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Leflunomide tablet for treating adult rheumatoid arthritis

A technology for rheumatoid arthritis and leflunomide tablets, applied in the field of leflunomide tablets, can solve the problems of difficulty in improving dissolution rate, affecting bioavailability and curative effect, poor water solubility of leflunomide, etc.

Inactive Publication Date: 2016-02-03
李正梅
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Leflunomide is poor in water solubility, and it is difficult to improve its dissolution rate by using ordinary tablet prescriptions and preparation methods, which also affects its bioavailability and curative effect

Method used

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  • Leflunomide tablet for treating adult rheumatoid arthritis

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Embodiment 1: the preparation of leflunomide crystal

[0014] (1) leflunomide is dissolved in the solvent of N-methylacetamide, and the required amount of solvent per g of leflunomide is 100ml; (2) after heating to 40°C for dissolution, add seed crystals after cooling to room temperature; (3) Cool to below 0°C, stir and crystallize, the crystallization temperature is -10°C, filter, dry, collect crystals to obtain leflunomide crystals.

[0015] The prepared leflunomide crystals are measured by powder X-ray diffractometry, and the X-ray powder diffraction patterns represented by 2θ ± 0.2° diffraction angle are at 26.6°, 30.02°, 33.16°, 34.02°, 35.5°, 35.56°, The characteristic diffraction peaks are shown at 44.1°, 53.34° and 72.9°.

Embodiment 2

[0017] Take 10g leflunomide, 50g lactose, 40g starch, 20g hydroxypropyl cellulose, 5g sodium lauryl sulfate, 5g micropowder silica gel, 1g polyethylene glycol 6000, 4g sodium carboxymethyl starch, 0.5g stearin Magnesium acid, the preparation method is as follows: Leflunomide is pulverized, weighed and mixed with lactose, starch, sodium lauryl sulfate, polyethylene glycol 6000, and then add hydroxypropyl Appropriate amount of cellulose-based aqueous solution, making soft materials, granulating, blast drying, and granulating, adding prescription amount of magnesium stearate and micropowder silica gel, mixing, and tableting to obtain 1000 Leflunomide tablets.

[0018] Described leflunomide is a crystal, which is measured by powder X-ray diffractometry. The X-ray powder diffraction spectrum represented by 2θ ± 0.2° diffraction angle is at 26.6°, 30.02°, 33.16°, 34.02°, 35.5°, 35.56° °, 44.1°, 53.34° and 72.9° showed characteristic diffraction peaks.

Embodiment 3

[0020] Take 15g leflunomide, 40g lactose, 50g starch, 15g hydroxypropyl cellulose, 7g sodium lauryl sulfate, 3g micropowder silica gel, 3g polyethylene glycol 6000, 2g sodium carboxymethyl starch, 0.7g stearin Magnesium acid, the preparation method is as follows: Leflunomide is pulverized, weighed and mixed with lactose, starch, sodium lauryl sulfate, polyethylene glycol 6000, and then add hydroxypropyl Appropriate amount of cellulose-based aqueous solution, making soft materials, granulating, blast drying, and granulating, adding prescription amount of magnesium stearate and micropowder silica gel, mixing, and tableting to obtain 1000 Leflunomide tablets.

[0021] Described leflunomide is a crystal, which is measured by powder X-ray diffractometry. The X-ray powder diffraction spectrum represented by 2θ ± 0.2° diffraction angle is at 26.6°, 30.02°, 33.16°, 34.02°, 35.5°, 35.56° °, 44.1°, 53.34° and 72.9° showed characteristic diffraction peaks.

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Abstract

The invention discloses a leflunomide tablet for treating adult rheumatoid arthritis, and belongs to the technical field of medicines. The composition is prepared from leflunomide, lactose, starch, hydroxy propyl cellulose, lauryl sodium sulfate, superfine silica powder, polyethylene glycol 6,000, sodium carboxymethyl starch and magnesium stearate. The leflunomide is a novel crystal compound. An experiment shows that the medicine is fast to dissolve, simple in preparation technology and applicable to mass production.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a leflunomide tablet for treating adult rheumatoid arthritis. Background technique [0002] Leflunomide (leflunomide) is the first new drug approved specifically for the treatment of rheumatoid arthritis in the past ten years. This product has immunosuppressive and anti-inflammatory effects, and its mechanism of action is novel. It inhibits cell adhesion and the activity of acid kinase, affects the information transmission of cytokines, and inhibits the activity of dihydroorotate dehydrogenase, thereby inhibiting the relationship between rheumatoid arthritis and rheumatoid arthritis. Proliferation of activated lymphocytes associated with the pathogenesis of arthritis. Animal experiments and clinical results show that leflunomide inhibits local inflammation and connective tissue hyperplasia as well as the systemic response of arthritis. Various signs and symptoms of rheumatoid art...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/42A61K47/38C07D261/18A61P19/02A61P29/00
Inventor 李正梅
Owner 李正梅
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