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
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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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