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Application of spiro piperazine quaternary ammonium salt derivative in preparation of medicine for treating irritable bowel syndrome

A technology of irritable bowel syndrome and medicine, which is applied in the field of medicine, can solve the problems such as inability to obtain curative effect, and achieve the effect of obvious symptoms of diarrhea and constipation, wide application range, and relief of symptoms of diarrhea and constipation

Pending Publication Date: 2022-07-26
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the conventional treatment methods and drugs for IBS cannot achieve satisfactory results.

Method used

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  • Application of spiro piperazine quaternary ammonium salt derivative in preparation of medicine for treating irritable bowel syndrome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Therapeutic effect of the compound of Example 1 on diarrhea-induced irritable bowel syndrome (D-IBS) rats constructed by drugs

[0036] 1. Materials and methods

[0037] 1.1 Experimental animals

[0038] SD male rats, weighing 180-220 g.

[0039] 1.2 Building the model

[0040] The rats were given senna by gavage at 8:00 in the morning, at a dose of 10 mL / kg, once a day, for 4 consecutive weeks, and for the second week, the rats were irritated with wooden clips by clipping their tails. Its fights for 30min a day. Modeling was stopped from the 5th week.

[0041] 1.3 Grouping and Drugs

[0042] Blank group: 8 normal rats that did not participate in the modeling were administered with normal saline by gavage, according to the body weight of 20 mL / kg;

[0043] Model group: 8 model rats, intragastric administration of normal saline, 20 mL / kg of body weight;

[0044] Positive control group: 8 model rats, intragastric administration of 1 mg / mL pinaverium bromide aqueous s...

Embodiment 2

[0067] Example 2 Therapeutic effect of compound on diarrhea-type irritable bowel syndrome (D-IBS) rats constructed by psychological stress method

[0068] 1. Materials and methods

[0069] 1.1 Experimental animals

[0070] SD male rats, weighing 180-220 g.

[0071] 1.2 Building the model

[0072] The IBS rat model was induced by chronic restraint tail-pinch stimulation. For every 5 rats in the same cage, use sponge-coated clips to clamp the proximal 1 / 3 of the rat's tail. Be careful not to damage the skin, make it irritated, and fight with other rats, so as to provoke the whole cage of rats to fight. Observe Rats were stimulated by irritating stress response (groaning, standing confrontation, writhing, screaming, biting, etc.) for 30 minutes. One hour after the end of the tail clipping stimulation, the rats were anesthetized with 30% chloral hydrate (3 mL / kg), and the front shoulders, front upper limbs and chest were bound with paper tape to restrain them from scratching t...

Embodiment 3

[0101] Example 3 Therapeutic effect of compound DXL-A-24 on constipation-predominant irritable bowel syndrome (C-IBS) rats

[0102] 1. Materials and methods

[0103] 1.1 Experimental animals

[0104] SD rats, half male and half female, weighing 180-220 g.

[0105] 1.2 Building the model

[0106] The C-IBS model was established by gavage with ice water. The rats were raised in a single cage and were given 2 mL of normal saline at 0-4°C by gavage every day. The model was established for 14 days and observed. Decreased stool water content.

[0107] 1.3 Grouping and administration

[0108] Blank group: 8 normal rats that did not participate in the modeling were administered with normal saline by gavage, according to the body weight of 20 mL / kg;

[0109]Model group: 8 model rats, intragastric administration of normal saline, 20 mL / kg of body weight;

[0110] Positive control group: 8 model rats, intragastric administration of 0.4 mg / mL cisapride suspension, according to body ...

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Abstract

The invention belongs to the field of medicines, and particularly relates to application of a spiro piperazine quaternary ammonium salt derivative in preparation of a medicine for treating irritable bowel syndrome. The compound disclosed by the invention can be used for remarkably improving diarrhea type or / and constipation type irritable bowel syndrome, and has the treatment effects on abdominal pain, abdominal distension, abnormal stool consistency, abnormal stool frequency, intestinal behavior change, flatulence (such as abdominal flatulence), constipation, diarrhea, alternate diarrhea and constipation, gastrointestinal flatulence, belching, mucus stool, abdominal distention, abdominal distention, abdominal distention, abdominal distention, abdominal distention, abdominal distention, abdominal distention, abdominal distention and abdominal distention. And one or more symptoms of the upper digestive tract are inhibited. The traditional Chinese medicine composition has a good regulating effect on hormones such as 5-HT of model rats and has a remarkable relieving effect on diarrhea and constipation symptoms of the model rats.

Description

technical field [0001] The invention belongs to the field of medicine and relates to the medicinal use of a spirocyclic piperazine quaternary ammonium salt derivative, in particular to the use of the compound DXL-A-24 in the preparation of a medicine for treating irritable bowel syndrome. Background technique [0002] Irritable bowel syndrome (IBS) is a common non-organic bowel disorder in the gastrointestinal tract, with chronic and recurrent clinical features, often accompanied by changes in bowel habits (frequency and / or character), defecation Symptoms improved afterward. For the diagnosis of IBS, Rome IV criteria are generally used internationally: the course of disease is more than 6 months, the past 3 months, repeated abdominal pain, abdominal pain at least one day a week, and accompanied by two or more of the following abnormal changes : (1) abdominal pain is related to defecation; (2) abdominal pain is accompanied by changes in defecation frequency; (3) abdominal pa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/499A61K45/06A61P1/00A61P1/10A61P1/12A61P1/14C07D487/10
CPCA61K31/499A61K45/06A61P1/00A61P1/10A61P1/12A61P1/14C07D487/10A61K2300/00
Inventor 姚景春徐燕卢小艳
Owner SHANDONG NEWTIME PHARMA
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