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DMF (dimethyl fumarate) enteric-coated micropellet and preparation method thereof

A technology of dimethyl fumarate enteric and dimethyl fumarate, which is applied in the field of dimethyl fumarate enteric-coated pellets and its preparation, can solve the problem of not being able to obtain the release advantages of multi-unit enteric-coated preparations To reduce gastrointestinal irritation, easy sublimation loss of dimethyl fumarate and other problems, to achieve the effect of reducing gastrointestinal side effects, complete drug release, and controllable quality

Active Publication Date: 2015-02-18
SHANDONG BESTCOMM PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, CN1182844A (Notice No. CN1182844C), US6509376, etc. also provide a micropill of dimethyl fumarate, but from the examples in the description, the micropill is just a common pill that adopts wet granulation and is poured into a common pellet. In hard capsules or enteric-coated hard capsules, the release advantages of multi-unit enteric-coated preparations further prepared from enteric-coated mini-tablets or pills cannot be obtained, and the effect of reducing gastrointestinal irritation cannot be achieved at all. effect
And in the process of granulation and drying, dimethyl fumarate is easily lost by sublimation

Method used

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  • DMF (dimethyl fumarate) enteric-coated micropellet and preparation method thereof
  • DMF (dimethyl fumarate) enteric-coated micropellet and preparation method thereof
  • DMF (dimethyl fumarate) enteric-coated micropellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Composition of dimethyl fumarate enteric-coated pellets:

[0042] Ball core composition:

[0043] Raw material name 1000 dosage (g)

[0044] Dimethyl fumarate 120

[0045] Microcrystalline Cellulose 150

[0046] Sodium carboxymethyl starch 20

[0047] Hydroxypropyl Cellulose 13

[0048] 95% ethanol 103

[0049] Purified water 116

[0050] Composition of the inner enteric coating layer:

[0051] Raw material name dosage (g)

[0052] Udage L12.5 12.5

[0053] Triethyl citrate 1

[0054] Talc powder 3

[0055] 95% ethanol 170

[0056] Composition of the outer enteric coating layer:

[0057] Raw material name dosage (g)

[0058] Eudragit L30D-55 water dispersion 150

[0059] Triethyl citrate 5

[0060] Talc 12

[0061] Purified water...

Embodiment 2

[0074] Composition of dimethyl fumarate enteric-coated pellets:

[0075] Ball core composition:

[0076] Raw material name 1000 dosage (g)

[0077] Dimethyl fumarate 120

[0078] Microcrystalline Cellulose 100

[0079] Lactose 50

[0080] Croscarmellose Sodium 25

[0081] Hypromellose 14

[0082] 95% ethanol 103

[0083] Purified water 116

[0084] Composition of the inner enteric coating layer:

[0085] Raw material name dosage (g)

[0086] Udrake L100 15

[0087] Triethyl citrate 2

[0088] Talc 4

[0089] 95% ethanol 200

[0090] Composition of the outer enteric coating layer:

[0091] Raw material name dosage (g)

[0092] Cellulose acetate phthalate 50

[0093] Triethyl citrate 5

[0094] Talc powder 10

[0095] Pu...

Embodiment 3

[0107] Composition of dimethyl fumarate enteric-coated pellets:

[0108] Ball core composition:

[0109] Raw material name 1000 dosage (g)

[0110] Dimethyl fumarate 120

[0111] Microcrystalline Cellulose 150

[0112] Croscarmellose Sodium 20

[0113] Povidone K30 14

[0114] 95% ethanol 103

[0115] Purified water 116

[0116] Composition of the inner enteric coating layer:

[0117] Raw material name dosage (g)

[0118] Udrake L100 15

[0119] Triethyl citrate 5

[0120] Talc 5

[0121] 95% ethanol 200

[0122] Composition of the outer enteric coating layer:

[0123] Raw material name dosage (g)

[0124] Eudragit L30D-55 aqueous dispersion 170

[0125] Triethyl citrate 5

[0126] Talc 15

[0127] Purified water 220 ...

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Abstract

The invention relates to a DMF (dimethyl fumarate) enteric-coated micropellet and a preparation method thereof. The DMF enteric-coated micropellet comprises a pellet core and a double-layer enteric coating, wherein the pellet core is coated with the double-layer enteric coating. The enteric-coated micropellet is prepared by the following steps: the pellet core is prepared with the extrusion-spheronization method; and the pill-containing pellet core is coated with the double-layer enteric coating to form the enteric-coated micropellet. The obtained DMF enteric-coated micropellet is simple in preparation technology, complete in drug release and good in reproducibility, and external dose dumping risk is reduced.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to dimethyl fumarate enteric-coated pellets and a preparation method thereof. technical background [0002] Pellets generally refer to spherical or spherical preparations with a diameter between 0.3mm and 2.5mm. As a multi-unit drug delivery system, micropills have the following advantages compared with traditional single drug delivery systems: (1) The absorption of micropellets with a diameter of less than 2.5 mm in the gastrointestinal tract is basically not affected by gastric emptying, Therefore, individual differences are small. (2) After taking the pellets, they are widely distributed in the gastrointestinal tract. Due to the dispersion of the dose, the distribution area of ​​the drug on the surface of the gastrointestinal tract increases, which can reduce the irritation to the gastrointestinal tract. (3) The drug release behavior of the micropills is the sum of the ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/225A61K47/38A61K47/32A61P17/06A61P37/02
Inventor 冯丽杰杨娟华曹亮赵广强
Owner SHANDONG BESTCOMM PHARMA CO LTD
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