title: Applying the Taguchi design for optimized formulation of sustained release gliclazide chitosan beads: an in vitro/in vivo study.
abstract: Gliclazide is a second generation of hypoglycemic sulfonylurea and acts selectively on pancreatic beta cell to control diabetes mellitus. The objective of this study was to produce a controlled release system of gliclazide using chitosan beads. Chitosan beads were produced by dispersion technique using tripolyphosphate (TPP) as gelating agent. The effects of process variables including chitosan molecular weight, concentration of chitosan and TPP, pH of TPP, and cross-linking time after addition of chitosan were evaluated by Taguchi design on the rate of drug release, mean release time (MRT), release efficiency (RE(8)%), and particle size of the beads. The blood glucose lowering effect of the beads was studied in normal and streptozotocin-diabetic rats. The optimized formulation CL(2)T(5)P(2)t(10) with about 31% drug loading, 2.4 h MRT, and 69.16% RE(8)% decreased blood glucose level in normal rats for 24 h compared to pure powder of gliclazide that lasted for just 10 h.
authors.affiliation: Isfahan Pharmaceutical Sciences Research Center and Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran. varshosaz@pharm.mui.ac.ir
authors.forename: J
authors.initials: J
authors.lastname: Varshosaz
authors.forename: N
authors.initials: N
authors.lastname: Tavakoli
authors.forename: M
authors.initials: M
authors.lastname: Minayian
authors.forename: N
authors.initials: N
authors.lastname: Rahdari
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000187:drug effects*; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D003432:Cross-Linking Reagents / Q000737:chemistry; D003692:Delayed-Action Preparations; D003921:Diabetes Mellitus, Experimental / Q000097:blood / Q000188:drug therapy*; D004337:Drug Carriers; D004339:Drug Compounding; D005782:Gels; D005907:Gliclazide / Q000737:chemistry / Q000494:pharmacology*; D006863:Hydrogen-Ion Concentration; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000494:pharmacology*; D007700:Kinetics; D008297:Male; D015233:Models, Statistical; D008970:Molecular Weight; D010316:Particle Size; D011122:Polyphosphates / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D001786:Blood Glucose; D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005782:Gels; D007004:Hypoglycemic Agents; D011122:Polyphosphates; D048271:Chitosan; D005907:Gliclazide; C005692:triphosphoric acid