Emulsion gel beads of calcium pectinate capable of floating on the gastric fluid: effect of some additives, hardening agent or coating on release behavior of metronidazole.
Emulsion gel (EMG) beads of calcium pectinate capable of floating in the gastric condition were developed using an emulsion-gelation method and their release properties were investigated. Attempts to modify the drug release were made by applying some additives into the starting solution prior to bead formation, by hardening with glutaraldehyde, and by coating with polymer. The metronidazole-loaded EMG beads were found to float on simulated gastric fluid. Increasing the drug to pectin ratio in the beads slowed the drug release from the conventional and the EMG beads. However, the drug release from these beads was rapid, i.e., about 80% of drug loading released within 20-80 min. The additives (PEG10000, glyceryl monostearate and Eudragit L) had a slight, insignificant, effect on the drug release. Using 2% glutaraldehyde as a hardening agent prolonged the drug release. Coating the beads with Eudragit RL significantly sustained the drug release while the beads remained buoyant. The results suggest that EMG beads are suitable as a carrier for intragastric floating drug delivery and that their release behaviour could be modified by hardening with glutaraldehyde or by coating with Eudragit RL.
Sriamornsak
Pornsak
P
Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand. pornsak@email.pharm.su.ac.th
Thirawong
Nartaya
N
Puttipipatkhachorn
Satit
S
D002118:Calcium / Q000737:chemistry* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004655:Emulsions; D005750:Gastric Juice / Q000378:metabolism; D005782:Gels; D008795:Metronidazole / Q000737:chemistry* / Q000493:pharmacokinetics; D010368:Pectins / Q000737:chemistry* / Q000493:pharmacokinetics; D013608:Tablets, Enteric-Coated
D003692:Delayed-Action Preparations; D004655:Emulsions; D005782:Gels; D013608:Tablets, Enteric-Coated; D008795:Metronidazole; D010368:Pectins; D002118:Calcium