Mooring Los Gresham, Nicotinic Acid And Polyethylene Glycol, Hydrazine Flexor Oxazine Macromolecule Prodrug Of Controlled Drug Release And Synthesis

Macromolecular prodrugs of nicotinic acid and hydralazine were prepared and characterized through elementary analysis, IR and DSC. The controlled release studies were performed in various media.Nicotinic acid was covalently linked to poloxamer via ester bonds, The average molecular weight used for poloxamer are8350(F68) and11500(F127), respectively, the synthesis of nicotinic acid prodrugs by two steps:(1) synthesis of niacin chloride;(2) synthesis of F68-Nic and F127-Nic. The two prodrugs were characterized by DSC and IR analysis. The release studies were performed in pH1.1,7.4,10.0buffer solutions and pH=8.0buffer solutions in the presence of α-chymotrypsin. The results demonstrated that, two macromolecular prodrugs can be released nicotinic acid; In the presence of α-chymotrypsin, poloxamer-nicotinic conjugate can released from more amounts of nicotinic acid.The hydralazine hydrochloride were linked to poly(ethylene glycol)(PEG) via succinic anhydride. The average molecular weight used for PEG are6000and10000. The prodrugs PEG6000-HLZ and PEG10000-HLZ have been synthesized. Then prodrugs were characterized by DSC and IR analysis. The release studies were performed in pH1.1,7.4,10.0buffer solutions and pH=8.0buffer solutions in the presence of α-chymotrypsin. The results demonstrated that, the drug release rate is the fastest in the alkaline environment and is the slowest in acidic environment. In the present of α-chymotrypsin, more amounts of hydralazine can be released from PEG-HLZ conjugate...