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Composition containing azabicyclic derivatives and application thereof

A technology of azabicyclo and composition, which is applied in the direction of medical preparations containing active ingredients, drug combinations, plant raw materials, etc., and can solve problems such as strong adverse reactions and drug resistance

Pending Publication Date: 2020-01-03
黄泳华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although traditional chemotherapy drugs prolong the survival period of patients, their strong adverse reactions and the emergence of drug resistance make the search for new drugs to treat tumors a hot spot in the current research field.

Method used

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  • Composition containing azabicyclic derivatives and application thereof
  • Composition containing azabicyclic derivatives and application thereof
  • Composition containing azabicyclic derivatives and application thereof

Examples

Experimental program
Comparison scheme
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 10 to 20 times (v / w) of water was added for ultrasonic extraction, 60 min each time, and the extraction was repeated 3 times. Concentrate after filtration and store in a refrigerator at 4°C until use.

[0022] The plant material is selected from the group consisting of blueberry (PE1), stone see wear (PE2), grifola frondosa (PE3), eye tree lotus (PE4), sessile five plus (PE5), goldenflower sunflower (PE6), golden camellia (PE7), Snakevine (PE8), Pinellia (PE9), Hedyotis diffusa (PE10), Zhemu (PE11), Ashen (PE12), African Malus (PE13), Jade Fungus (PE14), It is one of Euphorbia (PE15), Brown Algae (PE16), Clover (PE17) and Tibetan Capillary (PE18).

Embodiment 1

[0098] Example 1 Preparation of Liquid Preparations Containing Azabicyclic Derivatives and Polyhydroxyl Compounds

[0099] Prescription (10000 unit dose)

[0100]

[0101]

[0102] Note:

[0103] a Represents no added plant extracts

[0104] Preparation Process

[0105] Add the prescribed amount of citric acid, mixture X-Y-PEZ, edetate disodium, sodium chloride, benzalkonium chloride, and mannitol, add 20% of the prescribed amount of water for injection to dissolve, and filter through a 0.22 μm microporous membrane, Use sodium hydroxide to adjust the pH value to about 6.3, pass through a 220-mesh sieve, seal and boil for 60 minutes, cool to room temperature, and add water for injection to the full amount.

Embodiment 2

[0106] Embodiment 2 Preparation of oral solid preparation containing a mixture of azabicyclic derivatives

[0107] Prescription (1000 unit dose)

[0108]

[0109]

[0110] Preparation

[0111] 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;

[0112] Take the mixture X-Y-PEZ and auxiliary materials in the prescribed amount, and pass through a 100-mes...

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PUM

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Abstract

The invention provides a composition containing a mixture of two azabicyclic derivatives different from each other. The specific azabicyclic derivatives are defined as shown in the specification. Themixture can have synergistic anti-tumor effect with extracts of plants such as camellia nitidissima chi, celastrus orbiculatus, pinellia ternata, hedyotis diffusa, cudrania tricuspidata bur and anthriscus sylvestris.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a composition containing an azabicyclic derivative and a polyhydroxy compound and an application thereof. Background technique [0002] Tumor is one of the diseases that pose the greatest threat to human health. According to WHO statistics, there are about 8 million new cases and 7 million deaths from malignant tumors in the world every year on average, and this number is increasing year by year. The three major methods of Western medicine clinical treatment of tumors are surgical resection, radiotherapy and chemotherapy. However, although traditional chemotherapeutic drugs prolong the survival period of patients, their strong adverse reactions and drug resistance make the research of seeking new drugs to treat tumors become a hot spot in the current research field. [0003] Azabicyclo is the structural core shared by various anti-tumor active compounds. Specific ex...

Claims

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Application Information

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IPC IPC(8): A61K31/473A61K31/439A61K31/4725A61K36/82A61K36/37A61K36/8888A61K36/748A61K36/60A61K36/23A61P35/00A61P35/02
CPCA61K31/439A61K31/4725A61K31/473A61K36/23A61K36/37A61K36/60A61K36/748A61K36/82A61K36/8888A61P35/00A61P35/02A61K2300/00
Inventor 向飞赵震震
Owner 黄泳华
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