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Namdeo Jadhav, Atmaram Pawar and Anant Paradkar

Effect of drug content and agglomerate size on tabletability and drug release characteristics of bromhexine hydrochloridetalc agglomerates prepared by crystallo-co-agglomeration

The objective of the investigation was to study the effect of bromhexine hydrochloride (BXH) content and agglomerate size on mechanical, compressional and drug release properties of agglomerates prepared by crystallo-co-agglomeration (CCA). Studies on optimized batches of agglomerates (BXT1 and BXT2) prepared by CCA have showed adequate sphericity and strength required for efficient tabletting. Trend of strength reduction with a decrease in the size of agglomerates was noted for both batches, irrespective of drug loading. However, an increase in mean yield pressure (14.189 to 19.481) with an increase in size was observed for BXT2 having BXH-talc (1:15.7). Surprisingly, improvement in tensile strength was demonstrated by compacts prepared from BXT2, due to high BXH load, whereas BXT1, having a low amount of BXH (BXH-talc, 1:24), showed low tensile strength. Consequently, increased tensile strength was reflected in extended drug release from BXT2 compacts (Higuchi model, R2 = 0.9506 to 0.9981). Thus, it can be concluded that interparticulate bridges formed by BXH and agglomerate size affect their mechanical, compressional and drug release properties.

Open access

Atmaram Pawar, Anil Gadhe, Prabakaran Venkatachalam, Praveen Sher and Kakasaheb Mahadik

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.