Improvement of physicochemical and biopharmaceutical properties of theophylline by poly(ethylene glycol) conjugates.
In the present paper two theophylline esters with poly (ethylene glycol) (PEG) and methoxy poly (ethylene glycol) (mPEG) were prepared. Quantitative yields of the pure products were obtained. Unlike the free drug, the drug-polymer conjugates are freely water-soluble at room temperature. In vitro release experiments in aqueous buffer demonstrate that both conjugates are stable in buffer of pH 7.4 and 1.2. In vivo release studies after oral administration of theophylline conjugates demonstrate a good release of parent drug.
Zacchigna
Marina
M
Dipartimento di Scienze Farmaceutiche, piazzale Europa 1, 34127 Trieste, Italy. zacchigna@univ.trieste.it
Di Luca
G
G
Cateni
F
F
Zorzet
S
S
Maurich
V
V
D000818:Animals; D001702:Biopharmaceutics; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D008297:Male; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000493:pharmacokinetics*; D011817:Rabbits; D013806:Theophylline / Q000737:chemistry* / Q000493:pharmacokinetics*
D011092:Polyethylene Glycols; D013806:Theophylline