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A kind of teriflunomide microemulsion, preparation method and application

A technology of teriflunomide and microemulsion, which is applied in the field of new dosage forms of teriflunomide, can solve the problems of long half-life and irritation, and achieve the effects of reducing fluctuations in the body, promoting absorption, and facilitating penetration and absorption

Active Publication Date: 2020-04-07
ANHUI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

U.S. FDA (Food and Drug Administration, FDA) approved Sanofi-Aventis to develop A771726 (teriflunomide) oral tablet Aubagio on September 12, 2012, but because of its long half-life, often cause gastrointestinal irritation (such as nausea, vomiting , diarrhea), increased levels of liver alanine aminotransferase, etc. According to research results, more than 60% of patients within one year stopped taking it due to intolerance

Method used

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  • A kind of teriflunomide microemulsion, preparation method and application
  • A kind of teriflunomide microemulsion, preparation method and application
  • A kind of teriflunomide microemulsion, preparation method and application

Examples

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Effect test

Embodiment 1

[0033] This example includes the following components:

[0034] Teriflunomide: 5 mg, isopropyl myristate: 2.106 g, soybean lecithin: 1.053 g, absolute ethanol: 1.053 g, deionized water: 0.783 g.

[0035] The preparation process is as follows:

[0036] Accurately weigh IPM, soybean lecithin, and absolute ethanol. Mix and dissolve soybean lecithin and absolute ethanol first, then add IPM and mix thoroughly. Add teriflunomide reference substance into deionized water, ultrasonically dissolve, and slowly drop teriflunomide aqueous solution into the above liquid under stirring with a magnetic stirrer, and stir for 30 minutes to obtain a transparent mass ratio of 0.1% teriflunomide milk samples. The particle size distribution of teriflunomide microemulsion is detected by dynamic light scattering method, such as figure 1 As shown, the microemulsion particle size ranges from 10 to 100nm, the particle size is uniform, and the appearance is clear, such as figure 2 (a) shown.

Embodiment 2

[0038] This example includes the following components:

[0039] Teriflunomide: 12.5mg, isopropyl myristate: 2.106g, soybean lecithin: 1.053g, absolute ethanol: 1.053g, deionized water: 0.783g.

[0040] The preparation process is as follows:

[0041]Accurately weigh IPM, soybean lecithin, and absolute ethanol. Mix and dissolve soybean lecithin and absolute ethanol first, then add IPM and mix thoroughly. Add the teriflunomide reference substance into deionized water, dissolve it ultrasonically, slowly drop the teriflunomide aqueous solution into the above liquid under stirring with a magnetic stirrer, and stir for 30 minutes to obtain a transparent 0.25% teriflunomide microemulsion sample . The particle size distribution of the teriflunomide microemulsion was detected by the dynamic light scattering method. The particle size range of the microemulsion was 10-100nm, the particle size was uniform, and the appearance was clear. The results were as follows: figure 2 (b) shown. ...

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Abstract

The invention discloses a teriflunomide microemulsion, a preparation method and application. The preparation method includes: well mixing an emulsifier and a co-emulsifier, then adding an oil phase; dissolving teriflunomide into deionized water to obtain a teriflunomide solution aqueous phase; in the process of stirring, dropwise adding a teriflunomide solution into a mixed oil phase to form a transparent drug-containing microemulsion, wherein a proportion of the oil phase, the aqueous phase, the emulsifier and the co-emulsifier is optimized according to a pseudo-ternary phase diagram. Percutaneous administration, the microemulsion can improve solubleness of slightly soluble drug, form high concentration gradient and promote drug absorption; a hydrophobic portion of the microemulsion interacts with cuticle to disturb lipid bilayer structure, a hydrophilic portion can hydrate the cuticle, combined action of the hydrophobic portion and the hydrophilic portion can enhance permeability ofthe drug on the cuticle, and permeation and absorption of the drug are facilitated. A new dosage form is provided for clinic application of teriflunomide.

Description

technical field [0001] The invention relates to a new dosage form of teriflunomide, in particular to a teriflunomide microemulsion, a preparation method and application. Background technique [0002] Rheumatoid arthritis (rheumatoid arthritis RA) is an autoimmune disease characterized by inflammation of joints and periarticular tissues. It is recurrent and causes bone erosion and joint dysfunction. It is one of the intractable diseases in the world. The pathogenic mechanism of RA has not been fully elucidated. However, there are a large number of tumor necrosis factor (TNF-a) and T cells in the synovial fluid tissue of patients, which are important factors that cause joint inflammation and damage. The goal of RA treatment is to prevent joint destruction and maintain joint function. Early standardized treatment can control the condition of most RA patients and even cure them. Condition-modifying anti-rheumatic drugs (disease-modifying anti-rheu-matic drugs DMARDs) slow down...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/277A61K47/14A61K47/24A61P19/02A61P29/00
CPCA61K9/1075A61K31/277A61K47/14A61K47/24
Inventor 金涌曹雅茹王东李永怀高惠芳施艳群
Owner ANHUI MEDICAL UNIV
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