星点设计效应面法优选左乙拉西坦生物黏附缓释片的处方研究
关键词：左乙拉西坦；生物黏附缓释片；星点设计-效应面法；释放度
Study on the Formulation Optimization of Levetiracetam Bioadhesive Sustained-Release Tablets by Central Composite Design-Response Surface Methodology
Abstract: Objective To screen the optimizing prescription of bioadhesive sustained-release tablets of levetiracetam，establish the assay method for the release in vitro of levetiracetam. Method In this paper, the release rate in vitro was used as indicator to evaluate the effects of HPMC viscosity, Carpol viscosity, cohesives on the bioadhesive sustained-release tablets of levetiracetam. To determine the sustained-release tablets prescription. The prescription of was excellently screened by central composite design-response surface methodology, and the dosage of HPLC(X1) and Carbomer(X2) as the research factors. The release rate in vitro of each prescription was determined and analyzed so as to choose the best. Results UV method was developed to determine the releasing degree in vitro. The concentration of Levetiracetam over the range of 0.10~0.80 mg/mL, A = 0.7269 C + 0.0003(r = 0.9996)，which showed this method was accurate, reliable and reproducible. Determine the method for measuring adhesion in vitro and screening the optimal prescription. Conclusion The established model based on the theory of central composite design is suitable for screening the optimizing prescription of bioadhesive sustained-release tablets of levetiracetam, and it can be used for further research.
Keywords: levetiracetam; bioadhesive sustained-release tablets; central composite design-response surface methodology; release rat
目 录
1 绪论 1
1.1 生物黏附制剂研究进展 1
1.1.1 生物黏附机制 1
1.1.2 常用的生物黏附材料 2
1.1.3 生物黏附新剂型的开发 2
1.1.4 生物黏附性能测定 2
1.1.5 展望 3
1.2 左乙拉西坦研究综述 3
1.2.1 研究背景 3
1.2.2 研究进展 4
1.2.3 药效学研究 5
1.2.4 药理作用 6
1.2.5 临床研究 6
1.2.6 不良反应 6
1.3 课题立项意义 7
1.4 课题研究内容 7
2 左乙拉西坦生物黏附缓释片处方前研究 8
2.1 材料 8
2.1.1 仪器 8
2.1.2 试药 8
2.1.3 动物 8
2.2 体外释放度测定方法学研究 8
2.2.1 紫外吸收波长的选择 8