Titre du document / Document title

Oral sustained delivery of theophylline and cimetidine from in situ gelling pectin formulations in rabbits

Auteur(s) / Author(s)

KUBO Wataru ⁽¹⁾ ; ITOH Kunihiko ⁽¹⁾ ; MIYAZAKI Shozo ⁽¹⁾ ; ATTWOOD David ⁽²⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Hokkaido, JAPON
⁽²⁾ School of Pharmacy and Pharmaceutical Sciences, University of Manchester, Manchester, ROYAUME-UNI

Résumé / Abstract

The aim of this study was to evaluate the potential of an in situ gelling pectin formulation as a vehicle for the oral sustained delivery of theophylline and cimetidine. In vitro studies demonstrated diffusion-controlled release of theophylline from 1, 1.5, and 2% w/v pectin gels. Release of this drug from 1.5% w/v pectin gels formed in situ in rabbit stomach was sustained over a period of 12 hours giving a theophylline bioavailability some seven fold higher than when administered from a commercial syrup. In contrast, interactions between cimetidine and pectin led to weak gelation of the pectin sols that prevented any meaningful determination of in vitro release characteristics. Similarly, in vivo release profiles from pectin formulations containing cimetidine were similar to that from a solution of this drug in buffer, indicative of weak gelation. Examination of the content of the rabbit stomach 5 hours after administration of 1.5% w/v pectin sols containing drug confirmed gel formation, but gels containing cimetidine were noticeably softer than those containing theophylline.

Revue / Journal Title

Drug development and industrial pharmacy   ISSN 0363-9045 

Source / Source

2005, vol. 31, n^o8, pp. 819-825 [7 page(s) (article)] (14 ref.)

Langue / Language

Anglais

Editeur / Publisher

Taylor & Francis, Colchester, ROYAUME-UNI  (1977) (Revue)

Mots-clés anglais / English Keywords

H2 Histamine receptor ; Antihistaminic ; Antagonist ; Xanthine derivatives ; Dosage form ; Vertebrata ; Mammalia ; Lagomorpha ; Antiulcer agent ; Antisecretory agent ; Bronchodilator ; Antiasthma agent ; Respiratory analeptic ; Pharmaceutical technology ; Drug ; Gelation ; Colloidal gel ; Rabbit ; Animal ; Formulation ; Pectin ; In situ ; Cimetidine ; Theophylline ; Controlled release form ; Oral administration ;

Mots-clés français / French Keywords

Récepteur histaminergique H2 ; Antihistaminique ; Antagoniste ; Xanthine dérivé ; Forme pharmaceutique ; Vertebrata ; Mammalia ; Lagomorpha ; Antiulcéreux ; Antisécrétoire ; Bronchodilatateur ; Antiasthmatique ; Analeptique respiratoire ; Technologie pharmaceutique ; Médicament ; Gélification ; Gel colloïdal ; Lapin ; Animal ; Formulation ; Pectine ; In situ ; Cimétidine ; Théophylline ; Forme libération contrôlée ; Voie orale ;

Mots-clés espagnols / Spanish Keywords

Receptor histaminérgico H2 ; Antihistamínico ; Antagonista ; Xantina derivado ; Forma farmacéutica ; Vertebrata ; Mammalia ; Lagomorpha ; Antiulceroso ; Antisecretorio ; Broncodilatador ; Agente antiasma ; Analéptico respiratorio ; Tecnología farmacéutica ; Medicamento ; Gelificación ; Gel coloidal ; Conejo ; Animal ; Formulación ; Pectina ; In situ ; Cimetidina ; Teofilina ; Forma liberación controlada ; Vía oral ;

Mots-clés d'auteur / Author Keywords

Pectin gels ; In situ gelation ; Oral drug delivery ; Sustained release ; Theophylline ; Cimetidine ;

Localisation / Location

INIST-CNRS, Cote INIST : 17132, 35400013182127.0130