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A kind of ultrasonic-assisted preparation spherical praziquantel crystal and method

An ultrasound-assisted, praziquantel technology, applied in the direction of organic chemistry, organic chemistry, and resistance to vector-borne diseases, can solve problems such as difficult effects and product purity, and achieve cost savings, uniform crystal shape, and fluidity. Good results

Active Publication Date: 2022-05-20
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, traditional crystal habit additives are difficult to be effective, and the introduction of additives in the entire praziquantel production process will affect the purity of the product

Method used

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  • A kind of ultrasonic-assisted preparation spherical praziquantel crystal and method
  • A kind of ultrasonic-assisted preparation spherical praziquantel crystal and method
  • A kind of ultrasonic-assisted preparation spherical praziquantel crystal and method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046]Add 25.5g of praziquantel to 100.0g of isopropanol solution, start stirring, the stirring rate is 50rpm, the system temperature is 50°C, adopt the cooling crystallization method, cool down at 10°C / h, and insert the ultrasonic probe when the temperature drops to 30°C , set the ultrasonic power to 100W, and the ultrasonic time to 5min. During the ultrasonic process, crystals will be precipitated in the system. After maintaining the crystal for 30min, continue to cool down at 30°C / h until the temperature is lowered to 0°C, and keep warm for 30min. Then filter, wash with ice isopropanol (0° C.), and dry at 50° C. under normal pressure for 3 hours to constant weight to obtain praziquantel spherical crystal product. The mass fraction of crystals within the particle size range of 1 mm to 3 mm is 90.9%, the roundness value of the praziquantel spherical product is 0.94, the angle of repose is 7°, and the caking rate is 2.32%.

Embodiment 2

[0048] Add 25.5g of praziquantel to 100.0g of isopropanol solution, start stirring, the stirring rate is 50rpm, the system temperature is 50°C, adopt the cooling crystallization method, cool down at 10°C / h, and insert the ultrasonic probe when the temperature drops to 30°C , set the ultrasonic power to 100W, and the ultrasonic time to 5min. During the ultrasonic process, crystals will be precipitated in the system. After maintaining the crystal for 30min, continue to cool down at 30°C / h until the temperature is lowered to 0°C, and keep warm for 30min. Then filter, wash with ice isopropanol (0° C.), and dry at 50° C. under normal pressure for 3 hours to constant weight to obtain praziquantel spherical crystal product. The mass fraction of crystals within the particle size range of 1 mm to 3 mm is 91.7%, the roundness value of the praziquantel spherical product is 0.94, the angle of repose is 8°, and the caking rate is 2.98%.

Embodiment 3

[0050] Add 30.0g of praziquantel to 100.0g of isopropanol solution, start stirring, the stirring rate is 100rpm, the system temperature is 60°C, adopt the cooling crystallization method, cool down at 10°C / h, insert the ultrasonic probe when the temperature drops to 37.5°C , set the ultrasonic power to 100W, and the ultrasonic time to 5min. During the ultrasonic process, crystals will be precipitated in the system. After maintaining the crystal for 30min, continue to cool down at 20°C / h until the temperature is lowered to 0°C, and keep warm for 30min. Then filter, wash with ice isopropanol (0° C.), and dry at 50° C. under normal pressure for 3 hours to constant weight to obtain praziquantel spherical crystal product. The mass fraction of crystals within the particle size range of 1 mm to 3 mm is 92.9%, the roundness value of the praziquantel spherical product is 0.91, the angle of repose is 6°, and the caking rate is 3.12%.

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Abstract

The invention relates to an ultrasonic-assisted preparation of spherical praziquantel crystals and a method thereof. Add crude praziquantel into isopropanol solution, stir and dissolve at 50-60°C, prepare praziquantel-isopropanol solution, cool and crystallize by cooling crystallization, add ultrasound at 30-39.5°C, ultrasonic power 10- 100W / mL solution, ultrasonic time is 5-30min, then continue to cool down to crystallize to 0-5°C, keep the temperature for 30min-60min, filter, wash and dry to obtain spherical crystals of praziquantel. The average roundness value is above 0.85, and the angle of repose is below 11°. Spherical praziquantel crystals have the characteristics of high purity, good fluidity, high bulk density, high yield, small crystal particle size and uniform crystal shape, as well as excellent anti-agglomeration performance and bioavailability. The solvent used in the reaction process can be recovered, and the granulation step is omitted by direct forming into spheres, which is a method with great industrial application prospects.

Description

technical field [0001] The invention belongs to the technical field of chemical engineering crystallization, and in particular relates to a method for preparing spherical crystals of praziquantel. In particular, an ultrasonic-assisted preparation of spherical praziquantel crystals and a method thereof. Background technique [0002] Praziquantel is an anthelmintic used in humans and animals to treat tapeworms and trematodes. It is particularly effective for schistosomiasis, Chinese liver fluke, and Schizophrenia grandis. Praziquantel is a drug on the World Health Organization's Model List of Essential Drugs, and is one of the most important drugs for basic public health in the world. [0003] Praziquantel (also known as cyclic praziquantel), its chemical name is 2-cyclohexylcarbonyl-1,3,4,6,7,11-hexahydro-2-pyrazino(2,1-A) Isoquinolin-4-one, formula C 19 h 24 N 2 o 2 , its chemical structure is: [0004] [0005] Most of the currently disclosed praziquantel purific...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/04
CPCC07D471/04C07B2200/13Y02A50/30
Inventor 龚俊波张旭尹秋响吴送姑杜世超刘裕侯宝红李中华
Owner TIANJIN UNIV
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