Leflunomide tablet preparation and preparation method thereof

A technology for leflunomide and preparation, applied in the field of leflunomide tablet preparation and preparation thereof, can solve the problems of difficulty in improving dissolution, poor water solubility of leflunomide, affecting bioavailability and curative effect, and the like

Active Publication Date: 2013-05-01
JIANGSU YABANG AIPUSEN PHARMA
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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 preparation and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Preparation prescription of the present invention is made up of following components by weight:

[0012] Leflunomide 10g

[0013] Microcrystalline Cellulose 20g

[0014] Lactose 30g

[0015] Sodium carboxymethyl starch 10g

[0016] Poloxamer 188 30g

[0017] Magnesium Stearate 1g

[0018] A total of 1000 pieces were made

[0019] Preparation process: heat and melt poloxamer 188, add leflunomide while stirring to make a solution, stir evenly, quickly cool to solid, dry, crush through 80 mesh sieve, add other excipients to mix, granulate with 20 mesh sieve , 55 ℃ ~ 60 ℃ drying. 18 mesh sieve for granulation. Add magnesium stearate, mix well, and press into tablets.

[0020] The leflunomide tablet prepared by this method has a dissolution rate greater than 90% at 45 minutes.

Embodiment 2

[0022] Preparation prescription of the present invention is made up of following components by weight:

[0023] Leflunomide 10g

[0024] Microcrystalline Cellulose 20g

[0025] Lactose 30g

[0026] Sodium carboxymethyl starch 10g

[0027] Povidone 50g

[0028] Magnesium Stearate 1g

[0029] A total of 1000 pieces were made

[0030] Preparation process: Add the prescribed amount of povidone and leflunomide into an appropriate amount of absolute ethanol, stir to dissolve completely, heat on a water bath, stir until the mixture becomes viscous, rapidly cool, dry, and pulverize. Add other excipients and mix evenly, granulate with 20 mesh sieve, dry at 55°C-60°C, granulate with 18 mesh sieve, add magnesium stearate, mix evenly, and tablet.

[0031] The leflunomide tablet prepared by this method has a dissolution rate greater than 90% at 45 minutes.

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Abstract

The invention relates to a leflunomide tablet preparation and a preparation method thereof. The solid dispersion method is adopted for improving the dissolution rate of a drug, thereby improving the bioavailability of the drug. The in vitro dissolution experiment shows that the dissolution rate of leflunomide tablets prepared by the method can be more than 90% at 45min under the condition of taking water as a dissolution medium.

Description

technical field [0001] The invention relates to a leflunomide tablet preparation and a preparation method thereof, belonging to the field of pharmaceutical preparations. 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 r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/42A61K47/38A61P29/00A61P19/04
Inventor 赵晓红毛白杨陈再新尹雪琴杨旭跃葛育红谢瑞丽孙海棠黄凡
Owner JIANGSU YABANG AIPUSEN PHARMA
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