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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 transport characteristics of earthworm fibrinolytic enzyme (EFE) in the gastrointestinal tract of rats and reveal the main parts of gastrointestinal tract absorption and its possible mechanism. Methods: The anticoagulant effect of EFE was evaluated by euglobulin lysis time and clotting time. The translocation of EFE in rat gastrointestinal tract was studied by immunohistochemistry and fluorescent labeling. Results: EFE maintained its biological activity after oral administration and showed the strongest efficacy at about 1.5h. Oral EFE 1.5h oral rats, the stomach and duodenum there is a large number of drugs, the colon has scattered drug deposition. Transmembrane transmembrane experiments showed that the colon part of the transport capacity of the strongest. CONCLUSION: The stomach and duodenum are the main absorption sites when EFE is orally administered. The EFE has strong colon transport ability in vitro and provides an experimental basis for the preparation of its enteric-coated formulations.