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New application of sevelamer

A technology of Sevelamer and Sevelamer, which is applied in the field of medicine, can solve the problems of short retention time and large system toxicity, and achieve the effect of prolonging the survival period and high survival rate

Pending Publication Date: 2021-06-15
NANCHANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

From the perspective of pharmacokinetics, chemotherapeutic drugs are quickly washed through the tumor interstitium and blood vessels and returned to the circulatory system after embolization, and the short retention time in the tumor also caused greater systemic toxicity.

Method used

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  • New application of sevelamer
  • New application of sevelamer
  • New application of sevelamer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The preparation of embodiment 1 Sevelamer injection

[0031] Concentration is the preparation of the Sevelamer injection of 5 mg per milliliter, and concrete steps are as follows:

[0032] 1) Take 1500 mL of water for injection, add 27 grams of sodium chloride or 150 grams of glucose to dissolve completely, add 200 grams of hydrochloric acid or sevelamer carbonate raw material, and inert balls (dd15mm:dd5mm:dd2mm:dd0.05mm=50g:50g : 50g: 50g) mixed and put into the reactor.

[0033] 2) Perform ball milling for 2 hours at a speed of 300 r / min with a QM-3SP4 planetary ball mill (Nanjing Nanda Instrument Co., Ltd.).

[0034] 3) After high-temperature sterilization, prepare Sevelamer microspheres and add water to make up to 3000 mL.

[0035] 4) Filling under aseptic conditions, 2mL each, medium boron ampoules, melt-sealed, 1500 in total.

[0036] According to the scanning electron microscope, the size of Sevelamer microspheres after ball milling is between 0.3-7 microns, ...

Embodiment 2

[0037] Example 2 Sevelamer injection to the TASE operation process of the rabbit VX2 liver cancer model

[0038]In this example, the evaluation of TASE treatment was carried out on the rabbit VX2 liver cancer model. The rabbit VX2 liver cancer model is one of the few malignant tumor models with rich blood supply in the liver established in larger animals. The characteristics of the blood supply and imaging findings are very similar. Rabbit VX2 tumor is an ideal experimental model for TACE research of liver cancer, which has a guiding role in clinical practice.

[0039] The TASE operation process of Sevelamer injection on the rabbit VX2 liver cancer model is as follows:

[0040] A. Passage and preservation of VX2 tumor: Homogenate and resuscitate VX2 tumor cells from frozen rabbits preserved in previous studies were inoculated into the lateral muscle group of the right hind limb of healthy New Zealand white rabbits to make tumor-bearing breeding rabbits. Two weeks later, the ...

Embodiment 3

[0045] Embodiment 3 Postoperative treatment evaluation on living body level (imaging)

[0046] Ultrasound evaluation 14 days after the operation: Inject 3% amobarbital sodium (1ml / Kg) into the ear vein, fix the rabbit in the supine position on the animal operating table after coma, prepare the skin for disinfection, and lay a sterile towel, routinely Ultrasonography was used to observe tumor size, shape, and internal echo, and whether there was cystic necrosis. Color Doppler flow imaging (CDFI) was used to evaluate the blood supply of the tumor. Contrast-enhanced ultrasound (CEUS) ) to obtain contrast enhancement curves (within 120 seconds after contrast medium injection) of tumor and normal liver tissue at continuous time points to determine the necrosis rate of tumor imaging.

[0047] The result is as image 3 As shown, it can be seen that the tumor area is located near the diaphragm, the boundary is not clear, and the internal echo is uneven. CDFI shows that there is no ob...

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Abstract

The invention relates to the technical field of medicines, in particular to a novel application of sevelamer. The sevelamer is used as an active component, the sevelamer is prepared into a sevelamer injection, and the sevelamer injection is combined with transcatheter arterial embolization to treat liver cancer. Granules obtained after sevelamer is subjected to ball milling serve as a tumor blood supply artery embolization agent instead of traditional iodophol or polymer-based drug-loaded microspheres, so that tumor oxygen supply is blocked, inorganic phosphorus in the tumor environment is deprived, complete tumor necrosis is caused, residual active tumor tissue is not found, and the tumor blood supply artery embolization agent can be used for treating liver cancer.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new application of sevelamer. Background technique [0002] Sevelamer generally includes Sevelamer hydrochloride and Sevelamer carbonate, which have the same active ingredient. Taking sevelamer hydrochloride as an example, its chemical name is 2-propenyl-1-amino-2-chloromethyloxirane (1:1), and the molecular formula of the monomer is C 6 h 12 ClNO has a molecular weight of 149.619. Sevelamer Carbonate replaces chlorine ions with bicarbonate ions to reduce the electrolyte disturbance that may be caused after oral administration. There is no difference in the physical and chemical properties and phosphate binding properties of the two, so Sevelamer referred to in the present invention includes both Sevelamer Hydrochloride. Vilamer also includes sevelamer carbonate. The structural formulas of the two are shown below. [0003] Formula 1: Formula 2: [0004] F...

Claims

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Application Information

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IPC IPC(8): A61K31/785A61P35/00A61P35/04A61P1/16A61L24/00A61L24/04
CPCA61K31/785A61P35/00A61P35/04A61P1/16A61L24/0015A61L24/04C08L39/00
Inventor 唐群毕秋臣
Owner NANCHANG UNIV
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