Iodinated oil embolization agent easy to fast inject and preparation method therefor

A technology of embolic agent and iodized oil, which is applied in the field of iodized oil embolic agent and its preparation, can solve the problems of difficult drug loading and difficulty of injection of iodized oil, and achieve the effects of stable structure, reduced viscosity and increased solubility

Inactive Publication Date: 2020-06-19
陈传果
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to provide a kind of embolism that is easy to inject and have high drug loading and its preparation method for the problems of difficult injection of iodized oil and difficult drug loading in the clinical application process.

Method used

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  • Iodinated oil embolization agent easy to fast inject and preparation method therefor
  • Iodinated oil embolization agent easy to fast inject and preparation method therefor
  • Iodinated oil embolization agent easy to fast inject and preparation method therefor

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Embodiment 1: Preparation of antineoplastic drug-containing embolism

[0034] (1) Add 20 mg of paclitaxel to 150 mg of 1,2-propanediol, heat to 40°C, and stir magnetically for 20 min.

[0035] (2) Take 500 mg of iodized oil and 330 mg of Cremophor RH40 in vials, place them on a magnetic stirrer and stir at a stirring speed of 1200 rpm / min for 40 min.

[0036] (3) Mix the liquids in steps 1 and 2 and place them on a magnetic stirrer for stirring at a stirring speed of 1000 rpm / min for 45 min and maintain the temperature at 40°C. Finally, a light yellow homogeneous solution is obtained, which is the desired embolic agent. Dilute the embolic agent 5-10 times with water for injection before the operation to obtain emulsion droplets with a particle size of 5-110 μm (such as figure 1 ), easy to inject. Transcatheter arterial embolization was performed on patients with liver cancer, and it was found that the imaging effect was obvious (such as figure 2 ).

Embodiment 2

[0037] Embodiment 2: preparation containing antineoplastic drug embolism

[0038] (1) Add 30 mg of carmustine to 150 mg of medium-chain fatty acid glycerides and stir on a magnetic stirrer at a speed of 600 rpm / min for 50 min at a temperature of 45 °C.

[0039] (2) Add 400 mg of iodized oil, 300 mg of Cremophor RH40 and 120 mg of PEG 400 into a vial, and stir on a magnetic stirrer at a speed of 1000 rpm / min for 45 min.

[0040] (3) After mixing the liquids in steps 1 and 2, stir on a magnetic stirrer at a speed of 800 rpm / min for 60 min to obtain a light yellow homogeneous liquid, which is the required embolism. Dilute the embolic agent 5-10 times with water for injection before the operation to obtain emulsion droplets with a particle diameter of 50-400 μm (such as image 3 ), easy to inject. Transcatheter arterial embolization was performed on patients with liver cancer, and it was found that the imaging effect was obvious (such as Figure 4 ).

Embodiment 3

[0041] Embodiment 3: preparation containing antineoplastic drug embolism

[0042] (1) Take 450 mg of ethyl oleate and 30 mg of docetaxel in a vial, preheat to 45°C, place the vial on a magnetic stirrer, and stir at a speed of 500 rpm / min for 30 min. The docetaxel was fully dissolved in ethyl oleate.

[0043] (2) Take 520 mg of iodized oil and add it to the above ethyl oleate, place it on a magnetic stirrer and stir at a speed of 800 rpm / min for 45 min to obtain a slightly pale yellow homogeneous oil solution. The oil solution is the required embolic agent. Due to the lower viscosity of ethyl oleate, the viscosity of the mixed solution is significantly lower than that of iodized oil. Before the operation, the embolic agent is artificially emulsified to form small droplets with a particle size of 100-300 μm, which are used to embolize the distal end of the arteriole.

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Abstract

The invention relates to an iodized oil embolization agent easy to fast inject and high in drug load and a preparation method therefor. The embolization agent is proposed in allusion to the problems that fast injection and drug loading are not easy during iodized oil embolization in clinical application, is a mixture consisting of iodized oil, oil for injection, an emulsifier and antitumor drugs,and has the functions of embolization, development and chemotherapy. The embolization agent greatly reduces the viscosity of the iodized oil by introducing the oil for injection and emulsifier relatively low in viscosity, and thus bolus injection is facilitated; and the particle sizes of emulsion droplets obtained after emulsification can be controlled by adjusting the proportion of the emulsifier, and structures are relatively stable. The embolization agent not only can use the oil for injection and the emulsifier to solubilize oil-soluble antitumor drugs, but also can solubilize water-soluble antitumor drugs by a method of forming water-in-oil (W / O) emulsion, and preparation is simple and easy.

Description

technical field [0001] The invention relates to an iodized oil embolic agent which is easy to inject and has a high drug load and a preparation method thereof, belonging to the field of medical diagnosis and interventional therapy. Background technique [0002] Malignant tumor is the second leading cause of human death and a serious threat to human health. Among them, the top five cancers that die from malignant tumors are: gastric cancer, liver cancer, lung cancer, esophageal cancer and colorectal cancer. At present, the main methods for the treatment of malignant tumors include surgery, radiotherapy, chemotherapy and interventional therapy. Transcatheter arterial embolization (TCAE) has been proven to be an effective non-surgical method for the treatment of solid tumors. It selectively injects embolic materials into the supply vessels of a diseased organ through a catheter, occludes the corresponding vessels, and interrupts the blood supply. achieve the purpose of treatme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61L24/02A61L24/00
CPCA61L24/001A61L24/0015A61L24/02A61L2300/416A61L2400/06
Inventor 陈传果王雨
Owner 陈传果
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