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Tegafur/layered double hydroxide (TF/LDHs) nanohybrid-magnetic matrix compound and preparation method thereof

A nano-hybrid, magnetic matrix technology, applied in the direction of drug combination, medical preparations containing active ingredients, drug delivery, etc., can solve the problems of leukocyte and thrombocytopenia, and achieve the effect of mild reaction and simple process

Inactive Publication Date: 2013-07-10
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, TF) is a derivative of fluorouracil, which is used to treat various cancers such as stomach, intestine, liver, etc. Compared with fluorouracil, its therapeutic index is improved and its toxicity is reduced, but it still has myelosuppression, gastrointestinal reactions, leukopenia and thrombocytopenia and other side effects

Method used

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  • Tegafur/layered double hydroxide (TF/LDHs) nanohybrid-magnetic matrix compound and preparation method thereof
  • Tegafur/layered double hydroxide (TF/LDHs) nanohybrid-magnetic matrix compound and preparation method thereof
  • Tegafur/layered double hydroxide (TF/LDHs) nanohybrid-magnetic matrix compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] a. 5.95g (0.02mol) Zn (NO 3 ) 2 ·6H 2 O and 3.75g (0.01mol) Al(NO 3 ) 3 9H 2 O was dissolved in 150 mL deionized water.

[0032] b. The magnetic matrix MgFe 2 o 4 Dissolved in the mixed salt solution prepared in step a, the mass ratio of the magnetic matrix to the trivalent metal salt is 1:50;

[0033] c. preparation concentration is the NaOH solution of 0.3mol / L;

[0034] d. Dissolve 1.23 g of tegafur in the aqueous alkali solution prepared in step c to prepare a tegafur solution with a concentration of 0.08 mol / L.

[0035] e. Add the solution of step d to the solution of step b, stir and control the pH to 10, the reaction temperature is 20°C; the reaction time is 3 hours, and then the resulting slurry is aged at 20°C for 36 hours, filtered, and washed with water until neutral , dried at 60°C to obtain MgFe 2 o 4 (TF / LDHs) nanocomposites.

[0036] By XRD spectrum ( figure 1 f) It can be seen that the MgFe 2 o 4 (TF / LDHs) nanocomposites have a layered cry...

Embodiment 2

[0038] a. 5.95g (0.02mol) Zn (NO 3 ) 2 ·6H 2 O and 3.75g (0.01mol) Al(NO 3 ) 3 9H 2 O was dissolved in 150 mL deionized water.

[0039] b. The magnetic matrix MgFe 2 o 4 Dissolved in the mixed salt solution prepared in step a, the mass ratio of the magnetic matrix to the trivalent metal salt is 1:20;

[0040] c. Prepare NaCO with a concentration of 3mol / L 3 solution;

[0041] d. Dissolve 0.50 g of tegafur in the aqueous alkali solution prepared in step c to prepare a tegafur solution with a concentration of 0.02 mol / L.

[0042] e. Add the solution of step d to the solution of step b, stir and control the pH to 12, the reaction temperature is 80°C; the reaction time is 1 hour, and then the resulting slurry is aged at 80°C for 10 hours, filtered, and washed with water until neutral , dried at 60°C to obtain MgFe 2 o 4 (TF / LDHs) nanocomposites.

[0043] By XRD spectrum ( figure 1 g) It can be seen that the MgFe 2 o 4 (TF / LDHs) nanocomposites have a layered crystal...

Embodiment 3

[0046] a. 5.95g (0.02mol) Zn (NO 3 ) 2 ·6H 2 O and 3.75g (0.01mol) Al(NO 3 ) 3 9H 2 O was dissolved in 150 mL deionized water.

[0047] b. The magnetic matrix MgFe 2 o 4 Dissolved in the mixed salt solution prepared in step a, the mass ratio of the magnetic matrix to the trivalent metal salt is 1:10;

[0048] c. preparation concentration is the NaOH solution of 0.5mol / L;

[0049] d. Dissolve 1.40 g of tegafur in the aqueous alkali solution prepared in step c to prepare a tegafur solution with a concentration of 0.09 mol / L.

[0050] e. Add the solution of step d to the solution of step b, stir and control the pH to 11, and the reaction temperature is 65°C; the reaction time is 2 hours, then the resulting slurry is aged at 65°C for 24 hours, filtered, and washed with water until neutral , dried at 60°C to obtain MgFe 2 o 4 (TF / LDHs) nanocomposites.

[0051] By XRD spectrum ( figure 1 h) It can be seen that the MgFe 2 o 4 (TF / LDHs) nanocomposites have a layered cry...

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Abstract

The invention discloses a tegafur / layered double hydroxide (TF / LDHs) nanohybrid-magnetic matrix compound and a preparation method thereof. The preparation method utilizes LDHs as carriers to prepare the TF / LDHs nanohybrid-magnetic matrix compound. The TF / LDHs nanohybrid-magnetic matrix compound is used for targeted delivery and controlled release of tegafur, improves drug effects and reduces drug toxic and side effects. By a coprecipitation method, Fe3O4 or MgFe2O4 as a magnetic matrix is synthesized into the TF / LDHs nanohybrid-magnetic matrix compound which is a nano-complex composed of the magnetic matrix and TF intercalated LDHs coated on the magnetic matrix and is recorded as magnetic matrix @ (TF / LDHs). The TF / LDHs nanohybrid-magnetic matrix compound has strong magnetism and has good TF slow release effects. The preparation method has simple processes and allows mild reaction conditions. Through adjustment of magnetic matrix @ (TF / LDHs) nano-compound synthesis conditions and change of a drug concentration, a synthesis temperature, magnetic matrix content and applied magnetic field intensity, the structure, the composition and a release rate of the magnetic matrix @ (TF / LDHs) can be controlled.

Description

technical field [0001] The invention belongs to the technical field of materials and pharmaceutical preparations, and relates to a composite of tegafur / hydrotalcite-like nano-hybrids (TF / LDHs) and a magnetic matrix and a preparation method thereof. Background technique [0002] As we all know, the severe toxic and side effects of drugs, especially anticancer drugs, is a problem that plagues the medical field. Therefore, the research and development of new high-efficiency drug targeting-controlled release systems is one of the important topics in the field of pharmacy. Magnetically targeted drug delivery systems usually consist of magnetic substrates, carrier materials, drugs and other excipients. With the help of an external magnetic field, the drug-loading system with magnetic response can be gathered at the target site to release the drug, thereby increasing the drug concentration at the target site and reducing the side effects of the drug on normal tissues. [0003] Hyd...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/513A61K47/02A61P35/00
Inventor 徐洁侯万国赵满赵军
Owner QINGDAO UNIV OF SCI & TECH
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