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Iloperidone crystal, and preparation method and medicinal composition thereof

A technology of iloperidone and composition, applied in the direction of drug combination, pharmaceutical formula, medical preparations containing active ingredients, etc., can solve the problem of not mentioning iloperidone crystal form, unable to obtain stable and definite crystal form, etc. question

Active Publication Date: 2011-04-27
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Iloperidone, its preparation and therapeutic use are described in European Patent Application Publication EP402644A1, but no stable and defined crystal form can be obtained by the method described in this patent
The known literature does not mention the crystal form of iloperidone

Method used

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  • Iloperidone crystal, and preparation method and medicinal composition thereof
  • Iloperidone crystal, and preparation method and medicinal composition thereof
  • Iloperidone crystal, and preparation method and medicinal composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 : Preparation method of iloperidone crystal

[0038] The present embodiment is the preparation method of iloperidone crystal, specifically comprises the following steps:

[0039] With 5g iloperidone (prepared according to the method described in EP402644A1, its nuclear magnetic spectrum is as follows figure 1 Shown) mixed with 150ml of 50% (V / V) aqueous ethanol, heated to dissolve, after the solid was completely dissolved, naturally cooled to 50°C for 30 minutes, solids were precipitated, continued to cool naturally to room temperature 25°C, and then iced The water was cooled to 10°C, left standing for 4 hours, filtered, and vacuum-dried below 60°C to obtain 4 g of off-white solid, i.e. iloperidone crystals.

[0040] Using Japan Rigaku D / Max-2500 X-ray diffractometer (CuK α radiation) to characterize the above-prepared iloperidone crystals, the specific experimental parameters are set as follows: the 2θ angular scanning speed is 8°C / min, the scanning range...

Embodiment 2

[0043] Embodiment 2: Research on the physical properties of iloperidone crystals of the present invention

[0044] The physical properties of the iloperidone crystals of the present invention, such as solubility, hygroscopicity and stability, are studied below by comparing the iloperidone crystals of the present invention with iloperidone prepared according to the method described in EP402644A1.

[0045] 1. Solubility

[0046] According to the Chinese Pharmacopoeia 2005 edition two general example XIII method detection according to the dissolubility of iloperidone (control sample) prepared by the method described in EP402644A1 and iloperidone crystal of the present invention in 0.1M hydrochloric acid, the results are shown in Table 2 shown.

[0047] Table 2 Solubility comparison in 0.1M hydrochloric acid

[0048] sample name

0.1M hydrochloric acid

Solubility

Control sample (10mg dosage)

200ml

insoluble

Iloperidone crystal (10mg dosage)...

Embodiment 3

[0062] Example 3 : Pharmaceutical composition comprising iloperidone crystals

[0063] This embodiment is a pharmaceutical composition comprising iloperidone crystals prepared in embodiment 1.

[0064] The pharmaceutical composition is prepared into tablets, and the specific prescription is as follows (1000 tablets, each containing 1 mg, 4 mg or 6 mg of active ingredient iloperidone crystal):

[0065]

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PUM

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Abstract

The invention provides iloperidone crystal. X-diffracted ray diffraction peaks are formed at angles 2theta of 14.26+ / -0.2 and 21.50+ / -0.2 degrees in an X-ray diffraction pattern of the iloperidone crystal. The invention also provides a preparation method of the iloperidone crystal; and the method comprises the following steps of: 1) mixing the iloperidone and an organic solvent, heating and dissolving; 2) naturally cooling the solution to 45 to 55 DEG C, and separating the crystal out; and 3) continuing to naturally cool the obtained crystal to room temperature, cooling to 5 to 10 DEG C in anice water bath, filtering, and drying under vacuum at the temperature of less than 60 DEG C to obtain the iloperidone crystal. The iloperidone crystal has a stable structure, can be stored for a longtime, does not have special requirements on temperature, luminosity and humidity, and can be used for preparing a medicinal composition and medicaments for treating schizophrenia.

Description

technical field [0001] The invention belongs to the field of medicine, in particular, the invention relates to iloperidone crystal, its preparation method and its pharmaceutical composition. Background technique [0002] Iloperidone (iloperidone), as a serotonin and dopamine D2 receptor antagonist, has anti-schizophrenia activity, and its clinical phase III shows better tolerance and safety than existing antipsychotic drugs, and it is expected to Be a good anti-schizophrenia drug. [0003] The chemical name of iloperidone is 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]- 3-methoxyphenyl] ethyl ketone, its chemical structural formula is as follows: [0004] [0005] Iloperidone, its preparation and therapeutic use have been described in European Patent Application Publication EP402644A1, but a stable and defined crystal form cannot be obtained by the method described in this patent. The known literature also does not mention the crystal form of ilop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D413/04A61K31/454A61P25/18
Inventor 陈蔚潘毅臧可昕陶勇苏慕君梁劲松
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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