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Iodine oil emulsion or drug-loaded iodine oil emulsion as well as preparation method and application thereof

A technology of iodized oil emulsion and iodized oil, which is applied in the directions of medical formula, X-ray contrast agent preparation, drug combination, etc., can solve problems such as ischemic necrosis or ectopic embolism, and achieve the effect of expanding the indications of iodized oil

Pending Publication Date: 2021-06-11
太阳雨林(厦门)生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although the water-in-oil dosage form in this technical scheme can carry targeted drugs, it can only be used through hepatic artery injection. If it is used in other tissues and organs, it will still cause ischemic necrosis or ectopic embolism of the tissue, so it is necessary to use It is safer to use

Method used

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  • Iodine oil emulsion or drug-loaded iodine oil emulsion as well as preparation method and application thereof
  • Iodine oil emulsion or drug-loaded iodine oil emulsion as well as preparation method and application thereof
  • Iodine oil emulsion or drug-loaded iodine oil emulsion as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1 adopts ether to inject-ultrasonic emulsification method to prepare lipiodol emulsion

[0060] Weigh 1,320 mg of soybean lecithin and 220 mg of cholesterol into a beaker, add 200 μL of iodized oil (National Drug Approval H37022398) and 4 ml of absolute ethanol, and place at 50°C to fully dissolve. Pipette the dissolved lipid solution evenly and pour it into 6ml of phosphate buffer solution pH6.0, then transfer it to an eggplant-shaped bottle, and place it in a water bath at 50-60°C to remove ether by vacuum rotary evaporation. The vacuum degree is - 0.08MPa, treatment time 20min, transferred to a centrifuge tube or beaker containing 200mg Tween-80, and then ultrasonicated at 240W for 24min until a uniform emulsion was formed. See figure 1 . Obtaining the emulsion that iodine content is 9.6mg / ml, electron micrograph and particle size distribution see respectively figure 2 with image 3 . The emulsion is stored in a 4°C refrigerator for 12 months, and it...

Embodiment 2

[0062] Example 2 Preparation of Lipiodol-Mesylate Apatinib Nano-liposomes Using Ethanol Injection-Ultrasonic Method

[0063] Weigh 660 mg of soybean lecithin and 55 mg of cholesterol into a beaker, add 500 μL of super liquefied lipiodol, and 5 ml of absolute ethanol at 45°C to fully dissolve. Inject the dissolved lipid solution into 50ml of phosphate buffer (concentrated hydrochloric acid adjusted to pH 2) containing 500mg of apatinib mesylate, then transfer it to an eggplant-shaped bottle, place it in a water bath at 45°C under vacuum Remove ethanol by rotary evaporation, vacuum degree -0.08MPa, treatment time 20min, transfer to a centrifuge tube or beaker containing 5mg Tween-80, and then sonicate at 141W for 24min until a uniform emulsion is formed. Check the pH and adjust the pH to 7 with 10% NaOH. A homogeneous emulsion with iodine content of 4.8 mg / ml and apatinib content of 10 mg / ml was obtained. See Image 6 . Obtaining the emulsion that iodine content is 9.6mg / ml,...

Embodiment 3

[0065] Example 3 Preparation of Lipiodol-Adriamycin Liposomes Using Ethanol-DMSO Injection-Ultrasonic Method

[0066] Weigh 660mg of soybean lecithin and 220mg of cholesterol into a beaker, add 20mg of doxorubicin hydrochloride, add 1ml of lipiodol, 200mg of Tween-80, and 5ml of absolute ethanol, place at 50°C to fully dissolve. Inject the dissolved lipid solution into 9ml of phosphate buffer solution pH6.6 (0.05mol / L), then transfer it to an eggplant-shaped bottle, and place it in a water bath at 79°C for vacuum rotary evaporation to remove ethanol and dimethyl Sulfoxide, the vacuum degree is -0.1MPa, the treatment time is 20min, transferred to a 50ml centrifuge tube or beaker, and then ultrasonicated at 141W for 20min until a uniform emulsion is formed. See Figure 10 , the transmission electron microscope observation picture is shown in Figure 11 .

[0067] The animal experiment is as claimed in claim 1, using h22 cells to subcutaneously plant tumors in ICR mice, record...

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Abstract

The invention provides an iodine oil emulsion, which comprises iodine oil and an emulsifier carrier. The emulsifier carrier comprises one or more of lipid microspheres, cell membrane components, phospholipid and cholesterol, solid lipid and liquid lipid, and a co-emulsifier. The iodine oil emulsion can also carry drugs, and the mode is that the drugs are uniformly dispersed in the iodine oil, and then the drug-loaded iodine oil is prepared into an oil-in-water emulsion; or a water-in-oil-in-water emulsion is prepared from the aqueous solution of the medicine and iodophol. By emulsifying the iodophol, the iodophol which can only be subjected to natural tract angiography and hepatic artery injection is converted into the safe iodophol emulsion which can be used through whole body artery, vein and lymphatic vessel injection or direct tissue injection, the indications of the iodophol are expanded. Meanwhile, the iodophol emulsion can carry medicines, enhance the treatment effect and relieve the whole body side effects of the medicines.

Description

technical field [0001] The invention relates to the technical field of tumor diagnosis and treatment agents, and more specifically, relates to lipiodol emulsion or drug-loaded lipiodol emulsion and its preparation method and application. Background technique [0002] Transcatheter arterial chemoembolization (TACE) is one of the main methods in the treatment of advanced liver cancer. The embolic agent used in traditional TACE treatment is lipiodol, which is usually made into a temporary emulsion with one or two chemotherapy drugs and injected into the hepatic artery through a catheter. Lipiodol and the chemotherapy drugs carried by lipiodol will stay in tumor blood vessels or tissues to kill tumor cells. Under normal circumstances, lipiodol can remain in liver cancer lesions for a long time, but it is quickly cleared in normal liver tissue or cirrhotic liver tissue. [0003] At present, lipiodol is mostly used in hepatic artery interventional therapy for liver malignant tum...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/04A61K45/00A61K31/444A61K31/44A61K47/24A61K47/28A61K47/10A61K47/14A61P35/00
CPCA61K49/04A61K45/00A61K31/444A61K31/44A61K47/24A61K47/28A61K47/10A61K47/14A61P35/00
Inventor 赵一麟周媛媛陈炜斌张小红周旭张红建刘秋松潘恒刘凤武
Owner 太阳雨林(厦门)生物医药有限公司
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