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A kind of sustained-release microgel ointment with high drug loading and its preparation method and application

A high drug-loading, microgel technology, applied in the medical field, can solve the problems of low drug-loading microgels, waste of active ingredients, increase insecurity, etc., so as to improve drug loading and reduce drug Cost of use, effect of prolonged release time

Active Publication Date: 2021-06-11
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although microgels have been extensively studied as drug carriers, there are currently the following disadvantages when microgels are used for drug loading: (1) Cross-linking agents are often added during the preparation process, which increases unsafety to a certain extent; (2) The traditional microgel drug-loading method is to soak the microgel in the drug solution for loading. After the drug solution reaches a concentration balance inside and outside the microgel, the drug-loaded microgel is separated from the drug solution, resulting in drug loading. (3) Since the drug loading and release mechanism of the microgel is mainly affected by the physical diffusion driven by the difference in drug concentration inside and outside the microgel, the traditional The drug-loaded microgel obtained by the traditional microgel drug-loading method has a low drug-loading capacity. In addition, in use, due to the large difference in drug concentration inside and outside the microgel, the drug is easy to diffuse out of the microgel. Therefore, it is impossible to achieve long-term slow release

Method used

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  • A kind of sustained-release microgel ointment with high drug loading and its preparation method and application
  • A kind of sustained-release microgel ointment with high drug loading and its preparation method and application
  • A kind of sustained-release microgel ointment with high drug loading and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] (1) Preparation of quaternary ammonium chitosan / hyaluronic acid microgel

[0063] Prepare the quaternary ammonium chitosan with a concentration of 1 mg / mL respectively (dissolve the quaternary ammonium chitosan purchased in deionized water, filter with a 0.22 μm filter with a pore size, and then use a gel chromatograph (GPC, U.S. Waters1515) measured molecular weight is 10.0×10 4 ) aqueous solution and hyaluronic acid (dissolve the purchased hyaluronic acid in deionized water, filter it with a filter with a pore size of 0.22 μm, and then use a gel chromatograph (GPC, Waters1515, USA) to measure the molecular weight as 10.0×10 4 ) aqueous solution, prepare quaternary ammonium chitosan / hyaluronic acid microgel with quaternary ammonium chitosan: the mass ratio of hyaluronic acid=1:2: under magnetic stirring, utilize syringe pump to 10mL quaternary ammonium salt The chitosan solution was slowly injected into the 20mL hyaluronic acid solution at a rate of 5mL / h, and stirred...

Embodiment 2

[0069] (1) Preparation of quaternary ammonium chitosan / hyaluronic acid microgel

[0070] Prepare the quaternary ammonium chitosan that concentration is 0.1mg / mL respectively (the quaternary ammonium chitosan that buys is dissolved in deionized water, is that 0.22 μ m filter is filtered with aperture, then use gel chromatography (GPC, U.S. Waters1515) measured molecular weight is 20.0×10 4 ) and hyaluronic acid (dissolve the purchased hyaluronic acid in deionized water, filter it with a filter with a pore size of 0.22 μm, and then use a gel chromatography (GPC, Waters1515, USA) to measure the molecular weight as 20.0×10 4 ) aqueous solution, prepare quaternary ammonium chitosan / hyaluronic acid microgel with quaternary ammonium chitosan: the mass ratio of hyaluronic acid=1:1: under magnetic stirring, utilize syringe pump to 10mL quaternary ammonium salt The chitosan solution was slowly injected into 10 mL of the hyaluronic acid solution at a rate of 10 mL / h, and stirred for 1 h...

Embodiment 3

[0076] (1) Preparation of quaternary ammonium chitosan / hyaluronic acid microgel

[0077] The preparation concentration is the quaternary ammonium chitosan of 2.0mg / mL respectively (the quaternary ammonium chitosan that buys is dissolved in deionized water, is 0.22 μ m filter filtration with aperture, then uses gel chromatography (GPC, U.S. Waters1515) measured molecular weight is 2.0×10 4 ) and hyaluronic acid (dissolve the purchased hyaluronic acid in deionized water, filter it with a filter with a pore size of 0.22 μm, and then use a gel chromatograph (GPC, Waters1515, USA) to measure the molecular weight as 5.0×10 4 ) aqueous solution, with quaternary ammonium salt chitosan: the mass ratio of hyaluronic acid=1:3 prepares quaternary ammonium salt chitosan / hyaluronic acid microgel: under magnetic stirring, utilize syringe pump to 10mL quaternary ammonium salt Chitosan solution was slowly injected into 30mL hyaluronic acid solution at a speed of 10mL / h, and stirred for 6h to ...

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Abstract

The invention discloses a sustained-release microgel ointment with high drug loading, a preparation method and application thereof. In the present invention, the quaternary ammonium salt chitosan aqueous solution and the hyaluronic acid aqueous solution are mixed to obtain the quaternary ammonium chitosan / hyaluronic acid microgel aqueous solution; Uniformly, obtain the sustained-release microgel ointment with high drug loading. Hyaluronic acid and quaternary ammonium chitosan form a microgel through electrostatic interaction, which is safe and convenient; concentration increases the concentration of the drug solution outside the microgel, which can increase the drug loading capacity of the microgel, and the drug is not loaded by the microgel It can inhibit the release of the loaded drug from the microgel to a certain extent, and prolong the sustained release time; the thickener can make the drug-loaded microgel suspension into a paste, which is beneficial to smear on the skin surface, and the drug injected at the same time Can be 100% utilized, reducing the cost of drug use. The ointment can be used to prepare medicines for treating histamine-independent itching and analgesia.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a sustained-release microgel ointment with high drug loading and its preparation method and application. Background technique [0002] Microgel is a kind of hydrogel with three-dimensional cross-linked network structure and micro / nano size. In addition to the properties of traditional hydrogels such as elasticity, hydrophilicity, insolubility and infusibility, it can also be used as a drug carrier for drugs control release. Quaternary ammonium chitosan (HTCC) is a linear cationic polyelectrolyte, and hyaluronic acid (HA) is a linear anionic polyelectrolyte, both of which are natural polymer materials with good biocompatibility and Biodegradable, harmless to the human body, widely used in the field of biomedicine. Microgel preparation techniques include chemical cross-linking and physical cross-linking. Chemically cross-linked microgels are bonded by covalent bonds, and chemic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K47/36A61K45/00A61P29/00A61P17/04
CPCA61K9/06A61K47/36A61K45/00A61P29/00A61P17/04A61K31/352A61K31/4375A61K47/38A61K9/0014
Inventor 聂红赵剑豪朱涛吴琰
Owner JINAN UNIVERSITY