High bioavailability Leflunomide tablet and preparing method thereof

A leflunomide tablet and leflunomide technology are applied in the field of leflunomide tablet with high bioavailability and its preparation, which can solve problems such as large side effects, achieve small side effects, a simple preparation method, and repair the intestinal tract. organizational effect

Inactive Publication Date: 2017-07-07
FUJIAN HUITIAN BIOLOGICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commonly used crushing methods include low-temperature jet crushing, high-speed mechanical shearing, high-speed ball milling, etc. However, the production process of preparing leflunomide tablets after micronizing the leflunomide raw material and auxiliary materials has not been reported, and the current leflunomide There are limitations in the function of the tablet, and patients often need to take other tablets on the basis of taking leflunomide tablets, resulting in serious side effects. For this reason, we propose a highly bioavailable leflunomide tablet and its preparation method

Method used

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  • High bioavailability Leflunomide tablet and preparing method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A high bioavailability leflunomide tablet proposed by the present invention comprises the following raw materials in parts by weight: 1 part of leflunomide, 5 parts of starch, 1 part of hydroxypropyl methylcellulose, and 2 parts of povidone K30 , 0.5 parts of magnesium stearate, 0.1 parts of polysorbate-80, 0.1 parts of threonine, 1 part of glutamine, 1 part of β-carotene, and 0.1 parts of glutathione.

[0027] Its preparation method comprises the following steps:

[0028] S1, weigh leflunomide, starch, hydroxypropylmethylcellulose, povidone K30, magnesium stearate, polysorbate-80, threonine, glutamine, β-carotene according to the proportion , Glutathione are all micronized, and the particle size is controlled at D90 1-20µm;

[0029] S2, mixing the raw materials after the micronization treatment in S1 evenly to make a soft material;

[0030] S3, granulating the soft material, drying at 60°C, controlling the water content at 1-2%, to obtain the tablet core;

[0031] S...

Embodiment 2

[0033] A high bioavailability leflunomide tablet proposed by the present invention comprises the following raw materials in parts by weight: 2 parts of leflunomide, 15 parts of starch, 3 parts of hydroxypropyl methylcellulose, and 4 parts of povidone K30 , 1 part of magnesium stearate, 0.3 part of polysorbate-80, 0.8 part of threonine, 1.5 parts of glutamine, 2 parts of β-carotene, and 0.5 part of glutathione.

[0034] Its preparation method comprises the following steps:

[0035] S1, weigh leflunomide, starch, hydroxypropylmethylcellulose, povidone K30, magnesium stearate, polysorbate-80, threonine, glutamine, β-carotene according to the proportion Both glutathione and glutathione are micronized to control particle size D90 1-40µm;

[0036] S2, mixing the raw materials after the micronization treatment in S1 evenly to make a soft material;

[0037] S3, granulating the soft material, drying at 65°C, controlling the water content at 1-3%, and obtaining the tablet core;

[00...

Embodiment 3

[0040] A high bioavailability leflunomide tablet proposed by the present invention comprises the following raw materials in parts by weight: 3 parts of leflunomide, 30 parts of starch, 5 parts of hydroxypropyl methylcellulose, and 6 parts of povidone K30 , 3 parts of magnesium stearate, 0.8 parts of polysorbate-80, 2 parts of threonine, 2 parts of glutamine, 3 parts of β-carotene, and 1 part of glutathione.

[0041] Its preparation method comprises the following steps:

[0042] S1, weigh leflunomide, starch, hydroxypropylmethylcellulose, povidone K30, magnesium stearate, polysorbate-80, threonine, glutamine, β-carotene according to the proportion Both glutathione and glutathione are micronized to control particle size D90 1-60µm;

[0043] S2, mixing the raw materials after the micronization treatment in S1 evenly to make a soft material;

[0044] S3, granulating the soft material, drying at 75°C, controlling the water content at 1-4%, and obtaining the tablet core;

[0045]...

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Abstract

The invention discloses a high bioavailability Leflunomide tablet and a preparing method thereof. The Leflunomide tablet is prepared from, by weight, 1-5 parts of Leflunomide, 5-60 parts of filler, 1-15 parts of disintegrating agent, 0.5-5 parts of lubricant, 0.1-2 parts of surface active agent, 2-10 parts of adhesive, 0.1-5 parts of threonine, 1-3 parts of glutamine, 1-5 parts of beta-carotene and 0.1-2 parts of glutathione. The Leflunomide tablet is high in dissolution rate and bioavailability and little in side effect, and has a positive meaning of ensuring safety and effectiveness of clinical medication.

Description

technical field [0001] The invention relates to the technical field of medicine and medicine production, in particular to a leflunomide tablet with high bioavailability and a preparation method thereof. Background technique [0002] Leflunomide (chemical name: N-(4-trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide) is an isazole immunomodulator with anti-proliferative activity. Experiments and clinical trials at home and abroad have proved that it has anti-inflammatory and immune regulation effects. At present, it is widely used in the treatment of rheumatoid arthritis, and the effect is good. [0003] Leflunomide BCS (Biopharmaceutical Classification System) classification belongs to Class II, that is, drugs with low solubility and high permeability. Poorly soluble drugs usually mean low oral bioavailability due to their extremely poor water solubility and dissolution rate. Modifications in formulation or process are required to increase their dissolution rates for o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/06A61K31/42A61K9/28A61P19/02A61P29/00A61K31/198A61K31/015
CPCA61K9/2059A61K9/2095A61K9/28A61K31/015A61K31/198A61K31/42A61K38/063A61K2300/00
Inventor 吴军万兴平曹伟陈碧强
Owner FUJIAN HUITIAN BIOLOGICAL PHARMA
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