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A drug for treating ulcerative colitis

A technology for ulcerative colitis and drugs, applied in the directions of drug combinations, pharmaceutical formulations, organic active ingredients, etc., can solve problems such as poor long-term treatment effect, inability to achieve long-term prevention or treatment, and increased risk of infection and cancer.

Active Publication Date: 2021-09-14
THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Drug therapy includes: (1) sulfasalazine and salicylic acid preparations, which are the main drugs for the treatment of ulcerative colitis, but their long-term treatment effect is poor; (2) corticosteroids, such as dexamethasone or prednisone, However, long-term steroid maintenance cannot prevent the recurrence of ulcerative colitis; moreover, there are still differences in whether steroids can be used continuously in the chronic phase, and there are certain side effects (steroid drugs may increase the risk of infection); (3) immunosuppressants, but their Efficacy is questionable and may also increase the risk of infection and cancer
In short, none of the current drugs for the treatment of ulcerative colitis can achieve long-term preventive or therapeutic effect; , you must pay attention to the combination of work and rest, and you can't make yourself too tired, especially for some patients with serious illnesses, they should stay in bed in time

Method used

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  • A drug for treating ulcerative colitis
  • A drug for treating ulcerative colitis
  • A drug for treating ulcerative colitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Study on body weight change and survival rate of DSS-induced ulcerative colitis mice by LY3009120

[0019] Experimental method: 22-24g male C57BL / 6 mice were divided into 2 groups (8 mice in each group): Vehicle group (PBS, containing 10% DMSO and 20% cyclodextrin) and LY3009120 group (20mg / Kg mice, dissolved in PBS with 10% DMSO and 20% cyclodextrin). Feed 3% DSS (dextran sodium sulfate) every day, and inject Vehicle or LY3009120 (20mg / Kg mice) intraperitoneally every day. After seven days, withdraw DSS, continue to inject Vehicle or LY3009120 intraperitoneally, and no longer inject after 3 days. Mice are weighed every day and the death situation of mice is counted, and the test results are as follows: figure 1 and 2 shown.

[0020] Experimental results: figure 1 It shows that LY3009120 can significantly inhibit the weight loss of mice, *P figure 2 It shows that LY3009120 can significantly improve the survival rate of mice.

Embodiment 2

[0021] Example 2 Effect of LY3009120 on Colon Length of DSS-Induced Ulcerative Colitis Mice

[0022] Experimental method: 22-24g male C57BL / 6 mice were divided into 3 groups: 4 mice in the control group, 4 mice in the DMSO group, and 4 mice in the LY3009120 group. The control group was fed water every day; the Vehicle and LY3009120 groups were fed 3% DSS every day, and Vehicle or LY3009120 (20 mg / Kg mice) was injected intraperitoneally every day. Seven days later, the DSS was withdrawn, and the colon length of the mice was measured. Experimental results such as image 3 As shown, the results showed that LY3009120 could significantly inhibit DSS-induced colon shortening in mice.

Embodiment 3

[0023] Example 3 Effect of LY3009120 on DSS-induced intestinal epithelial cell barrier breakdown in ulcerative colitis

[0024] Experimental method: 22-24g male C57BL / 6 mice were divided into 3 groups: 4 mice in the control group, 4 mice in the DMSO group, and 4 mice in the LY3009120 group. The control group was fed with water every day; the Vehicle and LY3009120 groups were fed with 3% DSS every day, and the Vehicle or LY3009120 (10mg / Kg mice) was injected intraperitoneally every day. Seven days later, the DSS was removed, and the colon tissue was taken, fixed with 4% paraformaldehyde, and stained with HE . Experimental results such as Figure 4 as shown, Figure 4 It was shown that LY3009120 could significantly inhibit the damage of DSS-induced colonic epithelial cell barrier in mice.

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Abstract

The invention discloses a medicine for treating ulcerative colitis. The structural formula of the medicine is as follows: using the medicine of the present invention to treat ulcerative colitis has significant curative effects, including significantly inhibiting the weight loss of mice, significantly increasing the The survival rate of mice significantly inhibited DSS-induced colon shortening in mice and significantly inhibited DSS-induced disruption of the colonic epithelial cell barrier in mice.

Description

technical field [0001] The invention relates to a medicine for treating colitis, especially a medicine for treating ulcerative colitis. Background technique [0002] The treatment methods for ulcerative colitis mainly include drug therapy and surgery. Drug therapy includes: (1) sulfasalazine and salicylic acid preparations, which are the main drugs for the treatment of ulcerative colitis, but their long-term treatment effect is poor; (2) corticosteroids, such as dexamethasone or prednisone, However, long-term steroid maintenance cannot prevent the recurrence of ulcerative colitis; moreover, there are still differences in whether steroids can be used continuously in the chronic phase, and there are certain side effects (steroid drugs may increase the risk of infection); (3) immunosuppressants, but their Its efficacy is questionable and it may increase the risk of infection and cancer. In short, none of the current drugs for the treatment of ulcerative colitis can achieve lo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61P1/04A61P1/00
Inventor 晏杰陶爱林张冲何巧玲罗以琴刘帅何安东
Owner THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV