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Improvemrnt of Drug Absorption in Gastro intestinal Tract

改善胃肠道药物吸收

基本信息

批准号：
05454573
负责人：
AWAZU Shoji
金额：
$ 4.42万
依托单位：
Tokyo University of Pharmacy and Life Science
依托单位国家：
日本
项目类别：
Grant-in-Aid for General Scientific Research (B)
财政年份：
1993
资助国家：
日本
起止时间：
1993 至 1994
项目状态：
已结题

项目摘要

Relation between the Modified Structure of Digestive Tract and Absorption Ability, and the Absorption Improvement by Peyer's Patch. Absorption enhancers, both of C10 and PC increased the intracellular Ca level. Following the increase, C10 opened the tight junction by the activation of actomyosin ring cascade, but it was shown clearly that PC opened the junction b the different mechanism. Glucose did not show the enhancing effect. The absorbability of BSA and concanavalin A was larger in the rabbit Peyer's patch than in jejunum. The possibility to use Peyer's patch to enhance the macromolecules was shown. Among peptidases, the exo peptidases exhibited the absorption enhancing effect, showing the possible new type enhancer. Inhibition Effect of Vitamin A on Membrane Damage induced by Anticancer Drug. IEC-6 was not used successfully to investigate the vitamin A mechanism, but it was shown clearly that vitamin A inhibits the decrease of absorbability of intestins as well as structural change induced by methotrexate.Improvement of Absorption by Glucose Transporter.Tripeptide Tyr-Gly-Gly (TGG) which is a part of enkephaline was with glucose and galactose by coupline method. Every sugar-coupling inhibited the degradation of TGG and increased the absorbability. Na^+-dependent transport worked partly at least for the absorption. Aminopeptidase was inhibited by the sugar-coupling, but enkephalinase was not. The enkephalinase inhibitor increased the stability and absorbability of the sugar-coupled enkephalin. These findings suggests the absorption improvement peptides by sugar coupling. Sugar conjugates with acetaminophen were synthesized, and their absorptions proceeded partly by glucose transporter. The order of absorbability was alpha-glucoside > beta-glucode > beta-galactoside. This order coincided with the former reported one.

消化道结构改变与吸收能力的关系及派尔集合淋巴结促进吸收的作用吸收促进剂C10和PC均增加细胞内Ca水平。C10通过激活肌动球蛋白环级联反应开放紧密连接，而PC通过不同的机制开放连接B。葡萄糖没有增强作用。BSA和刀豆蛋白A在Peyer集合淋巴结中的吸收量大于空肠。显示了使用派伊尔斑增强大分子的可能性。在肽酶中，外切肽酶表现出吸收促进作用，显示出可能的新型促进剂。维生素A对抗癌药物致细胞膜损伤的抑制作用。IEC-6用于维生素A作用机制的研究尚不成功，但已明确表明维生素A可抑制甲氨蝶呤引起的维生素A吸收能力的降低和结构变化。葡萄糖转运蛋白促进脑啡肽的吸收利用偶联法将脑啡肽的一部分-各种糖偶联均能抑制TGG的降解，提高其吸收率。依赖Na^+的转运至少在一定程度上促进了吸收。氨基肽酶被糖偶联抑制，但脑啡肽酶没有。脑啡肽酶抑制剂可增加糖偶联脑啡肽的稳定性和吸收性。这些发现表明，吸收改善肽通过糖偶联。合成了对乙酰氨基酚的糖结合物，它们的吸收部分通过葡萄糖转运蛋白进行。吸收率大小顺序为α-葡萄糖苷> β-葡萄糖苷> β-半乳糖苷。这一命令与前一份报告的命令相吻合。