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5-flucytosine/hydrotalcite-like NANO hybrid compound and preparation method thereof

A technology of nano-hybrids and flucytosine, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, and inorganic non-active ingredients, etc. It can solve problems such as adverse reactions, leukopenia and thrombocytopenia, liver toxicity, etc., and achieve technological The effect of simplicity, mild reaction, and good sustained-release effect

Inactive Publication Date: 2007-12-12
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use is often accompanied by adverse reactions, mainly gastrointestinal reactions, bone marrow suppression, leukocyte and thrombocytopenia, and occasionally liver toxicity, etc.

Method used

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  • 5-flucytosine/hydrotalcite-like NANO hybrid compound and preparation method thereof
  • 5-flucytosine/hydrotalcite-like NANO hybrid compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Step a: 5.95g (0.020mol) of Zn(NO 3 ) 2 ·6H 2 O and 3.75g (0.010mol) Al(NO 3 ) 3 9H 2 O was dissolved in 35ml of water and heated to 40°C.

[0035] Step b: 1.29 g (0.010 mol) of solid 5-FC was dissolved in 78 ml of aqueous ammonia (6 wt%).

[0036] Step c: Add the solution of step b to the solution of step a, keep stirring and control the pH to 8.5, and the reaction temperature is 40°C. Then the resulting slurry was aged at 40° C. for 3 hours, filtered, washed with water until neutral, and aged at 60° C. for 24 hours to obtain a 5-FC / HTlc nano-hybrid.

[0037] Shown by the XRD spectrum (Fig. 1), the 5-FC / HTlc nano-hybrid has a hydrotalcite-like crystal structure, and the interlayer spacing (d 003 ) shows that 5-fluorocytosine has been inserted into the interlayer and coexists with nitrate ions in the interlayer.

[0038] The IR spectrum (Figure 2) further confirmed that 5-fluorocytosine had intercalated into the interlayer.

[0039] The sample was analyzed by u...

Embodiment 2

[0041] Step a: 5.95g (0.020mol) of Zn(NO 3 ) 2 ·6H 2 O and 3.75g (0.010mol) Al(NO 3 ) 3 9H 2 O was dissolved in 35ml of water and heated to 40°C.

[0042] Step b: 2.58g (0.020mol) of solid 5-FC was dissolved in 78ml of aqueous ammonia (6wt%).

[0043] Step c: Add the solution of step b to the solution of step a, keep stirring and control the pH to 10, and the reaction temperature is 40°C. Then the resulting slurry was aged at 40° C. for 3 hours, filtered, washed with water until neutral, and aged at 60° C. for 24 hours to obtain a 5-FC / HTlc nano-hybrid.

[0044] The XRD spectrum (Fig. 3) shows that the 5-FC / HTlc nano-hybrid has a hydrotalcite-like crystal structure, and the interlayer spacing d 003 It was found that 5-fluorocytosine was inserted into the interlayer.

[0045] The sample was analyzed by ultraviolet spectrophotometry, and the content of 5-fluorocytosine was determined to be 30.49%.

Embodiment 3

[0047] Step a: 0.030mol of ZnSO 4 ·6H 2 O and 0.010mol Al 2 (SO 4 ) 3 18H 2 O was dissolved in 35ml of water and heated to 40°C.

[0048] Step b: 1.29 g (0.010 mol) of solid 5-FC was dissolved in 78 ml of aqueous ammonia (6 wt%).

[0049] Step c: Add the solution of step b to the solution of step a, keep stirring and control the pH to 8.5, and the reaction temperature is 30°C. Then the resulting slurry was aged at 30° C. for 18 hours, filtered, washed with water until neutral, and aged at 60° C. for 24 hours to obtain a 5-FC / HTlc nano-hybrid.

[0050] The sample was analyzed by ultraviolet spectrophotometry, and the content of 5-fluorocytosine was determined to be 16.30%.

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Abstract

A nano-hybrid of 5-fluctyosine (5-FC) and hydrotalcite-like compounds (HTlc) belongs to technology field of new material and pharmaceutical preparation.5-FC / HTlc nanohybrid is synthesized by mixed salt solution of divalent metal ion trivalent metal ion and 5-fluctyosine alkali solution throug coprecipitation method, and has a chemical constitution general formula of [MII(1-x)MIIIx(OH)2](An-)a(5-FC-)b.nH2O.The inventive 5-FC / HTlc nanohybrid has simple and easy synthetic method, large drug loading dosage, certain sustained release effect compared with raw material of 5-FC, and important significance for clinical application of 5-FC.

Description

technical field [0001] The invention belongs to the technical field of materials and pharmaceutical preparations, in particular to a nano-hybrid material 5-fluorocytosine (5-FC) / hydrotalcite-like (HTlc) nano-hybrid and a preparation method thereof. Background technique [0002] Biological / HTlc nano-hybrid materials are a new class of functional materials developed in the interdisciplinary fields of materials science, pharmacology, chemistry, and microbiology in recent years. growing concern in the industry. [0003] Hydrotalcite-like compounds (Hydrotalcite-like Compounds, HTlc) is composed of divalent metal ions and trivalent metal ions with a hydrotalcite layered structure of hydroxide. HTlc has unique structural features: first, it has a layered crystal structure, and the layers have structural positive charges; second, there are exchangeable anions between the layers. The special structure endows it with special properties. Exploration and research have proved that HTl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/02A61K31/513A61P31/10
Inventor 侯万国刘春霞
Owner SHANDONG UNIV
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