溴吡斯的明脂质体体外释放和大鼠离体肠吸收的研究  

In vitro release and intestinal absorption of pyridostigmine bromide liposome

作　　者：张梨[1] 谭群友[2] 尹华峰[1] 陶绍霖[2] 刘雨[1] 张景勍[1] 

机构地区：[1]重庆医科大学药物高校工程研究中心和生物化学与分子药理学重点实验室,重庆400016 [2]第三军医大学大坪医院野战外科研究所全军胸外科中心,重庆400042

出　　处：《第三军医大学学报》2011年第18期1917-1919,共3页Journal of Third Military Medical University

基　　金：教育部博士点基金(20095503120008);重庆市教育委员会资助项目(首批高等学校优秀人才资助;KJ090308)~~

摘　　要：目的制备溴吡斯的明脂质体,考察其体外释药性质及各肠段的吸收情况。方法采用逆向蒸发法制备溴吡斯的明脂质体,测定其包封率,考察脂质体体外释放情况;运用大鼠离体外翻肠囊模型,采用RP-HPLC法测定肠囊液中溴吡斯的明浓度,考察脂质体肠道吸收行为。结果脂质体包封率为(51.81±2.15)%,72 h累积释放率(95.08±4.02)%;脂质体能显著增加溴吡斯的明在十二指肠、空肠、回肠和结肠段的吸收(P<0.05);溴吡斯的明溶液和脂质体在各肠段表观渗透系数分别为(1.41±0.73)×10-5、(2.21±0.62)×10-5、(2.13±0.27)×10-5、(1.30±0.79)×10-5 cm/s和(1.53±0.38)×10-5、(2.67±0.55)×10-5、(2.39±0.42)×10-5、(2.59±0.70)×10-5 cm/s,其中两者结肠段表观渗透系数值差异有统计学意义(P<0.05)。结论脂质体在体外介质中具有一定缓释作用。通过增加渗透性有望提高溴吡斯的明在体内生物利用度。Objective To study the in vitro release and intestinal absorption of pyridostigmine bromide liposome.Methods Pyridostigmine bromide liposome was prepared by reverse phase evaporation to detect its encapsulation and in vitro liposome release.An in vitro everted intestinal sac model was used to observe the intestinal absorption of liposome and measure the concentration of pyridostigmine bromide in intestine by RP-HPLC.Results The capsulation rate of liposome was 95.08%±4.02% and its 72 h cumulative release rate was 51.81%±2.15%,indicating that liposome could significantly increase the absorption of pyridostigmine bromide in duodenum,jejunum,ileum and colon（P0.05）.The apparent permeability coefficient（Papp） of pyridostigmine bromide solution and liposome in different intestinal segments was（1.41±0.73）×10-5 cm/s,（2.21±0.62）×10-5 cm/s,（2.13±0.27）×10-5 cm/s,（1.30±0.79）×10-5 cm/s and（1.53±0.38）×10-5 cm/s,（2.67±0.55）×10-5 cm/s,（2.39±0.42）×10-5 cm/s,and（2.59±0.70）×10-5 cm/s,respectively（P0.05）.Conclusion Liposome release is delayed in in vitro medium,thus increasing the bioavailability of pyridostigmine bromide in vivo by its enhancing its permeability.

关 键 词：溴吡斯的明脂质体 体外释放 外翻肠囊法 肠吸收 

分 类 号：R971.92[医药卫生—药品] R944.9[医药卫生—药学]