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Enteric tablet containing dimethyl fumarate

A technology of dimethyl fumarate and tablet, which is applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, and pill delivery, etc. corruption, etc.

Pending Publication Date: 2021-11-12
CURACLE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the method of filling enteric-coated microtablets or pellets in a capsule matrix or preparing microtablets has disadvantages in that production costs are increased due to the need for additional processes and manufacturing equipment, and there are problems in that due to rich Sublimation properties of dimethyl maleate, loss of major components may occur during pellet manufacturing
In addition, since the capsule base contains animal (bovine cartilage)-derived components, there is a possibility of microbial spoilage, and there is a problem that it cannot be administered to a group of patients whose intake of animal-derived components is contraindicated due to religious concerns

Method used

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  • Enteric tablet containing dimethyl fumarate
  • Enteric tablet containing dimethyl fumarate
  • Enteric tablet containing dimethyl fumarate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0085] Example: Preparation of Enteric Coated Tablets

[0086] Table 1

[0087]

[0088]

[0089] Table 2

[0090]

[0091] Preparation of enteric-coated tablets containing dimethyl fumarate

[0092] Blends containing dimethyl fumarate have an angle of repose of 40° or less, and if the angle of repose is less than 40°, flowability is generally assessed to be good enough to allow direct compression. On the other hand, when the wet granulation method is applied to improve fluidity, there is a problem of loss due to sublimation of dimethyl fumarate due to use of a solvent and drying. Therefore, an enteric-coated tablet including dimethyl fumarate was prepared as follows by minimizing contact with water and applying a direct compression method with a simple manufacturing process.

[0093] According to the composition of Tables 1 and 2, enteric-coated tablets according to Examples 1 to 12 were prepared by the following steps:

[0094] Dimethyl fumarate and pharmaceut...

experiment example 1

[0106] Measurement of Coating Layer Thickness

[0107]In order to measure the thickness of the enteric coating layer of the enteric coating tablet according to Example 11, Example 12 and Comparative Example 4, using ESEM (Thermo Fisher, Quattro S) under scanning electron microscope (SEM) The coating layers of the primary coating layer (seal coating), the tablets of Example 11, Example 12 and Comparative Example 4 were observed. At this time, based on the total weight of the tablet core, the weight of the enteric coating layer (secondary coating layer) of the tablet in Example 11 was 6%, in Example 12 it was 8%, in Comparative Example 4 it was 12%. For SEM observation, the coating layers of the tablets of the primary coating layer (seal coating), Example 11, Example 12, and Comparative Example 4 were pretreated by depositing Os as thin as 10 nm or less using an Os coater . The results are shown in Table 5 and figure 1 shown.

[0108] table 5

[0109]

[0110] In the r...

experiment example 2

[0111] Evaluate the elution rate according to the ratio of enteric coating

[0112] 2-1 According to the enteric coating ratio, the elution rate of the tablet at pH 6.8

[0113] In order to evaluate the elution rate of the tablets according to the enteric coating ratio, the elution rate of the enteric-coated tablets according to Examples 1 to 3 in a pH 6.8 solution was evaluated. The tablets of Examples 1-3 contained 10.8 mg / tablet, 16.2 mg / tablet and 21.6 mg / tablet of Acryl-EZE MP 93O18508 (methacrylic acid and ethyl acrylate copolymer 60% w / w) as an enteric coating clothing matrix.

[0114] To evaluate the elution rate, a pH 6.8 buffer solution (Mcilvane buffer) was prepared, and each eluate was subjected to a dissolution test according to the second method (paddle method). Specifically, the buffer solution was kept at 900ml, the stirring speed was kept at 75rpm, and the temperature of the buffer solution was kept at 37±0.5°C. After the start of the dissolution test duri...

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Abstract

The present invention relates to an enteric coating tablet comprising a core containing, as an active ingredient, dimethyl fumarate or a pharmaceutically acceptable salt thereof; and an enteric coating layer. The present invention also provides a tablet which exhibits an effect equal to that of a capsule dosage form currently on the market, can be prepared through a simple preparation process, and is a dosage form having excellent storage stability and administration convenience, and thus can be applied to various patient groups.

Description

technical field [0001] The invention relates to a pharmaceutical preparation containing dimethyl fumarate. In particular, the present invention relates to an enteric-coated tablet comprising dimethyl fumarate and an enteric coating layer, and the tablet of the present invention allows dimethyl fumarate to be stably delivered to the absorption site and quickly dissipated, This makes it possible to obtain the desired therapeutic effect in vivo. The tablet of the present invention exhibits the same effect as the capsule dosage forms currently on the market, has advantages in terms of productivity and economy due to the simpler preparation method than the capsule dosage forms currently on the market, and has a smaller size than capsules, This can improve patient medication compliance. In particular, the tablet of the present invention does not contain ingredients of animal origin, so it can be used in a group of patients whose capsules are contraindicated due to religious concer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/32A61K9/34A61K31/225A61P43/00A61P25/28A61P17/06A61P19/02A61P3/10A61P37/02A61P7/06A61P1/16A61P27/02A61P25/00
CPCA61K31/225A61K9/2866A61K9/284A61K9/2846A61K9/2886A61K9/2853A61P43/00A61P25/28A61P17/06A61P19/02A61P3/10A61P37/02A61P7/06A61P1/16A61P27/02A61P25/00Y02A50/30A61K9/2013A61K9/2054A61K9/2027A61K9/2009A61K47/14
Inventor 金明华表定忍毛钟贤李哲宇池贤具
Owner CURACLE CO LTD
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