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Cariprazine tartrate, preparation method therefor and medical use thereof

A technology of cariprazine and tartaric acid, applied in the field of medicine, can solve the problems of inconvenient research of cariprazine hydrochloride, water solubility, poor stability and fluidity of hydrochloride, and achieve the effects of good solubility and not easy to absorb moisture.

Active Publication Date: 2016-01-06
ANHUI HEALSTAR PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This new type of drug called Carpazolam citric acid (CAR) can be used effectively without losing its effectiveness over time due to moisture absorption from other materials like tablets or pills containing it. It's also very stable when stored dry compared to existing drugs such as Prozac® which have been previously developed.

Problems solved by technology

This patented technical problem addressed in this patent relates to finding novel ways to improve the performance or effectiveness of certain substances called cilazapril due to changes caused by different physical chemistry characteristics such as pH value, temperature range, ionization potential, etc., while still maintaining sufficient therapeutic activity against various diseases like Parkinson' s disease.

Method used

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  • Cariprazine tartrate, preparation method therefor and medical use thereof
  • Cariprazine tartrate, preparation method therefor and medical use thereof
  • Cariprazine tartrate, preparation method therefor and medical use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: the preparation of cariprazine tartrate

[0029] Dissolve 30g of cariprazine in 650ml of absolute ethanol, stir and heat to 60-65°C, add 10.5g of tartaric acid, keep stirring for 2h, cool to 0-5°C, let stand for 5h, filter, and use proper amount of absolute ethanol for solid After washing, vacuum drying at 65-70°C for 6 hours, 35.8 g of cariprazine tartrate was obtained, with a yield of 74%, mp: 266-268°C (decomposition). HPLC content 99.2%.

[0030]

[0031] 1 H—NMR (400MHz, CDCl 3 / TMS,ppm):

[0032] δ: 6.91~7.15(m, 3H, Ar- H ), 1.08~1.53(m, 7H, cyclohexane- H ), 2.55~2.62(m, 4H, piperazine-7 H ), 3.11~3.26(m, 4H, piperazine- H ), 1.79~1.82 (m, 2H, -NC H 2 CH 2 -), 2.07~2.12(t, 2H, J=7.6Hz, -NCH 2 C H 2 -), 3.76~3.79(m, 1H, piperazine-1 H ), 6.54~6.57 (m, 1H, N H ), 2.83~2.95(m, 6H, N(C H 3 ) 2 ).

[0033] MS: m / z (M + ) 428 (M-C 4 h 6 o 6 +H).

Embodiment 2

[0034] Embodiment 2: the preparation of cariprazine hydrochloride

[0035] Dissolve 15g of cariprazine in 150ml of N-methylpyrrolidone, stir and heat to 30-35°C, drop in 12ml of isopropanol solution of 25-35% hydrogen chloride, keep stirring for 1h, then add 300ml of isopropanol, and stir for 10min , cooled to 0-5°C, let stand for 2h, filtered, washed the solid with an appropriate amount of isopropanol, and dried in vacuum at 65-70°C for 6h to obtain 12.3g of cariprazine hydrochloride.

Embodiment 3

[0036] Embodiment 3: physicochemical property comparison

[0037] According to the four routine tests of the Chinese Pharmacopoeia 2015 edition.

[0038] Conclusion: Cariprazine tartrate of the present invention has good solubility and fluidity, and is not hygroscopic.

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Abstract

The invention relates to cariprazine tartrate (I), a crystal form, a preparation method therefor and use of cariprazine tartrate for treating schizophrenia and dual-phase type I disorder drugs. The compound provided by the invention is excellent in water solubility, flowability of powder and stability, and is an excellent medicinal form of cariprazine. The formula is shown in the description.

Description

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Claims

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Application Information

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Owner ANHUI HEALSTAR PHARM CO LTD
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