Optimization of the entrapment efficiency and release of ambroxol hydrochloride alginate beads.

ABSTRACT

The objective of the current study was to optimize the composition of alginate beads to produce ambroxol hydrochloride alginate beads with optimum specifications. The study employed beads based on sodium alginate solution (2% w/v) as the main component with calcium chloride solution as crosslinking agent as the prototype beads. The beads were prepared by syringe method. The effect of viscosity modifiers on the morphology, entrapment efficiency and drug release was studied. The prototype beads were spherical semitransparent with entrapment efficiency (EE) of 23%. Incorporation of polyvinylpyrrolidone (PVP) as a viscosity modifier produced spherical semitransparent beads with higher EE values compared with the prototype. Addition of carboxymethyl cellulose (CMC) produced oval opaque beads which have larger size and higher EE values compared with the prototype beads or those containing PVP only. Replacement of CMC with hydroxypropyl methyl cellulose (HPMC) produced semitransparent spherical beads with significant increase in the EE. Monitoring the drug release rate from different beads, the all the tested beads were able to retain the drug in the stomach condition. In the intestinal conditions the release rate depended on the composition of the beads with prototype beads librating most of its contents in the first 15 minutes. Formulations containing either CMC or HPMC were able to retard the drug release in the intestinal phase. In conclusion the study developed beads with optimum entrapment and release of ambroxol hydrochloride.