Mesalazine enteric positioned controlled-release preparation and preparation method thereof

A technology of mesalazine and controlled-release preparations, which is applied in the field of medicine, can solve the problems of aggravating the condition of patients with colonic ulcers, complex control of industrial preparation parameters, and low drug loading of mesalazine, achieving remarkable technological progress, Symptom improvement, effect of simple preparation method

Active Publication Date: 2016-08-31
UNIV OF SHANGHAI FOR SCI & TECH +1
View PDF7 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Study on dosage forms with mesalazine adhesion localization : Biointerfaces 2012,94:199~205], but the above studies have the disadvantages of low drug loading of mesalazine and complex control of industrial preparation parameters. In addition, patients need to take mesalamine for a long time, which is commonly used in adhesive preparations. The irritation and toxicity of adhesive materials to the gastrointestinal mucosa is a key issue that cannot be ignored. It has been reported that some adhesive materials can cause irritation to the mucosa [Yang Chunli, Ma Jing. "Chinese Journal of Pharmaceutical Industry "2000,11:490~491] [Lv Yi, Wu Canrong, Tan Hanyu. "Journal of Hunan University of Traditional Chinese Medicine" 2009,1:38~40], the irritation of adhesive materials to the mucosa will further aggravate the condition

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
  • Mesalazine enteric positioned controlled-release preparation and preparation method thereof
  • Mesalazine enteric positioned controlled-release preparation and preparation method thereof
  • Mesalazine enteric positioned controlled-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

1.1％

[0035] The preparation method of the above mesalazine enteric-coated positioning and controlled-release preparation is as follows:

[0036] (1) Preparation of mesalazine-containing pellets

[0037] Take the mesalazine with a composition of 66.7% by weight and pass through an 80-mesh screen to make the volume average particle size of the drug particles ≤200μm; then take the composition of hydroxypropyl cellulose (Klucel MF) with a composition of 9.2% by weight and the composition by weight as After passing through a 60-mesh sieve, 5.8% lactose is mixed with mesalazine; take a small amount of the above mixture and place it in a fluidized bed, and use ethanol-water (70:30) solvent for fluidized granulation, and control the fluidized bed temperature 45 ℃, after the granules are dried, 40 meshes are sized, and 40-60 mesh granules are selected as the mother core. The pellets are prepared in the WL-300 pill making machine, and the rotation speed of the turntable is controlled to 200...

Embodiment 2

1.1％

[0046] The preparation method of the above mesalazine enteric controlled-release preparation is as follows:

[0047] (1) Preparation of mesalazine-containing pellets

[0048] Take the 66.7% by mass of mesalazine and pass it through an 80-mesh sieve to make the volume average particle size of the drug particles ≤200μm; then take the 9.2% by mass of hydroxypropyl cellulose and 10.8% of lactose and pass through a 60-mesh sieve After meshing, mix with mesalazine; take a small amount of the above mixture and place it in a fluidized bed, use ethanol-water (70:30) solvent for fluidized granulation, control the temperature of the fluidized bed at 45°C, and dry the granules to 40 mesh Select the 40-60 mesh particles as the mother core, prepare the pellets in the WL-300 pill making machine, control the rotating speed of the turntable to 200-300rpm, and the inlet temperature of 40℃ to prepare the drug-containing pellets. The diameter of the pellets is controlled to be 0.8- 1.5mm; Mix t...

Embodiment 3

1.1％

[0055] The preparation method of the above mesalazine enteric-coated positioning and controlled-release preparation is as follows:

[0056] (1) Preparation of mesalazine-containing pellets

[0057] Take mesalazine with a mass percentage composition of 79.5% and pass it through an 80-mesh sieve to make the volume average particle size of the drug particles ≤200μm; then take the hydroxypropyl cellulose with a mass percentage composition of 8.5% and pass it through a 60-mesh sieve. Mix the salazine; take the above-mentioned small amount of mixture and place it in a fluidized bed, use ethanol-water (70:30) solvent for fluidized granulation, control the temperature of the fluidized bed at 45°C, and dry the granules to 40 meshes and sieving to 40~ The 60-mesh particles are used as the core, and the pellets are prepared in the WL-300 pelletizing machine, the rotating speed of the turntable is controlled to be 200-300rpm, the inlet temperature is 40°C, and the drug-containing pellets...

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

PropertyMeasurementUnit
viscosityaaaaaaaaaa
viscosityaaaaaaaaaa
particle diameteraaaaaaaaaa
Login to view more

Abstract

The invention discloses mesalazine enteric positioned controlled-release preparation, comprising a core, a controlled-release coating layer, an adhesive coating layer, and an enteric coating layer. The core includes mesalazine, hydroxyl propyl cellulose and talc powder, the controlled-release coating layer is composed of ethyl cellulose and triethyl citrate, the adhesive coating layer is made from sodium alginate, the enteric coating layer is composed of methacrylic acid and methyl methacrylate copolymer, triethyl citrate and talc powder. The invention also provides a preparation method of the enteric positioned controlled-release preparation. The preparation method is simple with controllable parameters, prepared pellets do not release in gastric acid and may release slowly for 24 hours in a dissolution medium at pH 7.5. This preparation is irritating to gastrointestinal adhesion and may be used in acute stage treatment for ulcerative colitis (inflammation accompanied ulcers) and maintenance treatment for preventing recurrence.

Description

Technical field [0001] The invention belongs to the field of medicine, and relates to a sustained-release preparation, in particular to a mesalazine enteric-coated positioning and controlled-release preparation and a preparation method thereof. Background technique [0002] Mesalazine is the active ingredient of sulfasalazine. According to clinical results, the therapeutic effect of this product after oral administration is similar to that of rectal administration. It is a local effect. It is used for the treatment of acute ulcerative colitis (inflammation with ulcer). Maintenance treatment to prevent recurrence and symptom improvement treatment of active Crohn's disease. Mesalazine can inhibit leukocyte chemotaxis, reduce cytokine and leukotriene production, and scavenge free radicals in vivo and in vitro. Existing studies have shown that mesalazine is nephrotoxic to experimental animals. The pharmacological characteristics of mesalazine indicate that the ideal drug release si...

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): A61K9/16A61K31/606A61K47/38A61K47/32A61P1/04A61P1/00
CPCA61K9/0053A61K9/5073A61K31/606A61K47/32A61K47/38
Inventor 刘哲鹏潘风符雯谢阿静
Owner UNIV OF SHANGHAI FOR SCI & TECH
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