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We carried out the mechanochemical polymerization of methacryloyl derivatives of acetoaminophen and 5-fluorouracil in the presence of lactose. The reaction proceeded readily and the polymeric prodrugs were quantitatively prodruced. This method produces powdered polymeric produgs in which fine particles of lactose are homogeneously dispersed, sicne the reaction proceeds quantitatively through a totally dry process. It is difficult to prepare such a powdered polymeric prodrug by conventional solution polymerization.The rate of drug release of polymeric prodrugs increases with increasing content of lactose, as is shown to be true of the specific surface of polymeric prodrugs. These results suggest that lactose is homogeneously dispersed in powdered polymeric prodrugs.The present method seems applicable to a wide variety of pharmaceutical aids. If one takes the physicochemical property of pharmaceutical aids into consideration, novel polymeric prodrugs with a variety of drug release rates can be synthesized simultaneously with mixing.