摘要
目的:研制一种生物利用度高且具有缓释作用的口服胰岛素制剂。方法:通过钙离子交联制备羧甲基壳聚糖纳米粒,采用正交试验优化纳米粒制备条件,以透射电镜观察纳米粒形态,激光粒度分析仪测定粒度,高效液相色谱法测定纳米粒包封率和载药量,并对胰岛素的体外释放性能进行考察。结果:优化工艺制备的纳米粒外观形态圆整,平均粒径为(256.1±11.2)nm,包封率为(45±0.41)%,载药量为(17.2±0.33)%,药理相对生物利用度为14.71%。结论:口服载胰岛素羧甲基壳聚糖纳米粒具有降血糖作用和显著的缓释作用,药理相对生物利用度高。
OBJECTIVE To prepare oral insulin-loaded nanoparticles with high bioavailability and sustained release. METHODS Carboxymethyl chitosan nanoparticles were prepared through ionic gelification with calcium ions. Orthogonal test design was used to optimize preparation process. Shapes of nanoparticles were studied by TEM. Nanoparticle size was evaluated by laser particle size determination. High performance liquid chromatography was used to detect drug-loading rate and entrapment efficiency of particles, and the in vitro release was investigated. RESULTS Novel nanopartieles were spherical, homogeneous in particle size （256. 1 ± 11.2）nm, entrapment efficiency （45 ± 0. 4 1）% and drug-loading capacity （17. 2± 0. 33）%. The rela- tive pharmacological bioavailability of insulin-loaded nanoparticles reached 14. 71%. CONCLUSION The insulin-loaded nanop- articles show steady and effective hypoglycemic effects after oral administration and the relative pharmacological bioavailability is high.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2015年第10期887-890,共4页
Chinese Journal of Hospital Pharmacy
基金
国家自然科学基金(编号:50973088)
关键词
羧甲基壳聚糖
纳米粒
胰岛素
口服
降血糖作用
carboxymethyl ehitosan
nanoparticle
insulin
oral
hypoglycemic effect
