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Nitroimidazoles medicine nano montmorillonite sustained-release agent and preparation method thereof

A nano-montmorillonite and nitroimidazole technology, which is applied in the directions of drug delivery, pharmaceutical formulations, antibacterial drugs, etc., can solve the problems of difficulty in forming cations, improve bioavailability, and show alkalinity, so as to improve the concentration and reduce the Effects of dosage and type of drug

Inactive Publication Date: 2009-05-06
SOUTHERN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, nitroimidazole drug molecules are difficult to form cations in aqueous solution and are alkaline, so they cannot be inserted into Na-montmorillonite by known methods to make sustained-release preparations to improve bioavailability

Method used

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  • Nitroimidazoles medicine nano montmorillonite sustained-release agent and preparation method thereof
  • Nitroimidazoles medicine nano montmorillonite sustained-release agent and preparation method thereof
  • Nitroimidazoles medicine nano montmorillonite sustained-release agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] 1. Stir 20 g of raw material montmorillonite in 500 mL of saturated NaCl solution to form a stable suspension; stir the suspension at 35°C for 5 hours. Filter with suction, and then wash the filtrate 4 times with deionized water. Vacuum-dry at 70°C to constant weight, and ball mill until the particle size is 20-30 μm to obtain Na-montmorillonite. Store dry.

[0051] 2. Mix 10 g of Na-montmorillonite obtained above with 6 g of metronidazole, add 200 ml of deionized water, adjust the pH value to 5.0 with 3% hydrochloric acid solution, and stir the mixture at 60° C. for 2 hours. Suction filtration, then wash the filtrate several times with deionized water, detect the filtrate without metronidazole by ultraviolet spectrophotometer, dry it in vacuum at 60°C to constant weight, and ball mill until the particle size is 20-30 μm, to obtain metronidazole Nano montmorillonite. Store dry.

[0052] Collect all the filtrate in step 2, filter it with a 0.45um microporous membrane...

Embodiment 2

[0054] 1. Same as embodiment 1.

[0055] 2. Mix 10 g of Na-montmorillonite obtained above with 8 g of metronidazole, add 200 ml of deionized water, adjust the pH value to 4.0 with 3% hydrochloric acid solution, and stir the mixture at 70° C. for 3 hours. Suction filtration, and then wash the filtrate several times with deionized water, detect that there is no metronidazole in the filtrate by ultraviolet spectrophotometer, dry it in vacuum at 60°C to constant weight, and ball mill it until the particle size is 20-30 μm, then you can get metronidazole nano Montmorillonite. Store dry.

[0056] Collect all the filtrate in step 2, filter it with a 0.45um microporous membrane, take an appropriate amount of the filtrate and use a Biomat-5 ultraviolet spectrophotometer to measure the ultraviolet light absorbance value, and calculate the remaining drug 5.76g. That is, 2.24g of metronidazole was intercalated in 10g of montmorillonite; XRD test, IR test and UV spectrogravimetric analys...

Embodiment 3

[0058] 1. Same as embodiment 1.

[0059] 2. Mix 10 g of Na-montmorillonite obtained above with 8 g of metronidazole, add 200 ml of deionized water, adjust the pH to 3.0 with 3% hydrochloric acid solution, and stir the mixture at 80° C. for 4 hours. Suction filtration, and then wash the filtrate several times with deionized water, detect that there is no metronidazole in the filtrate by ultraviolet spectrophotometer, dry it in vacuum at 60°C to constant weight, and ball mill it until the particle size is 20-30 μm, then you can get metronidazole nano Montmorillonite. Store dry.

[0060] Collect all the filtrate in step 2, filter it with a 0.45um microporous membrane, take an appropriate amount of the filtrate and use a Biomat-5 ultraviolet spectrophotometer to measure the ultraviolet light absorbance value, and calculate the remaining drug 5.6g. That is, 2.4g of metronidazole is intercalated in 10g of montmorillonite; it is confirmed by XRD test, IR test and ultraviolet spectr...

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Abstract

The invention provides a nanometer montmorillonite sustained release agent of an azomycin medicament The sustained release agent is prepared by inserting 10 to 45 weight portions of the azomycin medicament into the interlayer of 100 weight portions of Na-montmorillonite in a protonizing way under the condition of the pH value of 1.0 to 5.0 by adopting a liquor intercalation method; the azomycin medicament is metronidazole or tinidazole; the Na-montmorillonite is obtained by using Na<+> to replace Ca<2+> and Mg<+2> in the material of montmorillonite. The sustained release agent takes the montmorillonite as the vector of the azomycin medicament, which not only has the effects of releasing the medicament and improving the targeting, but also combines the characteristic that the montmorillonite can absorb pathogens and toxins, and can greatly improve the concentration of the partial medicament in a body, thereby reducing the medication times and species of the medicament.

Description

technical field [0001] The invention relates to a medical preparation, in particular to a preparation of nitroimidazole drugs. Background technique [0002] Nitroimidazoles are a class of drugs with strong bactericidal power, broad antibacterial spectrum, less drug resistance and low price, and are widely used in clinic. Commonly used nitroimidazoles mainly include metronidazole, tinidazole, and ornidazole, among which metronidazole, tinidazole, and ornidazole have unique killing effects on anaerobic bacteria and protozoa. At present, the common dosage forms of nitroimidazoles are tablets and injections. The common side effects of tablets are gastrointestinal reactions, such as nausea, vomiting or diarrhea, etc.; while injections can cause nervous and blood system reactions, such as inducing epilepsy. , Reduce granulocytes, etc. [0003] In the prior art, antibacterial drugs such as chlorhexidine acetate, miconazole nitrate, and benzalkonium bromide are also inserted into ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4164A61K47/04A61P31/04
Inventor 韦莉萍路新卫杨建华
Owner SOUTHERN MEDICAL UNIVERSITY
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