马钱子碱固体脂质纳米粒凝胶骨架缓释片的研制  

Study on matrix sustained release tablets of brucine solid lipid nanoparticles

作　　者：邓向涛 阮晓东 郝海军 DENG Xiang-tao;RUAN Xiao-dong;HAO Hai-jun(Affiliated Cancer Hospital of Zhengzhou University,Zhengzhou 450003,China;Technique Center,Shanghai LeiYunShang Pharmaceutical Co.,Ltd.,Shanghai 201401,China;China State Institute of Pharmaceutical Industry,Shanghai 201203,China)

机构地区：[1]郑州大学附属肿瘤医院药学部,河南郑州450003 [2]上海雷允上药业有限公司技术中心,上海201401 [3]中国医药工业研究总院,上海201203

出　　处：《中草药》2018年第22期5298-5304,共7页Chinese Traditional and Herbal Drugs

基　　金：国家科技重大专项(2018ZX09201009-002-009)

摘　　要：目的制备马钱子碱固体脂质纳米粒(SLN)及其冻干粉,进一步制备成马钱子碱固体脂质纳米粒凝胶骨架缓释片(SLN-HMST),并探讨体外释药影响因素及释药机制。方法在单因素考察的基础上设计正交试验优化马钱子碱SLN-HMST处方。分别采用零级模型、一级模型和Higuchi模型对马钱子碱SLN-HMST体外释药模型进行拟合,采用Ritger-Pappas模型探讨缓释片释药机制。结果优化后的马钱子碱SLN-HMST体外释放行为符合一级释药模型,释药方程为ln(1-Mt/M∞)=-0.212 1 t+0.106 4(r=0.992 3),12 h内累积释放度为91.48%,具有明显的缓释特征,释药机制为扩散和溶蚀共存。结论制备的马钱子碱SLN-HMST,工艺重复性较好,在12 h内具有良好的体外缓释作用。Objective To prepare brucine solid lipid nanoparticles(SLN) and its lyophilized powder, and then hydrogel matrix sustained-release tablets(HMST) of brucine SLN(SLN-HMST) were prepared. The factors that may influence drug release in vitro and release mechanism were also investigated in present study. Methods Based on single factor test, orthogonal test was designed to gain the optimum prescription. Zero-order, First-order and Higuchi models were used for the model fitting of drug release. Ritger-Pappas models were employed to study release mechanism of brucine SLN-HMST. Results Brucine SLN-HMST was better agreed with First-order kinetics model. The equation was ln(1-Mt/M∞) =-0.212 1 t + 0.106 4(r = 0.992 3). The cumulative release could achieve 91.48% in 12 h. The sustained release features were obviously. The drug release from the tablets was controlled by diffusion and degradation of the matrix. Conclusion The prepared brucine SLN-HMST can deliver drug continually for 12 h with good reproducibility.

关 键 词：马钱子碱 固体脂质纳米粒 冻干粉 骨架缓释片 释药机制 正交设计 

分 类 号：R283.6[医药卫生—中药学]