Aim The aim of the present study was to prepare tablets which can rapidlydisintegrate in saliva, containing active ingredient in high dose (37.5% W/W). Methods Rapidlydisintegrating tablets containing rotundine were prepared by direct compression, wet granulation andmoulding, respectively . Different disintegrants and excipients were decided by single factor test.The typical disintegration time measurement and a new method of wetting time measuring wereintroduced for assessing rapidly disintegrating tablets. Results The tablets (80 mg) prepared bydirect compression have the crushing strength of 4.0 kg ?mm^(-2) and rapidly disintegratewithin 15 s in the saliva of healthy volunteers; the tablets prepared by wet granulation also havesufficient strength, a little longer but acceptable disintegration time (within 25 s in saliva) ;and the tablets obtained by moulding show disintegration within 40 s in saliva but low strength (2kg·mm^(-2)) . Disintegration time profiles of tablets are similar to those of wetting time, and thedisintegration and wetting times in vitro are similar to the disintegration time in vivo, thelatter having higher correlation with that in oral cavity. Conclusion The rapidly disintegratingtablets can be prepared by using these three techniques and excipients. Both in vitro disintegrationtime and wetting time are necessary indexes for judgment of in vitro disintegration profile.
