| abstract |
A novel positively charged prodrug of diclofenac represented by formula (1) was synthesized. The positively charged amino groups of these prodrugs not only greatly increase the solubility of the drug, but also bind to the negative charge on the membrane phosphate head group, pushing the prodrug into the cytosol. The prodrug, diethylaminoethyl 2 [(2,6-dichlorophenyl) amino] benzene acetate acetate, is ~ 250 times faster than diclofenac and ethyl 2 [(2,6-dichlorophenyl) amino] benzene acetate Diffuse through. Prodrugs can be used pharmaceutically not only for oral administration but also transdermally for the treatment of diclofenac-treatable conditions in humans or animals, avoiding the side effects of most diclofenac. A controlled transdermal delivery system for prodrugs allows diclofenac to continually reach optimal therapeutic blood levels, increase efficacy and reduce its side effects. |