A kind of dimethyl fumarate enteric-coated pellets 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 the preparation thereof, and can solve the problem of easy sublimation loss of dimethyl fumarate and inability to obtain dimethyl fumarate. The release advantage of multi-unit enteric-coated preparations can not reduce the irritation of the gastrointestinal tract, and achieve the effect of reducing the toxic and side effects of the gastrointestinal tract, reducing the risk of in vitro dose dumping, and completely releasing the drug

Active Publication Date: 2017-06-09
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 of the description, the micropill is just a common pill that adopts wet granulation and is poured into ordinary In hard capsules or hard capsules coated with enteric coating, the release advantages of multi-unit enteric-coated preparations further prepared from enteric-coated mini-tablets or pills cannot be obtained, so 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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  • A kind of dimethyl fumarate enteric-coated pellets and preparation method thereof
  • A kind of dimethyl fumarate enteric-coated pellets and preparation method thereof
  • A kind of dimethyl fumarate enteric-coated pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Composition of dimethyl fumarate enteric-coated pellets:

[0043] Ball core composition:

[0044] Raw material name 1000 dosage (g)

[0045] Dimethyl fumarate 120

[0046] Microcrystalline Cellulose 150

[0047] Sodium carboxymethyl starch 20

[0048] Hydroxypropyl Cellulose 13

[0049] 95% ethanol 103

[0050] Purified water 116

[0051] Composition of the inner enteric coating layer:

[0052] Raw material name dosage (g)

[0053] Udage L12.5 12.5

[0054] Triethyl citrate 1

[0055] Talc powder 3

[0056] 95% ethanol 170

[0057] Composition of the outer enteric coating layer:

[0058] Raw material name dosage (g)

[0059] Eudragit L30D-55 water dispersion 150

[0060] Triethyl citrate 5

[0061] Talc 12

[0062] Purified water 220

[0063] Note: The dry polymer content of Eudragit L30D-55 aqueous dispersion is 30%

[0064] Preparation Process:

[0065] (1) Accurately weigh dimethyl fumarate, microcrystalline cellulose, sodium carboxymethyl starch a...

Embodiment 2

[0075] Composition of dimethyl fumarate enteric-coated pellets:

[0076] Ball core composition:

[0077] Raw material name 1000 dosage (g)

[0078] Dimethyl fumarate 120

[0079] Microcrystalline Cellulose 100

[0080] Lactose 50

[0081] Croscarmellose Sodium 25

[0082] Hypromellose 14

[0083] 95% ethanol 103

[0084] Purified water 116

[0085] Composition of the inner enteric coating layer:

[0086] Raw material name dosage (g)

[0087] Udrake L100 15

[0088] Triethyl citrate 2

[0089] Talc 4

[0090] 95% ethanol 200

[0091] Composition of the outer enteric coating layer:

[0092] Raw material name dosage (g)

[0093] Cellulose acetate phthalate 50

[0094] Triethyl citrate 5

[0095] Talc powder 10

[0096] Purified water 220

[0097] Preparation Process:

[0098] (1) Accurately weigh dimethyl fumarate, microcrystalline cellulose, lactose, croscarmellose sodium and hydroxypropyl cellulose, and weigh 95% ethanol separately.

[0099] (2) Mix 95% etha...

Embodiment 3

[0108] Composition of dimethyl fumarate enteric-coated pellets:

[0109] Ball core composition:

[0110] Raw material name 1000 dosage (g)

[0111] Dimethyl fumarate 120

[0112] Microcrystalline Cellulose 150

[0113] Croscarmellose Sodium 20

[0114] Povidone K30 14

[0115] 95% ethanol 103

[0116] Purified water 116

[0117] Composition of the inner enteric coating layer:

[0118] Raw material name dosage (g)

[0119] Udrake L100 15

[0120] Triethyl citrate 5

[0121] Talc 5

[0122] 95% ethanol 200

[0123] Composition of the outer enteric coating layer:

[0124] Raw material name dosage (g)

[0125] Eudragit L30D-55 aqueous dispersion 170

[0126] Triethyl citrate 5

[0127] Talc 15

[0128]Purified water 220

[0129] Note: The dry polymer content of Eudragit L30D-55 aqueous dispersion is 30%

[0130] Preparation Process:

[0131] (1) Accurately weigh dimethyl fumarate, microcrystalline cellulose, croscarmellose sodium and hydroxypropyl cellulose, and...

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Abstract

The invention relates to a dimethyl fumarate enteric-coated pellet and a preparation method thereof. The dimethyl fumarate enteric-coated pellets contain a pellet core and double-layer enteric coatings coated on the pellet core. The enteric-coated pellets are prepared through the following methods, including: preparing pellet cores by extrusion spheronization; and performing double-layer enteric-coating on the pellet cores to obtain enteric-coated pellets. The dimethyl fumarate enteric-coated pellets obtained by the invention have a simple preparation process, complete drug release and good reproducibility, and reduce the risk of in vitro dose dumping.

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. [0002] technical background [0003] 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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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