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Lurasidone hydrochloride tryptophan coamorphous substance/lurasidone hydrochloride L-proline coamorphous substance and production method and application thereof

A technology for lurasidone hydrochloride tryptophan and lurasidone hydrochloride, which is applied in the field of medicine, can solve the problems of low solubility and slow dissolution rate, and achieves the effects of simple preparation, improved applicability, and improvement of clinical adverse reactions

Active Publication Date: 2020-11-24
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Purpose of the invention: Aiming at the problems of lurasidone hydrochloride low solubility and slow dissolution rate and adverse reactions in clinical use, the present invention provides lurasidone hydrochloride tryptophan Co-amorphous substance and lurasidone hydrochloride L-proline two co-amorphous substances, compared with the original lurasidone hydrochloride, the two co-amorphous substances can significantly improve the solubility and dissolution of lurasidone hydrochloride rate, and two amino acid ligands can improve the adverse reactions of lurasidone hydrochloride

Method used

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  • Lurasidone hydrochloride tryptophan coamorphous substance/lurasidone hydrochloride L-proline coamorphous substance and production method and application thereof
  • Lurasidone hydrochloride tryptophan coamorphous substance/lurasidone hydrochloride L-proline coamorphous substance and production method and application thereof
  • Lurasidone hydrochloride tryptophan coamorphous substance/lurasidone hydrochloride L-proline coamorphous substance and production method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0062] Preparation of lurasidone hydrochloride tryptophan co-amorphous

[0063] Weigh 0.5g of lurasidone hydrochloride and 0.193g of tryptophan into the same 100mL eggplant-shaped bottle, add 50mL of methanol, stir at room temperature and sonicate until completely dissolved to obtain a clear and transparent solution. The solution was placed on a vacuum rotary evaporator, and the temperature of the water bath was 55 °C. After the methanol solvent evaporated completely, the corresponding solid product was obtained. Place it in a vacuum drying oven at room temperature for 24 hours to remove the residual solvent in the rotary evaporated product, take out the final product in an environment with a relative humidity of less than 30% RH, and store it at 4°C with a humidity of less than 30% RH.

Embodiment 2

[0065] Preparation of lurasidone hydrochloride tryptophan co-amorphous

[0066] Weigh 0.5g of lurasidone hydrochloride and 0.193g of tryptophan into the same 100mL eggplant-shaped bottle, add 50mL of methanol, stir at room temperature and sonicate until completely dissolved to obtain a clear and transparent solution. The solution was placed on a vacuum rotary evaporator, and the temperature of the water bath was 35 °C. After the methanol solvent evaporated completely, the corresponding solid product was obtained. Place it in a vacuum drying oven at room temperature for 24 hours to remove the residual solvent in the rotary evaporated product, take out the final product in an environment with a relative humidity of less than 30% RH, and store it at 4°C with a humidity of less than 30% RH.

Embodiment 3

[0068] Preparation of lurasidone hydrochloride tryptophan co-amorphous

[0069] Weigh 0.5g of lurasidone hydrochloride and 0.193g of tryptophan into the same 100mL eggplant-shaped bottle, add 60mL of ethanol, stir at room temperature and sonicate until completely dissolved to obtain a clear and transparent solution. The solution was placed on a vacuum rotary evaporator, and the temperature of the water bath was 60 °C. After the ethanol solvent evaporated completely, the corresponding solid product was obtained. Place it in a vacuum drying oven at room temperature for 24 hours to remove the residual solvent in the rotary evaporated product, take out the final product in an environment with a relative humidity of less than 30% RH, and store it at 4°C with a humidity of less than 30% RH.

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Abstract

The invention discloses a lurasidone hydrochloride tryptophan coamorphous substance / lurasidone hydrochloride L-proline coamorphous substance and a production method and application thereof. The coamorphous substance comprises the lurasidone hydrochloride tryptophan coamorphous substance or the lurasidone hydrochloride L-proline coamorphous substance, and is formed by mixing lurasidone hydrochloride and tryptophan according to a molar ratio of 1:1 or is formed by mixing lurasidone hydrochloride and L-proline according to a molar ratio of 1:1. The two coamorphous substances are in amorphous states, and are completely different from lurasidone hydrochloride bulk medicine crystals, powder X-ray diffraction, DSC spectrograms and infrared spectroscopy are all different from those of the lurasidone hydrochloride, Cu-Kalpha radiation is used, and a powder X-ray diffraction spectrum does not have sharp diffraction peaks. A glass-transition temperature of the lurasidone hydrochloride tryptophancoamorphous substance is 71.7 DEG C, and the characteristic speed is improved by about ten times compared with that of the original lurasidone hydrochloride; and a glass-transition temperature of thelurasidone hydrochloride L-proline coamorphous substance is 65.0 DEG C, and the characteristic speed is improved by about five times compared with that of the original lurasidone hydrochloride.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to two co-amorphous forms of lurasidone hydrochloride formed by lurasidone hydrochloride, tryptophan and L-proline, and a preparation method and application thereof. Background technique [0002] Lurasidone hydrochloride (Lurasidone hydrochloride), the chemical name is (3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl) )piperazin-1-ylmethyl]cyclohexylmethyl}hexahydro-1H-4,7-methylisoindole-1,3-dione hydrochloride is a new type of atypical antipsychotic . Compared with similar drugs, it has significant curative effect on both positive and negative symptoms of mental patients, and is widely used clinically. However, its clinical use also has many side effects, such as drowsiness, gastrointestinal reactions, eye system diseases, metabolic and nutritional diseases, and blood system diseases. According to the classification system of biopharmaceuticals, lurasidone h...

Claims

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Application Information

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IPC IPC(8): C07D417/12C07D209/20C07D207/16A61K31/496A61K47/18A61P25/18
CPCC07D417/12C07D209/20C07D207/16A61K31/496A61K47/183A61P25/18
Inventor 张建军乔旗洋王亚茹
Owner CHINA PHARM UNIV
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