蚯蚓纤溶酶口服后在大鼠胃肠道的转运分布特点  

Distribution of earthworm fibrinolytic enzyme in rat gastrointestinal tract after oral administration

作　　者：王学清[1] 张源[1] 潘荣[2,3] 赫荣乔[2] 

机构地区：[1]北京大学药学院药剂系,北京100191 [2]中国科学院生物物理研究所脑与认知国家重点实验室,北京100101 [3]北京百奥药业有限责任公司,北京100101

出　　处：《中国新药杂志》2010年第15期1360-1364,共5页Chinese Journal of New Drugs

基　　金：国家973计划(2009CB930300)

摘　　要：目的:研究蚯蚓纤溶酶(EFE)在大鼠胃肠道的转运特点,揭示其胃肠道吸收的主要部位及可能机制。方法:采用优球蛋白溶解时间及凝血时间评价EFE口服后的抗凝血效果;采用免疫组化法、荧光标记法研究EFE在大鼠胃肠道的转运情况。结果:EFE口服后保持生物学活性,在1.5h左右表现出最强药效。大鼠口服EFE1.5h时,胃和十二指肠中存在大量药物,结肠有散在药物沉积。离体跨膜实验表明结肠部位转运能力最强。结论:EFE口服给药后出现最大药效时,胃及十二指肠为主要吸收部位,EFE体外结肠转运能力强,为制备其肠溶剂型提供了实验依据。Objective： To study the distribution characteristics of earthworm fibrinolytic enzyme （EFE） in rat gastrointestinal tract after oral administration for elucidating the main absorption sites and possible absorption mechanism. Methods： The efficacy of EFE was evaluated by determining euglobulin lysis time （ELT） and the clotting time （CT）. The distribution characteristics of EFE in rat gastrointestinal tract were evaluated by immunohistochemical and fluorescence labeling methods. Results： EFE maintained its biologic activity after oral administration. The largest effects were obtained at about 1.5 h, and much EFE was distributed in stomach and duodenum In colon, there were sporadic drug deposited. In the in vitro transport at different segments of intestinal tract, the colon showed the largest transport capacity. Conclusion： At the largest effect time of EFE, the main absorption sites are stomach and duodenum. The transport is the largest in colon in vitro, indicating that it is useful to prepare it into enteric formulations.

关 键 词：蚯蚓纤溶酶 胃肠道 药效 分布 

分 类 号：R969.1[医药卫生—药理学]