[Pharmaceutical evaluation of fast-disintegrant tablet containing nicorandil-loaded particles].
OBJECTIVE
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, Tmax, Cmax 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 Tmax and lower Cmax.


CONCLUSIONS
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.
Jin
Y
Y
College of Pharmacy, Zhejiang University, Hangzhou 310031, China. jinyizhz@mail.hz.zj.cn
Ohkuma
H
H
Wang
C F
CF
Natsume
H
H
Sugibayashi
K
K
Morimoto
Y
Y
D000284:Administration, Oral; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001682:Biological Availability; D002266:Carboxymethylcellulose Sodium; D002626:Chemistry, Pharmaceutical; D004285:Dogs; D004337:Drug Carriers; D016503:Drug Delivery Systems; D007785:Lactose / Q000737:chemistry; D008297:Male; D008353:Mannitol / Q000737:chemistry; D020108:Nicorandil / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012995:Solubility; D013607:Tablets / Q000008:administration & dosage / Q000493:pharmacokinetics; D013678:Technology, Pharmaceutical
D000889:Anti-Arrhythmia Agents; D004337:Drug Carriers; D013607:Tablets; D020108:Nicorandil; D008353:Mannitol; D007785:Lactose; D002266:Carboxymethylcellulose Sodium