姜黄素醇质体的体外释放及在体胃肠吸收研究  

In vitro release and in vivo gastrointestinal absorption of curcumin ethosomes

作　　者：赵静 李嫄[2] 李开玲 余忠姝 张景勍 Zhao Jing;Li Yuan;Li Kailing;Yu Zhongshu;Zhang Jingqing(Chongqing Research Center for Pharmaceutical Engineering, College of Pharmacy, Chongqing Medical University;Department of Pharmacy,Shuangliu Hospital of Traditional Chinese Medicine , Chengdu City,Sichuan Province)

机构地区：[1]重庆医科大学药学院重庆高校药物工程研究中心,重庆400016 [2]四川省成都市双流县中医医院药剂科,成都610200

出　　处：《重庆医科大学学报》2019年第3期275-281,共7页Journal of Chongqing Medical University

基　　金：重庆市科委资助项目(编号:cstc2015jcyjBX0027)

摘　　要：目的:探究姜黄素醇质体(curcunmin ethosomes,CMET)的体外释放特征及在体胃肠吸收情况。方法:文中分为姜黄素(curcumine,CM)、姜黄素脂质体(curcumine liposome,CMLP)和CMET 3组,采用动态透析法考察体外释放特征;建立大鼠在体单向灌流模型,分别给予CM、CMLP和CMET,考察胃和各肠段中CM的吸收情况。结果:CMET在释放介质(p H 1.2 HCl,p H6.8 PBS)中的累积释放率分别为(87.77±0.20)%和(84.72±0.53)%,分别是CM的2.25倍和2.26倍,释放曲线均符合Weibull模型。CMET在大鼠十二指肠、空肠、回肠、结肠等各肠段的吸收速率常数值分别是11.28、5.24、6.12、5.93×10-2 L/min,分别为CM的1.9、1.1、1.6、2.6倍,CMET在四肠段的有效渗透率值分别是9.15、4.21、5.11、6.41×10-3 cm/s,分别为CM的2.4、1.3、1.8、3.2倍。统计分析结果提示,CMET在胃、十二指肠、回肠、结肠的吸收速率常数与CM差异有统计学意义(P分别为0.006、0.007、0.001、0.004)。CMET在十二指肠、空肠、回肠、结肠的有效渗透率与CM差异有统计学意义(P分别为0.000、0.028、0.000、0.005)。结论:CMET能改善药物的体外释放行为,促进小肠对CM的吸收。Objective:To investigate the in vitro release characteristics and in vivo gastrointestinal absorption of curcumin ethosomes(CMET). Methods:Curcumin(CM)group,curcumin liposome(CMLP)group,and CMET group were established in this study. The dynamic dialysis method was used to evaluate in vitro release characteristics. A rat model of in vivo single-pass perfusion was established and CM,CMLP,and CMET were administered,respectively,to investigate the absorption of CM in the stomach and intestinal segments. Results:The cumulative release rates of CMET in the release media(p H 1.2 HCl,p H 6.8 PBS)were(87.77±0.20)% and(84.72±0.53)%,respectively,which were 2.25 and 2.26 times those of CM,respectively,and the release curves were consistent with the Weibull model. The absorption rate constants(Ka)of CMET in the duodenum,the jejunum,the ileum,and the colon were 11.28×10-2,5.24×10-2,6.12×10-2,and 5.93×10-2 L/min,respectively,which were 1.9,1.1,1.6,and 2.6 times those of CM;the effective permeability(Peff)values of CMET in these four intestinal segments were 9.15×10-3,4.21×10-3,5.11×10-3,and 6.41×10-3 cm/s,respectively,which were 2.4,1.3,1.8,and 3.2 times those of CM. The statistical analysis showed that there were significant differences between CMET and CM in Ka in the duodenum,the jejunum,the ileum,and the colon(P=0.006,0.007,0.001,and 0.004,respectively)and Peff in these four intestinal segments(P=0.000,0.028,0.000,and 0.005,respectively). Conclusion:CMET can improve the in vitro release behavior of CM and promote the absorption of CM in the small intestine.

关 键 词：姜黄素 醇质体 体外释放 胃肠吸收 吸收百分率 

分 类 号：R944.9[医药卫生—药剂学]