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Polycrystal substance of piperaquine phosphate and preparation method thereof

A technology of piperaquine phosphate and crystal form, applied in the field of piperaquine phosphate polymorph and its preparation, can solve the problems of easy discoloration, unstable physical and chemical properties, increase of related substances, etc., and achieves low toxicity, harm to people and the environment Friendly, easy-to-use effects

Active Publication Date: 2012-07-11
珠海润都制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The piperaquine phosphate raw material drug is easy to change color when exposed to light in the air, resulting in unstable physical and chemical properties such as the increase of related substances, thus causing inconvenience in the production and processing process

Method used

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  • Polycrystal substance of piperaquine phosphate and preparation method thereof
  • Polycrystal substance of piperaquine phosphate and preparation method thereof
  • Polycrystal substance of piperaquine phosphate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1: Preparation of piperaquine phosphate crystal form A

[0053] Add 112.0kg of piperazine hexahydrate (II) into the synthesis tank, heat until the solid melts completely, keep the temperature in the tank at 50-60°C, slowly add 30.0kg of 4,7-dichloroquinoline under stirring, and continue heating to 100 -110°C, stirred and refluxed for 4-6 hours. Stop heating and stirring, lower the temperature to 88-90°C, keep warm and let stand to separate layers. Take the oil in the lower layer, add 50L of purified water, heat to 70-80°C, stir for 5-10 minutes, let stand to separate layers, take the oil in the lower layer, and wash with water repeatedly until pH=7-8. Put the oily substance back into the synthesis tank, add 25kg of concentrated hydrochloric acid with a concentration of 35.8% and 100kg of purified water at 80°C under stirring, acidify to pH=2.5-3.5, stop stirring, and filter to remove insoluble matter. Inhale the filtrate into a synthesis tank, lower the temper...

Embodiment 2

[0056] Embodiment 2: Preparation of piperaquine phosphate crystal form B

[0057] Weigh 50mg of piperaquine phosphate crystal form A, suspend in 1mL of ethanol, suspend and stir at room temperature to 50°C for 2-3 days, filter, and vacuum-dry the filter cake to obtain piperaquine phosphate crystal form B, and pass XRPD, DSC and Characterized by TGA (e.g. Figure 4-6 shown).

Embodiment 3

[0058] Example 3: Preparation of Piperaquine Phosphate Form C

[0059] Weigh 50 mg of piperaquine phosphate crystal form A, suspend in 1 mL of acetone or acetonitrile, suspend and stir at room temperature for 2-3 days, filter, and vacuum-dry the filter cake to obtain piperaquine phosphate crystal form C, and pass XRPD, DSC and TGA To characterize (such as Figure 7-9 shown).

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PUM

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Abstract

The invention discloses a novel polycrystal substance of piperaquine phosphate. Compared with amorphous piperaquine phosphate, the polycrystal substance of the piperaquine phosphate, which is disclosed by the invention, has better stability and better facilitates the production, the storage and the circulation of raw medicine and preparations thereof, wherein a crystal form A of the piperaquine phosphate has the best stability, the best dissolution rate and the best dissolubility. The invention further discloses a preparation method of the polycrystal substance of the piperaquine phosphate. The method has the advantages of low toxicity, people friendliness, environment friendliness, easily-controlled technological parameters, and the like, is simple to operate and is suitable for mass production.

Description

technical field [0001] The invention relates to a novel polymorphic form of piperaquine phosphate and a preparation method thereof. Background technique [0002] As one of the three catastrophic diseases, malaria is caused by Plasmodium, which is mainly transmitted through mosquito bites. The main symptoms are fever, headache and vomiting. If not treated in time, malaria may be fatal. According to the World Health Organization (WHO), about 3.3 billion people worldwide are at risk of malaria, and there were about 225 million malaria cases worldwide in 2009. Malaria is particularly severe in Africa, where 709,000 of the 781,000 global malaria deaths in 2009 were in Africa. Artemisinin drugs are effective drugs for the treatment of malaria, but due to the overuse of the drug, it leads to the emergence of drug resistance. Therefore, WHO calls for stopping the use of artemisinin single-drug therapy and recommends the use of compound drugs to treat malaria. Resistance to antimal...

Claims

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Application Information

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IPC IPC(8): C07D215/46
Inventor 莫泽艺陈新民周爱新张炎峰关东
Owner 珠海润都制药股份有限公司
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