首页> 外国专利> MODIFIED OLIGOPEPTIDES FOR TREATING PANCREATITIS, GASTRIC ULCERS AND OTHER HYPERENZYMEMIAS BASED ON A PEPTIDIC ENZYME INHIBITOR AND METHOD FOR PRODUCING SAID MODIFIED OLIGOPEPTIDES

MODIFIED OLIGOPEPTIDES FOR TREATING PANCREATITIS, GASTRIC ULCERS AND OTHER HYPERENZYMEMIAS BASED ON A PEPTIDIC ENZYME INHIBITOR AND METHOD FOR PRODUCING SAID MODIFIED OLIGOPEPTIDES

机译:基于肽酶抑制剂治疗胰腺炎,胃溃疡和其他高血氧症的修饰寡肽及制备所述修饰寡肽的方法

摘要

The invention can be used to create oral and parenteral drugs in pharmaceutics and medicine for the treatment of pancreatitis, gastric ulcers and other hyperenzymemias. The modified oligopeptides for treating pancreatitis, gastric ulcers and other hyperenzymemias based on peptidic enzyme inhibitors are characterized in that a mixture (ensemble) of chemically modified oligopeptides is used as the main active agent, said oligopeptides being the product of the autologous hydrolysis of the proteolytic enzymes trypsin, chymotrypsin and papain, and the charges of the oligopeptide molecules being changed to opposite charges by acylation with succinic anhydride and alkylation with monochloroacetic acid. The resultant mixture (ensemble) of modified oligopeptides rapidly stops the inflammatory process caused by the excessive secretion of proteolytic enzymes. The process of manufacturing the proposed drug is simple, economically viable, environmentally benign, produces zero waste and comprises three stages. As a result of the effect of selective complementary hybridization, the peptides produced interact only with their precursor enzymes, thus inhibiting the function thereof. The low molecular weight of the peptides produced and their resistance to hydrolytic enzymes enables them to easily cross biological membranes, be absorbed from the intestines, and build up in the nidus with a high concentration of target enzymes. These properties make it possible for the proposed peptides to be used to produce, inter alia, oral drug forms for the treatment of chronic pancreatitis and gastric ulcers.
机译:本发明可用于在药物和药物中产生用于治疗胰腺炎,胃溃疡和其他高酶血症的口服和肠胃外药物。基于肽酶抑制剂的用于治疗胰腺炎,胃溃疡和其他高酶血症的修饰寡肽的特征在于,化学修饰的寡肽的混合物(集合)用作主要活性剂,所述寡肽是蛋白水解的自体水解的产物酶胰蛋白酶,胰凝乳蛋白酶和木瓜蛋白酶,寡肽分子的电荷通过与琥​​珀酸酐酰化并与一氯乙酸烷基化而变成相反的电荷。所得的修饰寡肽混合物(集合体)迅速停止了由于蛋白水解酶过度分泌而引起的炎症过程。制造所提出的药物的过程是简单的,经济上可行的,环境友好的,产生零废物的并且包括三个阶段。由于选择性互补杂交的作用,产生的肽仅与它们的前体酶相互作用,从而抑制了其功能。产生的肽的低分子量及其对水解酶的抗性使它们易于穿过生物膜,从肠中吸收,并在具有高浓度目标酶的尼杜氏菌中积累。这些特性使得所提出的肽尤其可以用于生产治疗慢性胰腺炎和胃溃疡的口服药物形式。

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