Preparation of paliperidone sustained-release tablets
Objective To prepare matrix membrane controlled sustained release tablets of paliperidone,optimize the formulation and preparation process,and investigate its release characteristics in vitro.Methods By searching the relevant information of the original formulation and other generic drugs,the sustained-release materials such as sodium alginate(SA),hydroxypropyl methylcellulose(HPMC)and polyoxyethylene(PEO)were selected as the gel skeleton core for research,and different kinds of sustained-release materials and different proportions of dosage were selected to determine the core formulation.The coating materials and dosage were optimized to determine the coating prescription.The preparation process of sustained-release tablets was determined by investigating the coating aging temperature and aging time.Results After optimization,SA and HPMC K100LV CR with a mass ratio of 1∶1 were selected as the hydrophilic gel skeleton,anhydrous lactose was used as the filler,and magnesium stearate was used as the lubricant.The sustained-release film was coated with ethyl cellulose aqueous dispersion Surelease,HPMC SH-E3 and triethyl citrate(TEC).And the mass ratio of the main components in the coating system was ethyl cellulose mEC∶mHPMC∶mTEC=80:20:15.The aging process was determined as follows:aging for 3 hours at 55-60 ℃ with coating machine.Conclusion The matrix membrane controlled sustained release tablets of paliperidone were successfully prepared.The formulation and preparation process were reasonable.The dissolution curve in vitro was between that of reference listed drug(RLD)and that of reference preparation,so it would be more likely to pass the consistency evaluation.
万方数据
维普
