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Glucosamine-behenic acid grafting substance and preparation method

A technology of glucosamine and ‐behenic acid, which is applied in the directions of drug combinations, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., can solve the problems of increasing the water solubility, poor water solubility, and low bioavailability of poorly soluble drugs, and achieves The effect of ideal biodegradability, no pollution to the environment, and simple treatment process

Inactive Publication Date: 2016-09-07
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Many drugs have poor water solubility and low bioavailability, so a suitable drug delivery system is needed to increase the water solubility of these poorly soluble drugs in clinical application

Method used

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  • Glucosamine-behenic acid grafting substance and preparation method
  • Glucosamine-behenic acid grafting substance and preparation method
  • Glucosamine-behenic acid grafting substance and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Accurately weigh 5 mg of the glucosamine-behenic acid graft provided by the present invention, add it to 5 mL of deionized water, and dissolve it ultrasonically in a water bath to obtain a glucosamine-behenic acid graft micelle solution, which is measured with a Malvern laser particle size potentiometer The number average particle size is 55nm, see figure 1 .

Embodiment 2

[0025] Accurately weigh 4 mg of valproic acid, dissolve it in 4 mL of ethanol, add it to a 25 mL rotary evaporator, then add 20 mg of glucosamine-behenic acid graft, and dissolve it ultrasonically in a water bath. The ethanol was removed by rotary evaporation, and the obtained solid was sonicated with 20 mL of water, namely drug-loaded micelles-1. The number-average particle diameter measured with a Malvern laser particle size potentiometer is 29nm, see figure 2 .

Embodiment 3

[0027] Accurately weigh 10 mg of valproic acid, dissolve it in 4 mL of ethanol, add it to a 25 mL rotary evaporator, then add 20 mg of glucosamine-behenic acid graft, and dissolve it ultrasonically in a water bath. The ethanol was removed by rotary evaporation, and the obtained solid was sonicated with 20 mL of water, namely drug-loaded micelles-2. The number-average particle diameter measured with a Malvern laser particle size potentiometer is 102nm, see image 3 .

[0028] Adopt high performance liquid chromatography to measure its encapsulation efficiency and drug loading capacity, the chromatographic conditions are as follows: mobile phase: (tetrabutylammonium bromide (5mmol / L)-potassium dihydrogen phosphate (20mmol / L)):methanol=25: 75, pH=3.6; column temperature 40°C; detection wavelength 216nm; injection volume 20μL. Adopt standard curve method to measure valproic acid content, standard curve preparation method is as follows: prepare the valproic acid solution of 500 μ...

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Abstract

The invention provides a glucosamine-behenic acid grafting substance which is prepared by taking glucosamine and behenic acid as raw materials and performing amidation reaction under the catalysis of EDC.HCl. The glucosamine-behenic acid grafting substance provided by the invention can be loaded with a hydrophobic drug in a form of a micelle, so that the drug-loaded micelle with high drug loading capacity is obtained, and the dissolvability and the stability of the hydrophobic drug in water are enhanced, so that the application to the preparation of the drug-loaded micelle with high drug loading capacity can be realized. The glucosamine-behenic acid grafting substance provided by the invention has ideal biocompatibility and biodegradability and is harmless to human bodies. The grafting substance formed by the reaction of the glucosamine and the behenic acid can be assembled into the micelle in the water; moreover, a synthetic method and the treatment processes are simple; no pollution is caused to the environment.

Description

technical field [0001] The invention relates to the field of drug delivery systems, in particular to a hydrophobic drug capable of being entrapped in water in the form of micelles, and in particular to a glucosamine-behenic acid graft and a preparation method thereof. Background technique [0002] Many drugs have poor water solubility and low bioavailability, so a suitable drug delivery system is needed to increase the water solubility of these poorly soluble drugs in clinical application. Nowadays, nano-preparation has attracted more and more attention from scholars. Nanoparticles are small in size and can prevent phagocytosis by the reticuloendothelial system. There have been many studies on related preparations. Micelles are a new type of drug carrier, the hydrophobic inner core is the drug storage, and the hydrophilic outer shell can effectively prolong the circulation time in the blood, which plays an important role in the solubilization of hydrophobic drugs and the ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/107A61K31/7008A61P19/02A61P19/04
CPCA61K9/107A61K31/7008
Inventor 掲丽勇应晓英邬嘉晖杜永忠
Owner ZHEJIANG UNIV