摘要
目的:为改善布洛芬的溶出度,提高生物利用度,采用超临界CO2流体技术制备布洛芬-β-环糊精包合物。方法:以包封率为响应值,考察压强、温度和制备时间等工艺条件对制备布洛芬包合物的影响,并用Box Behnken法优化工艺条件。结果:主客分子摩尔比0.87,在包合温度39.64℃和包合压强19.05 MPa条件下反应5 h得到的优化产品中,药物包合率(84.83%)和溶出度(5 min,82%)较高。同时差示热量扫描(DSC)和X-射线粉末扫描(XRPD)的结果显示,布洛芬完全分散在辅料中,呈无定形态。结论:超临界CO2流体技术制备布洛芬包合物可大幅提高包合率和溶出度。
Obiective： To improve the dissolution rate and bioavailability of ibuprofen by preparing it as ibuprofen inclusion complex using supercritical CO2 fluid technology. Methods： The effects of several process parameters such as pressure,temperature,and time on the preparation of ibuprofen inclusion complex were investigated,taking inclusion rate as the response index,and the Box Behnken method was used to optimize the process.Results： The optimal conditions for the preparation of ibuprofen inclusion complex with supercritiacl CO2 fluid technology were as follows： mole ratio of β-CD/ibuprofen was 0. 87,pressure was 19. 05 MPa,temperature was39. 64 ℃,reaction time was 5 h. Under such conditions the inclusion rate was 84. 83% and the dissolution rate was82% at 5 min. Ibuprofen was dispersed in the excipients completely in amorphous form according to the results of differential scanning calorimetry（ DSC） and X-ray powder diffraction（ XRPD）. Conclusion： The inclusion rate and dissolution rate of ibuprofen inclusion complex prepared by supercritical CO2 fluid technology can be increased substantially.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2018年第4期465-470,共6页
Chinese Journal of New Drugs
基金
2016年辽宁省大学生创新创业训练项目(201610163073)
关键词
超临界CO2
布洛芬
Β-环糊精
包合物
包合率
supercritical CO2
ibuprofen
β-cyclodextrin
inclusion complex
inclusion rate
