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Purification method of high-purity lobaplatin trihydrate for preparing antitumor drugs

A pure lobaplatin trihydrate, lobaplatin trihydrate technology, applied in antitumor drugs, drug combinations, platinum group organic compounds, etc., can solve problems such as affecting product quality, failing to meet requirements, and introducing impurities into products

Active Publication Date: 2021-07-27
KUNMING GUIYAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] From the perspective of the route for preparing lobaplatin trihydrate, the synthetic route is long, and the chemical raw materials used are more, and impurities are easily introduced into the product, thereby affecting product quality and failing to meet the safety of lobaplatin used in antineoplastic drugs Require
[0007] In addition, the content of the crude lobaplatin prepared by the above process is generally between 60% and 80%, which cannot meet the requirements for high-purity lobaplatin used in antineoplastic drugs

Method used

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  • Purification method of high-purity lobaplatin trihydrate for preparing antitumor drugs
  • Purification method of high-purity lobaplatin trihydrate for preparing antitumor drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Embodiment 1: the purification method of lobaplatin, concrete operation is as follows:

[0033] (1) Dissolve 50 g of the crude product containing lobaplatin 70.65% in 300 mL of 80°C water in a dark environment, stir for 5 minutes and then filter, place the filtrate in an environment of 0°C, stir rapidly for 3 hours, filter, and wash the filter cake with ice water 1 time, filter dry, and air-dry at 35°C for 4 hours.

[0034] (2) Product testing

[0035] In this example, the measured product content is 98.72%, the water content is 12.07% (the theoretical water content of lobaplatin trihydrate is 11.98%), and the yield is 53.37%.

Embodiment 2

[0036] Embodiment 2: the purification method of lobaplatin, concrete operation is as follows:

[0037] (1) Dissolve 50 g of the crude product containing lobaplatin 82.76% in 150 mL of 95°C water in a dark environment, stir for 2 minutes and then filter, place the filtrate in an environment of 9°C, stir rapidly for 2 hours, filter, and wash the filter cake with ice water 1 time, filter dry, and air-dry at 45°C for 2 hours.

[0038] (2) Product testing

[0039] In this example, the measured product content is 99.03%, the water content is 12.02% (the theoretical water content of lobaplatin trihydrate is 11.98%), and the yield is 52.98%.

Embodiment 3

[0040] Embodiment 3: the purification method of lobaplatin, concrete operations are as follows:

[0041] (1) Dissolve 50 g of the crude product containing lobaplatin 82.01% in 300 mL of water at 90° C. in a dark environment, stir for 3 minutes, and then filter. Add 1500 mL of diethyl ether to the collected filtrate, place in -10°C environment, stir rapidly for 2 hours, filter, stir and wash the filter cake twice with ice water, filter dry, and blow dry at 55°C for 1 hour.

[0042] (2) Product testing

[0043] In this example, the measured product content is 99.93%, the water content is 11.92% (the theoretical water content of lobaplatin trihydrate is 11.98%), and the yield is 83.18%.

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Abstract

The invention relates to a purification method of a high-purity lobaplatin trihydrate for preparing an antitumor drug. The method comprises the following steps: 1, dissolving a lobaplatin crude product in a high-temperature aqueous solution, filtering, crystallizing at low temperature, re-filtering, and drying to obtain the lobaplatin trihydrate; and 2, dissolving the lobaplatin crude product in a high-temperature aqueous solution, filtering, adding diethyl ether into the filtrate, crystallizing at low temperature, filtering, and drying to obtain the lobaplatin trihydrate. According to the invention, the purification can be repeated multiple times until the high-purity lobaplatin trihydrate is obtained; according to the purification method, the lobaplatin crude product with the content of 55-95% is purified, the purity of the lobaplatin crude product can be improved to 98% or above, the used purification solvent is water or diethyl ether, and after the sample is fully washed with water, the obtained product is high in safety; purification belongs to conventional operation, and preparation is easy; the prepared high-purity lobaplatin trihydrate can be applied to antitumor drugs; and the preparation method is short in preparation time, simple to operate, low in production cost and suitable for industrial production.

Description

technical field [0001] The invention relates to a method for purifying lobaplatin, in particular to a method for purifying high-purity lobaplatin trihydrate for preparing antitumor drugs. Background technique [0002] Lobaplatin (lobaplatin), also known as Lobaplatin and Lobaplatin, has a chemical name of cis-(trans-1,2-diaminomethyl-cyclobutane)-lactate platinum (Ⅱ), which is produced by German ASTA Medica The third-generation platinum-based antineoplastic drug developed by the company has a chemical structural formula as shown in the following formula (a), and a trihydrate structural formula as shown in the following formula (b). Because lobaplatin in the state of formula (a) is easy to deliquesce, difficult to preserve, and difficult to make preparations, the existing synthetic methods all make it into formula (b). [0003] [0004] At present, the process route for synthesizing lobaplatin trihydrate is still relatively complicated, using chloroplatinic acid as the st...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00
CPCC07F15/0093A61P35/00
Inventor 刘其星丛艳伟谢丽娇王应飞陈红娟郭明里
Owner KUNMING GUIYAN PHARMA
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