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

Iguratimod oral double-layer sustained-release preparation

A controlled-release preparation, double-layer technology, applied in anti-inflammatory agents, non-central analgesics, medical preparations containing active ingredients, etc., to achieve the effect of improving bioavailability and accelerating time to peak

Inactive Publication Date: 2008-01-02
TIANJIN INSTITUTE OF PHARMA RESEARCH
View PDF2 Cites 14 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The Iguratimod double-layer controlled-release tablet developed by the inventor has not yet seen the report of relevant literature

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
  • Iguratimod oral double-layer sustained-release preparation
  • Iguratimod oral double-layer sustained-release preparation
  • Iguratimod oral double-layer sustained-release preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The preparation of embodiment 1 Airamod crystalline micropowder

[0051] Take 1.0g of the raw material of iguratimod and add 17.5ml of dimethylformamide to dissolve it, slowly (or drop it) into 500ml of water, add dropwise while stirring, the stirring speed is 800r / min, iguratimod will precipitate and disperse immediately In the water. Filter, stir wash three times with distilled water, filter, and dry at 60°C for 2 hours. The above-mentioned powder was taken for powder X-ray diffraction measurement and powder particle size inspection, and the average particle size of the above-mentioned powder was about 4 μm. The yield was 97.5%. The powder X-ray diffraction pattern is shown in accompanying drawing 1.

Embodiment 2

[0052] Embodiment 2 Alamode quick-release layer process investigation (1000):

[0053] prescription composition

[0054] making process:

[0055] (1) Crush the raw materials and auxiliary materials and pass through a 200-mesh sieve respectively, and set aside.

[0056] (2) In addition to povidone K30 and magnesium stearate, take the prescription amount according to the prescription, mix evenly with a 60-mesh sieve, add 10% povidone K30 solution to make soft materials, granulate with a 30-mesh sieve, and dry at 60°C for 2 Hour.

[0057] (3) Get the above granules, add the prescribed amount of magnesium stearate, and granulate through a 20-mesh sieve. Compress the tablet, control the pressure to 3-4 kg.

[0058] Dissolution Determination:

[0059] According to the requirements of the Chinese Pharmacopoeia in 2000, phosphate buffer (pH is 7.8) is used as the dissolution medium, the slurry method, the rotating speed is 100 rpm, and the ultraviolet spectrophotometric ...

Embodiment 3

[0062] The impact of embodiment 3 different HPMC dosages on the release of iguratimod sustained-release layer (1000 tablets)

[0063] prescription composition

Prescription 4

Prescription 5

Prescription 6

Alamode micronized powder

50g

50g

50g

HPMC (K4M)

50g

35g

24g

lactose

80g

80g

80g

microcrystalline cellulose

20g

20g

20g

Povidone K30

Appropriate amount

Appropriate amount

Appropriate amount

Magnesium stearate

2％

2％

2％

[0064] Pass HPMC (K4M), lactose, and microcrystalline cellulose through a 80-mesh sieve, fully mix with micronized iguratimod, add an appropriate amount of 50% ethanol solution with a concentration of 10% povidone K30 to make a soft material, and make a 30-mesh sieve Granules, wet granules were dried at 60°C for 2 hours and sieved through a 20-mesh sieve, added magnesium stearate, mixed evenly, and compressed into...

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 relates to oral double iguratimod controlled release formulation, which comprises fast release layer and slow release layer that are composed of 8-30% micronizing iguratimod crystal powder and medical findings, and the granule size of iguratimod crystal powder is 1-10 um. The effective component in fast release layer is released in short time and reaches to effective blood chemical concentration for effective action; the iguratimod in sloe release layer is released gradually and maintains effective blood medical concentration for continuous effective action. The invention overcomes shortcomings of short effective action time and a little high toxic effect.

Description

technical field [0001] The invention relates to an insoluble drug iguratimod crystalline micropowder and a preparation method of the micropowder, in particular to an iguratimod oral double-layer controlled-release preparation and a preparation method thereof. Background technique [0002] Iguratimod’s generic name is Iguratimod, and its chemical name is N-[3-(formamido)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]-methanesulfonate Amide, the English name is: N-[3-(formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]-methanesulfonamide, its chemical structure, production method and use are disclosed in Japanese Patent Application 2001- The Patent Bulletin of 240540 has been recorded, and Japanese Patent Application No. 2-49778 and Japanese Zai Gong Biaoping No. 6-623714 have publicly published the antipyretic and analgesic, anti-arthritis effects of iguratimod, immunoregulatory effects, and autoimmune Disease prevention and treatment. [0003] Iguratimod is a disease-modifying anti-...

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): A61K31/352A61K9/22A61P29/00A61P37/02A61P19/02
Inventor 王杏林高晶梅林雨刘昌孝
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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