Nano hybrid of cytarabine/layered double-metal hydroxides and preparation process of nano hybrid

A nano-hybrid, layered bimetallic technology, applied in the direction of pharmaceutical formulations, drug combinations, medical preparations of non-active ingredients, etc., can solve the problem of losing anti-tumor activity, achieve good sustained-release effect, mild conditions, and easy preparation The effect of simple method

Inactive Publication Date: 2013-02-13
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the deoxycytosine enzyme in normal tissues can rapidly deaminate it into uracil cytarabine and lose its anti-tumor activity. In order to maintain its effective blood concentration, it must be administered repeatedly and continuously

Method used

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  • Nano hybrid of cytarabine/layered double-metal hydroxides and preparation process of nano hybrid
  • Nano hybrid of cytarabine/layered double-metal hydroxides and preparation process of nano hybrid
  • Nano hybrid of cytarabine/layered double-metal hydroxides and preparation process of nano hybrid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Step a: 10.26g (0.040mol) Mg(NO 3 ) 2 ·6H 2 O and 7.50g (0.020mol) Al(NO 3 ) 3 9H 2 O was dissolved in 120ml deionized water.

[0046] Step b: Dissolve 0.69 g of SDS in 120 ml of deionized water.

[0047] Step c: Dissolve 2.4g of NaOH in 120ml of deionized water.

[0048] Step d: Dissolve 5.59 g of cytarabine in 50 ml of deionized water.

[0049] Step e: Add the solution of step a and the solution of step c to the solution of step b at the same time, stir and control the pH to 10, the reaction temperature is 65°C, stir and react for 24 hours; filter, wash with water until neutral, filter cake at 80°C Peptization for 24 hours to obtain SDS-modified LDHs;

[0050] f. Disperse 0.2 g of the SDS-modified LDHs solid obtained in step e into the solution in step d, mix thoroughly, and react at 65° C. for 2 days to obtain a cytarabine / LDHs nanohybrid.

[0051] By XRD spectrum ( figure 1 ) shows that the cytarabine / LDHs nano-hybrid has a layered crystal structure, and t...

Embodiment 2

[0054] Step a: 0.030mol of Ni(NO 3 ) 2 ·6H 2 O and 0.010mol Fe(NO 3 ) 3 9H 2 O was dissolved in 40ml deionized water.

[0055] Step b: Dissolve 0.60 g of SDS in 40 ml of deionized water.

[0056] Step c: Dissolve 4.0 g of NaOH in 40 ml of deionized water.

[0057] Step d: Dissolve 11.18 g of cytarabine in 50 ml of deionized water.

[0058] Step e: Add the solution of step a and the solution of step c to the solution of step b at the same time, stir and control the pH to 11, the reaction temperature is 45°C, stir and react for 36 hours; filter, wash with water until neutral, filter cake at 80°C Peptization for 24 hours to obtain SDS-modified LDHs;

[0059] f. Disperse 0.2 g of the SDS-modified LDHs solid obtained in step e into the solution in step d, mix thoroughly, and react at 45° C. for 4 days to obtain a cytarabine / LDHs nanohybrid.

[0060] The sample was analyzed by ultraviolet spectrophotometry, and the content of cytarabine was determined to be 45.63%.

Embodiment 3

[0062] Step a: 0.010mol of ZnCl 2 ·6H 2 O and 0.010mol AlCl 3 ·6H 2 O was dissolved in 35ml deionized water.

[0063] Step b: Dissolve 0.11 g of SDS in 40 ml of deionized water.

[0064] Step c: Dissolve 1.6 g of NaOH in 40 ml of deionized water.

[0065] Step d: 2.79 g of cytarabine was dissolved in 50 ml of deionized water.

[0066] Step e: Add the solution of step a and the solution of step c to the solution of step b at the same time, stir and control the pH to 9, the reaction temperature is 20°C, stir and react for 20 hours; filter, wash with water until neutral, filter cake at 80°C Peptization for 24 hours to obtain SDS-modified LDHs;

[0067] f. Disperse 0.2 g of the SDS-modified LDHs solid obtained in step e into the solution in step d, mix thoroughly, and react at 25° C. for 3 days to obtain a cytarabine / LDHs nanohybrid.

[0068] The sample was analyzed by ultraviolet spectrophotometry, and the content of cytarabine was determined to be 1.05%.

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Abstract

The invention relates to a nano hybrid of an anti-cancer drug of cytarabine / layered double-metal hydroxides (LDHs) and a preparation process of the nano hybrid. The process comprises the steps of preparing the nano hybrid of the cytarabine / LDHs for slow releasing of the cytarabine with LDHs serving as carriers, so that the drug effect is improved, and the toxic side effect of the drug is reduced. The process comprises that LDHs serve as main bodies, the cytarabine serves as an intercalated object, and the cytarabine is assembled between layers of LDHs through a secondary assembling method or a structure reconstruction method to prepare the nano hybrid of the cytarabine / LDHs. The process has the advantages that the drug loading capacity of nano hybrids obtained through two methods is large, and the good slow releasing effect can be achieved; the adopted preparation process is simple and conditions are mild; and the structure, the composition and the releasing speed of the nano hybrid of the cytarabine / LDHs can be controlled by adjustment of the synthetic method or synthetic conditions or by changing of the concentration of the drug and factors such as the pH, the temperature and the ageing time of the synthetic process.

Description

technical field [0001] The invention belongs to the technical field of new materials and pharmaceutical preparations, and relates to a cytarabine / 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 developmen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K47/02A61K31/7068A61P35/00A61P35/02
Inventor 赵军徐洁
Owner QINGDAO UNIV OF SCI & TECH
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