Apremilast gel for injection to articular cavity and preparation method of apremilast gel

A special gel and gel technology, applied in the field of medicine, can solve problems such as increased risk of depression and weight loss, achieve the effects of reducing systemic adverse reactions, reducing frequent drug administration, and expanding clinical application value

Inactive Publication Date: 2017-07-07
CHONGQING UNIV
View PDF9 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, in clinical studies, it was found that the risk of depression in patients after treatment with Apremilast tablets increased, and the weight loss was significant, which made the treatment of Apremilast discontinued.

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 gel for injection to articular cavity and preparation method of apremilast gel
  • Apremilast gel for injection to articular cavity and preparation method of apremilast gel
  • Apremilast gel for injection to articular cavity and preparation method of apremilast gel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025]

[0026] Below 30°C, add the prescribed amount of poloxamer 407, poloxamer 188 and glycerin into purified water, and stir to form a poloxamer sol solution. After adding Apremilast, use a 12000rpm high-speed shear emulsifier to mix for 1h, and stir at 50rpm for 5h to dissolve. Centrifuge at 10,000rpm for 10 minutes to take the supernatant, and use a 0.22μm membrane to filter and sterilize in a sterile operating room to obtain this product (sample 1).

Embodiment 2

[0028]

[0029] Below 30°C, add the prescribed amount of poloxamer 407 and glycerin into purified water, and stir to form a poloxamer sol solution. After adding Apremilast, use a 12000rpm high-speed shear emulsifier to mix for 1h, and stir at 50rpm for 5h to dissolve. Centrifuge at 10,000rpm for 10 minutes to get the supernatant, filter and sterilize with a 0.22μm membrane in a sterile operating room to obtain this product (sample 2).

Embodiment 3

[0031]

[0032] Below 30°C, add the prescribed amount of poloxamer 407, poloxamer 188 and glycerin into purified water, and stir to form a poloxamer sol solution. After adding Apremilast, use a 12000rpm high-speed shear emulsifier to mix for 1h, and stir at 50rpm for 5h to dissolve. Centrifuge at 10,000rpm for 10 minutes to take the supernatant, and use a 0.22μm membrane to filter and sterilize in a sterile operating room to obtain this product (sample 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 mainly provides apremilast gel for injection to the articular cavity and a preparation method of the apremilast gel. According to the apremilast gel and the preparation method, polymer with the temperature-sensitive reverse gel property is adopted as a carrier material, and medicines are dispersed or dissolved in an aqueous solution of the carrier material. When the temperature is lower than the body temperature, a sample exists in the form of sol, and is injected into the body through a common syringe; when the temperature of the injected part rises to the body temperature, the sol is transformed into semi-solid gel, along with the slow dissolving of the carrier material, the medicines are released from the gel at the low rate, and the release of the medicines can last for several weeks to several months. The release ratio of the medicines can be realized by changing the variety, concentration, proportion and molecular weight of the gel material. The dosing interval of the gel is long, the preparation process is simple, the preparation process is mature, and the method is suitable for industrial mass production.

Description

technical field [0001] The invention belongs to the technical field of medicine and provides an apremilast gel for intra-articular injection and a preparation method thereof. Background technique [0002] On March 21, 2014, the U.S. FDA approved Celgene's Apremilast for the treatment of adult patients with active psoriatic arthritis (PsA), which is the first oral PsA treatment approved by the FDA drug. In September 2014, the US FDA approved Apremilast for the treatment of patients with moderate to severe plaque psoriasis who are suitable for phototherapy and systemic treatment. Apremilast has been marketed as an immediate-release tablet, which needs to be taken twice a day. Common adverse reactions of Apremilast tablets include diarrhea, nausea, headache, and upper respiratory tract infection (incidence >5%). In addition, in clinical studies, it was found that the risk of depression in patients after treatment with Apremilast tablets increased, and the weight loss was ...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/10A61K31/4035A61P17/06A61P19/02
CPCA61K9/0024A61K9/0002A61K9/06A61K31/4035A61K47/10
Inventor 胡平黄诗贵余灏唐美琼郑强贺耘
Owner CHONGQING UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap