Application of PEG (Polyethylene Glycol) compound in preparation of embolism agent

Abstract

The invention relates to an application of a PEG (Polyethylene Glycol) compound in preparation of an embolism agent, which comprises the following steps: the PEG compound is prepared into embolism agent microspheres, the PEG compound is a straight-chain or multi-arm PEG compound, the multi-arm PEG compound is a three-arm PEG compound, a four-arm PEG compound, a six-arm PEG compound or an eight-arm PEG compound, the PEG compound is covalently bound with an iodine-containing group, and the iodine-containing group is covalently bound with the embolism agent microspheres. The iodine-containing group is triiodobenzene or triiodobenzoic acid. According to the application of the PEG compound in preparation of the embolism agent, the PEG compound is prepared into embolism agent microspheres, the iodine-containing group introduced on the PEG structure can change the relaxation efficiency of water protons in local tissues in vivo, and contrast with surrounding tissues is formed, so that the purpose of radiography is achieved. Therefore, the embolic agent disclosed by the invention has a self-developing effect under the DSA technology, does not need to be mixed with an additional contrast agent for use, and is more convenient to use and more efficient to operate.

Description

technical field

[0001] The present invention relates to embolic agent, more specifically relates to the application of a PEG compound as the preparation of embolic agent. Background technique

[0002] Embolic agents are commonly used products for tumor embolization or intervention of hypervascular tumors. By embolizing the blood supply vessels of the tumor, the tumor blood supply is insufficient and the tumor tissue lacks the nutrients necessary for its growth to "starve to death". The use of embolic agents needs to be delivered to the blood supply vessels of the lesion through a microcatheter. This operation needs to be performed under the technique of digital subtraction angiography (DSA). The embolic agents currently used do not develop themselves, and additional imaging needs to be added before use. Agent and mixed with it to achieve the developing effect, it is cumbersome to use. Contents of the invention

[0003] In order to solve the problem of cumbersome operation...

Examples

Embodiment 1

[0026] Dissolve 10.0 g of 3-arm-2,3,5-triiodobenzamide acrylamide polyethylene glycol, 0.2 g of N,N-methylene acrylamide, 0.5 g of ethyl methacrylate, and 0.12 g of ammonium persulfate In 30ml of purified water, sonicate for 10min, filter with a 0.45um water filter membrane, and obtain the filtrate for later use.

[0027] Add 8.0 g of liquid paraffin to 2.0 liters of petroleum ether, ultrasonically degas for 30 minutes, stir and cool down to 0-10°C, and set aside.

[0028] After cooling the oil phase to 0-10°C, add 0.3g of tetramethylethylenediamine and stir for 3min at a speed of 300r / min, slowly drop half of the water phase into it, stir for 10-30min, then drop into the other half, and stir for 10- 30min, raise the temperature to 30°C, adjust the speed to 600r / min, stir for 1h, raise the temperature to 60°C, continue to stir for 5h, add 200ml of purified water, stir for 20min, filter to obtain microspheres, and swell the microspheres with normal saline for injection After 3...

Embodiment 2

[0030] Dissolve 10.0 g of 8-arm-2,3,5-triiodobenzamide acrylamide polyethylene glycol, 0.2 g of N,N-methylene acrylamide, 0.5 g of ethyl methacrylate, and 0.12 g of ammonium persulfate In 30ml of purified water, sonicate for 10min, filter with a 0.45um water filter membrane, and obtain the filtrate for later use.

[0031] Add 8.0 g of liquid paraffin to 2.0 liters of petroleum ether, ultrasonically degas for 30 minutes, stir and cool down to 0-10°C, and set aside.

[0032] After cooling the oil phase to 0-10°C, add 0.3g of tetramethylethylenediamine and mix for 3min at a speed of 300r / min, slowly drop half of the water phase into it, stir for 10-30min, then drop into the remaining half, and stir 10-30min, heat up to 30°C, adjust the speed to 600r / min, stir for 1h, heat up to 60°C, continue stirring for 5h, add 200ml of purified water, stir for 20min, filter to get microspheres, use the microspheres for injection Saline was swollen for 30 minutes, injected into the microcathet...

Embodiment 3

[0034] Dissolve 10.0 g of 6-arm-2,3,5-triiodophenol acrylamide polyethylene glycol, 0.2 g of N,N-methylene acrylamide, 0.5 g of ethyl methacrylate, and 0.12 g of ammonium persulfate in 30 ml Purified water was sonicated for 10 min, filtered with a 0.45um water filter membrane, and the filtrate was obtained for future use.

[0035] Add 8.0 g of liquid paraffin to 2.0 liters of petroleum ether, ultrasonically degas for 30 minutes, stir and cool down to 0-10°C, and set aside.

