Colon delivery of prednisolone based on chitosan coated polysaccharide tablets.
Colon drug delivery is advantageous in the treatment of colonic disease and oral delivery of drugs unstable or suceptible to enzymatic degradation in upper GI tract. In this study, multilayer coated system that is resistant to gastric and small intestinal conditions but can be easily degraded by colonic bacterial enzymes was designed to achieve effective colon delivery of prednisolone. Variously coated tablets containing prednisolone were fabricated using chitosan and cellulose acetate phthalate (CAP) as coating materials. Release aspects of prednisolone in simulated gastrointestinal fluid and rat colonic extracts (CERM) were investigated. Also, colonic bacterial degradation study of chitosan was performed in CERM. From these results, a three layer (CAP/Chitosan/CAP) coated system exhibited gastric and small intestinal resistance to the release of prednisolone in vitro most effectively. The rapid increase of prednisolone in CERM was revealed as due to the degradation of the chitosan membrane by bacterial enzymes. The designed system could be used potentially used as a carrier for colon delivery of prednisolone by regulating drug release in stomach and the small intestine.
Park
Hyun-Sun
HS
College of Pharmacy, Ewha Womans University, Seoul 120-750, Korea.
Lee
Jue-Yeon
JY
Cho
Sun-Hye
SH
Baek
Hyon-Jin
HJ
Lee
Seung-Jin
SJ
D000818:Animals; D002686:Chitin / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D048271:Chitosan; D003106:Colon / Q000187:drug effects* / Q000378:metabolism; D016503:Drug Delivery Systems / Q000379:methods*; D005750:Gastric Juice / Q000187:drug effects / Q000378:metabolism; D007419:Intestinal Secretions / Q000378:metabolism; D011134:Polysaccharides / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011239:Prednisolone / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051381:Rats; D013607:Tablets
D011134:Polysaccharides; D013607:Tablets; D002686:Chitin; D048271:Chitosan; D011239:Prednisolone