Drug – bio-affecting and body treating compositions – In vivo diagnosis or in vivo testing – Magnetic imaging agent
Patent
1983-03-15
1986-11-11
Wiseman, Thomas G.
Drug, bio-affecting and body treating compositions
In vivo diagnosis or in vivo testing
Magnetic imaging agent
424258, 424263, 424264, 424266, 424267, 2602395, 2603974, 564381, 564382, 514 19, 514176, 514 11, 514311, 514356, 514277, 514357, 514492, A61K 4900, A61K 31455, A61K 3344, A61K 3147, C07J 100, C01G 4106, C07C 8728, C07D23902
Patent
active
046222189
ABSTRACT:
Testicularly acting drug species are site-specifically/sustainedly delivered to the testes by administering to a male in need of such treatment a pharmacologically effective amount of the target drug species [D] tethered to a reduced, blood-testis barrier penetrating lipoidal form [D--DHC] of a dihydropyridine.revreaction.pyridinium salt type redox carrier, e.g. 1,4-dihydrotrigonelline. Oxidation of the dihydropyridine carrier moiety in vivo to the ionic pyridinium salt type drug/carrier entity [D--QC].sup.+ prevents elimination thereof from the testes, while elimination from the general circulation is accelerated, resulting in significant and prolongedly sustained testicular-specific drug activity, whether ascribable to the cleavage of the [D--QC].sup.+ entity and sustained release of the drug [D] in the testes and/or to [D--QC].sup.+ itself.
REFERENCES:
patent: 4479932 (1984-10-01), Bodor
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Bodor, N. et al. (including Hassan H. Farag) Science, V. 214, No. 4527, Dec. 1981, pp. 1370-1372.
Bodor, N. et al. (including Hassan H. Farag) J. Medicinal Chem., V. 26, Mar. 83, pp. 313-317.
Cowie et al. J. Phys., V. 171, p. 1976 (London) 1964.
Kurmano, M. Actal Physiol. Scand., V. 71, p. 125, 1967.
Teskin Robin Lyn
University of Florida
Wiseman Thomas G.
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