[0036] After cooling the oil phase to 0-10°C, add 0.3g of tetramethylethylenediamine and mix for 3min at a speed of 300r / min, slowly drop half of the water phase into it, stir for 10-30min, then drop into the remaining half, and stir 10-30min, heat up to 30°C, adjust the speed to 600r / min, stir for 1h, heat up to 60°C, continue stirring for 5h, add 200ml of purified water, stir for 20min, filter to get microspheres, use the microspheres for injection Saline was swollen for 30 minutes, injected into the mi...

technical field

[0001] The present invention relates to embolic agent, more specifically relates to the application of a PEG compound as the preparation of embolic agent. Background technique

[0002] Embolic agents are commonly used products for tumor embolization or intervention of hypervascular tumors. By embolizing the blood supply vessels of the tumor, the tumor blood supply is insufficient and the tumor tissue lacks the nutrients necessary for its growth to "starve to death". The use of embolic agents needs to be delivered to the blood supply vessels of the lesion through a microcatheter. This operation needs to be performed under the technique of digital subtraction angiography (DSA). The embolic agents currently used do not develop themselves, and additional imaging needs to be added before use. Agent and mixed with it to achieve the developing effect, it is cumbersome to use. Contents of the invention

[0003] In order to solve the problem of cumbersome operation...

Examples

Embodiment 1

[0026] Dissolve 10.0 g of 3-arm-2,3,5-triiodobenzamide acrylamide polyethylene glycol, 0.2 g of N,N-methylene acrylamide, 0.5 g of ethyl methacrylate, and 0.12 g of ammonium persulfate In 30ml of purified water, sonicate for 10min, filter with a 0.45um water filter membrane, and obtain the filtrate for later use.

[0027] Add 8.0 g of liquid paraffin to 2.0 liters of petroleum ether, ultrasonically degas for 30 minutes, stir and cool down to 0-10°C, and set aside.

[0028] After cooling the oil phase to 0-10°C, add 0.3g of tetramethylethylenediamine and stir for 3min at a speed of 300r / min, slowly drop half of the water phase into it, stir for 10-30min, then drop into the other half, and stir for 10- 30min, raise the temperature to 30°C, adjust the speed to 600r / min, stir for 1h, raise the temperature to 60°C, continue to stir for 5h, add 200ml of purified water, stir for 20min, filter to obtain microspheres, and swell the microspheres with normal saline for injection After 3...

Embodiment 2

[0030] Dissolve 10.0 g of 8-arm-2,3,5-triiodobenzamide acrylamide polyethylene glycol, 0.2 g of N,N-methylene acrylamide, 0.5 g of ethyl methacrylate, and 0.12 g of ammonium persulfate In 30ml of purified water, sonicate for 10min, filter with a 0.45um water filter membrane, and obtain the filtrate for later use.

[0031] Add 8.0 g of liquid paraffin to 2.0 liters of petroleum ether, ultrasonically degas for 30 minutes, stir and cool down to 0-10°C, and set aside.

[0032] After cooling the oil phase to 0-10°C, add 0.3g of tetramethylethylenediamine and mix for 3min at a speed of 300r / min, slowly drop half of the water phase into it, stir for 10-30min, then drop into the remaining half, and stir 10-30min, heat up to 30°C, adjust the speed to 600r / min, stir for 1h, heat up to 60°C, continue stirring for 5h, add 200ml of purified water, stir for 20min, filter to get microspheres, use the microspheres for injection Saline was swollen for 30 minutes, injected into the microcathet...

Embodiment 3

[0034] Dissolve 10.0 g of 6-arm-2,3,5-triiodophenol acrylamide polyethylene glycol, 0.2 g of N,N-methylene acrylamide, 0.5 g of ethyl methacrylate, and 0.12 g of ammonium persulfate in 30 ml Purified water was sonicated for 10 min, filtered with a 0.45um water filter membrane, and the filtrate was obtained for future use.

[0035] Add 8.0 g of liquid paraffin to 2.0 liters of petroleum ether, ultrasonically degas for 30 minutes, stir and cool down to 0-10°C, and set aside.

[0036] After cooling the oil phase to 0-10°C, add 0.3g of tetramethylethylenediamine and mix for 3min at a speed of 300r / min, slowly drop half of the water phase into it, stir for 10-30min, then drop into the remaining half, and stir 10-30min, heat up to 30°C, adjust the speed to 600r / min, stir for 1h, heat up to 60°C, continue stirring for 5h, add 200ml of purified water, stir for 20min, filter to get microspheres, use the microspheres for injection Saline was swollen for 30 minutes, injected into the mi...

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