MODIFIED POLYELECTROLYTES AS SOLUBILIZERS FOR PARENTERAL ADMINISTRATION

Up to now there is no excipient for the solubilization of poorly water soluble drugs that can be used without limitations in pharmaceutical p reparations for intravasal application. The available surfactants show considerable hemolytic activity, cause anaphylactic reactions are che mically instable or have no sufficient solubilizing capacity. By polym erisation of non-ionic surfactants amphiphilic side-chain-polymers are obtained which show in vitro the same solubilization capacity as the monomers but exhibit practically no hemolytic activity. The objective of this work was to investigate, if this findings are also true for io nic oligomers. For this purpose, polyacrylic acids were substituted wi th long-chain alkyl amines. The solubilization capacity of these oligo meres exceeds that of non-ionic amphiphilic sidechain-polymers and tha t of other surfactants. The hemolytic activity of the oligomers was be low that of common ionic surfactants. The solubilization capacity as w ell as the hemolytic activity depends on the oligomers degree of subst itution. Considering their high solubilization capacity and their low hemolytic activity, these oligomers may be excipients in preparations for parenteral application.