摘要
目的研究灯盏花素自微乳化释药系统的处方及特性。方法通过溶解度试验、处方配伍和伪三相图的绘制,筛选油相、表面活性剂、助表面活性剂的最佳搭配和配比。并对灯盏花素自微乳化释药系统的理化性质、体外溶出度和大鼠在体肠吸收情况进行了测定。结果灯盏花素自微乳化最终优化处方为:Maisine 35-1、Cremo-phor RH40、PEG400、TEA比例为25∶40∶35∶7。灯盏花素自微乳化释药系统的粒径为88.6 nm,在1 h时体外溶出率达到97.8%,约是灯盏花素原料药的8.0倍,是灯盏花素片剂的5.1倍。大鼠在体肠吸收灯盏花素自微乳化释药系统的肠壁通透系数分别是灯盏花素原料的3.4倍,灯盏花素片剂的3.3倍。结论所制备的灯盏花素自微乳化释药系统促进了灯盏花素的溶出和吸收,为灯盏花素的新制剂开发提供了实验依据。
Objective To study formulation and characteristics of self-microemulsifying drug delivery system for breviseapine （BRV-SMEDDS）. Methods The optimum formulations of BRV-SMEDDS were screened by solubility tests, formula compatibility, and pseudo-ternary phase diagrams. And the physieo chemical characters, dissolution in vitro and in situ rat＇s intestine absorption of BRV-SMEDDS were also observed. Results The optimum formulation of SMEDDS was composed of Maisine 35-1-Cremophor RH40-PEG400-TEA=25 ： 40 ： 35 ： 7. The particle diameter was 88.6 nm. The percent of accumulated dissolution of BRV in SMEDDS in vitro was up to 97.8% at lh, which was 8.0 times as much as that of BRV powder, and 5.1 times as BRV tablets. In the tests of in situ rat＇s intestine absorption, the permeability coefficient of BRV-SMEDDS was increased by 3.4 times as much as BRV powder, and 3.3 times as BRV tablets. Conclusion The dissolution and absorption of BRV is improved by formulation of SMEDDS. It could provide reference for the new dosage form of BRV.
出处
《中草药》
CAS
CSCD
北大核心
2009年第3期374-378,共5页
Chinese Traditional and Herbal Drugs
基金
湖北省自然科学基金课题(2007ABA071号)
关键词
灯盏花素
自微乳化释药系统
处方研究
特性评价
breviscapine （BRV）
self-microemulsifying drug delivery system （SMEDDS）
formulation design
evaluation on characteristics
