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The control method of piperaquine phosphate impurity

A technology of piperaquine phosphate and control method, which is applied in the field of control of piperaquine phosphate impurities, can solve the problems that impurity control methods are difficult to remove, and achieve the effects of wide sources of equipment and medicaments, cost reduction, and simple process

Active Publication Date: 2017-04-19
GUILIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In the related art, in the synthetic crude piperaquine phosphate, it contains various impurities, such as 1,4-bis(3-(4-(7-chloroquinolin-4-yl)piperazin-1-yl)propane Base) piperazine, 7-chloro-4-(4-(3-((7-chloroquinolin-4-yl) oxo) propyl) piperazin-1-yl) quinoline, N1-(7-chloroquine Lin-4-yl)-N2-(3-(4-(7-chloroquinolin-4-yl)piperazin-1-yl)propyl)ethane-1,2-diamine, the above three impurities The structure and properties are relatively similar to piperaquine phosphate; therefore, the impurity control methods in the related art are difficult to remove the three impurities at the same time, and make their content in the finished piperaquine phosphate medicine be controlled within the corresponding standard range

Method used

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  • The control method of piperaquine phosphate impurity
  • The control method of piperaquine phosphate impurity
  • The control method of piperaquine phosphate impurity

Examples

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Embodiment 1

[0042] The method for controlling the impurities of piperaquine phosphate provided in this example includes: adding crude piperaquine phosphate into a non-polar solvent, stirring and then filtering to obtain a primary purified solid. The primary purified solid is added into a polar solvent, refluxed and stirred, and filtered to obtain a filtered solid, and the filtered solid is dried to obtain a secondary purified solid. The secondary purified solid was added into a polar mixed solvent, stirred and dissolved at 100° C., and then activated carbon was added for decolorization and then filtered to obtain a filtrate. The filtrate is cooled and crystallized, and then filtered, washed and dried to obtain purified piperaquine phosphate.

Embodiment 2

[0044] The method for controlling the impurities of piperaquine phosphate provided in this example includes: adding the crude piperaquine phosphate to ethyl acetate whose weight is 9 times its weight, stirring at 50° C. for 1.5 hours and then filtering to obtain a primary purified solid. The primary purified solid was added into ethanol, refluxed and stirred for 1.5 hours at a temperature of 35°C, and then filtered to obtain a filtered solid, which was dried to obtain a secondary purified solid. The secondary purified solid was added to a mixed solution of water and ethanol with a volume ratio of 100:1, stirred and dissolved at 90° C., and activated carbon was added to incubate for 28 minutes and then filtered to obtain a filtrate. The filtrate was cooled and crystallized at room temperature for 7 hours, followed by filtration, washing with purified water and drying to obtain purified piperaquine phosphate.

Embodiment 3

[0046] The method for controlling the impurities of piperaquine phosphate provided in this example comprises: adding the crude piperaquine phosphate into methylene chloride 10 times its weight, stirring at 55° C. for 2 hours and then filtering to obtain a primary purified solid. The primary purified solid was added into acetone, refluxed and stirred for 2 hours at a temperature of 70°C, and then filtered to obtain a filtered solid, which was dried to obtain a secondary purified solid. The secondary purified solid was added to a mixed solution of water and ethanol with a volume ratio of 500:1, stirred and dissolved at 100° C., and then activated carbon was added to incubate for 30 minutes and then filtered to obtain a filtrate. The filtrate was cooled and crystallized at room temperature for 8 hours, followed by filtration, washing with purified water and drying to obtain purified piperaquine phosphate.

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Abstract

The invention relates to the field of piperaquine phosphate impurity control, and specifically relates to a control method of piperaquine phosphate impurity. The control method of piperaquine phosphate impurity comprises the following steps: 1), adding a non-polar solvent into a piperaquine phosphate crude product, stirring and filtering; 2), adding a polar solvent, conducting reflux, stirring and filtering; 3), adding a water / polar mixed solvent, stirring and dissolving at 90-110 DEG, adding activated carbon for decoloring and filtering to obtain a filtrate, cooling, crystallizing, filtering, washing and drying. The steps 1) 2) and 3) are not in a particular order. The control method of piperaquine phosphate impurity provided by the invention has the advantages of simple process, and extensive equipment and reagent sources, thus indirectly reducing cost for drug impurity removal, and can be widely applied to preparation of piperaquine phosphate.

Description

technical field [0001] The invention relates to the field of impurity control of piperaquine phosphate, in particular to a method for controlling the impurity of piperaquine phosphate. Background technique [0002] As one of the most dangerous diseases, malaria is still widely prevalent in the world (especially in tropical areas), and it threatens human health, and the situation is severe. With the intensification of drug resistance and changes in the human living environment, the current malaria epidemic situation is more serious than 30 years ago, involving more than 100 countries, with a population of 3 billion, and 500 million cases of clinical diagnosis each year. [0003] Piperaquine is a bisquinoline antimalarial drug, which was synthesized by Shanghai Institute of Pharmaceutical Industry in my country and RhonePoulenc in France in the 1960s. The initial research results showed that piperaquine was effective against falciparum malaria, including anti-chloroquine falc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D215/46C07D215/42G01N30/02
CPCC07D215/42C07D215/46G01N30/02
Inventor 郑清四蒋超意潘梅齐文杰
Owner GUILIN PHARMA
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