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Composition containing triazolopyrimidine derivative mixture and purpose of composition

A technology of the first triazolopyrimidine and azolopyrimidine, which is applied in the direction of medical preparations containing active ingredients, plant raw materials, organic active ingredients, etc., and can solve problems that need to be further improved

Inactive Publication Date: 2020-04-28
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 triazolopyrimidine derivative mixture and purpose of composition
  • Composition containing triazolopyrimidine derivative mixture and purpose of composition
  • Composition containing triazolopyrimidine derivative mixture and purpose of composition

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0068] The preparation of preparation example 1 plant extract

[0069] 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. After filtration, it was concentrated to dryness and stored in a refrigerator at 4°C until use.

[0070] Table 1 Organic solvents for ultrasonic extraction of different plant extracts

[0071] plant material Extract number Organic solvent for extraction hairy tiger PE1 Isopropanol red yaozi PE2 n-heptane white diamond PE3 Methanol Bone style PE4 acetone june snow PE5 ethanol Peace of mind PE6 Methanol

Embodiment 1

[0142] Embodiment 1 Preparation of solid formulation containing the composition of triazolopyrimidine derivative mixture

[0143] prescription

[0144]

[0145]

[0146]

[0147] Preparation

[0148] The active ingredients and auxiliary materials of the prescribed amount are all passed through a 100-mesh sieve. Get the active ingredient, lactose, microcrystalline cellulose, crospovidone and starch and mix thoroughly; get the hypromellose of the prescription amount, and prepare a solution with a concentration of 10% based on hypromellose, add lactic acid 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, add the prescribed amount of micropowder silica gel and magnesium stearate, mix well, and fill into capsules with a weight of about 500 mg each;

[0149] The active ingredients and auxiliary materials of the prescribed amount are all p...

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Abstract

The invention provides a composition containing a mixture of a first triazolopyrimidine derivative and a second triazolopyrimidine derivative which are not the same mutually, and specific definitionsof triazolopyrimidine derivatives are as seen in the description. The mixture disclosed by the invention can synergistically reinforce the restraining effects of extracts of plants of hyptis suaveolens and the like on bacteria of acinetobacter calcoaceticus and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition containing a mixture of triazolopyrimidine 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] Li Mingjian et al. (Journal of Wuhan University (Natural Science Edition), 2017,63(04):325-329.) Yue Wei et al. (Shandong Chemical Industry, 2016,45(20):3-5.) and Liu Tingting et al. (Guangzhou Chemical Industry, 2014,42(17):62-64.) disclosed triazolopyrimidine compounds with antibacterial activity in their respective studies. [00...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K36/53A61K36/28A61K36/704A61K36/79A61K36/57A61K36/41A61K36/282A61K36/47A61K36/74A61K36/48A61P31/04
CPCA61K31/519A61K36/28A61K36/282A61K36/41A61K36/47A61K36/48A61K36/53A61K36/57A61K36/704A61K36/74A61K36/79A61P31/04A61K2300/00Y02A50/30
Inventor 向飞唐建涛
Owner 黄泳华
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