Taste masking of azithromycin by resin complex and sustained release through interpenetrating polymer network with functionalized biopolymers.
OBJECTIVE
The objective was to evaluate taste masking of azithromycin (AZI) by ion exchange resins (IERs) and the formation of covalent semi interpenetrating polymer network (IPN) beads using chitosan (CS) and sodium carboxylated agarose (SCAG) for sustained release of drug.


METHODS
Methacrylic acid (MAA)-based IERs were prepared by suspension polymerization method. Drug release complexes (DRCs) were prepared by different drug:resin ratios i.e. 1:1, 1:2 and 1:4. The resultant DRCs were characterized using DSC, FTIR, PXRD, in vivo and in vitro taste masking, and in vitro drug release at gastric pH. IPN beads were prepared by entrapping DRCs with bio polymers and cross linked with trisodium citrate (NaCIT), and further cross-linked with glutaraldehyde (GA) for sustained release of AZI.


RESULTS
In vitro and in vivo taste masking studies showed that MD1:4 DRC formulation was optimal. The release of AZI from DRC was found to be very fast at gastric pH i.e. 97.37 ± 1.02% within 45 min. The formation of IPN beads was confirmed by FTIR. The release of drug from IPN beads at gastric and intestinal pH was found to be "<28% and <60%", respectively. The release kinetics showed Fickian diffusion profile for ionically cross-linked beads and zero-order release mechanism for GA cross-linking beads.


CONCLUSIONS
DRCs can be effectively used for taste masking and newly formulated IPN beads demonstrated sustained release of AZI.
a Reverse Osmosis Membrane Division , Central Salt and Marine Chemicals Research Institute, Council of Scientific & Industrial Research (CSIR) , Bhavnagar , Gujarat , India.|b Academy of Scientific and Innovative Research , Central Salt and Marine Chemicals Research Institute, Council of Scientific & Industrial Research (CSIR) , Bhavnagar , Gujarat , India.
A Michael
AM
Rajesh
a Reverse Osmosis Membrane Division , Central Salt and Marine Chemicals Research Institute, Council of Scientific & Industrial Research (CSIR) , Bhavnagar , Gujarat , India.|b Academy of Scientific and Innovative Research , Central Salt and Marine Chemicals Research Institute, Council of Scientific & Industrial Research (CSIR) , Bhavnagar , Gujarat , India.
Kiritkumar Mangaldas
KM
Popat
D000293:Adolescent; D000328:Adult; D017963:Azithromycin / Q000737:chemistry*; D001704:Biopolymers / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D048271:Chitosan / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004058:Diffusion; D065546:Drug Liberation / Q000187:drug effects; D005260:Female; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007475:Ion Exchange Resins / Q000737:chemistry*; D008297:Male; D012685:Sepharose / Q000737:chemistry; D013649:Taste / Q000187:drug effects*; D055697:Taste Perception / Q000187:drug effects*; D055815:Young Adult
D001704:Biopolymers; D003692:Delayed-Action Preparations; D007475:Ion Exchange Resins; D017963:Azithromycin; D012685:Sepharose; D048271:Chitosan
Ion exchange resins; functionalized biopolymers; interpenetrating polymer network; sustained release; taste masking