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Sodium alginate polymer, novel sodium alginate blood vessel embolism chemotherapy composition, and preparation method and application thereof

A sodium alginate and vascular embolization technology, which is applied in the field of interventional medicine, can solve the problems of complex embolization operation of emulsion-embolizing agent, inability to complete chemoembolization treatment in one step, and increase adverse reactions, etc., and achieves good drug sustained release effect and is suitable for large-scale The effect of industrialized production and high drug encapsulation efficiency

Inactive Publication Date: 2018-12-18
深圳市比德泰克生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are several main defects in traditional TACE treatment: ① lipiodol emulsion will have local deposition, and as time goes on, the cytotoxic effect of the drug on the tumor will also decrease; ② although the emulsion reduces systemic adverse reactions compared with traditional chemotherapy, it still has Some drugs enter the circulatory system, increasing adverse reactions; ③In tumor treatment, the therapeutic effect requires maintaining a certain drug concentration inside the tumor, and this depends on the sustained release of drugs, which is difficult for lipiodol emulsions; ④Emulsion-Embolism The embolization operation is complicated, and chemoembolization cannot be completed in one step
The preparation method disclosed in this patent requires two reaction steps to obtain modified sodium alginate embolization microspheres

Method used

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  • Sodium alginate polymer, novel sodium alginate blood vessel embolism chemotherapy composition, and preparation method and application thereof
  • Sodium alginate polymer, novel sodium alginate blood vessel embolism chemotherapy composition, and preparation method and application thereof
  • Sodium alginate polymer, novel sodium alginate blood vessel embolism chemotherapy composition, and preparation method and application thereof

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Experimental program
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Embodiment 1

[0040] Embodiment 1: the preparation of microsphere

[0041] Using the reverse phase suspension polymerization method, add 60mL of liquid paraffin and 60mg of Span 80 into the three-necked flask, blow nitrogen to drive oxygen, and then dissolve 4.0g of sodium alginate, 2.0g of acrylic acid, 60mg of N,N'-methylene Add bisacrylamide (crosslinking agent) and 60mg potassium persulfate (initiator) solution dropwise to the oil phase at 70°C. After pre-crosslinking for 15 minutes, add 60mg tetramethylethylenediamine (catalyst) and stir at 250rpm After reacting for 2.5 hours, separate the microspheres, wash them, and sieve out different specifications according to the particle size. -1250μm and >1250μm) microspheres (SAMs). The shape, size and adhesion were observed under an optical microscope. After the 700-900μm microspheres were dried, they were scanned by SEM, and the results were as follows figure 1 shown. The dried microspheres are round particles, regular in shape, similar ...

Embodiment 2

[0042] Embodiment 2: the particle size distribution investigation of microsphere

[0043] Take the microsphere SAMs prepared in Example 1, disperse them in deionized water (DW) or normal saline (NS), and use a laser scattering particle size analyzer to test their average particle size and particle size distribution. The average particle size measured in DW or NS is 632.7μm and 555.1μm respectively, and the particle size distribution is basically normal distribution. The results are as follows figure 2 shown.

Embodiment 3

[0044] Embodiment 3: Preparation of malic acid-loaded sunitinib microspheres

[0045] Get each 1mL of the wet microspheres of each particle size range that embodiment 1 makes respectively, after absorbing the surface moisture, place in the sunitinib malate solution of 25.0mg / L, after soaking at room temperature for 2 hours, use Wash off the unexchanged drug on the surface with ion water.

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Abstract

The invention provides a sodium alginate polymer which is generated by carrying out a polymerization reaction, which is initiated by free radicals, to sodium alginate with a monomer which contains anunsaturated double bond and an anionic group, and optionally, a crosslinking agent being poly-functionality water-soluble acrylate or acrylamide. Compared with a sodium alginate microsphere embolic agent on market, the sodium alginate polymer, being a carrier, can adsorb and carry a drug in vitro through ions, wherein the sodium alginate polymer is high in drug carrying capacity and can slowly release the drug in vivo, thus increasing local medicine concentration, prolonging action time of the drug, reducing systemic toxicity of the drug and further improving curative effect of the chemotherapy of the embolism. The invention also provides a novel sodium alginate blood vessel embolism chemotherapy composition, in which the sodium alginate polymer, as the embolic agent and medicine, can be co-delivered to a target blood vessel via a catheter, so that the curative effect of the chemotherapy medicine is fully achieved. The product is free of damage on surrounding normal tissue and can reduce relapse of the diseases.

Description

technical field [0001] The invention belongs to the field of interventional medicine, and relates to a sodium alginate polymer, a novel sodium alginate vascular embolization chemotherapy composition, a preparation method and application thereof. Background technique [0002] Interventional radiology is a new discipline developed in recent years. It is a minimally invasive medical technology guided by imaging equipment. It has the characteristics of small trauma, fast recovery, and good curative effect. treatment pathway. At present, it has become the three most important therapeutic disciplines along with internal medicine and surgery. Interventional embolization is an important part of interventional therapy, and it is increasingly playing an important role in the treatment of malignant tumors, vascular malformations, uterine fibroids and hemostasis. [0003] Arterial chemoembolization (TACE) treatment combines embolization and chemotherapy. It is a non-surgical and minim...

Claims

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Application Information

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IPC IPC(8): C08F251/00C08F220/06C08F222/38A61L24/06A61L24/00
CPCA61L24/0015A61L24/06A61L2300/416A61L2300/602C08F251/00C08L51/02C08F220/06C08F222/385
Inventor 杜玲然付纪军周毅黄剑文严立标余宗峻
Owner 深圳市比德泰克生物医药科技有限公司
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