Preparation and characterization of nifedipine skeleton frame sustained release tablets with hydroxypropyl-beta-cyclodextrin and polyethylene glycolas as matrix / 重庆医学

ABSTRACT

Objective To prepare nifedipine (NP)skeleton frame sustained release tablets by adopting hydroxypropyl-beta-cy-clodextrin (HPC)and polyethylene glycol (PEG)as the matrix and to investigate its sustained release effect on NP.Methods NP skeleton frame sustained release tablets were prepared by the direct compression method after forming the inclusion complex with NP and HPC on a 1∶1 ratio and mixing with PEG.The in vitro drug release curves and the in vivo concentration-time curves of NP skeleton frame sustained release tablets were detected with the NP-PEG tablet without inclusion complex,NP-HPC tablet and NP powder capsule (NP capsule)as the control.Results The 5 h cumulative release rate of NP skeleton frame sustained release tablet in the simulated gastric fluid test(pH 1.2)was 36.4%,its sustained release effect was significantly stronger than that of the NP-HPC tablet group (80%,P<0.01)and the NP-PEG tablet group (100%,P<0.01).The in vivo test showed that AUC0-12 [(6 413±436)h/(ng·mL)],Cmax[(983±192)ng/mL]and tmax[(5.7±1.1)h]in the NP skeleton frame sustained release group were significantly higher than those in the NP-HPC tablet group,the NP-PEG tablet group and the NP Capsule group (all P<0.01 or 0.05).Conclusion NP skeleton frame sustained release tablets exhibits the sustained release effect on NP,can extend the NP in vitro release time,and improve the NP′s bioavailability,which is a novel NP sustained release tablet with excellent properties.