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Drug-loading in-situ reticular gel sustained release preparation taking phospholipid and mucopolysaccharide derivative as matrixes, and preparation method thereof

An in-situ gel and preparation technology, applied in the field of medicine, can solve the problems of short action time, accelerated drug release rate and small burst release.

Active Publication Date: 2020-04-17
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, we have also found in our research that the effect of using this type of phospholipid gel preparation to entrap many chemical drugs is not ideal. Although it also has a certain slow-release effect, the slow-release time can only last for a few days and cannot last for a long time. The effective blood concentration of the drug, and the sudden release is relatively serious
First of all, some highly water-soluble drugs have a short action time. It is speculated that the reason may be that the subcutaneous tissue of the human body is an aqueous environment. Water-soluble drugs are entrapped in a small molecule gel system, which lacks barriers and easily diffuses out through body fluids.
Secondly, some highly fat-soluble drugs have good compatibility with phospholipids, and are easy to penetrate, diffuse and release in phospholipid carriers, resulting in a significantly faster release rate, a relatively short sustained release time, and more burst releases. Narrow drug that may raise safety concerns
[0006] Therefore, for a wide range of chemical drugs, it is necessary to find a drug carrier with a wide range of applications, a small burst release, and a long sustained release time to solve the problem of long-acting sustained release for injection.

Method used

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  • Drug-loading in-situ reticular gel sustained release preparation taking phospholipid and mucopolysaccharide derivative as matrixes, and preparation method thereof
  • Drug-loading in-situ reticular gel sustained release preparation taking phospholipid and mucopolysaccharide derivative as matrixes, and preparation method thereof
  • Drug-loading in-situ reticular gel sustained release preparation taking phospholipid and mucopolysaccharide derivative as matrixes, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Take 100 mg of ivermectin, dissolve it in 2.0 g of ethanol, filter through a 0.22 μm microporous membrane to obtain a drug solution, and then add 6.0 g of injection-grade soybean lecithin S100 and injection-grade medium-chain fatty acid glycerol under sterile conditions 1.0 g of ester and 1.0 g of chondroitin sulfate octadecylamine coupling product, stirred magnetically for about 1 h under sterile conditions, and mixed evenly at S100 to obtain a liquid containing a large number of bubbles, which was left to stand until the bubbles completely disappeared, then packed and sealed, that is have to.

Embodiment 2

[0064] Under sterile conditions, take an appropriate amount of doxorubicin hydrochloride and grind it in a mortar to obtain doxorubicin hydrochloride powder. Take 1.5 g of absolute ethanol, 6.5 g of injection-grade egg yolk phospholipid E80, 0.5 g of chondroitin sulfate octadecylamine conjugate, and 1.5 g of soybean oil, and magnetically stir for about 1 h under sterile conditions until they are evenly mixed. Take 20 mg of doxorubicin hydrochloride powder and mix it evenly with the above liquid to obtain a liquid containing a large number of bubbles, let it stand until the bubbles completely disappear, divide it into packages, seal it, and get ready.

Embodiment 3

[0066] Under aseptic conditions, an appropriate amount of ebiprazole is ground and pulverized in a mortar to obtain ebiprazole powder. Take 1.5 g of absolute ethanol, 1.0 g of hyaluronic acid hexadecylamine conjugate and 7.5 g of injection-grade soybean lecithin S100, and magnetically stir for about 1 h under sterile conditions until the mixture is uniform, and a milky yellow liquid containing a large number of bubbles is obtained. Under sterile conditions, take 200 mg of ebiprazole powder and mix it with the above-mentioned liquid evenly, let it stand until the bubbles completely disappear, divide it into packages, and seal it to obtain the product.

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Abstract

The invention provides a drug-loading in-situ reticular gel sustained release preparation taking phospholipid and a mucopolysaccharide derivative as matrixes, and a preparation method thereof. According to the invention, phospholipid, a mucopolysaccharide derivative, an active pharmaceutical ingredients and ethanol solutions with different concentrations are prepared into the phospholipid mucopolysaccharide derivative sustained-release preparation by adopting a simple method; the drug-loading in-situ reticular gel sustained release preparation has the advantages of good biocompatibility, smalladverse reaction, strong burst release inhibition capability and release time prolonging, is suitable for various administration forms such as subcutaneous injection, external administration and thelike, can conveniently adjust the amount of the entrapped drug according to the clinical dosage of the drug, and has wide application prospect.

Description

technical field [0001] The invention relates to an in-situ phase-change network gel slow-release system which uses phospholipids and mucopolysaccharide derivatives as substrates and biocompatible organic solvents as solvents, and is suitable for a wide range of drugs, and belongs to the technical field of medicine. Background technique [0002] Water-soluble chemical drugs have outstanding and irreplaceable important effects on human health. They have clear physical and chemical properties, fast dissolution in vivo, fast absorption, and fast elimination, so the maintenance time of curative effect is relatively short. Some water-soluble molecular drugs with low permeability have poor tissue affinity due to their poor permeability. There are obvious peaks and troughs in the blood concentration of fat-soluble drugs after administration, which makes them more toxic and side effects and lowers the drug effect. For chronic diseases, continuous injection or intravenous infusion is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/24A61K47/36A61K31/7048A61K31/704A61K31/496A61K31/522A61K31/573A61K31/616A61K31/4164A61K31/445A61K31/519A61K31/401A61K31/5513A61K31/5415A61K31/17A61K31/05A61K31/357
CPCA61K9/06A61K31/05A61K31/17A61K31/357A61K31/401A61K31/4164A61K31/445A61K31/496A61K31/519A61K31/522A61K31/5415A61K31/5513A61K31/573A61K31/616A61K31/704A61K31/7048A61K47/24A61K47/36
Inventor 龚涛罗静雯张培宋旭张志荣孙逊
Owner SICHUAN UNIV