Pharmacokinetic results on naproxen prodrugs based on poly(ethyleneglycol)s.
Five prodrugs of S(+)-2-(6-methoxy-2-naphthyl)propionic acid (naproxen), in which the drug was bound by ester linkages to diethyleneglycol (I), triethyleneglycol (II), octanediol (III), butyl-triethyleneglycol (IV), and butyl-tetraethyleneglycol (V), respectively, were prepared and tested for their pharmacokinetic properties after oral administration. It was found that bioavailabilities decreased in the order, and in all cases were lower than that of the free drug.
Ranucci
E
E
Dipartimento di Ingegneria Meccanica, Università di Brescia, Italy.
Sartore
L
L
Peroni
I
I
Latini
R
R
Bernasconi
R
R
Ferruti
P
P
D000284:Administration, Oral; D000818:Animals; D004337:Drug Carriers; D008297:Male; D015394:Molecular Structure; D009288:Naproxen / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D011092:Polyethylene Glycols; D011355:Prodrugs / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D004337:Drug Carriers; D011355:Prodrugs; D011092:Polyethylene Glycols; D009288:Naproxen