白屈菜红碱介孔二氧化硅纳米粒缓释片的制备及体外释药考察
Preparation and in vitro drug release mechanism of sustained-release tablets of chelerythrinemesoporous silica nanoparticles
周敬 1郑宝玉 1李阳杰 1方晓东2
作者信息
- 1. 郑州工业应用技术学院药学与化学工程学院,河南郑州 451150
- 2. 河南大学药学院,河南开封 475004
- 折叠
摘要
目的:制备白屈菜红碱介孔二氧化硅纳米粒缓释片(CHE-MSNs-SRTs),并进行体外释药考察.方法:溶剂挥发法制备CHE-MSNs,测定包封率、载药量、粒径、Zeta电位,扫描电镜观察微观形态,X射线粉末衍射法分析晶型.羟丙基甲基纤维素为骨架材料制备CHE-MSNs-SRTs.单因素考察结合Box-Behnken响应面法优化CHE-MSNs-SRTs处方,对释药模型和释药机理进行探讨.结果:CHE-MSNs平均包封率为(93.58±1.17)％,载药量为(23.15±0.72)％,粒径为(223.7±9.24)nm,Zeta电位为(0.74±0.06)mV,纳米粒呈球形或类球形,白屈菜红碱以无定型状态存在于CHE-MSNs中.CHE-MSNs-SRTs最佳处方为:HPMC 4K和HPMC 15K比例为1.9∶1,缓释材料用量为17.8 mg/片,PEG用量为10.6 mg/片,缓释特征明显,12h累积释放度为93.68％.体外释药符合Higuchi模型,释药机制为扩散和骨架溶蚀并存.结论:CHE-MSNs-SRTs工艺重复性良好,体外释药缓释特征明显.
Abstract
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.
关键词
白屈菜红碱/介孔二氧化硅纳米粒/缓释片Key words
chelerythrine/mesoporous silica nanoparticles/sustained-release tablets引用本文复制引用
出版年
2024
NETL
NSTL
维普
万方数据