The controlled release of prednisolone using alginate gel.
In a release study of alginate gel beads, swelling and erosion of the beads were observed at pH 6.8, whereas no swelling occurred at pH 1.2. The amount of released prednisolone (PL) was greater at pH 6.8 than at pH 1.2. The lower the ratio of mannuronic acid block to guluronic acid block in alginate, the slower the release of PL. An increase in loaded PL in the beads resulted in a slower release of PL. The decrease in bead size caused a rapid release of PL. The addition of sodium alginate propylene glycol ester elevated the extent of PL release. The plasma profile of PL showed sustained-release behavior after the oral administration of the beads to beagles. Furthermore, the correlation between in vitro release and in vivo absorption of PL for various alginate gel beads was evaluated using deconvolution and convolution methods. The in vivo absorption of PL was correlated with the PL release at pH 1.2, and it differed from that at pH 6.8. The release of PL from alginate gel beads in vivo appeared to occur under conditions that cause little swelling.
Sugawara
S
S
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Imai
T
T
Otagiri
M
M
D000042:Absorption; D000284:Administration, Oral; D000464:Alginates / Q000737:chemistry*; D000818:Animals; D003692:Delayed-Action Preparations; D004285:Dogs; D004337:Drug Carriers; D020723:Glucuronic Acid; D006603:Hexuronic Acids / Q000737:chemistry; D008297:Male; D008863:Microspheres; D011239:Prednisolone / Q000008:administration & dosage* / Q000378:metabolism / Q000493:pharmacokinetics; D014574:Uronic Acids / Q000737:chemistry
D000464:Alginates; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D006603:Hexuronic Acids; D014574:Uronic Acids; C007896:guluronic acid; C038550:propylene glycol alginate ester; D020723:Glucuronic Acid; C008324:mannuronic acid; D011239:Prednisolone