灯盏花素脂质体体外释放及在酸和胆盐中稳定性研究  

Breviscapine Liposome in Vitro Release and the Stabilities in Acid and Bile Salt

作　　者：董晓东[1] 邓英杰[1] 陈超[1] 王晓宇[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016

出　　处：《中国药学杂志》2010年第8期597-601,共5页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(30672555)

摘　　要：目的制备灯盏花素脂质体,并对其体外释放特性以及在酸性和胆盐环境下的稳定性进行研究。方法利用不同的数学模型拟合,考察灯盏花素普通脂质体和阳离子脂质体的体外释放行为;以包封药物量为指标,采用微柱离心法研究灯盏花素脂质体的不同处方在模拟胃肠道环境中的稳定性。结果体外释放实验中,灯盏花素溶液8 h释放完全,普通脂质体8 h累计释放(44.2±2.38)%,阳离子脂质体8 h累计释放(8.23±3.21)%;灯盏花素普通脂质体和阳离子脂质体的释放过程均符合Weibull模型,拟合方程为lnln[1/(1-Q)]=0.779 7lnt-2.318 7、lnln[1/(1-Q)]=0.355 3lnt-3.197。脂质体处方中加入胆固醇对于提高脂质体在酸和胆盐中的稳定性有很大影响,十八胺(SA)能显著提高脂质体的包封率,但对实验中样品的稳定性没有影响。结论体外释放实验模拟了灯盏花素脂质体的体外释放规律,通过研究可能找到进一步提高脂质体在胃肠道中稳定性的途径。OBJECTIVE To prepare breviscapine liposomes and study the stabilities in acid and bile salt.METHODS The in vitro release profiles of the liposomes were investigated with a few of mathematical models.The stabilities of all formulations in the stimulated gastrointestinal tract environment were determined with releases were（44.2±2.38）% for entrapsulated drug as indicator.RESULTS In vitro release experiments,the breviscapine was released completely in 8 h.Meanwhile,cumulative the ordinary liposomes and（8.23±3.21）% for the cationic liposome.And the release profiles of both kinds of liposomes agreed with Weibull model well,the fitting equations were lnln[1/（1-Q）]=0.779 7lnt-2.318 7 and lnln[1/（1-Q）]=0.355 3lnt-3.197,respectively.Cholesterol played the important role for improving the stabilities of liposomes in the acid and bile salt situations.SA improved the entrapment efficiency and had little influence on the stabilities.CONCLUSION The in vitro release examinations showed the liposomes had some sustained release effect.The study is helpful to improve the stabilities of liposome in the gastrointestinal tract.

关 键 词：灯盏花素脂质体 体外释放 胆盐 稳定性 

分 类 号：R944[医药卫生—药剂学]