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Intestinal-lysis non-steroidal antipyretic-antalgic anti-inflammatory agent and preparation thereof

A technology of antipyretic, analgesic and anti-inflammatory drugs, which is applied in the direction of antipyretics, anti-inflammatory agents, non-central analgesics, etc. It can solve the problem of different selection effects and achieve good absorption effect

Inactive Publication Date: 2011-09-21
QINGDAO KDN BIOTECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The use of non-steroidal anti-inflammatory drugs (NSAIDs) in human clinical practice After more than a century of continuous research and clinical use, it has been found that most antipyretic, analgesic and anti-inflammatory drugs have an effect on COX-1 and COX -2 is not selective, just different drugs have different selective effects on COX-1 and COX-2

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: First heat and dissolve 45g of hypromellose peptidate (HP55) with 1000ml (ethanol: water = 80:20) solution, then add 150g of diclofenac sodium, heat and stir until dissolved and clear, then concentrate to thicken while stirring shape, cooled, and dried to obtain enteric-coated clothes. Coating weight gain: 22.98%.

[0025] Determination of encapsulation efficiency: According to the dissolution rate of the coating in acidic medium is 0 (this conclusion can be drawn in the following dissolution test), it is advisable to quickly filter the coating after stirring in 0.1mol / L HCl solution (PH=1.0) , the contained drug will not dissolve, but the free drug will dissolve, the amount of free drug can be measured W free, in addition the total amount of drug W is known, according to the encapsulation rate=(W total-W free) / W total × 100%, the calculated encapsulation efficiency is 98.1%.

[0026] Dissolution determination: according to the second method in the dissolut...

Embodiment 2

[0029] Example 2: First heat and dissolve 15 g of hypromellose peptidate (HP55) with 800 ml (ethanol: water = 80: 20) solution, then add 150 g of diclofenac sodium, heat and stir until dissolved and clear, and concentrate to thicken while stirring shape, cooled, and dried to obtain enteric-coated clothes. Coating weight gain: 9.0%.

[0030] Determination of encapsulation efficiency: According to the dissolution rate of the coating in acidic medium is 0 (this conclusion can be drawn in the following dissolution test), it is advisable to quickly filter the coating after stirring in 0.1mol / L HCl solution (PH=1.0) , the contained drug will not dissolve, but the free drug will dissolve, the amount of free drug can be measured W free, in addition the total amount of drug W is known, according to the encapsulation rate=(W total-W free) / W total × 100%, the calculated encapsulation efficiency is 92.5%.

[0031]Dissolution determination: according to the second method in the dissoluti...

Embodiment 3

[0034] Example 3: First heat and dissolve 5g of hypromellose peptidate (HP55) with 500ml (ethanol: water = 80:20) solution, then add 100g of diclofenac sodium, heat and stir until dissolved and clear, and spray dry to obtain enteric coating Pack clothing. Coating weight gain: 4.72%.

[0035] Determination of encapsulation efficiency: According to the dissolution rate of the coating in acidic medium is 0 (this conclusion can be drawn in the following dissolution test), it is advisable to quickly filter the coating after stirring in 0.1mol / L HCl solution (PH=1.0) , the contained drug will not dissolve, but the free drug will dissolve, the amount of free drug can be measured W free, in addition the total amount of drug W is known, according to the encapsulation rate=(W total-W free) / W total × 100%, the calculated encapsulation efficiency is 90.7%.

[0036] Dissolution determination: according to the second method in the dissolution determination method of appendix XC of Chinese...

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Abstract

The invention relates to non-sterides antipyretic-analgesic and anti-inflammatory drug with enteric solubility and the preparation thereof; when the non-sterides antipyretic-analgesic and anti-inflammatory drug is taken orally, the confessed side effects such as nausea, emesis, gastric ulcer, gastric perforation, gastrorrhagia, edema, and the like on the gastrointestinal tract of human body and animals caused by the drug are avoided.

Description

technical field [0001] The invention relates to a preparation method of an enteric-coated preparation of a non-steroidal antipyretic, analgesic and anti-inflammatory drug. Background technique [0002] Nonsteroidal antiinflammatory drugs (NSAIDs) are antipyretic, analgesic and anti-inflammatory drugs commonly used clinically, and are widely used in rheumatic diseases, chronic inflammatory arthritis, and fever and pain diseases caused by various reasons . [0003] In the more than a century since aspirin was launched on the market in 1898, nonsteroidal antiinflammatory drugs (NSAIDs) have increased to more than a hundred varieties, which can be divided into formic acids, also known as salicylates, according to their chemical structures. Acids (representing the drugs aspirin, diclonisal, etc.); acetic acids (representing the drugs diclofenac, indomethacin, sulindac and etofenamate); propionic acids (representing the drugs ibuprofen, ketoprofen Fen, fenbufen, naproxen, oxapro...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K45/00A61K47/30A61P29/00
Inventor 袁卫
Owner QINGDAO KDN BIOTECH
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