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Lurasidone hydrochloride-amino acid coamorphous material

A technology of lurasidone hydrochloride and amorphous substance, applied in the field of medicine, can solve the problems of low dissolution rate, poor water solubility, low oral bioavailability and the like

Active Publication Date: 2017-09-15
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Lurasidone hydrochloride has poor water solubility and low dissolution rate, resulting in low oral bioavailability

Method used

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  • Lurasidone hydrochloride-amino acid coamorphous material
  • Lurasidone hydrochloride-amino acid coamorphous material
  • Lurasidone hydrochloride-amino acid coamorphous material

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Example 1: Preparation of lurasidone hydrochloride L-cysteine ​​hydrochloride co-amorphous

[0065] Add 0.50g of lurasidone hydrochloride and 0.15g of L-cysteine ​​hydrochloride into 250mL of ethanol, and ultrasonically dissolve at room temperature to obtain a clear solution. Rotate the solvent under reduced pressure at 40°C to dry the clear solution under vacuum at 25°C. After 24 hours, 0.38 g of white powder was obtained.

Embodiment 2

[0066] Example 2: Preparation of lurasidone hydrochloride L-cysteine ​​hydrochloride co-amorphous

[0067] Add 0.50g of lurasidone hydrochloride and 0.15g of L-cysteine ​​hydrochloride into 50mL of methanol, and ultrasonically dissolve at room temperature to obtain a clear solution. Rotate the solvent under reduced pressure at 50°C to dry the clear solution under vacuum at 25°C. After 24 hours, 0.53 g of white powder was obtained.

Embodiment 3

[0068] Example 3: Preparation of lurasidone hydrochloride L-cysteine ​​hydrochloride co-amorphous

[0069] Add 0.50 g of lurasidone hydrochloride and 0.15 g of L-cysteine ​​hydrochloride into 60 mL of methanol-ethanol (50:50, v / v) mixed solvent, and ultrasonically dissolve at room temperature to obtain a clear solution. The solvent was rotary evaporated under reduced pressure at 45°C, and dried in vacuum at 25°C for 24 hours to obtain 0.51 g of white powder.

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Abstract

The invention relates to a lurasidone hydrochloride-L-cysteine hydrochloride coamorphous material capable of significantly improving the solubility dissolution rate of highly-insoluble drug lurasidone hydrochloride. The coamorphous material is amorphous, is completely different from lurasidone hydrochloride crystal, and different from the lurasidone hydrochloride crystal in melting point, powder X ray diffraction spectra, DSC spectra and infrared spectroscopy. The powder X ray diffraction spectra shown by 2 theta and obtained by Cu-K alpha radiation has no sharp diffraction peak. The glass transition temperature is about 71.7 DEG C. The characteristic dissolving experiment shows that the characteristic dissolving rate of the lurasidone hydrochloride-L-cysteine hydrochloride coamorphous material is improved by about 5 times compared with that of the original lurasidone hydrochloride crystal.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a compound of lurasidone hydrochloride L-cysteine ​​hydrochloride formed by combining lurasidone hydrochloride and L-cysteine ​​hydrochloride at a molar ratio of 1:1. Shaped product and its preparation method. Background technique [0002] Lurasidone hydrochloride (Lurasidone hydrochloride), the chemical name is (3aR, 4S, 7R, 7aS)-2-[(1R,2R)-2-(4-(1,2-Phenylisothiazol-3-yl )piperazin-1-ylmethyl)cyclohexylmethyl]hexahydro-4,7-methylisoindole-1,3-dione hydrochloride is a new type of atypical antipsychotic. Compared with similar drugs, it has the advantages of good curative effect, high safety, and good tolerance, and has been used as a first-line antipsychotic drug. According to the biopharmaceutical classification system, it belongs to BCS class II drug, which has the characteristics of low solubility and high permeability. Lurasidone hydrochloride has poor water solubility an...

Claims

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Application Information

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IPC IPC(8): C07D417/12
CPCC07D417/12
Inventor 高缘王晓洁钱帅张建军梁淑君周生研
Owner CHINA PHARM UNIV
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