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Tegafur-layered double-metal hydroxide nanometer hybrid modified with polyethylene glycol derivative on surface and preparation of nanometer hybrid

A nano-hybrid, layered bimetallic technology, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of leukopenia and thrombocytopenia, and achieve mild and good reactions. Dispersion and stability, good sustained release effect

Inactive Publication Date: 2014-01-15
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Tegafur (Tegafur, TF) is a derivative of fluorouracil, which is used to treat various cancers of the stomach, intestine, liver, etc. Compared with fluorouracil, the therapeutic index is improved and the toxicity is reduced, but there are still bone marrow suppression, gastrointestinal reactions, leukopenia and thrombocytopenia and other side effects

Method used

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  • Tegafur-layered double-metal hydroxide nanometer hybrid modified with polyethylene glycol derivative on surface and preparation of nanometer hybrid
  • Tegafur-layered double-metal hydroxide nanometer hybrid modified with polyethylene glycol derivative on surface and preparation of nanometer hybrid
  • Tegafur-layered double-metal hydroxide nanometer hybrid modified with polyethylene glycol derivative on surface and preparation of nanometer hybrid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] a: Preparation of tegafur-layered double hydroxide nanohybrid (TF-LDH)

[0036] Weigh 0.020mol of Zn(NO 3 ) 2 ·6H 2 O and 0.010mol AlCl 3 ·6H 2 O was dissolved in 60ml ultrapure water to form a mixed salt solution; tegafur was dissolved in the above mixed salt solution; a NaOH solution with a concentration of 0.5mol / L was prepared; under stirring, the tegafur salt solution was added dropwise to In NaOH alkali solution, adjust the pH value of the system to 10; react at 60°C for 3h; centrifuge and wash and peptize at 80°C for 24h to obtain the TF-LDH nano-hybrid product.

[0037] b: Synthesis of polyethylene glycol monomethyl ether sulfate (MPS)

[0038] Dissolve 0.0006mol of polyethylene glycol monomethyl ether with a molecular weight of 5000 in 35mL of chloroform solution, pour it into a 100ml three-necked flask, control the temperature at 10°C, and stir under reflux; add 0.00075mol of chlorosulfonic acid dropwise, and react in a water bath at 25°C for 1 hour; Aft...

Embodiment 2

[0044] a: Preparation of tegafur-layered double hydroxide nanohybrid (TF-LDH)

[0045] Weigh 0.030mol of Zn(NO 3 ) 2 ·6H 2 O and 0.010mol AlCl 3 ·6H 2 O was dissolved in 40ml ultrapure water to form a mixed salt solution; tegafur was dissolved in the above mixed salt solution; a NaOH solution with a concentration of 1.0mol / L was prepared; under stirring, the tegafur salt solution was added dropwise to In NaOH alkaline solution, adjust the pH value of the system to 12; react at 90°C for 1h; centrifuge and wash and peptize at 90°C for 12h to obtain the TF-LDH nano-hybrid product.

[0046] b: Synthesis of polyethylene glycol monomethyl ether sulfate (MPS)

[0047] Dissolve 0.005mol of polyethylene glycol monomethyl ether with a molecular weight of 600 in 35mL of chloroform solution, pour it into a 100ml three-neck flask, control the temperature at 10°C, and stir under reflux; add 0.01mol of chlorosulfonic acid dropwise, and react in a water bath at 25°C for 2 hours; After t...

Embodiment 3

[0052] a: Preparation of tegafur-layered double hydroxide nanohybrid (TF-LDH)

[0053] Weigh 0.010mol of Zn(NO 3 ) 2 ·6H 2 O and 0.010mol AlCl 3 ·6H 2 O was dissolved in 100ml ultrapure water to form a mixed salt solution; tegafur was dissolved in the above mixed salt solution; a NaOH solution with a concentration of 0.3mol / L was prepared; under stirring, the tegafur salt solution was added dropwise to In NaOH alkali solution, adjust the pH value of the system to 8; react at 45°C for 2h; centrifuge and wash and peptize at 60°C for 18h to obtain the TF-LDH nano-hybrid product.

[0054] b: Synthesis of polyethylene glycol monomethyl ether sulfate (MPS)

[0055] Dissolve 0.003mol of polyethylene glycol monomethyl ether with a molecular weight of 5000 in 35mL of chloroform solution, pour it into a 100ml three-necked flask, control the temperature at 10°C, and stir under reflux; add 0.0075mol of chlorosulfonic acid dropwise, and react in a water bath at 25°C for 0.5h ; After ...

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Abstract

The invention discloses a tegafur-layered double-metal hydroxide nanometer hybrid modified with polyethylene glycol monomethyl ether sulfate on the surface (abbreviated to TF-LDH-MPS) and a preparation method of the nanometer hybrid. The invention aims to provide a method as follows: using the tegafur (TF) intercalated LDH (TF-LDH) nanometer hybrid as a model system, using the polyethylene glycol derivative (PEG) polyethylene glycol monomethyl ether sulfate (MPS) with pretending invisibility as a modifier to prepare the MPS modified TF-LDH nanometer hybrid. The nanometer hybrid can be used for improving the dispersion stability and the pretending invisibility of the tegafur-layered double-metal hydroxide, and improving targeted transport and controlled release effects of tegafur, so that the pharmaceutical effect is improved, and the toxic and side effects of the drug are reduced, and the like.

Description

technical field [0001] The invention belongs to the technical field of materials and pharmaceutical preparations, and relates to a surface-modified polyethylene glycol derivative tegafur-layered double metal hydroxide nano hybrid (TF-LDH-MPS) 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 anticancer drugs, the research and development of new high-efficiency drug targeting-controlled release systems is one of the important topics in the field of pharmacy. [0003] Layered double hydroxides (Layered Double Hydroxides, LDH), also known as hydrotalcite-like compounds (HTlc), ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/513A61K9/14A61P35/00A61K47/60
Inventor 徐洁李东祥侯万国
Owner QINGDAO UNIV OF SCI & TECH
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