Dimethyl fumarate enteric-coated pellet and preparation method thereof

A technology for enteric and enteric-coated pellets of dimethyl fumarate, which can be applied to pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., and can solve the problem of slow drug release and unfavorable drug activity. , influence and other issues, to achieve the effect of stable quality

Active Publication Date: 2015-04-22
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the general enteric coating is an acidic material, which adversely affects the activity of the drug. At present, the way to solve this problem is to increase the intermediate coating layer. However, after adding the intermediate coating layer, although the stability of the drug is increased, it is often Slow drug release, affecting drug absorption

Method used

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  • Dimethyl fumarate enteric-coated pellet and preparation method thereof
  • Dimethyl fumarate enteric-coated pellet and preparation method thereof
  • Dimethyl fumarate enteric-coated pellet and preparation method thereof

Examples

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specific Embodiment approach

[0036] In order to enable those skilled in the art to better understand the technical solutions of the present invention, some non-limiting examples are further disclosed below to further describe the present invention in detail.

[0037] The reagents used in the present invention can be purchased from the market or can be prepared by the methods described in the present invention.

[0038] In the present invention, mg means milligram, mL means milliliter, h means hour, and min means minute.

Embodiment 1

[0039] Embodiment 1 preparation of enteric-coated pellets

[0040]

[0041] Preparation Process:

[0042] 1) Core preparation:

[0043] Pass dimethyl fumarate, lactose monohydrate Flowtac100, silicified microcrystalline cellulose, croscarmellose sodium and micropowder silica gel through the comill finishing machine (032R screen) in sequence, and mix in the mixing hopper at a speed of 10rpm for 10min , adding magnesium stearate and mixing at a speed of 10 rpm for 5 minutes. Micro-tablets were compressed using a Feite tablet press, the die size of the tablet was 3mm, and the hardness and friability were tested during the tableting process to meet the regulations.

[0044] 2) Preparation of intermediate coating layer

[0045]Dissolve the prescribed amount of copovidone S630 in isopropanol, stir until clear and transparent, add the prescribed amount of talc powder into the copovidone solution under stirring, homogenize with a high-speed shear emulsifier for about 10 minutes,...

Embodiment 2

[0052] Embodiment 2 preparation of enteric-coated pellets

[0053]

[0054]

[0055] The preparation process is the same as in Example 1.

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Abstract

The invention provides a dimethyl fumarate enteric-coated pellet. The dimethyl fumarate enteric-coated pellet comprises a core, an intermediate coating layer and an enteric layer, wherein the coating material of the intermediate coating layer is copovidone; by calculating in percentage by weight with respect to the core, the increased weight of the intermediate coating layer is 4%-40%; the enteric-coated pellet can be further filled with a capsule so as to be prepared into a capsule, or mixed with other auxiliary materials so as to be prepared into a tablet, or mixed with other auxiliary materials so as to be prepared into a suspension. Even the weight of the intermediate coating layer is increased, the medicine in the prepared enteric-coated pellet still can retain a high release rate. The preparation method is simple and feasible, and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a dimethyl fumarate enteric-coated pellet and a preparation method thereof. Background technique [0002] Dimethyl fumarate is a kind of medicine for treating multiple sclerosis (MS), and its structure is as follows formula (I), [0003] [0004] Multiple sclerosis is a disease of the central nervous system. The typical development process is chronic or intermittent. The impact on the body can range from minor physical inconvenience to major loss of major functions. Dimethyl fumarate works by activating the nuclear factor-2-like pathway, which enables cells in the body to defend against the damage of inflammation and oxidative stress that accompany diseases such as MS. Currently on the market are BiogenIdec's dimethyl fumarate sustained-release capsules, trade name Tecfidera. [0005] Exposure of dimethyl fumarate to acidic substances will lead to hydrolysis, and c...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/32A61K31/225A61P25/28A61P25/00
Inventor 齐宜广
Owner SUNSHINE LAKE PHARM CO LTD
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