AIM To improve the bioavailability and taste of
fast disintegrating tablet (FD tablet) containing nicorandil loaded particles.
METHODS A FD tablet
containing nicorandil loaded particles with 1%-4% croscarmellose sodium in addition of D mannitol and lactose (9∶1) was prepared and the dissolution and absorption characteristics were examined, in comparison with FD tablet and commercial tablets of nicorandil. In vivo absorption of nicorandil from FD tablet was evaluated in beagle dogs. RESULTS The disintegration time of FD tablets containing 1% croscarmellose sodium with 6 mm and 10 mm in diameter were about 12 and 23 seconds, respectively. When nicorandil loaded particles consist of myristyl alcohol and stearyl alcohol were put in FD tablet, nicorandil release from FD tablet continued until 6 h while nicorandil release from Sigmart and FD tablet containing nicorandil crystals finished within 5 min. In vivo absorption of nicorandil from Sigmart and FD tablet containing nicorandil crystals was very similar after oral administration in beagle dogs and no statistic difference in AUC, T max , C max was observed between these tablets. However pharmacokinetics parameters of nicorandil after oral administration of FD tablet containing nicorandil loaded particles showed that nicorandil was delivered into the body at a suitable absorption rate with similar AUC, delayed T max and lower C max . CONCLUSION The reports suggest that the modification of properties of myristyl alcohol and stearyl alcohol released from the drug loaded particles system would lead to more acceptable bioavailability of the system. However, The formulation of particles and may have a masking effect against the bitter taste and irritation of the drug.