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Diflunisal slow-releasing preparation and its making method

A technology of diflunisal and sustained-release preparations, which is applied in anti-inflammatory agents, pharmaceutical formulas, non-central analgesics, etc., can solve the problems that diflunisal slow-release preparations have not been reported, and achieve improved anti-inflammatory, The effect of reducing side effects

Inactive Publication Date: 2007-01-17
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, no research on diflunisal sustained-release preparations has been reported.

Method used

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  • Diflunisal slow-releasing preparation and its making method
  • Diflunisal slow-releasing preparation and its making method
  • Diflunisal slow-releasing preparation and its making method

Examples

Experimental program
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Effect test

Embodiment 1

[0044] Take 1.53g (6mmol) Mg (NO 3 ) 2 ·6H 2 O and 0.75g (2mmol) Al(NO 3 ) 3 9H 2 O was dissolved in 10mL deionized water, stirred to dissolve to obtain mixed liquid A; 1.79g (6mmol) of diflunisal (full name diflunisal, referred to as Dif) was dissolved in 30mL of deionized water, and the pH was adjusted with 2mol / L NaOH solution The value is 10, and the mixed liquid B is obtained. Under vigorous stirring, drop solution A into solution B, N 2 Protection, reaction at 65°C for 48h. The product was filtered, the filter cake was washed and dried in vacuo. The deionized water used in the process was double distilled water.

[0045] According to the characterization, the chemical composition of the obtained Dif-LDHs is: Mg 0.70 Al 0.30 (OH) 2 (Dif) 0.30 0.70H 2 O, wherein the content of diflunisal is 49.7%.

Embodiment 2

[0047] (1) Take 11.88g (0.04mol) Zn(NO 3 ) 2 ·6H 2 O and 7.5gAl(NO 3 ) 3 9H 2 O (0.02mol) was dissolved in 100mL deionized water to make solution A; then 4.8g NaOH solid was dissolved in an appropriate amount of deionized water to make 2mol / L solution C; N 2 Under protection, add solution A and solution C dropwise to 100ml of deionized water at a certain drop rate, keep the pH value of the solution between 9 and 10, and continue to stir for half an hour after the dropwise addition. After the obtained slurry was crystallized at 65°C for 18 hours, it was suction-filtered, washed with deionized water until neutral, dried at 65°C, ground, weighed, and stored in a desiccator. denoted as LDHs-NO 3 - .

[0048] (2) Dissolve 1.79g (6mmol) Dif in 30mL deionized water to obtain solution D, and then take 1gLDHs-NO 3 Dissolve in 50mL of deionized water to obtain solution E, under full stirring, mix the two solutions of D and E, adjust pH=10, stir vigorously, N 2 Protection, reac...

Embodiment 3～4

[0052] By the method of embodiment 2, change the pH value in embodiment 2 (2), be respectively 9,11, other operations are with embodiment 2. The deionized water used in the process was double distilled water.

[0053] It was found that at a pH of 10, the obtained Dif-LDHs material has a better crystal structure and represents the d of the interlayer spacing 003 maximum. The specific XRD data are as follows: pH=9, d 003 = 1.91nm; pH = 10, d 003 = 1.96nm; pH = 11, d 003 = 1.84nm.

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Abstract

A slow-releasing diflunisal with high anti-inflammatory and antalgic effect and its preparing process are disclosed. It uses the anionic laminar hydrotalcite as its main body and has the intercalated hydrotalcite crystal structure.

Description

(1) Technical field [0001] The invention relates to a slow-release agent of non-steroidal anti-inflammatory drugs and a preparation method thereof, in particular to a sustained-release agent of diflunisal and a preparation method thereof. (2) Background technology [0002] Non-steroidal anti-inflammatory analgesics (NSAIDs) have anti-inflammatory, anti-rheumatic, analgesic, antipyretic and anti-coagulant effects, and are widely used clinically for osteoarthritis, rheumatoid arthritis, various fevers and various diseases. relief of pain symptoms. NSAIDs are currently one of the most widely used drugs in the world. About 30 million people use it every day around the world. However, treatment also brings some side effects at the same time, which can endanger people's life seriously. Therefore, with the increasing use of NSAIDs, the safe use of these drugs has attracted more and more attention from clinicians, pharmacists, patients, society and the government. Reducing the s...

Claims

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Application Information

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IPC IPC(8): A61K31/603A61K33/30A61K33/34A61K33/06A61P29/00
Inventor 倪哲明李丹王力耕
Owner ZHEJIANG UNIV OF TECH
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