodine/kg body weight for regular x-ray visualization of the gastrointestinal tract.
Claim 18
Dependent Claim 41 words
A method as claimed in claim 15 wherein the amount of contrast agent administered to said patient will be in the range of from about 1 to about 600 mg iodine/kg body weight for CT scan visualization of the gastrointestinal tract.

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