IngentaConnect Oral sustained delivery of theophylline from thermally reversible...

Authors: Miyazaki S.¹; Kawasaki N.¹; Endo K.¹; Attwood D.²

Source: Journal of Pharmacy and Pharmacology, Volume 53, Number 9, 1 September 2001 , pp. 1185-1191(7)

Abstract:

Thermally reversible gels formed in-situ following the oral administration of dilute aqueous solutions of an enzyme-degraded xyloglucan to rabbits were evaluated as sustained-release vehicles for the delivery of theophylline. In-vitro release of theophylline from gels formed by warming xyloglucan sols (0.5, 1.0 and 1.5% w/w) to 37°C followed root-time kinetics over a period of 4h. Gels formed after oral administration to rabbits of chilled 1.5% w/w aqueous solutions of xyloglucan containing dissolved drug showed sustained-release characteristics with a maximum plasma concentration at 4.5h. The theophylline bioavailability from a 1.5% w/w xyloglucan gel was 1.7–2.5 times that of commercial oral sustained-release liquid dosage forms containing an identical theophylline concentration. It was concluded that dilute solutions of the enzyme-degraded xyloglucan had suitable rheological properties and in-situ gelling characteristics for use as sustained-release vehicles for oral drug delivery. The in-vivo release characteristics of theophylline in a rabbit model suggested the potential for the use of these vehicles in humans for the oral delivery of this drug.

Document Type: Research article

DOI: 10.1211/0022357011776621

Affiliations: 1: Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Ishikari-Tohbetsu, Hokkaido, Japan, 061-0293 2: School of Pharmacy and Pharmaceutical Sciences, University of Manchester, Manchester, UK, M13 9PL

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Oral sustained delivery of theophylline from thermally reversible xyloglucan gels in rabbits