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Apremilast oral preparation and preparation method thereof

A technology of oral preparations and fillers, which is applied in the field of pharmaceutical preparations and can solve problems such as dissolution and bioavailability limitations

Inactive Publication Date: 2016-02-24
CHANGSHA BAISHUN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Apremilast is a poorly soluble drug, and its dissolution and bioavailability are limited by this

Method used

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  • Apremilast oral preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Plain Tablet Prescription:

[0020] Aprester 8g

[0021] Lactose 35g

[0022] Microcrystalline cellulose 28g

[0023] Crospovidone 14g

[0024] Sodium carboxymethyl starch 10g

[0025] Hypromellose 3g

[0026] Micropowder silica gel 2g

[0027] Coating Solution Prescription:

[0028] Opadry 85F421297g

[0029] 75% ethanol 93g

[0030] Preparation:

[0031] ①Mix the prescription amount of Apremilast with lactose and microcrystalline cellulose evenly, pass through a 200-mesh sieve for use; crospovidone and sodium carboxymethyl starch are respectively passed through a 80-mesh sieve for use;

[0032] ② mix the above-mentioned mixture of Apremilast, lactose and microcrystalline cellulose with crospovidone and sodium carboxymethyl starch;

[0033] ③ Add hydroxypropyl cellulose to ② and mix evenly to make a soft material; the soft material is granulated with a 24-mesh screen;

[0034] ④Dry the above wet granules, and control the temperature of the material at 50~55°...

Embodiment 2

[0038] Plain Tablet Prescription:

[0039] Aprester 4g

[0040] Lactose 37g

[0041] Microcrystalline cellulose 30g

[0042] Crospovidone 10g

[0043] Sodium carboxymethyl starch 14g

[0044] Hypromellose 3g

[0045] Micropowder silica gel 2g

[0046] Coating Solution Prescription:

[0047] Opadry 85F421297g

[0048] 75% ethanol 93g

[0049] Preparation:

[0050] ①Mix the prescription amount of Apremilast with lactose and microcrystalline cellulose evenly, pass through a 200-mesh sieve for use; crospovidone and sodium carboxymethyl starch are respectively passed through a 80-mesh sieve for use;

[0051] ② mix the above-mentioned mixture of Apremilast, lactose and microcrystalline cellulose with crospovidone and sodium carboxymethyl starch;

[0052] ③ Add hydroxypropyl cellulose to ② and mix evenly to make a soft material; the soft material is granulated with a 24-mesh screen;

[0053] ④Dry the above wet granules, and control the temperature of the material at 50~55°...

Embodiment 3

[0057] Plain Tablet Prescription:

[0058] Apremilast 12g

[0059] Lactose 26g

[0060] Microcrystalline cellulose 33g

[0061] Crospovidone 8g

[0062] Sodium carboxymethyl starch 16g

[0063] Hypromellose 3g

[0064] Micropowder silica gel 2g

[0065] Coating Solution Prescription:

[0066] Opadry 85F421297g

[0067] 75% ethanol 93.g

[0068] Preparation:

[0069] ①Mix the prescription amount of Apremilast with lactose and microcrystalline cellulose evenly, pass through a 200-mesh sieve for use; crospovidone and sodium carboxymethyl starch are respectively passed through a 80-mesh sieve for use;

[0070] ② mix the above-mentioned mixture of Apremilast, lactose and microcrystalline cellulose with crospovidone and sodium carboxymethyl starch;

[0071] ③ Add hydroxypropyl cellulose to ② and mix evenly to make a soft material; the soft material is granulated with a 24-mesh screen;

[0072] ④Dry the above wet granules, and control the temperature of the material at 50~55...

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Abstract

The invention provides an apremilast oral preparation and a preparation method thereof. The apremilast oral preparation consists of the following ingredients in percentage by weight: 2-20% of apremilast which serves as an active ingredient, 20-70% of a filling agent, 3-30% of a disintegrating agent, 1-10% of a binding agent, 0.2-5% of a lubricating agent and 2-6% of a coating material. The apremilast oral preparation prepared by the invention is above 95% in dissolution rate and high in bioavailability; the shortcomings of poor dissolution degree of the active ingredient and low bioavailability are overcome; and the oral preparation is stable and reliable in quality and is high in market development prospect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to an oral preparation of apremilast and a preparation method thereof. The invention also provides an oral preparation of apremilast with good quality, safety and stability. 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. [0003] Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/4035A61K47/38A61P17/06A61P19/02
CPCA61K9/2866A61K31/4035
Inventor 卢洪成其他发明人请求不公开姓名
Owner CHANGSHA BAISHUN BIOTECH
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