IMPROVEMENT OF DISSOLUTION OF POORLY SOLUBLE DRUGS BY SOLID DEPOSITION ON A SUPER DISINTEGRANT .2. THE CHOICE OF SUPER DISINTEGRANTS AND EFFECT OF GRANULATION
Gk. Bolhuis et al., IMPROVEMENT OF DISSOLUTION OF POORLY SOLUBLE DRUGS BY SOLID DEPOSITION ON A SUPER DISINTEGRANT .2. THE CHOICE OF SUPER DISINTEGRANTS AND EFFECT OF GRANULATION, European journal of pharmaceutical sciences, 5(2), 1997, pp. 63-69
It is demonstrated that the dissolution from capsules and tablets of p
oorly soluble, hydrophobic drugs can be strongly improved by solid dep
osition of the drug upon hydrophilic, strongly swelling carriers like
the super disintegrants sodium starch glycolate and croscarmellose sod
ium. As an effect of its lower swelling power, the super disintegrant
crospovidone is far less effective than the other super disintegrants.
Wet granulation of poorly soluble drugs with high concentrations of s
odium starch glycolate resulted likewise in a strongly improved drug r
elease and bioavailability from capsules and tablets. It was found, ho
wever, that granules containing a too high concentration of the super
disintegrant slow down the drug release from tablets. This effect is c
aused by the formation of a viscous barrier of the super disintegrant
in the granules during the dissolution process.