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Solid dispersion of amorphous apremilast and preparation method of solid dispersion

A solid dispersion and amorphous technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve problems such as difficulties in the development of pharmaceutical formulations and restrictions on the total amount of excipients, and achieve Fast dispersion and dissolution speed, increased dissolution rate, easy to achieve effect

Inactive Publication Date: 2017-05-31
CHANGZHOU AINUOXINRUI PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pharmaceutical preparations must use a variety of pharmaceutical excipients, and the total amount of excipients is also limited. For example, when a single excipient is used in a large amount, it will also bring certain difficulties to the development of pharmaceutical formulations.

Method used

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  • Solid dispersion of amorphous apremilast and preparation method of solid dispersion
  • Solid dispersion of amorphous apremilast and preparation method of solid dispersion
  • Solid dispersion of amorphous apremilast and preparation method of solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Apremilast (50 mg), hydroxypropylcellulose SSL (50 mg) and povidone K30 (50 mg) were added to methanol (800 microliters), heated to 60 ° C and stirred to dissolve, and evaporated in vacuo Solvent to obtain a white solid, that is, a solid dispersion of amorphous apremilast, hydroxypropyl cellulose SSL and povidone K30. The X-ray powder diffraction pattern of this solid dispersion is as follows figure 1 As shown, there is no characteristic peak of the apremilast crystal form in the X-ray powder diffraction pattern after deducting the background peak of the pharmaceutical excipient.

Embodiment 2

[0052] Apremilast (50 mg), polyacrylic acid resin Eudragit L100 (50 mg), and polyethylene glycol 4000 (200 mg) were dissolved in ethanol (600 μl) and water (600 μl) at -40 °C Stir and mix evenly under low pressure, remove the solvent by vacuum evaporation, and obtain a white solid, that is, a solid dispersion of amorphous apremilast, polyacrylic resin Eudragit L100 and polyethylene glycol 4000. In the X-ray powder diffraction pattern of the solid dispersion, there is no characteristic peak of the apremilast crystal form after deducting the background peaks of the pharmaceutical excipients.

Embodiment 3

[0054] Add Apremilast (2g), lactose (2g) and polyethylene glycol 8000 (10g) into water (300ml), heat to 60°C and stir to dissolve. Dry the above solution with JISL micro spray dryer LSD-48, maintain the inlet temperature at 60°C and the outlet temperature at 50°C, collect the outlet material to obtain a white solid, and further vacuum dry to obtain amorphous apremilast, lactose and polyethylene glycol 8000 solid dispersion. In the X-ray powder diffraction pattern of the solid dispersion, there is no characteristic peak of the apremilast crystal form after deducting the background peaks of the pharmaceutical excipients.

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Abstract

The invention provides a solid dispersion of amorphous apremilast and a preparation method of the solid dispersion. The solid dispersion contains apremilast and two or more pharmaceutical adjuvants, wherein the weight ratio of apremilast to all the pharmaceutical adjuvants is 1: (0.1-100), apremilast in the solid dispersion is in the amorphous state, and in the X-ray powder diffraction spectrum of the solid dispersion, besides the background peak of the pharmaceutical adjuvants, the characteristic peak of the apremilast crystal does not exist. The solid dispersion of apremilast is good in stability and dispersibility, the dissolution rate of apremilast is increased, the bioavailability of the medicinal preparation and the absorption of the medicine in the body are favorably improved, and under the condition of the acceleration test, the good physical stability and chemical stability can be maintained. The preparation method of the amorphous solid dispersion is easy to operate, low in cost, good in reproducibility, easy to realize, and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid dispersion of amorphous apremilast and a preparation method thereof. The present invention also relates to a pharmaceutical composition, which comprises apremilast in amorphous form and two or more pharmaceutically acceptable adjuvants for the treatment of active psoriatic arthritis and moderate to severe plaque psoriasis. Background technique [0002] Apremilast, chemical name N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-2 ,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]acetamide, trade name OTEZLA. Apremilast is a small molecule phosphodiesterase 4 (PDE4) inhibitor developed by Celgene, which was approved for marketing by the US Food and Drug Administration (FDA) on March 21, 2014. For the treatment of adult patients with active psoriatic arthritis. The drug is the first and only PDE4 inhibitor approved by the FDA for the treatment of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/19A61K9/14A61K31/4035A61K47/10A61K47/38A61K47/22A61K47/32A61K47/36A61P19/02A61P17/06
CPCA61K9/145A61K9/146A61K9/1617A61K9/1635A61K9/1641A61K9/1652A61K9/19A61K31/4035
Inventor 张席妮熊志刚资春鹏张三丰
Owner CHANGZHOU AINUOXINRUI PHARMA LTD
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