Preparation and in vitro drug release mechanism of sustained-release tablets of chelerythrinemesoporous silica nanoparticles
OBJECTIVE To prepare sustained-release tablets of mesoporous silica nanoparticles containing berberine(CHE-MSNs-SRTs)and conduct in vitro drug release.METHODS CHE-MSNs were prepared by solvent evaporation method.Encapsulation efficiency,drug loading,particle size and Zeta potential of CHE-MSNs were determined.Morphology was observed by scanning electron microscope(SEM)and crystal form of chelerythrine was analyzed by X-ray powder diffraction(XRPD).Hydroxypropyl methyl cellulose was used as hydrophilic matrix to prepare CHE-MSNs-SRTs.Single factor investiga-tion and Box-Behnken design-response surface methodwere used to optimize formulation of CHE-MSNs-SRTs.Release model and release mechanism of CHE-MSNs-SRTs were also studied.RESULTS Encapsulation efficiency,drug loading,particle size and Zeta potential of CHE-MSNs were(93.58±1.17)％,(23.15±0.72)％,(223.7±9.24)nm and(0.74±0.06)mV,respectively.CHE-MSNs were spherical or quasi-spherical,and chelerythrine existed as an amorphous form in CHE-MSNs.Optimal formulation of CHE-MSNs-SRTs∶HPMC 4K to HPMC 15K ratio was 1.9∶1,sustained-release material dosage was 17.8 mg/tablet,PEG 4000 dosage was 10.6 mg/tablet.Sustained-release characteristics of CHE-MSNs-SRTs were obvious,and cumulative release rate in 12 h was 93.68％.CHE-MSNs-SRTs were better accorded with Higuchi model,and release mechanism was diffusion and matrix degradation.CONCLUSION The reproducibility of CHE-MSNs-SRTs was favorable,and sustained-release characteristics were obvious.
NETL
NSTL
万方数据
维普
