Abstract

FORMULATION AND COMPARITIVE IN-VITRO EVALUATION OF ZOLPIDEM TARTRATE SOLID DISPERSION SUBLINGUAL TABLET

*Tharini L. and Satish C. S.

Abstract

The present study is an attempt to increase solubility of an antipsychotic drug Zolpidem tartrate by designing it as solid dispersionsublingual (SDSL) tablets to maintain the desired plasma concentration of the drug. The solid dispersion and physical mixtures of Zolpidem Tartrate in PEG-6000, PEG-4000 and Poloxamer-188 with different ratios were prepared by solvent evaporation method and melting method. The pre- compression and post-compression parameters and release profiles of Zolpidem Tartrate with polymers are carried out to select the optimized formulation, among which Zolpidem Tartrate in Poloxamer-188 (ratio 1:5) by solvent evaporation method resulted in highest increase in dissolution rate and optimum rate of release of the drug. The SDSL tablets was prepared by direct compression technique using Crospovidone, Sodium starch glycolate, crosscarmellose sodium as superdisintegrant, directly compressible Mannitol as diluent, MCC as diluent, tablet disintegrant, Magnesium stearate as lubricant and Aspartame as sweetening agent. The disintegration efficiency was found to be better for Croscarmellose sodium when compared to Crospovidone and Sodium starch glycolate. FTIR spectrum of pure drug and the mixture of drug-polymers revealed no chemical interaction. The pre-compression study indicated good flow properties of bulk powder which is within an acceptable range. In-vitro drug release from the formulations was studied using buffer pH 6.8. From the entire formulations, the best in vitro disintegration time, in vitro drug release was obtained with the optimized formulation F6 containing 5% of Croscarmellose sodium. The tablets of formulation F6 have a hardness 3.3±0.5 kg/cm2, disintegration time of 14.00±1.41 seconds and % drug release of 99.87±0.42% in 30mins. The optimized formulations were also found to be stable during stability studies conducted for 3 months as per ICH guidelines.

Keywords: ZolpidemTartrate, Poloxamer-188, Solid dispersion, Croscarmellose sodium, Crospovidone, Sodium Starch Glycolate, Dissolution, Sublingual tablet.