Compositions of iodophenoxy alkylene ethers and pharmaceutically acceptable clays for visualization of the gastrointestinal tract
AssigneeSterling Winthrop Inc.
InventorsStephen B. Ruddy, Gregory L. McIntire, Mary E. Roberts, Edward R. Bacon
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Abstract
Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkylene ethers and pharmaceutically acceptable clays in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
Claims22
An x-ray contrast composition for oral or retrograde examination of the gastrointestinal tract comprising on a % weight per volume basis:
- (a) from about 5 to 45% of an x-ray contrast producing agent having the formula, or a pharmaceutically acceptable salt thereof ##STR15## wherein Z is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;
- R is C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR16## or halo-lower-alkyl;
- each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;
- (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;
- R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H or lower-alkyl, optionally substituted with halo;
- x is 1-4;
- n is 1-4;
- m is 1-15;
- p is 1-20;
- and
- Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;
- (b) from about 0.1 to 10% of a pharmaceutically acceptable clay selected from the group consisting of:
- montmorillonite, beidelite, nontronite, hectorite and saponite;
- (c) from about 1.0 to 20% of a surfactant selected from the group consisting of nonionic, anionic, cationic and zwitterionic surfactants;
- (d) from about 0 to 15% of an excipient;
- and
- (e) water to make 100% by volume.
The x-ray contrast composition of claim wherein said surfactant is polyoxyethylene sorbitan fatty acid ester of the formulas (1) and (2) ##STR18## wherein w+x+y+z is selected from the group consisting of 20, 5, and 4.
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 an x-ray contrast formulation comprising:
- (a) from about 5 to 45% of an x-ray contrast producing agent having the formula, or a pharmaceutically acceptable salt thereof ##STR19## wherein Z is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;
- R is C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR20## or halo-lower-alkyl;
- each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;
- (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;
- R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H or lower-alkyl, optionally substituted with halo;
- x is 1-4;
- n is 1-4;
- m is 1-15;
- p is 1-20;
- and
- Q is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;
- (b) from about 0.1 to 10% of a pharmaceutically acceptable clay selected from the group consisting of:
- montmorillonite, beidelite, nontronite, hectorite and saponite;
- (c) from about 1.0 to 20% of a surfactant selected from the group consisting of nonionic, anionic, cationic and zwitterionic surfactants;
- (d) from about 0.0 to 15% of an excipient;
- and
- (e) water to make 100% by volume.
Dependencies are inferred from the claim text.