http://dx.doi.org/10.4314/tjpr.v12i4.4
Abstract
Purpose: To formulate simvastatin
orodispersible tablets with high dissolution rate and
enhanced bioavailability.
Methods: Simvastatin solid
dispersions in β-
cyclodextrin, hydroxylpropyl-β-cyclodextrin, and
hydroxylbutyl-β-cyclodextrin were prepared
in different drug: polymer ratios by kneading and
solvent evaporation methods. Compatibility was
investigated by Differential scanning calorimetry (DSC)
and Fourier transform infrared spectroscopy (FTIR) Based
on the results of solubility studies, the most suitable
solid dispersion was selected and formulated into
orodispersible tablets using Emcosoy and K-polacrillin
as superdisintegrants, and mannitol and Pullulan as
diluents. The tablets were evaluated for wetting and
disintegration times, water absorption, and in vtro
dissolution.
Results: Increase in drug
solubility was dependent on polymer type, concentration
and preparation method.
Simvastatin-hydroxylbutyl-β-cyclodextrin solid
dispersion mixture prepared in 1:2 drug: polymer ratio
by solvent evaporation method had a higher solubility
than other dispersions. DSC and FTIR indicated the
formation of solid dispersion without chemical
interaction between simvastatin and polymer.
Orodispersible tablet prepared with Emcosoy and Pullulan
showed least wetting and disintegration times (20 and 35
s, respectively), fastest water sorption rate, and the
highest dissolution rate (100 % after 20 min).
Conclusion: Orodispersible tablets
prepared with Emcosoy as superdisintegratnt and Pullulan
as diluents and containig simvastatin solid dispersion
in hydroxylbutyl-β-cyclodextrin provides
optimum water solubility and hence, drug
bioavailability.
Keywords:
Simvastatin, Emcosoy,
Hydroxylbutyl-β-cyclodextrins, Pullulan,
Polacrillin, Orodispersible, Solid dispersion