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Hydrotalcite doxifluridine slow release formulation and preparation method thereof

A technology of oxyfluridine sustained-release agent and deoxyfluridine, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., and can solve the problem of deoxyfluridine bioavailability It can improve the bioavailability, reduce the irritating effect, and reduce the irritating effect.

Inactive Publication Date: 2009-02-18
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the common sustained and controlled release systems use organic matter as the skeleton material, which may have the following problems: low mechanical strength, easy aging, and plasticizer required; poor thermal stability, poor water solubility and fluidity; low drug loading; preparation During the process, organic solvents are highly toxic and difficult to recycle (Gao Shen, New dosage forms and new technologies for modern drugs, People's Military Medical Publishing House, 2002)
Therefore, the bioavailability of doxifluridine taken in a conventional way is low, and the development of a new doxifluridine sustained-release preparation has very obvious practical significance
[0006] However, there are no reports of doxifluridine sustained-release dosage forms based on hydrotalcite materials.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (1). Firing of carbonate-type hydrotalcite precursor and its LDO

[0030] Accurately weigh 25.64g (0.100mol) Mg(NO 3 ) 2 ·6H 2 O and 18.75g (0.050mol) Al(NO 3 ) 2 9H 2 O was dissolved in 150ml deionized water to obtain solution A. Where Mg / Al is 2 / 1. Another weighed 14g (0.35mol) NaOH and 10.6g (0.1mol) NaOH 2 CO 3 Dissolve in 150 ml deionized water to obtain solution B. The two solutions were quickly mixed in a fully back-mixing explosive nucleation reactor, stirred vigorously for 2 minutes, transferred the slurry to a three-neck flask for crystallization at 100°C for 12 hours, centrifuged, washed until the pH value was 7, and dried at 60°C for 24 hours to obtain MgAl-CO 3 -LDH. The prepared MgAl-CO 3 -LDH is placed in a muffle furnace, in air at 5°C min -1 Raise the temperature to 500°C, keep the temperature constant for 2 hours, and then cool down to room temperature with the furnace temperature to obtain the roasted sample MgAl-LDO.

[0031] (2). Prepa...

Embodiment 2

[0035] (1). Firing of carbonate-type hydrotalcite precursor and its LDO

[0036] Accurately weigh 25.64g (0.100mol) Mg(NO 3 ) 2 ·6H 2 O and 12.37g (0.033mol) Al(NO 3 ) 2 9H 2 O was dissolved in 150ml deionized water to obtain solution A. Where Mg / Al is 3 / 1. Another weighed 8g (0.20mol) NaOH and 5.3g (0.05mol) NaOH 2 CO 3 Dissolve in 150 ml deionized water to obtain solution B. The two solutions were quickly mixed in a fully back-mixed explosive nucleation reactor, stirred vigorously for 5 minutes, transferred the slurry to a three-neck flask for crystallization at 100°C for 6h, centrifuged, washed until the pH value was 7, and dried at 60°C for 24h to obtain MgAl-CO 3 -LDH. The prepared MgAl-CO 3 -LDH placed in muffle furnace, 10°C min in air -1 Raise the temperature to 450°C, keep the temperature constant for 4 hours, and then cool down to room temperature with the furnace temperature to obtain the roasted sample MgAl-LDO.

[0037] (2). Preparation of doxiflurid...

Embodiment 3

[0041] (1). Firing of carbonate-type hydrotalcite precursor and its LDO

[0042] Accurately weigh 25.64g (0.100mol) Mg(NO 3 ) 2 ·6H 2 O and 9.29g (0.025mol) Al(NO 3 ) 2 9H 2 O was dissolved in 150ml deionized water to obtain solution A. Where Mg / Al is 4 / 1. Another weighed 4g (0.1mol) NaOH and 5.3g (0.05mol) NaOH 2 CO 3 Dissolve in 150 ml deionized water to obtain solution B. The two solutions were quickly mixed in a fully back-mixing explosive nucleation reactor, stirred vigorously for 2 minutes, transferred the slurry to a three-neck flask for crystallization at 100°C for 12 hours, centrifuged, washed until the pH value was 7, and dried at 60°C for 48 hours to obtain MgAl-CO 3 -LDH. The prepared MgAl-CO 3 -LDH is placed in a muffle furnace, in air at 10°C min -1 Raise the temperature to 450°C, keep the temperature constant for 4 hours, and then cool down to room temperature with the furnace temperature to obtain the roasted sample MgAl-LDO.

[0043] (2). Prepara...

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PUM

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Abstract

The invention relates to a hydrotalcite doxifluridine sustained release agent and a preparation method thereof, which belong to the technical field of hydrotalcite materials. The formula of the hydrotalcite doxifluridine sustained release agent is (M<2+>)1-x(N<3+>)x(OH) 2(5dFUR<->)a(B)bN(OH)3.mH2O. The hydrotalcite doxifluridine sustained release agent is a medicine-hydrotalcite composite material; the mass percent of doxifluridine in the sustained release agent is between 29.72 and 38.85 percent and the mass percent of water in the sustained release agent is between 4 and 11 percent; and the lasting period of sustained release is between 0.1 and 15 hours. The preparation method comprises the following steps: carbonate hydrotalcite is prepared by the coprecipitation method at first and then is sintered into composite oxide LDO; and the composite oxide LDO is mixed with a doxifluridine solution and doxifluridine intercalative hydrotalcite with the sustained release performance is obtained by the restoring method to assemble the doxifluridine between hydrotalcite layers. The hydrotalcite doxifluridine sustained release agent and the preparation method have the advantages of reinforcing the stability, improving the bioavailability, avoiding direct contact of the doxifluridine and a gastrointestinal tract and reducing the stimulary function of the doxifluridine on the gastrointestinal tract.

Description

technical field [0001] The invention belongs to the technical field of hydrotalcite materials, and in particular provides a hydrotalcite-like doxifluridine slow-release agent and a preparation method thereof. Background technique [0002] There are more or less disadvantages in conventional drug use, such as short half-life and poor selectivity, resulting in side effects such as high blood drug concentration in a short period of time. In particular, anticancer drugs have a very large stimulating effect on the gastrointestinal tract, and there have even been reports of death due to diarrhea (Fang Jiahua, Journal of Bengbu Medical College, Volume 31, No. 5, September 2006). In response to these problems, the researchers proposed the concept of drug controlled release technology. Drug controlled release technology refers to the existence of a specific system, the active agent in the system can be released into the surrounding environment at a preset speed or at a preset locati...

Claims

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Application Information

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IPC IPC(8): A61K31/7072A61K47/02A61K47/48A61P35/00A61K47/52
Inventor 张慧盘登科马文瑞段雪
Owner BEIJING UNIV OF CHEM TECH
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