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High-density dimethyl fumarate enteric-coated granules and preparation method thereof

A technology of dimethyl fumarate enteric and dimethyl fumarate, which is applied in the field of high-density dimethyl fumarate enteric-coated granules and the preparation thereof, can solve the problem of large size, large drug dosage specification, abnormal swallowing problems

Inactive Publication Date: 2015-04-08
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The dimethyl fumarate preparations prepared above have a common feature, that is, the dosage of the drug is large. If it is made into a final dosage form such as a capsule or tablet, it will inevitably lead to a large size that is difficult to swallow, especially for patients who have difficulty swallowing. , the elderly or children
The currently marketed product has a specification of 240mg and uses a size 0 capsule, which is so large that it cannot be swallowed normally, which will affect the patient's medication compliance

Method used

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  • High-density dimethyl fumarate enteric-coated granules and preparation method thereof
  • High-density dimethyl fumarate enteric-coated granules and preparation method thereof
  • High-density dimethyl fumarate enteric-coated granules and preparation method thereof

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specific Embodiment approach

[0039] 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.

[0040] 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.

[0041] In the present invention, mg means milligram, mL means milliliter, h means hour, and min means minute

Embodiment 1

[0042] Example 1 Preparation of enteric-coated granules

[0043] From the inside to the outside, it is the core, the middle coating layer, and the enteric coating layer. The composition of the prescription is as follows:

[0044]

[0045]

[0046] Preparation Process:

[0047] 1) Core preparation:

[0048] Pass dimethyl fumarate, microcrystalline cellulose PH102, silicified microcrystalline cellulose, calcium hydrogen phosphate, croscarmellose sodium and micropowder silica gel through the comill finishing machine (032R screen) in sequence, and put them in the mixing hopper Mix at 10 rpm for 10 minutes, add magnesium stearate and mix at 10 rpm for 5 minutes. Micro-tablets were pressed using a Feite tablet press, the die size of the tablet was 2 mm, and the hardness and friability were tested during the tableting process to meet the regulations.

[0049] 2) Intermediate coating layer preparation:

[0050] Dissolve Eudragit L100 in 50% of the prescribed amount of 95% et...

Embodiment 2

[0057] Example 2 Investigation of content uniformity

[0058] According to the "Chinese Pharmacopoeia 2010 Edition Appendix XE Content Uniformity Inspection Method", the content uniformity of the finished products prepared from prescriptions 1 to 3 was investigated, and the results are shown in the table below.

[0059] Table 1. Content Uniformity

[0060]

[0061] Among them, AVE represents the average value; A represents the absolute value of the difference between the marked amount and the mean value, where the marked amount is 100; S represents the standard deviation.

[0062] Discussion: The data in Table 1 show that the content uniformity of the prepared preparation meets the quality standard.

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Abstract

The invention discloses high-density dimethyl fumarate enteric-coated granules and a preparation method thereof. The density of the high-density dimethyl fumarate enteric-coated granules is 1.0g / mL or higher, or is 1.3g / mL or higher, or is 1.6g / mL or higher. Preparation size of the high-density dimethyl fumarate enteric-coated granules is small; the high-density dimethyl fumarate enteric-coated granules are convenient for administration, and are especially suitable for patients, elders, and children with swallowing difficulty, and are capable of increasing patient compliance; preparation content uniformity is high; rapid release is realized; stability is high; and the preparation method is simple, and is suitable for industrialized production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to high-density dimethyl fumarate enteric-coated granules and a preparation method thereof. Background technique [0002] Dimethyl fumarate, the following structure formula (I), is a kind of medicine for the treatment of multiple sclerosis (MS). BiogenIdec's dimethyl fumarate extended-release capsules, trade name Tecfidera, has been approved by the FDA for the treatment of multiple sclerosis (MS). [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. Prior art CN99812388.9 disclos...

Claims

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Application Information

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IPC IPC(8): A61K9/62A61K9/60A61K31/225A61P25/28A61P25/00
Inventor 齐宜广
Owner SUNSHINE LAKE PHARM CO LTD
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