Pharmaceutical composition for treating hyperuricemia

A technology of hyperuricemia and composition, which is applied in the field of chemical medicine, can solve the problems of decreased uric acid-lowering effect, liver function damage, gastrointestinal discomfort, etc., and achieve the goal of reducing toxic and side effects, improving safety, and good uric acid-lowering effect Effect

Active Publication Date: 2020-09-29
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the increase of clinical application of these drugs, their adverse reactions are gradually exposed.
[0004] Benzbromarone is a drug that promotes uric acid excretion. It was launched in France in 1976 and brought a new approach to the treatment of chronic gout. It has a significant effect on the treatment of hyperuricemia, but it can cause gastrointestinal Discomfort, especially diarrhea; it was reported in 2003 that it may cause severe liver damage and was restricted by the European market, and the FDA also rejected its marketing application due to adverse reactions. However, some countries, including my country, still allow its use, but only Decreased uric acid-lowering effect due to administration of drug dosage based on muscle narcotic clearance rate
[0

Method used

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  • Pharmaceutical composition for treating hyperuricemia
  • Pharmaceutical composition for treating hyperuricemia
  • Pharmaceutical composition for treating hyperuricemia

Examples

Experimental program
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Effect test

Embodiment 1

[0038] This example provides the extraction method and characterization of compound 1, compound 4-8 in the active ingredient.

[0039] The ethanol, ethyl acetate, petroleum ether, and methanol used in this example are all commercially available products, and the silica gel columns used are all 3.5L-silica gel columns (Ф8cm*70cm).

[0040] Take 50kg of dried rhizome of Atractylodes macrocephalae, smash it and soak and extract 3 times with 8 times the volume of 90% ethanol solution, then concentrate under reduced pressure to remove organic solvent (solid content 2.5kg); the concentrated solution is passed through 50L-D101 column (Ф22cm*150cm) Rinse 4 column volumes with 40% and 95% ethanol, collect the 95% ethanol fraction, concentrate under reduced pressure to remove the organic solvent (solid content 1kg); add 3 times the volume of ethyl acetate to the concentrate for extraction, collect the ethyl acetate fraction , Concentrate under reduced pressure to remove the organic solvent (...

Embodiment 2

[0049] This example provides the extraction method and characterization of compounds 9-14 in the active ingredients.

[0050] The ethanol, petroleum ether, ethyl acetate, and methanol used in this embodiment are all commercially available products, and the silica gel columns used are all 3.5L-silica gel columns (Ф8cm*70cm).

[0051] Take 50kg of Inulina medicinal material, smash it and soak and extract 3 times with 8 times the volume of 90% ethanol solution, and concentrate under reduced pressure to remove organic solvent; the concentrated solution is passed through 50L-D101 column (Ф22cm*150cm), and 40% and 95% ethanol are used respectively Rinse 4 column volumes, collect the 95% ethanol fraction, concentrate under reduced pressure to remove the organic solvent (solid content 3.2kg), add 3 times the volume of petroleum ether to the concentrated solution and extract 3 times, recover the extraction solvent under reduced pressure to obtain the petroleum ether fraction 2kg. The petro...

Embodiment 3

[0057] This embodiment provides a hyperuricemia pharmaceutical composition, which is prepared by mixing benzbromarone and compound 1 in a weight ratio of 3:5. The compound 1 used in this example was prepared according to Example 1. The structural formula of the compound 1 is as follows:

[0058]

[0059] As an alternative to this embodiment, the compound 1 can be replaced with one of the compounds 2-14, and the benzbromarone can be replaced with risinard.

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Abstract

The invention belongs to the field of chemical medicines, and particularly relates to a pharmaceutical composition for treating hyperuricemia. The invention relates to application of a sesquiterpene lactone compound with a structure shown as a formula (I) and pharmaceutically acceptable salts, esters, prodrugs, solvates, polymorphs, hydrates or derivatives of the sesquiterpene lactone compound topreparation of combined drugs for treating the hyperuricemia in combination with hyperuricemia drugs, and further provides the pharmaceutical composition for treating the hyperuricemia. The pharmaceutical composition comprises the compound and one of benzbromarone or lesinurad. The pharmaceutical composition for treating the hyperuricemia can achieve the uric acid reducing effect equivalent to oreven better than that of the drugs for treating the hyperuricemia in the prior art, can obviously reduce the toxic and side effects of the drugs for treating the hyperuricemia in the prior art and improve the safety, and can be used for treating the hyperuricemia and gout or gout complications caused by the hyperuricemia.

Description

Technical field [0001] The invention relates to the field of chemical medicine, in particular to a hyperuricemia pharmaceutical composition. Background technique [0002] In the field of chemical medicine, uric acid is the final metabolite of human purine compounds. Disorders of purine metabolism lead to hyperuricemia. Under a normal purine diet, the fasting blood uric acid level of men is higher than 416μmol / L twice on different days and that of women is higher than 360μmol / L, which is called hyperuricemia. Normally, there is no conscious symptom for simply being in a state of hyperuricemia, but if you stay in this state for a long time, urate in the blood will crystallize and deposit in joints, subcutaneous tissues, kidneys, etc., and then gout and gout will be complicated. A series of clinical manifestations such as disease. According to the recently published "White Paper on China's Gout Status Report 2017", the number of patients with hyperuricemia in my country has reach...

Claims

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Application Information

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IPC IPC(8): A61K31/343A61K31/365A61K31/122A61K31/4196A61P19/06A61P13/12A61P19/02
CPCA61K31/343A61K31/365A61K31/122A61K31/4196A61P19/06A61P13/12A61P19/02A61K2300/00Y02A50/30
Inventor 徐海霞陈佳玲逄龙
Owner CATCH BIO SCI & TECH
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