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A kind of preparation method of feilimotuo

A technology of limotine and dextran, which is applied in the field of preparation of filimote, can solve the problems of low product stability, poor reproducibility, and difficult control of the reaction process, and achieves stable raw materials, uniform particle size, and convenient quality. control effect

Active Publication Date: 2020-03-10
LIANYUNGANG RUNZHONG PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] However, the inventors have found that as a superparamagnetic iron oxide coated and modified by polyglucose sorbitolcarboxymethylether (polyglucose sorbitolcarboxymethylether, a modified dextran), the preparation of Ferimox in the prior art exists Many difficulties, such as difficult control of the reaction process, low product stability, poor reproducibility, etc. (WO 00 / 61191A2)

Method used

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  • A kind of preparation method of feilimotuo

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 The preparation of feilimotuo

[0024] Step 1: Reduction reaction

[0025] Dextran T10 (100g) was dissolved in water (300mL), sodium borohydride (11.3g) was added, stirred at 30°C for 24h, and 6M HCl aqueous solution was added dropwise to quench the reaction, and the pH was adjusted to 6.5. The completed reaction solution was transferred into a dialysis bag of MWCO 3kDa, and the dialysis bag was placed in distilled water for dialysis for 24 hours, and the distilled water was replaced every 6 hours. The dialysate was concentrated using a MWCO 3kDa ultrafiltration membrane, and the concentrated solution was filtered through a 0.22 μm filter membrane, and then absolute ethanol was added to the filtrate to obtain a white emulsion. After vacuum concentration, 80 g of a white solid substance, namely reduced dextran T 10, was obtained.

[0026] Step 2: Alkylation reaction

[0027] The reduced dextran T 10 (10 g) prepared in step 1 was dissolved in water (50 mL),...

Embodiment 2

[0030] Example 2 Preparation of Ferimox

[0031] Step 1: Reduction reaction

[0032] Dextran T10 (100g) was dissolved in water (300mL), sodium borohydride (3.77g) was added, stirred at 30°C for 24h, and 6M HCl aqueous solution was added dropwise to quench the reaction, and the pH was adjusted to 6.5. The completed reaction solution was transferred into a dialysis bag of MWCO 3kDa, and the dialysis bag was placed in distilled water for dialysis for 24 hours, and the distilled water was replaced every 6 hours. The dialysate was concentrated using a MWCO 3kDa ultrafiltration membrane, and the concentrated solution was filtered through a 0.22 μm filter membrane, and then absolute ethanol was added to the filtrate to obtain a white emulsion. After vacuum concentration, 80 g of a white solid substance, namely reduced dextran T 10, was obtained.

[0033] Step 2: Alkylation reaction

[0034] The reduced dextran T10 (10 g) prepared in step 1 was dissolved in water (50 mL), and bromoa...

Embodiment 3

[0037]Example 3 Determination of the average particle size (diameter) and particle size polydispersity coefficient of the obtained product (whole micelle) (the instrument is a Malvern Nano ZS90 particle size potential analyzer, and the product is diluted to the same concentration and then measured)

[0038] Experimental process: first prepare the sample, dilute the product to be tested with water to obtain two samples with a concentration of 1mg / mL and 0.1mg / mL, and add 1mL of the sample to the sample pool. Secondly, run the equipment and detection software to detect the particle size of the product at two different concentrations, and then take the average value of the particle size data of the two samples. The particle size of the two concentrations of the samples should be relatively close and should not depend on the sample concentration. .

[0039]

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Abstract

The invention relates to a method for preparing ferumoxytol. The method comprises the following steps: a reduction reaction, an alkylation reaction and a coprecipitation method to obtain ferumoxytol. According to the preparation method, the particle size of the prepared ferumoxytol is uniform, coating thickness is more uniform, bulk drugs of ferumoxytol is more stable, and reaction reappearance is high.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and relates to a method for preparing phenimotol, specifically, preparing phenimotox through reduction, alkylation and co-precipitation methods. Background technique [0002] Anemia is a clinical syndrome in which the volume of red blood cells in the peripheral blood of the human body decreases, which is lower than the lower limit of the normal range. The prevalence of anemia in the Chinese population is about 20.1%, and there are many causes, half of which are caused by iron deficiency. Clinical treatment methods include blood transfusion, drug therapy, splenectomy and hematopoietic stem cell transplantation. [0003] Among drug treatments, iron supplementation has the most significant therapeutic effect on patients with iron deficiency anemia. Currently clinically used iron supplements mainly include intravenous iron supplements and oral iron supplements. Although oral iron is more conveni...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K9/51A61K47/36A61K33/26A61P3/02A61P7/06
Inventor 顾宁刘飞陈博刘彦龙吉民
Owner LIANYUNGANG RUNZHONG PHARMA CO LTD