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

Mesalazine sustained-release pellets, preparation method thereof and mesalazine sustained-release capsule

A technology of sustained-release pellets and mesalazine, applied in the field of mesalazine sustained-release pellets and its preparation, and mesalazine capsules, which can solve the problems that the drug release effect needs to be improved, and achieve favorable treatment and high drug loading , reduce the effect of stimulation

Active Publication Date: 2016-04-06
XINAN PHARMA
View PDF4 Cites 8 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for Crohn's disease, which is most commonly located in the small intestine and terminal ileum, the release effect of existing mesalazine preparations needs to be improved

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 sustained-release pellets, preparation method thereof and mesalazine sustained-release capsule
  • Mesalazine sustained-release pellets, preparation method thereof and mesalazine sustained-release capsule
  • Mesalazine sustained-release pellets, preparation method thereof and mesalazine sustained-release capsule

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0055] Correspondingly, the present invention provides a method for preparing mesalazine sustained-release pellets, comprising: mixing 5-aminosalicylic acid, microcrystalline cellulose and a binder, and extruding and spheronizing to obtain a pellet containing a core ;

[0056] Using a material including ethyl cellulose, wrapping a sustained-release coating layer on the core of the drug-containing pill;

[0057] The enteric coating layer is wrapped on the sustained release coating layer by adopting the enteric material and processing aid to obtain the mesalazine sustained release pellets; the enteric material is a copolymer of methacrylic acid and ethyl acrylate.

[0058] The embodiment of the present invention adopts an extrusion spheronization process, adding water to 5-aminosalicylic acid and auxiliary materials including microcrystalline cellulose and a binder, and drying them to make a drug-containing pellet core.

[0059] Wherein, the contents of the microcrystalline cel...

Embodiment 1

[0075] Prescription with pill core (1000 capsules):

[0076]

[0077] Adhesive preparation: Weigh 119g of pure water and 21g of PVPk30, add 21g of PVPk30 to 119g of pure water under constant stirring at 500rpm, and stir for 20min to obtain a 15% PVPk30 aqueous solution.

[0078] Ball core preparation: Take the prescribed amount of mesalazine and microcrystalline cellulose and mix them evenly after sieving respectively, use the prepared 15% PVPk30 aqueous solution as a binder to prepare a soft material, and place the soft material in an extrusion spheronizer The pellets were prepared with an extrusion speed of 25 rpm, a spheronization speed of 900 rpm, and a spheronization time of 3 minutes; the pellets were dried in an oven at 40°C, and sieved to 20-30 meshes to obtain coating cores.

[0079] Sustained-release layer coating liquid prescription:

[0080] Su Lisi (Shanghai Colorcon Coating Technology Co., Ltd.) 150g

[0081] Pure water 100g

[0082] Preparation of sustaine...

Embodiment 2

[0092] Prescription with pill core (1000 capsules):

[0093]

[0094] Adhesive preparation: Weigh 127g of pure water and 11g of HPMCE15, add 11g of HPMCE15 into 127g of pure water under constant stirring at 500rpm, stir for 20min, and leave overnight to obtain an 8% HPMCE15 aqueous solution.

[0095] Ball core preparation: Take the prescribed amount of mesalazine and microcrystalline cellulose, sieve them and mix them evenly, use the prepared 8% HPMCE15 aqueous solution as a binder to prepare a soft material, and place the soft material in an extrusion spheronizer Micropellets were prepared; the extrusion speed was 25 rpm, the spheronization speed was 900 rpm, and the spheronization time was 3 min. The pellets were dried in an oven at 40°C, and sieved to 20-30 meshes to obtain pellet cores for coating.

[0096] Sustained-release layer coating liquid prescription:

[0097] Su Lisi (with embodiment 45g1)

[0098] Pure water 30g

[0099] Preparation of sustained-release co...

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
particle size (mesh)aaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention provides mesalazine sustained-release pellets, a preparation method thereof and a mesalazine sustained-release capsule. The preparation method comprises the steps that 5-aminosalicylic acid, microcrystalline cellulose and a binding agent are mixed, and cores with pills are obtained through an extrusion rolling technology; materials comprising ethyecellulose are adopted, and cores with the pills are coated with sustained-release coating layers; the sustained-release coating layers are coated with enteric coating layers by the adoption of enteric materials and a processing aid, and mesalazine sustained-release pellets are obtained; the enteric materials are methacrylic acid and ethyl acrylate copolymer. PH dependent form and time dependent form drug release mechanisms are combined to achieve an ideal drug release curve, and the drug release position accuracy is improved. The mesalazine sustained-release capsule comprises the mesalazine sustained-release pellets, can be better released in the gastrointestinal tract and is beneficial to treatment on ulcerative colitis and Crohn's disease.

Description

technical field [0001] The invention relates to the technical field of mesalazine pharmaceutical preparations, in particular to a mesalazine sustained-release pellet, a preparation method thereof and a mesalazine capsule. Background technique [0002] Inflammatory bowel disease (IBD) is a chronic and relapsing intestinal inflammatory disease, narrowly divided into ulcerative colitis (UC) and Crohn's disease (CD). Ulcerative colitis is a common non-specific chronic inflammatory disease that occurs in the colonic mucosa. The main symptoms are abdominal pain and diarrhea. The pathogenesis of the disease is unknown, and it has been listed as one of the modern refractory diseases by the World Health Organization. Crohn's disease, also known as Crohn's disease or granulomatous enteritis, can occur anywhere in the entire gastrointestinal tract, most commonly in the small intestine and terminal ileum. At present, there is no fundamental cure for the disease, and it is accompanied ...

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): A61K9/36A61K31/606A61K9/52A61P1/00A61P1/04
CPCA61K9/0002A61K9/2054A61K9/2846A61K9/5031A61K31/606
Inventor 蒲道俊李标徐洁田旭余春梅罗娟向俭林美玲
Owner XINAN PHARMA
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