Application of olsalazide sodium as a medicine for preventing and treating hyperuricemia and gout

A technology of hyperuricemia and ossalazide sodium, applied in the field of pharmaceuticals, can solve the problems of toxic epidermolysis necrosis, nephropathy and calculi, and high mortality due to hypersensitivity reactions, so as to shorten research and development time and save research and development costs. Effect

Inactive Publication Date: 2018-09-07
KUNMING MEDICAL UNIVERSITY +1
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Problems solved by technology

Allopurinol is a purine analog and a competitive XO inhibitor, but allopurinol can easily cause xanthine nephropathy and calculus (Zhu Shenyin, Zhou Yuanda, Du Guanhua. Research progress of gout drugs[J]. Medical Herald 2006,25 :(8):803-806.) and hypersensitivity reactions, and the mortality rate of hypersensitivity reactions is extremely high, especially HLA-B58 positive patients are prone to Stevens-Johnson syndrome and toxic epidermolysis after taking allopurinol necrosis (Perez-Ruiz F, Liote F.Lowering serum uric acid levels:whatis the optimal target for improving clinical outcomes in gout[J].ArthritisRheum 2007,57:1324-132.), and it is contraindicated in severe liver damage, coronary Cardiac disease and heart failure patients

Method used

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  • Application of olsalazide sodium as a medicine for preventing and treating hyperuricemia and gout
  • Application of olsalazide sodium as a medicine for preventing and treating hyperuricemia and gout
  • Application of olsalazide sodium as a medicine for preventing and treating hyperuricemia and gout

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Embodiment Construction

[0023] 1. The inhibitory effect of the inventive compound on xanthine oxidase

[0024] Xanthine oxidase (EC 1.1.3.22) is a product of Sigma Company, prepared with sodium pyrophosphate buffer solution to an appropriate concentration for use. Osalazide sodium was prepared into a series of concentrations with sodium pyrophosphate buffer solution for future use. After incubating xanthine oxidase with serial concentrations of olsalazide sodium solution at 25°C for 15 minutes, refer to the literature method [Kong LD, Zhang Y, Pan X, Tan RX, and Cheng CHK (2000) Inhibition of xanthine oxidase by liquiritigenin and isoliquiritigenin isolated from Sinofranchetia chinensis.Cell Mol Life Sci57:500–505] was used to measure the activity of xanthine oxidase, and the results showed that sodium olsalazide had a strong inhibitory effect on the activity of xanthine oxidase, and its IC 50 9.8μmol / L ( Figure 2-4 ), the suppression type is mixed suppression ( Figure 5-7 ).

[0025] 2. Effect...

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Abstract

The invention provides an application of olsalazine sodium in preparation of medicines for preventing and treating hyperuricemia and gout. The olsalazine sodium obviously inhibits the activity of xanthine oxidase in vitro, has IC50 of 9.8mu mol / L, and is a hybrid type xanthine oxidase inhibitor. The in vivo study shows that intraperitoneal injection of the 5.0mg / kg compound obviously reduces the level of serum uric acid of an oteracil potassium induced hyperuricemia mouse, and the dosage for reducing serum uric acid is very less than the dosage for treating ulcerative colitis clinically; and the olsalazine sodium has the characteristics of high efficiency and low toxicity and can be used for preparing medicines and health products for preventing and treating hyperuricemia and gout.

Description

technical field [0001] The invention belongs to medicines, in particular to medicines for preparing and preventing hyperuricemia and gout. Background technique [0002] Gout is a metabolic disease that seriously threatens human health. The high incidence age of the disease is middle-aged and elderly men and postmenopausal women. It is listed as one of the 20 chronic diseases in the 21st century. Uric acid (UA) is the end product of purine metabolism in the human body. It is decomposed into soluble allantoin and excreted from the body. It is an important measure to reduce and control blood uric acid level and treat and prevent gout. However, the human body lacks uric acid decomposing enzymes, and the result of accumulation makes it very easy to form hyperuricemia. As an index for the treatment of gout, the European League Against Rheumatism and the American College of Rheumatology recommend that the blood uric acid index should not be higher than 6mg / dl. [0003] Xanthine O...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/655A61P19/06A23L33/00
CPCA23V2002/00A61K31/655A23V2200/30A23V2250/02
Inventor 牛艳芬李玲李宏健高丽辉林华刘旭梁广锡王文汉林李家宓孔祥复
Owner KUNMING MEDICAL UNIVERSITY
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