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Title: Pro-drug forms of digoxin and method of preparing and using same

Abstract: There is provided, a novel pro-drug form of digoxin having the following formula: ##STR1## wherein R represents a member selected from the group consisting of a hydrogen atom, a residue of any naturally occurring amino acid, and a ##STR2## group, wherein X and Y, which may be the same or different, each represent a member selected from the group consisting of a methyl group and an ethyl group, or wherein X and Y may form a (CH.sub.2).sub.4 or (CH.sub.2).sub.5 heterocyclic ring with the N atom to which each of X and Y are attached, and a non-toxic inorganic or organic pharmaceutically acceptable acid addition salt thereof, with the proviso that: When R is a member other than a hydrogen atom, all of said R's must be the same member. These novel compounds will be cleaved in the bloodstream of a warm-blooded animal, thus delivering digoxin in a cardiotonic effective amount. Due to their higher solubility and superior absorption characteristics, the compounds of the instant invention permit a higher and more reproducible level of digoxin bioavailability to be attained in comparison with that which could be attained if digoxin per se was administered.


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Inventors: Bodor, Nicolae S. (Lawrence, KS, US)

Application Number: 664687
Filing Date: 1976-03-08
Publication_date: 1977-05-03
Assignee: Interx Research Corporation (Lawrence, KS)
Primary Class(es): 514/26 536/6.1, 536/6.2
Other Classes:
US Patent Ref:
3884905May, 1975Bodor260/210.

Other Refs:
Primary Examiner: Gotts, Lewis
Assistant Examiner: Owens, Cary
Attorney: Blitzer; Charles N.