Abstract
Background: Design and evaluation of sustained release microspheres incorporated in orally disintegrating tablet for glimepiride and comparison with conventional tablet.
Method: Glimepiride (GLP) was encapsulated with different amount of ethyl cellulose polymer by an emulsion solvent evaporation technique. Optimization was done using 32 randomized full factorial design. The physicochemical properties of the formulation like particle Size, morphology, drug loading and encapsulation efficiency and yeild were evaluated using Scanning electron microscopy SEM), Differential scanning calorimetry(DSC) and X ray diffraction. A pharmacokinetic study was conducted on male wistar rats for bioequivalance testing. A single blind study was conducted for taste masking test and disintegration time in human volunteers.
Result: DSC study showed that there was no interaction between drug and polymer in GLP microspheres. Particle size and drug release were dependent on stirring speed and polymer concentration respectively. The drug release mechanism of optimized formulation can be explained with first order model which describes the concentration dependent drug release. Microspheres obtained showed good flow properties with entrapment efficiency of 80-100%.
Conclusion: It can be concluded that GLP microspheres ODT is potential delivery system for GLP as the controlled release of drug from GLP microspheres provides for higher plasma drug content and improved bioavailability which was more than conventional tablet.
Keywords: Orally disintegrating tablet, microspheres, solvent evaporation, direct compression, bioequivalence study, polymer concentration, stirring speed.
Graphical Abstract
44
3