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Apremilast solid dispersoid and preparation method thereof

A solid dispersion and preparation technology, applied in the field of Apremilast solid dispersion and its preparation, can solve the problems of dissolution, bioavailability limitation, and no Apremilast solid dispersion, etc., to accelerate the drug release rate , The effect of improving drug bioavailability and simple steps

Active Publication Date: 2015-04-22
CHANGSHA BAISHUN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no related reports and patents on Apremilast solid dispersion in China.
[0004] Apremilast is a poorly soluble drug, its dissolution and bioavailability are limited by this

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Prescription (percent by weight):

[0021] Apremilast 30%

[0022] Poloxamer 25%

[0023] Polyethylene glycol 6000 30%

[0024] Colloidal Silica 15%

[0025] Preparation:

[0026] 1) Grind apremilast, poloxamer, polyethylene glycol 6000, colloidal silicon dioxide and pass through 80-100 mesh sieve respectively;

[0027] 2) Weigh the prescribed amount of poloxamer, polyethylene glycol 6000, and colloidal silicon dioxide and heat to melt. 3) Add the prescribed amount of Apremilast to 2), stir to fully disperse evenly, the mixing speed is 450r / min, the stirring time is 4min, the mixing temperature is 80°C, and then cooled rapidly, the cooling temperature is -5°C, the cooling time for 30min. After it is completely solidified, take it out and put it in a vacuum drying oven, crush it after embrittlement, and pass it through a 150-mesh sieve.

Embodiment 2

[0029] Prescription (percent by weight):

[0030] Apremilast 30%

[0031] Poloxamer 28%

[0032] Polyvinylpyrrolidone K30 27%

[0033] Colloidal Silica 15%

[0034] Preparation:

[0035] 1) Grind apremilast, poloxamer, polyvinylpyrrolidone K30, colloidal silicon dioxide and pass through 80-100 mesh sieve respectively;

[0036] 2) Weigh the prescribed amount of poloxamer, polyvinylpyrrolidone K30, and colloidal silicon dioxide and heat to melt.

[0037] 3) Add the prescribed amount of Apremilast to 2), stir to fully disperse evenly, the mixing speed is 500r / min, the stirring time is 7min, the mixing temperature is 85°C, and then cooled rapidly, the cooling temperature is -8°C, the cooling time for 35min. After it is completely solidified, take it out and put it in a vacuum drying oven, crush it after embrittlement, and pass it through a 150-mesh sieve.

Embodiment 3

[0039] Prescription (percent by weight):

[0040] Apremilast 30%

[0041] Poloxamer 25%

[0042] Polyethylene glycol 6000 30%

[0043] Colloidal Silica 15%

[0044] Preparation:

[0045] 1) Grind apremilast, poloxamer, polyethylene glycol 6000, colloidal silicon dioxide and pass through 80-100 mesh sieve respectively;

[0046] 2) Weigh the prescribed amount of poloxamer, polyethylene glycol 6000, and colloidal silicon dioxide and heat to melt. 3) Add the prescribed amount of Apremilast to 2), stir to fully disperse, the mixing speed is 300r / min, the stirring time is 5min, the mixing temperature is 90°C, and then cooled rapidly, the cooling temperature is 0°C, and the cooling time is 30min. After it is completely solidified, take it out and put it in a vacuum drying oven, crush it after embrittlement, and pass it through a 150-mesh sieve.

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PUM

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Abstract

The invention provides an apremilast solid dispersoid and a preparation method thereof. The apremilast solid dispersoid is characterized by having a prescription comprising the following components in percentage by weight: 5-35% of apremilast, 5-70% of a carrier material and 2-30% of an adsorbing agent. The apremilast solid dispersoid has the advantages that drug releasing rate is increased, pharmaceutical function can be realized in short time, and pharmaceutical bioavailability is improved. The apremilast solid dispersoid is prepared by adopting a melting method, steps are simple, technological parameters are easy to control, and the apremilast solid dispersoid is applicable to large-scale production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a solid dispersion of apremilast and a preparation method thereof. Background technique [0002] Psoriatic arthritis (PsA) is an inflammatory joint disease associated with psoriasis, with a psoriatic rash accompanied by pain, swelling, tenderness, stiffness, and dyskinesia in the joints and surrounding soft tissues. Some patients may have sacroiliitis and (or) spondylitis, the course of the disease is protracted and easy to relapse. In the late stage, there may be joint stiffness. About 75% of patients had rash before arthritis, about 15% had rash at the same time, and about 10% had rash after arthritis. The disease can occur at any age, and the peak age is 30 to 50 years old. There is no gender difference, but the spine is more involved in men. The disease often has a tendency of family aggregation, the prevalence rate of first-degree family members is as high as ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4035A61K47/34A61K47/38A61K47/04A61P19/02A61P17/06
Inventor 不公告发明人
Owner CHANGSHA BAISHUN BIOTECH
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