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

A colon-localized drug delivery system for sodium p-aminosalicylate

A technology of sodium aminosalicylate and colon positioning, which is applied in the digestive system, drug combination, pharmaceutical formulation, etc., can solve the problems of large adverse reactions and low local concentration, and achieves reduction of toxic side effects, elimination of irritation, and reduction of dosage. Effect

Active Publication Date: 2012-02-08
上海新菲尔生物制药工程技术有限公司
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to overcome the shortcomings of low local concentration and large adverse reactions in the existing ordinary tablets and enteric-coated tablets of sodium p-aminosalicylate, and provide a kind of medicine that can overcome the above-mentioned shortcomings, and Sodium p-aminosalicylate pellets or granules with better colon localization effect

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
  • A colon-localized drug delivery system for sodium p-aminosalicylate
  • A colon-localized drug delivery system for sodium p-aminosalicylate
  • A colon-localized drug delivery system for sodium p-aminosalicylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 Sugar-coated pan pellets or granules

[0047] 1. Make the kernel

[0048] Steps (1)-(5) were carried out at 5°C, and steps (1)-(3) and (5) were carried out under dark light conditions.

[0049] (1) Take 500g of the original drug of sodium p-aminosalicylate (100% through 500 mesh), mix it with 300g of PVP-k30 and 100g of Eudragit S100 as material A (a total of 900g); dissolve 100g of Eudragit S100 in 100g of 20% Aqueous ethanol solution was used as material B (200 g in total).

[0050] The total formulation is: 50% sodium p-aminosalicylate, 30% binder (PVP-k30) and 20% framework material (Eudragit S100).

[0051] (2) Take and mix materials 450gA and 22.5gB respectively to make semi-dry and semi-wet soft materials, and pass through a 20-mesh upper screen to make fine particles as intermediate C.

[0052] (3) Put the intermediate C into the rotating sugar coating pan, add material A and material B alternately while rotating, and continuously sieve and grade at...

Embodiment 2

[0058] Example 2 Sugar-coated pan pellets or granules

[0059] 1. Make the kernel

[0060] Steps (1)-(5) are carried out at room temperature (25° C.), and steps (1)-(3) and (5) are carried out under dark light conditions.

[0061] (1) Get 980g of sodium p-aminosalicylate former drug (100% passes through 400 meshes), mix with 10g copovidone and 5g cellulose acetate phthalate as material A (995g in total); 5g cellulose acetate The phthalate was dissolved in 250 g of 50% ethanol in water as material B (255 g total).

[0062] The total formulation was: 98% sodium p-aminosalicylate, 1% binder (copovidone) and 1% framework material (cellulose acetate phthalate).

[0063] (2) Take and mix materials 19.6gA and 19.6gB respectively to make semi-dry and semi-wet soft materials, and pass through a 20-mesh upper screen to make fine particles as intermediate C.

[0064] (3) Put the intermediate C into the rotating sugar coating pan, add material A and material B alternately while rotatin...

Embodiment 3

[0070] Example 3 Sugar-coated pan pellets or granules

[0071] 1. Make the kernel

[0072] Steps (1)-(5) are carried out at room temperature (30° C.), and steps (1)-(3) and (5) are carried out under dark light conditions.

[0073] (1) Get 880g of sodium p-aminosalicylate former drug (100% through 80 mesh) and mix with 40g hydroxypropylmethylcellulose (HPMC), 10g microcrystalline cellulose and 30g sodium carboxymethylcellulose as material A (960 g in total); 40 g of Eudragit L100 was dissolved in 320 g of 80% by mass ethanol aqueous solution as material B.

[0074] The total formulation was: 88% sodium p-aminosalicylate, 3% binder (sodium carboxymethylcellulose), 8% matrix material (HPMC and Eudragit L100) and 1% porogen (microcrystalline cellulose).

[0075] (2) Take and mix materials 76.8g A and 19.2g B respectively to make a semi-dry and semi-wet soft material, and pass through a 10-mesh upper screen to make fine particles as intermediate C.

[0076] (3) Put the intermedi...

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 diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention relates to a para-aminosalicylate colon positioning drug delivery system which is a pellet or a particle. The inner part of the system is a kernel which contains the following components according to the mass percent: 50-98 percent of para-aminosalicylate, 1-30 percent of adhesive and 1-20 percent of skeleton material; and the surface of the kernel is coated with a layer of coatings which is 1 percent-40 percent of the mass of the whole pellet or the particle and contains film forming agent, sticking resistant agent and plasticizer. The invention also discloses a method for preparing the formulation, which comprises a sugar coating pot method, an extrusion-rolling method and a fluidized bed preparation method. Compared with the prior common tablet and a colon positioning tablet, the formulation has the better colon positioning effect, has the characteristics of increased specific surface area and good dissolving effect, is beneficial to absorbing and can reduce the poison and side effect caused by fast drug release by an individual difference of the formulation with a large dose, such as tablets, and the like.

Description

technical field [0001] The invention relates to a colon-localized drug delivery system for sodium p-aminosalicylate. Background technique [0002] After oral administration, the drug is generally absorbed or degraded before reaching the colon, but with rectal administration, the drug can directly enter the rectum or colon to achieve the purpose of local or systemic treatment. However, when administered rectally, the drug is limited to the rectum and descending colon, and cannot reach the transverse colon and ascending colon. Therefore, the development of a colon-targeted drug delivery system is of great significance for drugs used for the treatment of local lesions in the colon, and for drugs that need to be localized in the colon to avoid degradation by gastrointestinal enzymes. [0003] At present, the colon-localized drug delivery system can be roughly divided into the following categories according to the drug release principle: enzyme-controlled drug delivery system, p...

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 Patents(China)
IPC IPC(8): A61K9/16A61K31/606A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/40A61K47/42A61P1/00A61P1/04A61K47/10
Inventor 王懋杨学成
Owner 上海新菲尔生物制药工程技术有限公司
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