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Medicinal composition for treating autoimmune disease

An autoimmune and compositional technology, applied in the field of autoimmune disease treatment, can solve problems such as adverse reactions, achieve the effect of alleviating pathological manifestations, obviously relieving effect, and controlling deposition

Inactive Publication Date: 2003-01-01
SHANGHAI XINKAI MEDICINE DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, while suppressing the inflammatory response and tissue damage caused by the autoimmune response, they also suppress the immune system's ability to fight infection and can cause serious adverse reactions

Method used

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  • Medicinal composition for treating autoimmune disease

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The synthesis of embodiment 1 fluosemide

[0028] Take 10 g (0.037 mol) of leflunomide, add it into a flask containing 240 ml of 2% sodium hydroxide solution, and stir at 23-25° C. for 1 hour. Then add 1300ml of water to the reaction solution, filter out the insoluble matter, add 26ml of concentrated hydrochloric acid to the colorless filtrate, immediately obtain a white precipitate, and the pH of the filtrate at this time=1-2. The white solid was collected by filtration, washed with water (3×40ml), and concentrated in vacuo at 40°C to obtain about 10g of the crude product.

[0029] The crude product was recrystallized with 180 ml of absolute ethanol / ethyl acetate (1:8). The precipitated crystals were vacuum-dried at 40°C to obtain 8 g of needle-like crystals (melting point 230-231.5°C). Thin layer chromatography (with CH 2 Cl 2 / HOAc=3 / 1 is developing agent) and 1 H-NMR was used to detect product purity.

Embodiment 2

[0030] The preparation of embodiment 2 capsules

[0031] Formula (1000 Capsules):

[0032] Fluosemide 1g-1000g

[0033] Starch 2.5g-2500g

[0034] Grind the fluosemide raw material into fine powder and pass through a 100-mesh sieve; dry the starch and pass through a 120-mesh sieve; mix the raw and auxiliary materials by the equal-volume incremental method, and pass through a 120-mesh sieve 2-3 times to fully mix; after passing the inspection Fill the capsule.

Embodiment 3

[0035] The preparation formula of embodiment 3 tablet (1000):

[0036] Fluosemide 1g-1000g

[0037] Lactose 5.0g-5000g

[0038] Starch 1.5g-1500g

[0039] Talc powder 0.1g-200g

[0040] 5% starch slurry appropriate amount

[0041]Low-substituted hydroxypropyl cellulose 0.1g-1000g

[0042] OPADRY-OY-GM7305 Appropriate amount

[0043] WHITE

[0044] Grind the fluosemide raw material into fine powder and pass through a 100-mesh sieve; pass the auxiliary materials lactose, starch, and L-HPC through a 100-mesh; use the equal amount incremental method to mix the raw and auxiliary materials, and pass through a 80-mesh sieve 3-4 times to fully mix; Add starch slurry to the mixture to make soft materials, pass through 24 mesh to make wet granules, and dry them in a ventilated oven at 55-60°C; add talc powder after the dry granules are sized through 20 mesh, and punch them with a shallow concave with a diameter of 6.0mm Tablets are made into cores.

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Abstract

The medicine composition for treating autoimmune diseases contains fluothiamine derivative or its salt in the amount for effective treatment and pharmaceutically acceptable supplementary material. Itis one new kind of immunoregulator with inhibition to cellular immunity and humoral immunity. It is proved that the medicine composition has obvious curative effect and low toxicity to autoimmune diseases, including rheumatic arthritis, systemic lupus erythematosus, lupous nephritis, nephropathy syndrome, ankylosing spondylitis, psoriasis and other diseases.

Description

technical field [0001] The present invention relates to the treatment of autoimmune diseases, in particular to the treatment of autoimmune diseases with fluosemide pharmaceutical composition. Background technique [0002] Autoimmune diseases are disease states caused by the body's immune system reacting to its own components. Its basic features are: high-titer autoantibodies and / or self-responsive T cells can be detected; autoantibodies or responsive T cells act on self-tissue cells, causing damage or dysfunction; similar animal models can be replicated and used in patients Serum or sensitized lymphocytes can passively transfer the disease; the outcome of the disease is closely related to the intensity of the autoimmune response; recurrent and chronic migration of the disease; and genetic predisposition. [0003] Just because autoimmune diseases are chronic and relapsing, long-term treatment and monitoring are required. At present, drugs that control inflammation caused by...

Claims

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Application Information

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IPC IPC(8): A61K31/277A61P37/02
Inventor 肖飞
Owner SHANGHAI XINKAI MEDICINE DEV
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