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 rel...

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Bibliographic Details
Published in:Farmaco (Società chimica italiana : 1989) 2003-12, Vol.58 (12), p.1307-1312
Main Authors: Zacchigna, Marina, Di Luca, G., Cateni, F., Zorzet, S., Maurich, V.
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Biopharmaceutics
Chemical Phenomena
Chemistry, Physical
General pharmacology
Macromolecular prodrugs
Male
Medical sciences
Methoxy poly(ethylene glycol)
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Poly(ethylene glycol)
Polyethylene Glycols - chemistry
Polyethylene Glycols - pharmacokinetics
Rabbits
Respiratory system
Theophylline
Theophylline - chemistry
Theophylline - pharmacokinetics
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Summary: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.
ISSN:0014-827X
1879-0569
DOI:10.1016/S0014-827X(02)00019-8