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Amorphous levo-praziquantel solid and preparation method and application thereof

A kind of L-praziquantel, amorphous technology, applied in the field of medicine

Pending Publication Date: 2018-11-13
TONGLI BIOMEDICAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no patent or document describing the amorphous L-praziquantel. This application provides an amorphous L-praziquantel solid and its preparation method and application. To a certain extent, this substance is used as an important activity Provided technical support for the research and production of the ingredients of the drug

Method used

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  • Amorphous levo-praziquantel solid and preparation method and application thereof
  • Amorphous levo-praziquantel solid and preparation method and application thereof
  • Amorphous levo-praziquantel solid and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1: Dissolve L-praziquantel crystal powder and / or oily L-praziquantel in isopropanol, and then volatilize at 50°C-100°C to obtain amorphous L-praziquantel solid.

Embodiment 2

[0049] Example 2: Select L-praziquantel crystal powder and / or oily L-praziquantel and dissolve it in methyl isobutyl ketone, and then volatilize at 50°C-100°C to obtain amorphous L-praziquantel solid.

Embodiment 3

[0050] Example 3: Select L-praziquantel crystal form powder and / or oily L-praziquantel dissolved in a mixed solvent of methyl isobutyl ketone and dimethylacetamide, and then volatilize at 50°C-100°C , that is, the amorphous solid of L-praziquantel.

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Abstract

The invention discloses an amorphous levo-praziquantel solid and a preparation method thereof. The solid has no characteristic absorption peaks in a powder X-ray diffraction pattern. The preparation method of the amorphous levo-praziquantel solid includes a step (a) and a step (b) as follows: (a) dissolving levo-praziquantel crystal form powder and / or oily levo-praziquantel in a mixed solvent ofa first organic solvent or a second organic solvent and water, and then placing the mixture at 50 DEG C to 100 DEG C for volatilization; and (b) dissolving levo-praziquantel crystal form powder and / or oily levo-praziquantel in a third organic solvent, and then adding a high molecular polymer to induct precipitation of the solid. The method combines multiple clinical advantages of the levo-praziquantel and the advantages that the reactivity of an amorphous structure is generally greater than that of the same substance, and paves the way for the listing of the amorphous levo-praziquantel solidand / or medicine which contains the amorphous levo-praziquantel solid as an active ingredient and treats schistosomiasis and a plurality of parasitic diseases.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to an amorphous solid L-praziquantel and its preparation method and application. Background technique [0002] Praziquantel is a synthetic pyrazine isoquinoline derivative, also known as ciclopraziquantel, white or off-white crystalline powder, bitter in taste, and is currently the only drug of choice for broad-spectrum human, fluke and tapeworm infections. Because of its high efficiency, low toxicity, wide anti-parasitic spectrum, and convenient oral administration, it is popular among patients and soon became the main drug for treating schistosomiasis and various parasitic diseases in the world. It has been included in the pharmacopoeia of the United States, the United Kingdom and many other countries, as well as the "European Pharmacopoeia", "International Pharmacopoeia" and the World Health Organization's essential drug catalog. At present, praziquantel has been listed as a category A v...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/4985A61P33/00A61P33/12
CPCC07D471/04C07B2200/07Y02A50/30
Inventor 施俊巍钱明心
Owner TONGLI BIOMEDICAL
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