齐墩果酸脂质体在大鼠体内药代动力学的研究  

Pharmacokinetics of oleanolic acid liposomes in rats

作　　者：陈洪轩[1] 牛江秀[1] 肖衍宇[2] 陈志鹏[3] 和平[1] 游国叶[1] 

机构地区：[1]河南大学药物研究所,河南开封475004 [2]中国药科大学药学院,江苏南京210009 [3]南京中医药大学药学院,江苏南京210046

出　　处：《中成药》2010年第4期569-572,共4页Chinese Traditional Patent Medicine

摘　　要：目的:制备齐墩果酸脂质体,研究齐墩果酸脂质体在大鼠体内的药代动力学。方法:采用乙醇注入-探头超声法制备齐墩果酸脂质体;大鼠分别尾静脉注射齐墩果酸脂质体和齐墩果酸溶液剂,用反相高效液相色谱法测定不同时间血浆中齐墩果酸的浓度,采用3p97程序计算药代动力学参数,并进行统计学分析。结果:制得的脂质体透射电镜下为圆形或类圆形的小囊泡,平均粒径为(206.4±4.7)nm,包封率为(97.74±1.34)%;齐墩果酸脂质体和自制的溶液剂经大鼠尾静脉注射后,t1/2α分别为(4.22±1.86)和(0.80±0.34)min;t1/2β分别为(33.59±12.53)和(15.65±7.91)min;AUC分别为(240.13±23.62)和(168.31±18.47)μg/(mL.min),两种制剂的t1/2β和AUC0-t经方差分析后均存在显著性差异(P<0.05),齐墩果酸脂质体显著增加了齐墩果酸的AUC,延长了其在血液循环中的时间。结论:制备的齐墩果酸脂质体包封率较高,粒度均匀;与非脂质体相比,齐墩果酸脂质体静脉注射给药后,药代动力学参数发生了明显的改变。AIM： To study the pharmacokinetics of oleanolic acid liposomes in rats.METHODS： Oleanolic acid liposomes were prepared by ethanol injection-sonication;The pharmaceutical properties including morphology,encapsulation efficiency,particle size,zeta potential were determined.Rats were injected with oleanolic acid lipo-somes and oleanolic acid solution via the tail,respectively.The plasma concentrations of sample in rats were assayed by RP-HPLC.The pharmacokinetic parameters were computered by 3P97 program package.RESULTS： Oleanolic acid liposomes showed almost spherical,the mean diametre was（206.4 ± 4.7） nm.The encapsulation efficiency of oleanolic acid liposomes could be more than 90% based on orthogonal design,and no haemolyticus existed.The plasma concentration-time curves of the oleanolic acid liposomes conformed to a two-compartment model.T1/2β of oleanolic acid liposomes was（33.59 ± 12.53） min,AUC was（240.13 ± 23.62）（μg/mL.min）,obviously higher than that of the control preparation.CONCLUSION： The oleanolic acid liposomes with high entrapment efficiency and even size has a good pharmacokinetic parameters by comparison with non-liposomes.

关 键 词：齐墩果酸 脂质体 药代动力学 大鼠 

分 类 号：R969.1[医药卫生—药理学]