A simple method for the preparation of PEG-6-mercaptopurine for oral administration.
A new and efficient method for the synthesis of PEG-6-mercaptopurine is described. The key feature of the proposed approach is the protection of the thiol group against metabolic inactivation. Preliminary in vivo and in vitro evaluations of the macromolecular prodrug have been carried out.
Zacchigna
Marina
M
Department of Pharmaceutical Science, piazzale Europa 1, 34127 Trieste, Italy. zacchign@units.it
Cateni
Francesca
F
Di Luca
Gabriella
G
Drioli
Sara
S
D000284:Administration, Oral; D016503:Drug Delivery Systems; D006801:Humans; D015122:Mercaptopurine / Q000008:administration & dosage* / Q000097:blood / Q000138:chemical synthesis*; D011092:Polyethylene Glycols; D011355:Prodrugs / Q000008:administration & dosage / Q000138:chemical synthesis
D011355:Prodrugs; D011092:Polyethylene Glycols; D015122:Mercaptopurine