S. Miyazaki et al., Oral sustained delivery of theophylline from thermally reversible xyloglucan gels in rabbits, J PHARM PHA, 53(9), 2001, pp. 1185-1191
Thermally reversible gels formed in-situ following the oral administration
of dilute aqueous solutions of an enzyme-degraded xyloglucan to rabbits wer
e evaluated as sustained-release vehicles for the delivery of theophylline.
In-vitro release of theophylline from gels formed by warming xyloglucan so
ls (0.5, 1.0 and 1.5% w/w) to 37 degreesC followed root-time kinetics over
a period of 4 h. Gels formed after oral administration to rabbits of chille
d 1.5% w/w aqueous solutions of xyloglucan containing dissolved drug showed
sustained-release characteristics with a maximum plasma concentration at 4
.5 h. The theophylline bioavailability from a 1.5% w/w xyloglucan gel was 1
.7-2.5 times that of commercial oral sustained-re lease 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-releas
e vehicles for oral drug delivery. The in-vivo release characteristics of t
heophylline in a rabbit model suggested the potential for the use of these
vehicles in humans for the oral delivery of this drug.