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Orally taken colon-targeted preparation for treatment of inflammatory bowel diseases and preparation method thereof

An inflammatory bowel disease and colon-targeting technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas. The effect of simple operation and low solvent residue

Inactive Publication Date: 2013-09-25
SHANGHAI FIRST PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there have been no reports related to the Eudragit S100 encapsulated 5-aminosalicylic acid nanoparticles of the present invention and its preparation method

Method used

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  • Orally taken colon-targeted preparation for treatment of inflammatory bowel diseases and preparation method thereof
  • Orally taken colon-targeted preparation for treatment of inflammatory bowel diseases and preparation method thereof
  • Orally taken colon-targeted preparation for treatment of inflammatory bowel diseases and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036]This embodiment provides a nanoparticle coated with 5-aminosalicylic acid by Eudragit S100, the composition and weight percentage of which are: 25% of 5-aminosalicylic acid and the balance of Eudragit S100.

[0037] The preparation method of the nanoparticles of Eudragit S100 wrapping 5-aminosalicylic acid comprises the following steps:

[0038] Step (1), take 5-aminosalicylic acid and Eudragit S100 according to the mass ratio of 5-aminosalicylic acid and Eudragit S100 at 1:4, and then add dimethyl sulfoxide and acetone to a mixed solvent composed of 3:7 by volume In, get the solution;

[0039] Step (2), the CO 2 Pump into the high-pressure reaction kettle, after the reaction kettle reaches a temperature of 35°C and a pressure of 12MPa, keep it for 5 minutes, and pump the solution obtained in step (1) at a flow rate of 1ml / min;

[0040] Step (3), after the solution is pumped, continue to feed CO 2 45min, so that the solvent is dry, stop feeding CO 2 , release the pre...

Embodiment 2

[0043] This example provides a nanoparticle coated with 5-aminosalicylic acid by Eudragit S100, the composition and weight percentage of which are: 12.5% ​​of 5-aminosalicylic acid and the balance of Eudragit S100. Preparation method is with embodiment 1, and difference is:

[0044] In step (1), 5-aminosalicylic acid and Eudragit S100 are taken according to the mass ratio of 5-aminosalicylic acid and Eudragit S100 at 1:7;

[0045] In step (2), the CO 2 Pump into the high-pressure reaction kettle, after the reaction kettle reaches a temperature of 45°C and a pressure of 12MPa, keep it for 5 minutes, and pump the solution obtained in step (1) at a flow rate of 1ml / min;

[0046] The implementation effect of this example: Weigh an appropriate amount of nanoparticles, add them to a phosphate buffer solution with a pH of 7.4, and pump them into high performance liquid chromatography with a micro-sampler. The injection volume is 10 μL, and the calculated drug loading is 3.49%. ,As ...

Embodiment 3

[0048] This example provides a kind of Eudragit S100 coated 5-aminosalicylic acid nanoparticles, its composition and weight percentage are: 33.3% of 5-aminosalicylic acid, and the balance is Eudragit S100. Preparation method is with embodiment 1, and difference is:

[0049] In step (1), take 5-aminosalicylic acid and Eudragit S100 according to the mass ratio of 5-aminosalicylic acid and Eudragit S100 at 1:2;

[0050] In step (2), the CO 2 Pump into the high-pressure reaction kettle, after the reaction kettle reaches a temperature of 35°C and a pressure of 15MPa, keep it for 5 minutes, and pump the solution obtained in step (1) at a flow rate of 2ml / min;

[0051] The implementation effect of this example: Weigh an appropriate amount of nanoparticles, add them to a phosphate buffer solution with a pH of 7.4, and pump them into high performance liquid chromatography with a micro-injector. The injection volume is 10 μL, and the calculated drug loading is 9.87%. ,As shown in Tabl...

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Abstract

Belonging to the field of medicinal preparations, the invention relates to an orally taken colon-targeted preparation for treatment of inflammatory bowel diseases, particularly to an Eudragit S100 wrapped 5-aminosalicylic acid nanoparticle and its preparation method. In the invention, 5-aminosalicylic acid is taken as a model drug, and a pH sensitive Eudragit S100 is employed as a coating material to prepare the Eudragit S100 wrapped 5-aminosalicylic acid nanoparticle with a particle size of 70-400nm. The prepared nanoparticle can protect a 1, 5-aminosalicylic acid drug from being damaged by the digestive juice in a gastrointestinal tract until the drug reaches a colon region with pH greater than 7. The preparation method provided in the invention is simple to operate, and the prepared colon-targeted nanoparticle has the characteristics of small particle size and narrow distribution, as well as low solvent residue. The orally taken colon-targeted preparation can be used as a novel preparation of 5-aminosalicylic acid in treatment of inflammatory bowel diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an oral colon-targeting preparation for treating inflammatory bowel disease and a preparation method thereof, in particular to a Eudragit S100-coated 5-aminosalicylic acid nanoparticle and a preparation method thereof. Background technique [0002] Oral colon-targeted drug delivery refers to the use of drug delivery technology to make the drug not release the drug in the stomach, duodenum, jejunum, and ileum after oral administration, and release the drug after it is transported to the ileocecal to exert local or systemic therapeutic effects. A novel positioning drug delivery system. In recent years, great progress has been made in the research of colon-targeted drug delivery systems in the treatment of intestinal diseases and the oral administration of protein and polypeptide drugs. Among them, one of the most important applications of the colon-targeted drug delivery s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/606A61K47/32A61P1/00
Inventor 胡道德刘亮
Owner SHANGHAI FIRST PEOPLES HOSPITAL
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