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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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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cited_by cdi_FETCH-LOGICAL-c306t-8430e68eb1e809bc5e58beb10498c87b7e0ce5b932089b5389a0db903fb94ba33
cites cdi_FETCH-LOGICAL-c306t-8430e68eb1e809bc5e58beb10498c87b7e0ce5b932089b5389a0db903fb94ba33
container_end_page 1312
container_issue 12
container_start_page 1307
container_title Farmaco (Società chimica italiana : 1989)
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creator Zacchigna, Marina
Di Luca, G.
Cateni, F.
Zorzet, S.
Maurich, V.
description 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.
doi_str_mv 10.1016/S0014-827X(02)00019-8
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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
title Improvement of physicochemical and biopharmaceutical properties of theophylline by poly(ethylene glycol) conjugates
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