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Application of cyclo-dipeptide in preparation of drug for treating gastrointestinal ulcer

A technology for peptic ulcer and cyclic dipeptide, applied in the application field of medicine, can solve the problems of long treatment time, discounted curative effect and high recurrence rate, and achieve the effect of significant effect, reduced recurrence rate and small molecular weight.

Inactive Publication Date: 2016-02-10
陈光健
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, people don’t know enough about peptic ulcer, and they often only attract attention when they are serious. In the process of traditional drug treatment, the first-pass effect of most drugs used in the liver is greatly reduced, resulting in long treatment time, and the patient’s condition is under control. When the cure has not been completely cured, the treatment is often not continued
Therefore, the recurrence rate of the disease has been relatively high

Method used

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  • Application of cyclo-dipeptide in preparation of drug for treating gastrointestinal ulcer
  • Application of cyclo-dipeptide in preparation of drug for treating gastrointestinal ulcer
  • Application of cyclo-dipeptide in preparation of drug for treating gastrointestinal ulcer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1 The preparation method of ring-L-pro-L-propanedipeptide described in the present invention

[0017] Main pharmaceutical reagents: L-alanine, proline protected by Boc amino group

[0018] The process of preparing cyclo-L-pro-L-propane dipeptide:

[0019] (1) Preparation of alanine methyl ester hydrochloride: Add 10 g of L-alanine to a mixture of an appropriate amount of methanol and thionyl chloride, and stir at room temperature for 24 hours. TLC traced the completion of the reaction, and the solvent was spin-dried under reduced pressure to obtain 15.08 g of white alanine methyl ester hydrochloride.

[0020] (2) Neutralization and condensation reaction: Add alanine methyl ester hydrochloride obtained in step (1), 20 g of proline protected by Boc amino group, 20 ml of pyridine, and DMAP into 100 ml of anhydrous tetrahydrofuran, and wait until all are mixed , under the protection of argon, add (Boc) dissolved in anhydrous tetrahydrofuran 2 O, stirred at roo...

Embodiment 2

[0023] Application of Example 2 Cyclic-L-pro-L-propanedipeptide in Ulcers

[0024] 1. Experimental materials

[0025] 1.1 Sample: Sample obtained according to Example 1: cyclo-L-pro-L-propanedipeptide

[0026] 1.2 Experimental animals: KM mice, 18-22 g, 160, half male and half male. SD rats, 200-220g, 204, half male and half male.

[0027] 1.3 Experimental reagents: ranitidine hydrochloride capsules, Daxi (aluminum magnesium carbonate tablets).

[0028] 2. Method for evaluating the protective function of samples on gastric ulcer mucosa

[0029] 2.1 Absolute ethanol-induced gastric mucosal injury model test in mice

[0030] 160 KM mice were randomly divided into groups according to sex and body weight (see Table 1 for details), and each group was given corresponding drugs. Fasted for 24 hours after administration, and freely drank water. The mice in the other groups were administered for 10 consecutive days, and fasted for 24 hours after administration on the ninth day, an...

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Abstract

The invention provides an application of cyclo-dipeptide in preparation of a drug for treating gastrointestinal ulcer. The cyclo-dipeptide is cyclo-L-Pro-L-alanine dipeptide. The dipeptide is small in molecular weight and is simple in structure, has significant treatment effects on the gastrointestinal ulcer, can enter blood circulation quickly through mucous membrane tissue during treatment, can avoid first pass effect in liver and quickly arrive at lesion, achieves the best treatment effect on the gastrointestinal ulcer, is reduced in treatment time and use quantity and is also reduced in relapse rate.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to the application of a cyclic dipeptide in the preparation of medicine for treating peptic ulcer. Background technique [0002] Gastric ulcer and duodenal ulcer are collectively referred to as peptic ulcer disease. Due to the accelerated pace of life and increased work pressure, the incidence of peptic ulcer disease has not only not declined in recent years, but has an upward trend. The symptoms of this disease have also become atypical in the past 10 years, and the irregular stomach pain often does not attract people's attention until hematemesis or melena occurs before going to the hospital for treatment. Peptic ulcer mainly refers to chronic ulcers that occur in the stomach and duodenum, and can also occur in the lower esophagus, around the gastrojejunostomy, and Meckel's diverticulum containing ectopic gastric mucosa. The formation of these ulcers is related to the digestion of gas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/12C07K5/12C07K1/16C07K1/06A61P1/04
Inventor 陈光健
Owner 陈光健
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