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Application of compound in preparation of drug for treating gout

A compound and drug technology, applied in the field of medicine, can solve the problems of clinical application limitations, weakened uric acid excretion effect, liver toxicity, etc.

Active Publication Date: 2019-03-08
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition to inhibiting URAT1, probenecid also blocks OAT1 and OAT3, while OAT1 and OAT3 transport urate in the kidney and are responsible for the secretion of uric acid in the urine, which weakens the uric acid excretion effect, while benzene Bromarone is considered to have a higher selectivity for URAT1 and a stronger uric acid-lowering effect than benzsulfonid, but benzbromarone has potential hepatotoxicity, so the clinical application of probenecid and benzbromarone is limited

Method used

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  • Application of compound in preparation of drug for treating gout
  • Application of compound in preparation of drug for treating gout
  • Application of compound in preparation of drug for treating gout

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1 capsule

[0027] Mix 300g orange ketone, 31g starch, 5g low-substituted hydroxypropyl cellulose, 4.3g micropowder silica gel, 1.6g magnesium stearate, and an appropriate amount of 10% starch slurry, and pack them into capsules to obtain 1000 capsule preparations.

Embodiment 2

[0028] Embodiment 2 Granules

[0029] Mix 300g orange ketone with 1000g sucrose and 500g dextrin, and make 1000 packs of granules according to conventional methods.

Embodiment 3

[0030] Example 3 tablet

[0031] 300g orange ketone, 50g starch, 7.4g sodium carboxymethyl starch, 0.9g talcum powder, 50g dextrin, 0.8g magnesium stearate and an appropriate amount of 10% starch slurry were mixed, and made into 1000 tablets according to a conventional method.

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PUM

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Abstract

The invention relates to application of a compound in preparation of a drug for treating gout. The compound has a structure as shown in formula I. Through experiments, it shows that the compound can inhibit URAT1, reabsorption of uric acid is stopped, discharge of the uric acid of rats can be promoted, the serum urate levels is reduced, sodium urate induced THP-1 CELL IL-1 beta and TNF-alpha secretion can further be inhibited obviously, the degree of rat ankle swelling caused by sodium urate is reduced, inflammatory response is reduced, and arthralgia is relieved. It shows that the compound has effect of treating hyperuricemia and / or gout and has high application value.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the use of aurone. Background technique [0002] Gout is a common chronic inflammatory metabolic disease or rheumatic disease. Crystal-associated arthritis caused by urate deposition caused by disturbance of purine metabolism and decreased uric acid excretion. Acute gouty arthritis (AGA) is a characteristic symptom of gout, and it is a characteristic acute inflammatory reaction caused by the deposition of urate crystals in joints and surrounding connective tissue. It often breaks out at night, wakes up due to pain and cannot fall asleep all night, the disease recurs, and can develop into polyarthritis, or migratory arthritis, the affected joints are red, swollen, hot, painful, and the activities are limited. Patients with acute gouty arthritis account for the largest proportion of gout patients who see a doctor due to recurrent pain. If they are not actively treated, they will...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/343A61P19/06A61P19/02
CPCA61K31/343A61P19/02A61P19/06
Inventor 肖伟张红刘文君曹泽彧曹亮王振中
Owner JIANGSU KANION PHARMA CO LTD
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