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A combined drug for inhibiting multidrug-resistant tuberculosis bacilli

A Mycobacterium tuberculosis, multidrug-resistant technology, applied in the field of medicine, can solve problems such as large body damage, liver function damage, liver and kidney damage, etc., and achieve the effects of increasing medication compliance, reducing toxic side effects, and reducing medication dosage.

Active Publication Date: 2019-01-15
SICHUAN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to facilitate the treatment of multidrug-resistant tuberculosis and extensive multidrug-resistant tuberculosis, WHO divides anti-tuberculosis drugs into five groups. Rifampicin and isoniazid are the main drugs for the initial treatment of tuberculosis, but isoniazid has strong side effects, especially in At high concentration and high dose, it will cause liver function damage, allergy, high fever, epilepsy and peripheral neuritis, etc., which will cause greater damage to the body; taking rifampicin will cause gastrointestinal functional reactions, allergies, thrombocytopenia and leukopenia, convulsions and liver and kidney damage; the combination of rifampicin and isoniazid can reduce the drug resistance rate of Mycobacterium tuberculosis, but because rifampicin has a strong liver drug enzyme induction effect, it will accelerate the acetylation process of isoniazid in the liver , thereby aggravating the hepatotoxicity of the drug
And with the gradual development of drug-resistant bacteria, most Mycobacterium tuberculosis will quickly resist isoniazid after being resistant to rifampicin, and accelerate the increase in the number of multi-drug-resistant Mycobacterium tuberculosis. Gradually unable to meet treatment needs

Method used

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  • A combined drug for inhibiting multidrug-resistant tuberculosis bacilli
  • A combined drug for inhibiting multidrug-resistant tuberculosis bacilli
  • A combined drug for inhibiting multidrug-resistant tuberculosis bacilli

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 The preparation of forsythia ethyl acetate of the present invention

[0023] 1. Sample pretreatment

[0024] Take forsythia and wash it with water, then dry it in a drying oven at 60°C, pulverize the medicinal material with a grinder, and pass it through a No. 3 pharmacopoeia sieve for later use.

[0025] 2. Reflux extraction

[0026] Weigh 500g of Forsythia powder, pour it into a 10000mL round bottom flask, then pour 5000mL of 95% ethanol into the flask, soak for 24h, install the reflux device, reflux at 65°C for 1h, pour out the extract, and use the extract Buchner funnel filtration. Then add 5000 mL of 95% ethanol to the remaining medicinal residues, and extract twice more according to the above method. The three filtrates were combined, recovered under reduced pressure at 65°C and freeze-dried to obtain a freeze-dried powder.

[0027] Accurately weigh 30g of forsythia freeze-dried powder, crush it with a calender, add 600ml of ethyl acetate, ultraso...

Embodiment 2

[0028] Embodiment 2 The preparation of the combined drug solution for inhibiting multidrug-resistant Mycobacterium tuberculosis of the present invention

[0029] 1. Preparation of drug mother liquor

[0030] Weigh 1.6 mg of isoniazid, add 1 mL of ultrapure water to dissolve it, and filter it with a 0.22 μm filter membrane. At this time, the concentration of isoniazid mother liquor is 1.6 mg / mL, and prepare the parts of rifampicin and forsythia ethyl acetate in the same way. Concentrations of 4mg / mL and 2mg / mL mother liquors, the prepared drug mother liquors were filtered and then packed in sterile EP tubes and stored at -20°C for later use.

[0031] 2. Preparation of combined drug solution

[0032] 1) Take the aforementioned drug mother solution and return to room temperature;

[0033] 2) Take 100 μm mother liquors of isoniazid and rifampicin respectively and mix them evenly, then add 800 μm mother liquors of forsythia ethyl acetate parts, mix evenly, and filter with a 0.22 ...

Embodiment 3

[0034] Embodiment 3 The preparation of the combined drug solution for inhibiting multidrug-resistant Mycobacterium tuberculosis of the present invention

[0035] 1. Preparation of drug mother liquor

[0036] Weigh 1.28 mg of isoniazid, add 1 mL of ultrapure water to dissolve it, and filter it with a 0.22 μm filter membrane. At this time, the concentration of isoniazid mother liquor is 1.28 mg / mL, and prepare the parts of rifampicin and forsythia ethyl acetate in the same way. Concentrations of 3.2mg / mL and 2mg / mL mother liquors, the prepared drug mother liquors were filtered and then packed in sterile EP tubes and stored at -20°C for later use.

[0037] 2. Preparation of combined drug solution

[0038] 1) Take the aforementioned drug mother solution and return to room temperature;

[0039] 2) Take 50 μm of isoniazid and 150 μm of rifampicin mother liquor and mix them evenly, then add 800 μm of forsythia ethyl acetate part mother liquor, mix evenly, and filter with a 0.22 μm ...

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Abstract

A combined drug for inhibiting multidrug-resistant tuberculosis bacilli comprises ethyl acetate fraction of forsythiae, isoniazid and rifampicin for simultaneous or separate administration, and pharmaceutically acceptable carriers. The combined medicine of the invention can obviously reduce the dosage of isoniazid and rifampicin, remarkably increase the synergistic bacteriostatic effect, thereby reducing the toxic and side effects of isoniazid and rifampicin, increasing the medication compliance of patients, and providing a new choice for clinic.

Description

technical field [0001] The invention relates to a combined medicine for inhibiting multidrug-resistant Mycobacterium tuberculosis, which belongs to the field of medicine. Background technique [0002] Forsythia suspensa (Forsythia suspensa) is the dried fruit of Forsythia genus Oleaceae, which has the functions of sterilization, heat-clearing and detoxifying, anti-emetic, and anti-liver damage. "Materia Medica Zhengyi" records that forsythia can dissipate stagnation and relieve heat in the veins, and treat fistulas, carbuncles, sores, heat stagnation, and poisonous poisoning. [0003] Tuberculosis is one of the major infectious diseases that seriously endanger human health, and it has a history of more than 4,000 years. my country is one of the countries with the highest burden of tuberculosis in the world, and also one of the countries with a high burden of multidrug-resistant tuberculosis. Since entering the 21st century, my country has comprehensively implemented a mode...

Claims

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Application Information

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IPC IPC(8): A61K36/634A61P31/06A61K31/4409A61K31/496
CPCA61K31/4409A61K31/496A61K36/634A61K2236/333A61K2236/39A61P31/06A61K2300/00
Inventor 黎霞廖颖严伟冉然李艾妮吴灵俐佘诗琪
Owner SICHUAN NORMAL UNIVERSITY
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