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Preparation method of lurasidone hydrochloride nanocrystals based on solubility pH-dependent property

A technology of lurasidone hydrochloride and nanocrystals, which is applied in the field of medicine, can solve the problems of low solubility of lurasidone hydrochloride, poor oral bioavailability, slow dissolution rate, etc., to improve oral bioavailability, increase solubility and Effect of dissolution rate and low production cost

Inactive Publication Date: 2017-03-15
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to solve the problems of low solubility of lurasidone hydrochloride, slow dissolution rate, poor oral bioavailability, complex process, high cost and use of toxic and harmful organic solvents in the prior art for preparing lurasidone hydrochloride nanocrystals etc., provide a method for preparing nanocrystals based on the solubility of lurasidone hydrochloride with pH-dependent properties

Method used

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  • Preparation method of lurasidone hydrochloride nanocrystals based on solubility pH-dependent property
  • Preparation method of lurasidone hydrochloride nanocrystals based on solubility pH-dependent property
  • Preparation method of lurasidone hydrochloride nanocrystals based on solubility pH-dependent property

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Weigh 12 mg of lurasidone hydrochloride and dissolve it in a mixed solvent of 3 mL of pH4 hydrochloric acid solution and 1 mL of ethanol as a good solvent; weigh 8 mg of poloxamer and 4 mg of Tween 80 and dissolve it in 40 mL of deionized water as a poor solvent; The good solvent was dripped into the poor solvent at a dropping rate of 16mL / min, and the stirring rate was controlled at 200r / min. After the dropping, the stirring was continued for 1.5h to obtain lurasidone hydrochloride nanocrystals. Detected with a laser particle size analyzer, the average particle diameter is 579.8nm, and the polydispersity index is 0.34.

Embodiment 2

[0031] Weigh 20 mg of lurasidone hydrochloride and dissolve it in a mixed solvent of 16 mL of pH4 hydrochloric acid solution and 4 mL of propylene glycol as a good solvent; weigh 5 mg of methylvitamin and dissolve it in 160 mL of deionized water as a poor solvent; Drop into the poor solvent at a dropping speed of 3 mL / min, control the stirring speed at 400 r / min, and continue stirring for 1 h after the dropping to obtain lurasidone hydrochloride nanocrystals. Detected with a laser particle size analyzer, the average particle diameter is 238.3nm, and the polydispersity index is 0.22.

Embodiment 3

[0033] Weigh 10 mg of lurasidone hydrochloride and dissolve it in a mixed solvent of 3 mL of pH4 hydrochloric acid solution and 1 mL of propylene glycol as a good solvent; weigh 10 mg of polyethylene glycol and dissolve it in 300 mL of deionized water as a poor solvent; Drop into the poor solvent at a dropping speed of 5 mL / min, control the stirring speed at 1200 r / min, and continue stirring for 3 h after the dropping to obtain lurasidone hydrochloride nanocrystals. Detected with a laser particle size analyzer, the average particle diameter is 376.2nm, and the polydispersity index is 0.26.

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Abstract

The invention relates to a preparation method of lurasidone hydrochloride nanocrystals based on the solubility pH-dependent property and belongs to the technical field of medicine. The preparation method of the lurasidone hydrochloride nanocrystals includes the steps that 1, lurasidone hydrochloride is dissolved in a mixed solvent of a pH4 hydrochloric acid solution and a latent solvent, and the mixture serves as a good solvent; 2, a stabilizer is dissolved in deionized water, and the mixture serves as a poor solvent; 3, the good solvent with lurasidone hydrochloride dissolved is added into the poor solvent, magnetic stirring dispersion is carried out, after the good solvent is added into the poor solvent, the materials continue to be stirred, and the nanocrystals are prepared. The prepared nanocrystals are uniform in quality and appearance, the average grain diameter is 200-600 nm, and the solubility, dissolution rate and oral bioavailability of lurasidone hydrochloride are remarkably improved. The preparation process is simple, operation is easy to carry out, cost is low, no toxic or harmful organic solvent is used, no byproducts are generated, and industrial production is convenient.

Description

technical field [0001] The invention relates to a method for preparing lurasidone hydrochloride nanocrystals based on the solubility-dependent pH property, and belongs to the technical field of medicine. Background technique [0002] Lurasidone hydrochloride was approved by the US FDA in October 2010 for the treatment of schizophrenia. The drug belongs to the BCS Class II drug of the biopharmaceutics classification system, and its extremely low solubility and dissolution rate are the main reasons for its poor oral bioavailability (after a single oral administration, the absolute bioavailability in the human body is 9% to 19%. %). [0003] At home and abroad, there have been related research reports on making lurasidone hydrochloride into different dosage forms such as solid dispersion, microemulsion, and co-amorphous to improve its adverse properties. Although these methods can improve the solubility, dissolution rate and oral bioavailability of lurasidone hydrochloride, t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12
CPCC07D417/12C07B2200/13
Inventor 刘建平于盼盼李莹
Owner CHINA PHARM UNIV
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