ORALLY FAST DISINTEGRATING TABLETS OF SUMATRIPTAN LOADED EUDRAGIT E MICROPARTICLES: A PROMISING CHOICE FOR TASTE MASKINGAbstract
Sumatriptan succinate, a selective 5-hydroxytryptamine-1 receptor agonist, is an antimigraine drug with bitter-taste. The present study was performed to prepare and evaluate eudragit-E microparticles containing sumatriptan and formulate fast disintegrating tablets of drug microparticles to increase patient-compliance and improve the efficacy of drug. Microparticles were prepared by solvent-evaporation method using water-dichloromethane/PVA and water-dichloromethane/liquid paraffin systems. The effect of different variables (polymer:drug ratio, PVA concentration and solvents combination ratios) on particle size and encapsulation efficiency of the microparticles was investigated. The final microparticles were evaluated for particle size, loading percent, taste-masking, thermal analysis and in-vitro release profile. The drug loading were higher in w/o/o emulsion than w/o/w. Mean particle size was not statistically different for different formulations. Sumatriptan release rate from eudragit-E microparticles was very fast in HCl 0.1 N medium and release profile was acceptable for fast disintegrating tablets. The prepared tablets were evaluated for in-vitro disintegration time, weight variation, hardness, friability and in-vitro drug release. The optimized formulation (F6) (provided a pleasant taste and mouth-feel) disintegrated within 20 seconds and released more than 70% of drug within 15 minutes. Tablets formulated by drug loaded eudragit-E microparticles could be a promising formulation for taste-masking and decreasing failure in triptans therapy.
S. Mohammadi Samani, N. Zolfaghari, E. Parhizkar and F. Ahmadi *
Research Center for Nanotechnology in Drug Delivery, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran
18 October, 2016
12 December, 2016
16 December, 2016
01 May, 2017