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Teriflunomide dispersible tablet and preparation method thereof

A technology of teriflunomide dispersible tablets and teriflunomide, which is applied in pharmaceutical formulations, nitrile/isonitrile active ingredients, pill delivery, etc., can solve problems such as affecting drug absorption, difficult treatment for patients, and slow disintegration speed. To achieve the effects of good drug safety, good human absorption and fast disintegration speed

Inactive Publication Date: 2017-06-23
PEKING UNIV FOUNDER GRP CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The most important problem that teriflunomide exists is that because it itself is slightly soluble in water, after being made into tablets, the dissolution rate is low
Ordinary tablets have the disadvantage of slow disintegration speed, which affects the absorption of drugs; in addition, ordinary tablets have a large volume, or often need to use multiple tablets (grains) at a time, and need to be washed with water, which is inconvenient to take, especially for the elderly. , young and patients with swallowing dysfunction have certain difficulties in treatment

Method used

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  • Teriflunomide dispersible tablet and preparation method thereof
  • Teriflunomide dispersible tablet and preparation method thereof
  • Teriflunomide dispersible tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Prescription (Specification: 7mg)

[0032]

[0033] Preparation:

[0034] (1) Treatment of raw and auxiliary materials: the Dv90 of the active ingredient teriflunomide and mannitol co-micronized powder is 21.5 μm, and the remaining auxiliary materials are passed through an 80-mesh sieve for later use;

[0035] (2) making soft material: after taking the co-micronized product of recipe quantity, microcrystalline cellulose, 2% carboxymethyl starch sodium and mixing evenly, make soft material with water;

[0036] (3) Granulation: get above-mentioned soft material and granulate with 18 mesh screens;

[0037] (4) Drying: dry the wet granules, control the temperature of the material at 50±5°C, and make the moisture of the granules reach about 2%;

[0038] (5) Grain sizing: the dried granules are sieved with a 24-mesh sieve;

[0039] (6) Total blending: the granulated granules are added to the converted magnesium stearate and 1% sodium carboxymethyl starch and mixed evenl...

Embodiment 2

[0042] Prescription (Specification: 7mg)

[0043]

[0044] Preparation:

[0045] (1) Treatment of raw and auxiliary materials: the Dv90 of the active ingredient teriflunomide and mannitol co-micronized powder is 20.9 μm, and the rest of the auxiliary materials are passed through an 80-mesh sieve for later use;

[0046] (2) making soft material: after taking the co-micronized product of recipe quantity, microcrystalline cellulose, 2% carboxymethyl starch sodium and mixing evenly, make soft material with water;

[0047] (3) Granulation: get above-mentioned soft material and granulate with 18 mesh screens;

[0048] (4) Drying: dry the wet granules, control the temperature of the material at 50±5°C, and make the moisture of the granules reach about 2%;

[0049] (5) Grain sizing: the dried granules are sieved with a 24-mesh sieve;

[0050] (6) Total blending: the granulated granules are added to the converted magnesium stearate and 1% sodium carboxymethyl starch and mixed eve...

Embodiment 3

[0053] Prescription (Specification: 14mg)

[0054]

[0055] Preparation:

[0056] (1) Treatment of raw and auxiliary materials: the Dv90 of the active ingredient teriflunomide and lactose co-micronized powder is 19.1 μm, and the remaining auxiliary materials are passed through an 80-mesh sieve for later use;

[0057] (2) making soft material: after taking the co-micronized product of recipe quantity, microcrystalline cellulose, 2.86% carboxymethyl starch sodium and mixing evenly, make soft material with water;

[0058] (3) Granulation: get above-mentioned soft material and granulate with 18 mesh screens;

[0059] (4) Drying: dry the wet granules, control the temperature of the material at 50±5°C, and make the moisture of the granules reach about 2%;

[0060] (5) Grain sizing: the dried granules are sieved with a 24-mesh sieve;

[0061] (6) Total blending: the granules after the granulation are added into the converted magnesium stearate and 1.43% sodium carboxymethyl sta...

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Abstract

The invention provides a teriflunomide dispersible tablet and a preparation method thereof. The dispersible tablet consists of teriflunomide, which serves as an active ingredient, and a filler, a disintegrating agent and a lubricating agent which are used as pharmaceutical adjuvants. The teriflunomide dispersible tablet prepared by the invention can be completely disintegrated rapidly, so that a time to peak is shortened; a dissolution rate can reach 90% or above; the dispersible tablet is convenient to take, rapid in efficacy release and high in bioavailability; and the preparation method is simple in process, easy for control, convenient to operate and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a teriflunomide dispersible tablet and a preparation method thereof. Background technique [0002] Teriflunomide, the chemical name is (2Z)-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide. Its molecular formula is C 12 h 9 f 3 N 2 o 2 , the molecular weight is 270.21, and its compound structural formula is as follows: [0003] [0004] The drug developed and produced by Sanofi-Aventis for the treatment of relapsing multiple sclerosis in phase II and III clinical studies was approved by the US FDA on September 12, 2012. [0005] Teriflunomide is an oral pyrimidine synthase inhibitor and immunomodulator that reverses inhibition of dihydroorotate dehydrogenase (DHODH), a key enzyme involved in de novo pyrimidine synthesis. DHODH is an iron-containing flavin-dependent mitochondrial enzyme, which is the key enzyme for pyrimidine synthesis in nucleic acids, and...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/277A61P25/00A61P37/06A61P35/00
CPCA61K31/277A61K9/0056A61K9/2018A61K9/2059
Inventor 易崇勤王海超冀蕾
Owner PEKING UNIV FOUNDER GRP CO LTD
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