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Tumor targeting embolization therapeutic composition and preparation method thereof

A tumor targeting and composition technology, applied in the field of interventional medicine, can solve the problems of limiting the drug loading speed and drug loading capacity of polymers, limiting the therapeutic effect of drugs, and short drug retention time, so as to achieve the effect of preventing tumor recurrence and sustained release Improve the effect of drug loading speed

Active Publication Date: 2012-06-27
HYGEA MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, there are certain defects in this method. First, the drug solution perfused into the lesion diffuses rapidly, the drug concentration decreases sharply, and the local residence time of the drug is very short, which limits the therapeutic effect of the drug; Enter the whole body through the blood circulation, causing systemic toxic and side effects; third, common antineoplastic drugs also cause certain toxic and side effects on local normal tissues; fourth, after embolization, the expression of vascular endothelial growth factor (VEGF) is up-regulated, resulting in new blood vessels And the formation of collateral circulation can lead to the restoration of tumor blood supply and tumor recurrence
[0007] Chinese patent CN101670095A describes a pharmaceutical composition for embolism therapy, which comprises a polymer polymerized with a hydroxyl polymer material, an unsaturated double bond, an anionic monomer, and an optional vinyl monomer ;Since the drug is only combined with anionic groups, components other than unsaturated double bonds and anionic monomers in this technology limit the drug loading speed and drug loading capacity of the polymer

Method used

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  • Tumor targeting embolization therapeutic composition and preparation method thereof
  • Tumor targeting embolization therapeutic composition and preparation method thereof
  • Tumor targeting embolization therapeutic composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Embodiment 1: the preparation of microsphere

[0073] Using the reverse-phase suspension polymerization method, add 10 parts of liquid paraffin and an appropriate amount of Span80 into a three-necked flask, blow nitrogen, and then dissolve 1 part of acrylic acid, 0.02 parts of N, N'-methylenebisacrylamide (crosslinking agent), Add 0.02 parts of potassium persulfate (initiator) solution dropwise to the oil phase at 55°C, pre-crosslink for 10 minutes, then add 0.14 parts of tetramethylethylenediamine (catalyst), and react for 4 hours under stirring at 500 rpm. Separate the microspheres, wash them, and sieve out different specifications according to the particle size, and collect microspheres with particle sizes ranging from 150 to 350 μm, 350 to 560 μm and 560 to 710 μm.

Embodiment 2

[0074] Embodiment 2: the preparation of microsphere

[0075] Using the reverse phase suspension polymerization method, add 12 parts of liquid paraffin and an appropriate amount of Span85 into a three-necked flask, blow nitrogen, and then dissolve 1 part of acrylic acid, 0.04 parts of N, N'-methylenebisacrylamide (crosslinking agent), Add 0.04 parts of potassium persulfate (initiator) solution dropwise to the oil phase at 65°C. After pre-crosslinking for 10 minutes, add 0.14 parts of tetramethylethylenediamine (catalyst) and react for 4 hours under stirring at 400 rpm. Separate the microspheres, wash them, and sieve out different specifications according to the particle size, and collect microspheres with particle sizes ranging from 150 to 350 μm, 350 to 560 μm and 560 to 710 μm.

Embodiment 3

[0076] Embodiment 3: the preparation of microsphere

[0077] Using the reverse phase suspension polymerization method, add 10 parts of liquid paraffin and an appropriate amount of Span85 into a three-necked flask, blow nitrogen, and then dissolve 1 part of 2-acrylamido-2-methylpropanesulfonic acid, 0.02 parts of N, N' -Methylenebisacrylamide (crosslinking agent), 0.02 parts of potassium persulfate (initiator) solution was added dropwise to the oil phase at 55°C, and after pre-crosslinking for 10 minutes, 0.14 parts of tetramethylethylene di Amine (catalyst), after reacting for 4 hours under stirring at 500rpm, separate the microspheres, wash them, sieve out different specifications according to the particle size, and collect microspheres with particle sizes ranging from 150 to 350 μm, 350 to 560 μm and 560 to 710 μm .

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Abstract

The invention provides a tumor targeting embolization therapeutic composition and a preparation method thereof. The composition comprises the following ingredients: 1) polymers and 2) anti-tumor targeting medicine, wherein the polymers are generated by monomers containing unsaturated double bonds and anionic groups through polymerization reaction, and the anti-tumor targeting medicine is combined onto the anionic groups of the polymers. The anti-tumor targeting medicine is combined onto polymer carriers, and the efficacies of the anti-tumor targeting medicine of realizing the tumor targeting, not damaging the peripheral normal tissues, inhabiting the compensatory circulation and preventing the tumor recurrence can be fully realized in the chemoembolization. Compared with a medicine solution filling method, the preparation method has the advantages that medicine combined into the polymer carriers can be slowly released, the medicine can be maintained for a longer time at higher concentration in the local tumor part, the toxic or side effect of the medicine on the whole body is reduced, and the curative effect of the chemoembolization is improved.

Description

technical field [0001] The invention belongs to the field of interventional medicine, and relates to a tumor targeting pharmaceutical composition for embolization therapy and a preparation method thereof. Background technique [0002] Interventional therapy is one of the fastest growing disciplines in the 21st century. At present, it has kept pace with medical treatment and surgical treatment, and has become the third treatment system. [0003] Embolization therapy is an important part of interventional therapy and belongs to minimally invasive therapy. Embolization therapy is a local treatment that artificially blocks blood vessels by introducing embolic agents into the human body through precision instruments such as special catheters and guide wires under the guidance of medical imaging equipment. Embolization therapy has a good effect in the treatment of malignant tumors, uterine fibroids, hemangiomas, vascular malformations and hemostasis, and has become an alternativ...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61P35/00
Inventor 范田园崔代超赵子明张强
Owner HYGEA MEDICAL TECH CO LTD