Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Apremilast solid composition and preparation method thereof

A solid composition and coating material technology, which is applied in drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of low bioavailability, dissolution, limited bioavailability, poor solubility of active ingredients, etc., and achieve bioavailability High, extensive clinical application prospects, and stable quality effects

Inactive Publication Date: 2019-06-25
ZHEJIANG WAN SHENG PHARMA CO LTD
View PDF2 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, apremilast is a poorly soluble drug, and its dissolution and bioavailability are limited
Therefore, it is necessary to develop a drug composition of apremilast with high dissolution rate and stable quality to solve the defects of poor solubility and low bioavailability of its active ingredients.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Apremilast solid composition and preparation method thereof
  • Apremilast solid composition and preparation method thereof
  • Apremilast solid composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Plain Tablet Prescription:

[0024]

[0025] Coating Solution Prescription:

[0026] 3g

[0027] water 32g

[0028] Preparation:

[0029] ① Grind the prescribed amount of Apremilast and pass through a 250-mesh sieve; respectively pass through a 80-mesh sieve for lactose, microcrystalline cellulose, croscarmellose sodium, and micropowder silica gel;

[0030] ②Mix the above-mentioned Apremilast with lactose, microcrystalline cellulose, croscarmellose sodium, and micropowder silica gel for 20 minutes;

[0031] ③Transfer the uniformly mixed medicinal powder to a powder feeder and press into tablets;

[0032] ④The prescription amount It is dissolved in water and made into a solution of about 9% as a film coating solution to coat the drug-containing tablet core. During the coating process, the temperature of the material is controlled at 40°C to 42°C. After the process is completed, the weight of the tablet core increases by about 3%.

Embodiment 2

[0034] Plain Tablet Prescription:

[0035]

[0036] Coating Solution Prescription:

[0037] 3g

[0038] water 32g

[0039] Preparation:

[0040] ①Crush the prescription amount of Apremilast and pass through a 250-mesh sieve; lactose, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate are respectively passed through a 80-mesh sieve for later use;

[0041] ②Mix the above-mentioned Apremilast with lactose, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate for 10 minutes;

[0042] ③Transfer the uniformly mixed medicinal powder to a powder feeder and press into tablets;

[0043] ④The prescription amount It is dissolved in water and made into a solution of about 9% as a film coating solution to coat the drug-containing tablet core. During the coating process, the temperature of the material is controlled at 40°C to 42°C. After the process is completed, the weight of the tablet core increases by about 3%.

Embodiment 3

[0045] Plain Tablet Prescription:

[0046]

[0047] Coating Solution Prescription:

[0048] 3g

[0049] water 32g

[0050] Preparation:

[0051] ①Crush the prescription amount of Apremilast and pass through a 250-mesh sieve; lactose, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate are respectively passed through a 80-mesh sieve for later use;

[0052] ④ Mix the above-mentioned Apremilast with lactose, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate for 30 minutes;

[0053] ③Transfer the uniformly mixed medicinal powder to a powder feeder and press into tablets;

[0054] ④The prescription amount It is dissolved in water and made into a solution of about 9% as a film coating solution to coat the drug-containing tablet core. During the coating process, the temperature of the material is controlled at 40°C to 42°C. After the process is completed, the weight of the tablet core increases by about 3%.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention provides an apremilast solid composition. The apremilast solid composition is prepared by the following components in parts by weight: 5% to 14% of apremilast; 82% to 90% of a filler; 1%to 1.5% of a disintegrant; 0.5% to 1% of a lubricant; and 2% to 6% of a coating material. The apremila solid composition prepared by the invention has a dissolution rate of more than 95%, has high bioavailability, and stable and reliable quality, and has wide clinical application prospects.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a solid composition of apremilast with high dissolution rate and stable quality and a preparation method thereof. Background technique [0002] Psoriatic arthritis (PsA) is an inflammatory joint disease associated with psoriasis, with a psoriatic rash that causes pain, swelling, tenderness, stiffness, and dyskinesia in joints and surrounding soft tissues. There are sacroiliitis and / or spondylitis, the course of the disease is protracted, easy to relapse, and the joints may be ankylosing in the late stage, resulting in disability. In about 75% of PsA patients, the rash appeared before arthritis, in about 15% of those who appeared at the same time, and in about 10% of patients with rash after arthritis. [0003] This disease often has the tendency of family aggregation, the prevalence rate of first-degree family members is as high as 30%, and the risk of monozygotic ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/36A61K31/4035A61P19/02A61P17/06
Inventor 迟宗良单瑞平胡海燕叶锐孙军鲍黎林琳
Owner ZHEJIANG WAN SHENG PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com