Application of a compound in preparation of medicine for gout

A compound and drug technology, applied in the field of medicine, can solve problems such as weakened uric acid excretion effect, liver toxicity, and clinical application limitations, and achieve the effect of reducing swelling, reducing inflammation and pain, and relieving joint pain

Active Publication Date: 2021-06-22
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 a compound in preparation of medicine for gout
  • Application of a compound in preparation of medicine for gout
  • Application of a compound in preparation of medicine for 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 present invention relates to the application of a compound in the preparation of medicine for gout, the compound has the structure of formula I. Experiments of the present invention show that the compound can inhibit URAT1, block uric acid reabsorption, promote uric acid excretion in rats, reduce serum uric acid levels, and significantly inhibit sodium urate-induced THP-1 cells IL-1β, TNF-1 α secretion, and reduce sodium urate-induced ankle swelling in rats, reduce inflammatory response, and relieve joint pain. This shows that the compound has the effect and application value of treating hyperuricemia and / or gout diseases.

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 & AuthorityPatents(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
OwnerJIANGSU KANION PHARMA CO LTD