Application of elemonic acid and solid dispersion thereof in preparation of medicine for treating ulcerative colitis

A technology of ulcerative colitis and solid dispersion, which is applied in the field of medicine, can solve the problems of low side effects and lack of curative effect of ulcerative colitis, and achieve the effect of alleviating clinical symptoms and reducing inflammatory response

Active Publication Date: 2021-11-16
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] For this reason, the embodiment of the present invention provides the application of elemic acid in the preparation of ulcerative colitis medicine, especially provides the application of elemic acid and its solid dispersion in the preparation of ulcerative colitis medicine and its preparation method , to solve the problem of lack of therapeutic drugs with good curative effect and low side effects for ulcerative colitis in the prior art

Method used

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  • Application of elemonic acid and solid dispersion thereof in preparation of medicine for treating ulcerative colitis
  • Application of elemonic acid and solid dispersion thereof in preparation of medicine for treating ulcerative colitis
  • Application of elemonic acid and solid dispersion thereof in preparation of medicine for treating ulcerative colitis

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preparation example Construction

[0062] The present invention also provides a kind of preparation method of described solid dispersion, and described preparation method comprises the steps:

[0063] Step 1: weighing the elemone acid and the carrier according to the weight ratio; Step 2: melting the carrier at a melting temperature of 60° C. to 100° C.; Step 3: adding the elemone acid while stirring the molten carrier; step Four: Cooling, the cooling temperature is -20°C to 30°C; Step five: Drying; Step six: Crushing; Step seven: Mesh sieving.

[0064] In order to help to understand the content of the present invention more clearly, the in vivo pharmacodynamics experiment of elemic acid in mice, the prescription composition and preparation method of elemic acid solid dispersion are described, and the examples are described in detail as follows .

[0065] 1. In vivo pharmacodynamics experiment of elemone acid

[0066] 1 experimental reagent

[0067] 10×electrotransfer solution, Beijing Solarbio; 20×TBS, Beij...

Embodiment 1

[0088] 1 mouse disease activity index score (Disease Activity Index, DAI)

[0089]During the experiment, the body weight, activity status, feces properties, and hematochezia of the mice were recorded every day. The DAI score is performed according to the following standards, and the weight change score: no change in body weight, marked as 0 points; 0-5% weight loss, marked as 1 point; 5-10%, marked as 2 points; 10-15%, marked as 3 points Points; body weight change greater than 15%, recorded as 4 points. Stool character score: normal, 0 points; soft stools, 2 points; loose stools, 4 points. Fecal occult blood score: no blood in stool, 0 points; positive blood in stool test, 2 points; obvious blood in stool, 4 points. After scoring, the three parts were calculated and the average value was calculated as the mouse disease activity index score.

[0090] 2 Effects of elemonic acid on macroscopic changes in mice

[0091] Such as figure 2 , Compared with the control group, the ...

Embodiment 2

[0094] Histopathological evaluation of the colon

[0095] 1 Preparation of Paraffin Sections of Colon Tissue

[0096] ⑴Collection of specimens: take the colon tissue fixed in 10% formaldehyde solution, and cut out the colon tissue with a length of about 2 mm for use.

[0097] (2) Tissue dehydration: The prepared colon tissue was dehydrated with ethanol gradients of different concentrations: 70%, 30 min; 80%, 30 min; 90%, 60 min; 100%, 60 min.

[0098] (3) Transparent tissue: Soak the tissue twice in xylene for 20 minutes each time.

[0099] (4) Tissue immersion in wax: Tissues were respectively immersed in molten paraffin I, II and III for 60 minutes each.

[0100] (5) Tissue embedding: Place the tissue soaked in wax in a molten wax bath, fully embed the tissue in paraffin, the temperature of the embedding wax is 60°C, and take out the embedding box after cooling.

[0101] ⑹Tissue sectioning: slice the embedded tissue into slices with a thickness of 4 μm with a microtome; t...

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Abstract

The embodiment of the invention discloses application of elemonic acid and solid dispersion thereof in preparation of a medicine for treating ulcerative colitis, and belongs to the technical field of medicines. Experiments prove that the elemonic acid can remarkably relieve clinical symptoms of mice with ulcerative colitis, remarkably reduce necrosis of colon tissues of the mice, remarkably relieve damage to colon tissue structures, relieve inflammatory response and reduce lymphocyte infiltration; the levels of TNF-alpha and IL-1beta in colon tissues are obviously reduced, and meanwhile, the expression of TNF-alpha in serum is obviously reduced. The elemonic acid can be used for increasing the expression of tight binding proteins Occludin and claudin-1, protecting intercellular connection and enhancing the resistance of intestinal mucosa barriers of mice to exogenous microorganisms. The elemonic acid provided by the invention can be prepared into a medicine which has a good effect and is used for treating and / or preventing ulcerative colitis, and the dissolution rate of the medicine can be increased by preparing the elemonic acid into the solid dispersion, so that the oral absorption rate of the elemonic acid is increased.

Description

technical field [0001] The embodiments of the present invention relate to the technical field of medical technology, in particular to the application of elemonic acid and its solid dispersion in the preparation of ulcerative colitis medicine. Background technique [0002] Ulcerative colitis is a chronic nonspecific inflammatory disease of the colon and rectum whose etiology is not yet clear, and the lesions are limited to the mucosa and submucosa of the large intestine. The lesions are mostly located in the sigmoid colon and rectum, and can also extend to the descending colon, or even the entire colon. The course of the disease is long and often recurrent. [0003] In recent years, with the development of molecular biology, major breakthroughs have been made in the study of the etiology of ulcerative colitis. Accumulating evidence indicates that the MAPK (mitogen-activated protein kinase) pathway plays an important role in chronic inflammatory bowel diseases. Activation o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61K9/14A61K47/10A61P1/00A61P1/04
CPCA61K31/575A61K9/146A61P1/00A61P1/04Y02A50/30
Inventor 周昆张玥霍香香于英莉宋蕾陈梦颖皮佳鑫
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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