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Application of purine derivative in selective inhibition of gout calculus and uric acid renal calculus crystals

A uric acid crystallization and derivative technology, applied in the directions of drug combination, urinary system diseases, organic active ingredients, etc., can solve problems such as easy to cause recurrence, patient cost, difficult to completely remove, etc., and achieve convenient use, low price, and remarkable effect. Effect

Inactive Publication Date: 2018-08-21
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Existing methods of treating gout calculus often use surgical treatment, but since gout calculi often appear in many joints and muscle groups of the human body, and are difficult to completely remove, it is easy to cause recurrence
[0005] Existing treatment methods for uric acid stones often use surgical treatment, but it often results in patients spending a lot of time and economic costs

Method used

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  • Application of purine derivative in selective inhibition of gout calculus and uric acid renal calculus crystals
  • Application of purine derivative in selective inhibition of gout calculus and uric acid renal calculus crystals
  • Application of purine derivative in selective inhibition of gout calculus and uric acid renal calculus crystals

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Sodium urate crystallization inhibition effect:

[0041] Add 0.63mL of 1M (1M=1mol / L) NaOH, 84mg of uric acid and 818.6mg of sodium chloride into 100mL of deionized water, heat it on an electric stove until it boils, and remove the heat after visual inspection of complete dissolution. Then, it was naturally cooled and left to stand in an oven at 37° C. for 72 hours. Use a 0.45 μm filter membrane, filter and dry, and accurately weigh to obtain the crystal quality W of sodium urate 空 , as a blank sample (sodium urate solubility is about 7mg / dL).

[0042] Add 0.63mL of 1M (1M=1mol / L) NaOH, 84mg of uric acid, 4.2mg of inhibitors, and 818.6mg of sodium chloride into 100mL of deionized water, heat to boiling on an electric stove, and observe with the naked eye that after the complete dissolution, Remove from heat. Then, it was naturally cooled and left to stand in an oven at 37° C. for 72 hours. Use a 0.45 μm filter membrane, filter and dry, and accurately weigh the mass ...

Embodiment 2

[0046] Uric acid crystal inhibition effect:

[0047] Dissolve 40 mg of uric acid in 250 mL of boiling water, cool to 37°C, adjust pH=4 with hydrochloric acid, and store at 37°C for 72 hours. Use a 0.45 μm filter membrane, filter and dry, and accurately weigh to obtain the crystal quality W of sodium urate 空 , as a blank sample (the solubility of uric acid is about 4.8mg / dL).

[0048] Dissolve 40 mg of uric acid and 4 mg of inhibitor in 250 mL of boiling water, cool to 37°C, adjust pH=4 with hydrochloric acid, and store at 37°C for 72 hours. Use a 0.45 μm filter membrane, filter and dry, and accurately weigh to obtain the crystal quality W of sodium urate 抑 , and finally, the inhibition rate was calculated according to the following formula.

[0049] Inhibition rate = (W 空 -W 抑 ) / W 空

[0050] Uric acid crystallization inhibition rate

[0051] compound

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Abstract

The invention relates to application of a purine derivative in selective inhibition of gout calculus and uric acid renal calculus crystals. The structure of the purine derivative is shown as the specification. Application of the purine derivative provided by the invention to preparation of drugs treating gout calculus and uric acid renal calculus has the advantages of low price, convenient use, and remarkable effect.

Description

technical field [0001] The invention belongs to the technical field of preventing and inhibiting dissolution of gout calculi and uric acid nephrolithiasis, and in particular relates to the application of a purine derivative for selectively inhibiting gout calculi and uric acid nephrolithiasis crystals. Background technique [0002] Gout is a series of inflammatory reactions induced by the metabolic disorder of purine substances in the body or the decrease of renal uric acid excretion, resulting in the continuous increase of blood uric acid concentration, the formation of sodium urate crystals and deposition in soft tissues. When the uric acid in the serum rises to a supersaturated state, the extracellular fluid is deposited in the joints, tissues and organs around the joints, causing a group of gout syndrome (including gouty arthritis, tophi, uric acid kidney stones and gouty nephropathy) . Gouty arthritis is often the first manifestation of the syndrome, which is character...

Claims

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Application Information

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IPC IPC(8): A61K31/522A61P19/06A61P13/04
CPCA61K31/522A61P13/04A61P19/06
Inventor 刘永海付廷明符张玲沈桂云顾志远耿欣宇邵雪宁
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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