Effect of core and surface cross-linking on the entrapment of metronidazole in pectin beads.
The purpose of this study was to improve the entrapment efficiency of the water-soluble drug metronidazole using internal cross-linking agents. Calcium pectinate beads containing metronidazole were prepared by dropping a drug-pectin solution in 1% and 5% (m/V) calcium chloride for surface cross-linked beads. For the core cross-linked beads calcium carbonate was dispersed in the drug-pectin solution. The beads were characterized by particle size, swelling ratio, SEM, DSC, and in vitro drug release. It was found that the beads obtained by core cross-linking produced more drug entrapped beads than the surface cross-linked beads. Beads obtained using 1% (m/V) calcium chloride showed more drug entrapment than these obtained using 5% calcium chloride. The core cross-linking of pectin beads reduced drug loss by about 10-20%. The water lodging capacity of beads depended upon gel strength which is a function of the internal gelling agent and pectin concentration. Complete drug release was observed within 30-60 min in the acidic dissolution medium. This work has showed that the core cross-linking agent increases the water-soluble drug entrapment in calcium pectinate beads.
Pawar
Atmaram P
AP
Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune-411038, India. p_atmaram@rediffmail.com
Gadhe
Anil R
AR
Venkatachalam
Prabakaran
P
Sher
Praveen
P
Mahadik
Kakasaheb R
KR
D000890:Anti-Infective Agents / Q000737:chemistry*; D002119:Calcium Carbonate / Q000737:chemistry; D002122:Calcium Chloride / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D004337:Drug Carriers / Q000737:chemistry*; D005782:Gels / Q000737:chemistry; D008795:Metronidazole / Q000737:chemistry*; D008863:Microspheres; D010316:Particle Size; D010368:Pectins / Q000737:chemistry* / Q000648:ultrastructure; D013499:Surface Properties
D000890:Anti-Infective Agents; D004337:Drug Carriers; D005782:Gels; D008795:Metronidazole; D010368:Pectins; D002119:Calcium Carbonate; D002122:Calcium Chloride