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Application of clarithromycin in the preparation of anti-allergic drug

A technology for clarithromycin and allergic reaction, which is applied to the application field of clarithromycin in the preparation of anti-allergic drugs, can solve problems such as increased bioavailability, and achieve the effects of less side effects, good absorption and strong stability

Active Publication Date: 2020-06-19
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Food intake is generally considered to have no significant effect on the bioavailability of clarithromycin, although increased bioavailability in the presence of food in the stomach has been reported

Method used

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  • Application of clarithromycin in the preparation of anti-allergic drug
  • Application of clarithromycin in the preparation of anti-allergic drug
  • Application of clarithromycin in the preparation of anti-allergic drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] (1) Antagonize the release of human mast cell β-hexosaminidase induced by substance P

[0025] 1) Reagent

[0026] 0.1% Triton X-100 Lysis Solution: Dissolve 10 μL Triton X-100 in 10 mL PBS to obtain 0.1% Triton X-100 Lysis Solution.

[0027] 0.1mol / L citric acid / sodium citrate buffer solution (pH4.5): Weigh 2.101g of citric acid monohydrate and dissolve it in 100mL triple distilled water to obtain a 0.1mol / L citric acid solution, keep it away from light at 4°C save. Weigh 2.941g of sodium citrate, dissolve it in 100mL of triple distilled water to obtain a 0.1mol / L sodium citrate solution, and store it in the dark at 4°C. Before use, mix according to the ratio of 0.1mol / L citric acid: 0.1mol / L sodium citrate=10.4:9.6 (v / v) to obtain 0.1mol / L citric acid / sodium citrate buffer solution.

[0028] 1mmol / L β-hexosamine solution: Weigh 0.034g of β-hexosamine and dissolve it in 100mL 0.1mol / L citric acid / sodium citrate buffer solution to obtain 1mmol / L β-hexosamine solution...

Embodiment 2

[0047] 1) Reagent

[0048] The preparation of 0.5% CMC-Na solution, 0.5g CMC-Na is added in 100mL physiological saline, ultrasonically dissolves, prepares and obtains 0.5% CMC-Na solution. For the preparation of 60μg / mL substance P solution, weigh 6mg of substance P powder, add 0.1mL of normal saline, and dilute 100 times with normal saline after ultrasonic dissolution to obtain 60μg / mL substance P solution.

[0049] 2) Experimental steps

[0050] Use 0.5% CMC-Na solution to prepare clarithromycin suspension with corresponding concentration.

[0051] 50 C57BL / 6 mice at 7-8 weeks were randomly divided into 5 groups, including 3 different concentration administration groups, negative control group and blank control group, with 10 mice in each group.

[0052] For intragastric administration, 8.125, 16.25 and 32.5 mg / kg clarithromycin suspensions were administered to three different concentration administration groups; 0.2 mL of 0.5% CMC-Na solution was intragastrically administ...

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PUM

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Abstract

The invention discloses application of clarithromycin in preparation of medicine for resisting anaphylactoid reaction. The medicine has dosage forms such as tablets, controlled release formulations, injection or spray. The clarithromycin has an antagonistic effect of human mast cell released beta-hexosaminidase caused by substance P. Meanwhile, the clarithromycin has an effect of lowering rise ofhistamine in serum of mice caused by the substance P. The clarithromycin has the characteristics of being less in side effects, excellent in absorption, high in stability and the like, is capable of effectively inhibiting mast cell degranulation reaction caused by a substance P activated MRGPRX2 (Mas-Related G-Protein coupled Receptor X2), has effects of reducing mast cell released histamine on acellular level and an animal level, and is applicable to treatment of diseases having long course of treatment. In addition, the clarithromycin is discovered to have the activity of resisting anaphylactoid reaction in theoretical and clinical treatment, and has potential development value of treating immune diseases.

Description

technical field [0001] The invention belongs to the field of antibiotic drugs and relates to the application of clarithromycin in the preparation of anti-anaphylaxis drugs Background technique [0002] Clarithromycin (Clarithromycin) is the most favored and most promising species among the second-generation macrolide antibiotics. Its chemical name is 6-O-methylerythromycin A, which was developed by Taisho Corporation of Japan. The developed 14-membered ring erythromycin derivative has the structure shown below. The structure of clarithromycin is similar to that of erythromycin, but because its 6-hydroxyl group is replaced by a methyl group, the rearrangement of 6-9 and 9-12 of the lactone ring is blocked, so that clarithromycin overcomes the acidity of erythromycin The disadvantage of losing antibacterial activity due to the change of spiro ketal in macrocyclic molecules in the environment can reduce the adverse reactions of gastrointestinal tract. Clarithromycin also has ...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P37/08
CPCA61K31/7048A61P37/08
Inventor 贺浪冲张涛贺怀贞车德路
Owner XI AN JIAOTONG UNIV
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