Tegafur/layered duplex metal hydroxide nanometer hybrid and preparation method thereof

A layered bimetallic and nano-hybrid technology is applied in the direction of pharmaceutical formulations, drug combinations, and medical preparations containing active ingredients. release effect

Inactive Publication Date: 2010-07-28
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Tegafur (Tegafur) is a derivative of fluorouracil, which is used to treat various cancers such as stomach, intestine, and liver. Compared with fluorouracil, the therapeutic index is improved and the toxicity is reduced, but there are still side effects such as bone marrow suppression, gastrointestinal reactions, leukopenia and thrombocytopenia.

Method used

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  • Tegafur/layered duplex metal hydroxide nanometer hybrid and preparation method thereof
  • Tegafur/layered duplex metal hydroxide nanometer hybrid and preparation method thereof
  • Tegafur/layered duplex metal hydroxide nanometer hybrid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Step a: 5.95g (0.020mol) Zn(NO 3 ) 2 ·6H 2 O and 3.75g (0.010mol) Al(NO 3 ) 3 9H 2 O was dissolved in 60ml of water and heated to 30°C.

[0041] Step b: Dissolve 0.50 g (0.0025 mol) of solid Tegafur in the mixed salt solution of step a.

[0042] Step c: Prepare a NaOH solution with a concentration of 2 mol / L.

[0043] Step d: Add the solution of step c to the solution of step b, keep stirring and control the pH to 9.7, the reaction temperature is 30°C, the stirring reaction time is 2 hours, then the obtained slurry is aged at 30°C for 18 hours, filtered, and washed with water until Neutral, peptized at 80°C for 24 hours to obtain Tegafur / LDHs nano-hybrids; dry to obtain powder products.

[0044] By XRD spectrum ( figure 1 ) shows that the Tegafur / LDHs nano-hybrid has a layered structure, and the interlayer spacing (d 003 ) shows that tegafur has been intercalated.

[0045] The sample was analyzed by ultraviolet spectrophotometry, and the content of tegafur was...

Embodiment 2

[0047] Step a: 1.59g (0.0053mol) Zn(NO 3 ) 2 ·6H 2 O and 1.00g (0.0026mol) Al(NO 3 ) 3 9H 2 O was dissolved in 20ml of water and heated to 60°C.

[0048] Step b: 0.66 g (0.0033 mol) of solid Tegafur was dissolved in the mixed salt solution of step a.

[0049] Step c: Prepare a NaOH solution with a concentration of 0.5 mol / L.

[0050] Step d: Add the solution of step c to the solution of step b, keep stirring and control the pH to 11.70, the reaction temperature is 60°C, the stirring reaction time is 1.5 hours, then the obtained slurry is aged at 60°C for 3 hours, filtered, and washed with water until Neutral, peptized at 80°C for 24 hours to obtain Tegafur / LDHs nano-hybrids; dry to obtain powder products.

[0051] By XRD spectrum ( figure 2 ) shows that the Tegafur / LDHs nano-hybrid has a layered structure, and the interlayer distance d 003 It can be seen that tegafur has been intercalated.

[0052] The sample was analyzed by ultraviolet spectrophotometry, and the co...

Embodiment 3

[0054] Step a: 0.030mol of Ni(NO 3 ) 2 ·6H 2 O and 0.010mol of Al(NO 3 ) 3 9H 2 O was dissolved in 40ml of water and heated to 30°C.

[0055] Step b: Dissolve 0.50 g (0.010 mol) of solid Tegafur in the mixed salt solution of step a.

[0056] Step c: Prepare NH with a concentration of 1.0mol / L 4 OH solution.

[0057] Step d: Add the solution of step c to the solution of step b, keep stirring and control the pH to 10.06, the reaction temperature is 30°C, the stirring reaction time is 2 hours, then the obtained slurry is aged at 30°C for 15 hours, filtered, and washed with water until Neutral, peptized at 80°C for 24 hours to obtain Tegafur / LDHs nano-hybrids; dry to obtain powder products.

[0058] The sample was analyzed by ultraviolet spectrophotometry, and the content of tegafur was determined to be 10.05%.

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Abstract

The invention relates to a Tegafur/LDHs nanometer hybrid and a preparation method thereof, and aims to provide a method for preparing a Tegafur/LDHs nanometer hybrid for slow release of Tegafur to improve potency and reduce the toxic or side effect of medicaments by taking LDHs as a carrier. LDHs is taken as a main body, the Tegafur is taken as an intercalation object, and the Tegafur is assembled between LDHs layers by a coprecipitation method or a structure reconstruction method to prepare the Tegafur/LDHs nanometer hybrid. The Tegafur/LDHs nanometer hybrid and the preparation method have the advantages that: the nanometer hybrid prepared by the two methods is large in medicament-loading capacity and has good slow-release effect; the adopted preparation method is simple and the condition is moderate; the structure, compositions and the release rate of the Tegafur/LDHs can be controlled by adjusting a synthetic method or synthesis conditions or changing factors such as concentration, the pH, temperature, aging time and the like in the synthetic process of the medicaments.

Description

technical field [0001] The invention belongs to the technical field of new materials and pharmaceutical preparations, and relates to a Tegafur / layered double metal hydroxide (LDHs) nano hybrid and a preparation method thereof. Background technique [0002] With the development of science and the advancement of science and technology, people's requirements for the treatment effect and treatment methods of diseases are increasing day by day. How to improve the curative effect, simplify the way of medication, and reduce the toxic and side effects of drugs is the research focus of scientific and technological workers. Especially for highly toxic drugs, in order to facilitate patients to take them, while ensuring the effective therapeutic concentration, reduce the toxic and side effects of drugs, and avoid the emergence of drug resistance, the effective delivery and sustained release of drugs is undoubtedly an effective method. way. In this effective approach, the development o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/02A61K31/513A61P35/00
Inventor 侯万国徐洁张少杰
Owner QINGDAO UNIV OF SCI & TECH
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