Abstract:
OBJECTIVE To develop a preparation of pulsatile controlled-release pellets for doxofylline. METHODS The pellet cores containing doxofylline were prepared by extrude-spheronization method. Then the pellets were coated by croscarmellose sodium as swelling layer and the mixture of ethyl cellulose and hydroxypropyl methyl cellulose as controlled release layer via fluidized bed coating method. The effects of pellet cores, swelling layer and controlled release membrane on the profile of drug release in vitro were investigated by single factor test. RESULTS The high doxofylline-loading pellet cores with satisfactory characters were obtained by employing microcelluose, sodium carboxymethyl starch and lactose as ingredients. When the thickness of the swelling layer increased, the lag time of drug release was prolonged and the release rate was enhanced. With the HPMC quantity or molecular weight increasing, the lag time was reduced. The lag time could also be prolonged by plasticizer. CONCLUSION The obtained pellets display good pulsatile drug release behavior, which had a great potential for application.