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Iloperidone crystal and preparation method and medicinal composition thereof

A technology of iloperidone and its composition, applied in the field of iloperidone crystals, can solve problems such as inability to obtain stable and definite crystal forms, and no mention of iloperidone crystal forms

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

[0032] Example 1 : Preparation method of iloperidone crystal

[0033] The present embodiment is the preparation method of iloperidone crystal, specifically comprises the following steps:

[0034] First, according to the method described in EP402644A1, iloperidone is prepared, and its nuclear magnetic spectrum is as follows figure 1 shown.

[0035] Next, heat 1g of iloperidone in a vacuum drying oven at 125-130°C, while evacuating (30mmHg) until the solid is completely melted, then naturally cool to 80°C, crystallization is formed, and continue to naturally cool to room temperature (25°C). Grinding to prepare iloperidone crystals.

[0036] The prepared iloperidone crystals are characterized by the following powder X-ray diffraction patterns. The Japanese Rigaku D / Max-2500 X-ray diffractometer was used for the measurement, and the specific experimental parameters were set as follows: CuKα radiation, tube voltage: 40KV, tube current: 100mA, 2θ angle scanning range of 2 to 4...

Embodiment 2

[0038] Example 2 : Detection of physical properties of iloperidone crystals

[0039] In this example, the iloperidone prepared in Example 1 was used as a reference substance, and the physical properties of the iloperidone crystals prepared in Example 1 were tested, including solubility, hygroscopicity and stability.

[0040] 1. Solubility

[0041] According to the Chinese Pharmacopoeia 2005 edition, the dissolubility of the iloperidone crystals prepared in 0.1M hydrochloric acid is detected by the method XIII of the second part of the Chinese Pharmacopoeia, and compared with the iloperidone prepared in embodiment 1, the results are shown in Table 2 shown.

[0042] Table 2 Solubility comparison in 0.1M hydrochloric acid

[0043] sample name

[0044] From the results in Table 2, it can be seen that the solubility of iloperidone crystals in 0.1M hydrochloric acid is better than that of the reference substance.

[0045] 2. Hygroscopicity

[0046] According to " Chi...

Embodiment 3

[0057] Example 3 : Tablets of pharmaceutical composition comprising crystals of iloperidone

[0058] This embodiment is a pharmaceutical composition comprising iloperidone crystals prepared in embodiment 1.

[0059] 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):

[0060]

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PUM

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Abstract

The invention provides an iloperidone crystal, which has X-ray diffraction peaks at 17.16 degrees, 20.68 degrees, 14.30 degrees, 16.74 degrees, 19.92 degrees, 20.30 degrees, 21.54 degrees, 22.10 degrees, 7.10 degrees, 12.64 degrees, 17.50 degrees, 18.20 degrees, 24.62 degrees, 25.12 degrees, 26.34 degrees, 28.92 degrees, 29.94 degrees, 30.72 degrees and 31.76 degrees represented by a 2theta anglein an X-ray diffraction pattern. The invention also provides a method for preparing the iloperidone crystal. The iloperidone crystal has a stable structure, can be stored for a long time, does not have any special requirement on temperature and humidity, and can be used for preparing a medicinal composition for treating schizophrenia.

Description

technical field [0001] The invention belongs to the field of medicine. In particular, the present invention relates to crystal iloperidone, its preparation method and pharmaceutical composition containing it. 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 c...

Claims

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Application Information

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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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