Synthesis And Controlled Release Of Polyacrylamide / Dextran - Propafenone Macromolecule Prodrugs

Two kinds macromolecular prodrugs were synthesized with PHPMA and dextran which were used as the carrier,the products were characterized with modern technology(UV、IR、 DSC and element analysis).At last, The controlled release studies in vitro were characterized with UV in a series of buffer solutions.The first prodrug was the PHPMA-Propafenone.It was synthesized by the acylation reaction with between isopropanolamine and methacryloylchloride,then products that PHPMA which were different of molecular weight were synthesized by changing the dosages of AIBN.Then the Propafenone was connected to the PHPMA in the influence by the succinic anhydride as the linker and the products were obtained by it.the products were characterized by UV、IR and DSC.In the end, the controlled release of prodrug studies were advanced in several kinds of buffer solutions (pH=1.1、pH=7.4、pH=10.0). The results showed that three prodrugs all contain the active ingredient (Propafenone) and release it slowly.The rate of releasing propafenone in prodrugs was that:PHPMA 11000-Propafenone>PHPMA 16000-Propafenone>PHPMA23000-Propafenone. The release rate of the same prodrug in different of the buffer solutions was:pH=10.0>pH=7.4>pH=1.1.The another was dextran-propafenone.Firstly, two kinds of dextran in the average molecular weight of 20000 and 40000 were modified by succinic anhydride which was use as the linker.Then the propafenone was connected to previous product. In this way, Dextran-Propafenone(D20000-Propafenone and D40000-Propafenone) were synthesized.The final product was characterized by UV、IR and DSC.At last, the controlled release of prodrug studies were performed in different buffer solutions(pH=1.1、pH=7.4、pH=10.0).The data were showed that the release rate of the same prodrug in different of the buffer solutions was: pH=10.0>pH=7.4>pH=1.1.The release rate of the D20000-propafenone was faster than D40000-propafenone.