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Composition containing pyrazolopyrimidinamine derivative mixture and uses thereof

A technology of pyrazolopyrimidine amine and the second pyrazolopyrimidine amine, applied in the direction of medical preparations containing active ingredients, plant raw materials, organic active ingredients, etc., can solve problems that need to be further improved

Inactive Publication Date: 2020-01-14
黄泳华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Plant extracts are rich in a variety of ingredients with antibacterial activity. For example, Yang Ruoying et al. reported (Journal of Tropical Biology, 2019, 10(03): 226-230.) The extracts of plants such as Jiaofeng, Liuerbell, Tengnoginseng, Guanzhong, Jinxiancao, Cyclopedia, Babaili, and Punchstone have the effect on tobacco Ralstonia solanacearum at 100mg / L and / or 500mg / L Certain antibacterial activity, but the inventors found that the antibacterial activity of the above-mentioned plant extracts to other common pathogenic bacteria needs to be further improved

Method used

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  • Composition containing pyrazolopyrimidinamine derivative mixture and uses thereof
  • Composition containing pyrazolopyrimidinamine derivative mixture and uses thereof
  • Composition containing pyrazolopyrimidinamine derivative mixture and uses thereof

Examples

Experimental program
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Effect test

preparation example 1

[0020] The preparation of preparation example 1 plant extract

[0021] Ultrasonic extraction method is used to dry the shade-dried plant material at 40°C, crush it, pass through a 40-mesh sieve, and put it into a ziplock bag. Before the test, 50 g of plant dry powder was weighed, and different organic solvents were added for ultrasonic extraction (as shown in Table 1), and the extraction was repeated 3 times for 60 min each time. Concentrate after filtration and store in a refrigerator at 4°C until use.

[0022] Table 1 Organic solution of ultrasonic extraction of different plant extracts

[0023]

[0024]

Embodiment 1

[0101] Example 1 Preparation of Oral Solid Formulation Composition Containing a Mixture of Pyrazolopyrimidinamine Derivatives

[0102] Prescription (1500 unit dose)

[0103]

[0104] Preparation

[0105] Take the mixture X-Y-PEZ and auxiliary materials in the prescribed amount, and pass through a 100-mesh sieve. Take the mixture X-Y-PEZ, lactose, microcrystalline cellulose, crospovidone and starch and mix thoroughly; take the prescribed amount of hypromellose, and prepare a solution with a concentration of 10% based on hypromellose, Use lactic acid to adjust the pH to 3.0-4.0, add it to the above-mentioned mixture to make a soft material, granulate with a 16-mesh sieve, and dry at 80°C for 3-4 hours. Use a 16-mesh sieve to sieve the granules, add the prescribed amount of micropowder silica gel and magnesium stearate, mix well, fill the capsules, and obtain capsules;

[0106] Take the mixture X-Y-PEZ and auxiliary materials in the prescribed amount, and pass through a 10...

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Abstract

The invention provides a composition containing a mixture of a first pyrazolopyrimidinamine derivative and a pyrazolopyrimidinamine derivative which are different from each other. The specific definition of the pyrazolopyrimidinamine derivative is as described in the specification. The mixture can generate a synergistic antibacterial effect with extracts of plants such as Alocasia macrorrhiza (L.)Schott, shorthairy antenoron herb, cudrania cochinchinensis and Hyptis suaveolens Piot.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition containing a mixture of pyrazolopyrimidine amine derivatives and its application. Background technique [0002] Nosocomial infection is an important issue affecting the quality of hospital care. With the continuous development and progress of modern medical technology, antibacterial drugs are widely used, and the drug-resistant strains of clinical pathogens are increasing. Therefore, improving the antibacterial activity of existing drugs will help to improve the therapeutic effect of patients with bacterial infections. [0003] Trivedi A et al. (J Enzyme Inhib Med Chem.2010Dec; 25(6):893-9.) and BakavoliM et al. (Eur J Med Chem.2010Feb; 45(2):647-50.) reported various Pyrazolo[3,4-d]pyrimidine derivatives with antibacterial activity. [0004] Plant extracts are rich in a variety of ingredients with antibacterial activity. For example, Yang Ruoying et...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K36/888A61K36/28A61K36/53A61P31/04
CPCA61K31/519A61K36/28A61K36/53A61K36/888A61P31/04A61K2300/00Y02A50/30
Inventor 向飞曹新欣
Owner 黄泳华
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