Versuche zur Darstellung hochmolekularer Pharmazeutika, 1. Mitt.: Synthese, Reaktionen und14C-Markierung eines Acetylsalicylsäurestärkeesters

Polymeric salicylate derivatives

“…Some work on the incorporation of salicylates into polymers has been carried out. [13][14][15][16][17][18][19] Thus, O-acetylsalicyloyl chloride was allowed to react with soluble starch in the presence of potassium hydroxide, and a polymer having 0.7 aspirin groups per glucose unit was obtained.13-14 "Starch (2 g, 0.0124 mol, anhydroglucose units) in pyridine was ¡allowed to react with the chloroformate derivative of the salicylates obtained by reaction of the salicylate ester with phosgene in toluene (12.5% solution) in : the presence of triethylamine. The salicylate polymer was isolated as well as the salicylate dicarbonate obtained as a side product.…”

Prodrugs for the improvement of drug absorption via different routes of administration

“…As a recent example, one may mention dextran, soluble starch or hydroxyethyl starch -based ester -prodrugs of naproxen (31), but other polysaccharides have been tested for their usefulness as transport groups for therapeutic agents. Among them one can mention starch for acetyl salicylic acid (32,33), inulin for procainamide (34,35), agarose for mitomycin (36) or for adriamycin (37), soluble starch for nicotinic acid (38), or for salicylate (39), cellulose for metribuzin (40) or for insulin (41) and hydroxypropyl cellulose for estrone and testosterone (42,43). However, clinical experience with such prodrugs is still too limited for an adequate judgment on this aspect of macromolecular prodrugs.…”