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Self-expandable microgel pulse preparation with layer-by-layer assembled polyelectrolytes and preparation method thereof

A polyelectrolyte and microgel technology, applied in the field of medicine, can solve the problems of slow swelling speed and long release time, and achieve the effects of small tissue irritation, precise and controllable core particle size, and cheap and easy-to-obtain materials

Active Publication Date: 2011-05-18
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage is that the release time after the time lag is too long, the swelling speed of the traditional hydrogel is slow, and the time to absorb water takes hours or even days
Although slow swelling is beneficial for many applications, in pulsatile drug delivery systems it is necessary for the polymer network to swell quickly with a programmed time lag

Method used

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  • Self-expandable microgel pulse preparation with layer-by-layer assembled polyelectrolytes and preparation method thereof
  • Self-expandable microgel pulse preparation with layer-by-layer assembled polyelectrolytes and preparation method thereof
  • Self-expandable microgel pulse preparation with layer-by-layer assembled polyelectrolytes and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1 Preparation of polyelectrolyte layer-by-layer self-expanding microgel pulse preparation

[0052] (1) Preparation of chitosan-calcium chloride solution: take 0.2 g of chitosan powder with a relative molecular weight of 100 kd, disperse it in 100 ml of deionized water, add concentrated hydrochloric acid dropwise until chitosan is completely dissolved, and add 2 g of calcium chloride powder , adjust the pH of the solution to 1.2 with dilute hydrochloric acid, and set aside;

[0053] (2) Preparation of drug-containing sodium alginate solution: Take 80 mg of sodium alginate powder, add it to 3 ml of deionized water, heat it in a water bath at 50 ° C to dissolve it, and obtain a sodium alginate solution. Take 400 μg of drug and dissolve it in 1 ml of deionized water. The drug solution is obtained in deionized water, and the two solutions are mixed, and vortexed vigorously to make them dissolve evenly, and the sodium alginate solution containing the drug is obtained;...

Embodiment 2

[0061] This embodiment prepares the self-expanding microgel pulse preparation of polyelectrolyte layer-by-layer assembly as follows:

[0062] (1) Preparation of chitosan-calcium chloride solution: take 0.1 g of chitosan powder with a relative molecular weight of 700 kd, disperse it in 100 ml of deionized water, add concentrated hydrochloric acid until the chitosan is completely dissolved, and add 1 g of calcium chloride powder , adjust the pH of the solution to 1.2 with dilute hydrochloric acid, and set aside;

[0063] (2) Preparation of drug-containing sodium alginate solution: Take 60 mg of sodium alginate powder, add it to 3 ml of deionized water, heat it in a water bath at 50 ° C to dissolve it, and obtain a sodium alginate solution. Take 800 μg of drug and dissolve it in 1 ml of deionized water. The drug solution is obtained in deionized water, and the two solutions are mixed, and vortexed vigorously to make them dissolve evenly, and the sodium alginate solution containin...

Embodiment 3

[0069] This embodiment prepares the self-expanding microgel pulse preparation of polyelectrolyte layer-by-layer assembly as follows:

[0070] (1) Preparation of chitosan-calcium chloride solution: take 0.5 g of chitosan powder with a relative molecular weight of 20 kd, disperse it in 100 ml deionized water, add concentrated hydrochloric acid dropwise until chitosan is completely dissolved, and add 4 g of calcium chloride powder , adjust the pH of the solution to 1.2 with dilute hydrochloric acid, and set aside;

[0071] (2) Preparation of drug-containing sodium alginate solution: Take 100 mg of sodium alginate powder, add it to 3 ml of deionized water, heat it in a water bath at 50 ° C to dissolve it, and obtain a sodium alginate solution. Take 200 μg of drug and dissolve it in 1 ml of deionized water. The drug solution is obtained in deionized water, and the two solutions are mixed, and vortexed vigorously to make them dissolve evenly, and the sodium alginate solution contain...

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Abstract

The invention discloses a self-expandable microgel pulse preparation with layer-by-layer assembled polyelectrolytes and a preparation method thereof. The preparation consists of a self-expandable microgel nucleus and a polyelectrolyte coating layer and has the particle size of between 100 nanometers and 600 mu m, wherein the self-expandable microgel nucleus mainly comprises chitosan and sodium alga acid; and the polyelectrolyte coating layer consists of a 4-sodium styrene sulfonate layer and a poly(allylamine) hydrochloride layer which are arranged alternatively. The preparation is a pulse preparation under the coaction of system degradation and swelling pressure, releases a property which is fully dependent on the structure of the preparation and a high polymer material and has high time lag controllability. After administration, a large number of medicaments are released after a time lag period in which the medicaments are not released. An experiment indicates that the pulse preparation has low tissue stimulation, high safety and accurately-controllable core particle size, and uses cheap and readily available materials; moreover, chitosan sodium alga acid microgel has certain pH sensitivity, so that the releasing action of the preparation is more flexible and controllable.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a polyelectrolyte layer-by-layer self-expanding microgel pulse preparation and a preparation method thereof. Background technique [0002] Many physiological functions and physiological and biochemical indicators of the human body, such as blood pressure, gastric acid secretion, secretion of certain hormones, etc., show biological rhythm changes. The onset of many diseases, the aggravation and relief of symptoms also have their own regularity, such as Bronchial asthma, myocardial infarction, angina pectoris, rheumatic diseases, gastric ulcer, diabetes, attention deficit syndrome, hypercholesterolemia, high blood pressure, etc. The traditional sustained and controlled release preparations maintain the blood drug concentration for a long time, prolong the curative effect of the drug, and have a more positive effect on clinical treatment than ordinary preparations. However, the sl...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/36A61K47/32A61K47/20
Inventor 钟延强周闺臣邹豪高静鲁莹刘青锋黄景彬张磊陈琰俞媛张翮孙治国刘俊杰
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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