Iloperidone drug cocrystal and preparation method thereof

A technology of iloperidone and drugs, applied in the field of iloperidone drug co-crystal and its preparation, to achieve the effect of improving bioavailability and stability

Inactive Publication Date: 2013-04-17
苏州纳埃净化科技有限公司
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

Drug crystal form research and solid-state characterization of drugs are relatively mature and highly valued fields in ...

Method used

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  • Iloperidone drug cocrystal and preparation method thereof
  • Iloperidone drug cocrystal and preparation method thereof
  • Iloperidone drug cocrystal and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0028] Synthesis of co-crystals using iloperidone and 4-aminobenzoic acid as starting materials:

[0029] Accurately weigh 40.00 mg of iloperidone and 40.00 mg of 4-aminobenzoic acid with an analytical balance, accurately measure 1 ml of dichloromethane and 3 ml of acetone with a 5 ml pipette, and place them together in a 20 ml transparent glass vial.

[0030] Volatile at room temperature:

[0031] Cover the transparent glass vial and put it on the stirrer and stir for 30 minutes, so that the solid in the transparent glass vial is completely dissolved, take out the stirring bar, seal the bottle mouth with tinfoil, and place it in a quiet place at room temperature. Continue to volatilize slowly, and after 5 days, colorless massive crystals are precipitated at the bottom of the transparent vial, which is iloperidone-4-aminobenzoic acid co-crystal.

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Abstract

The invention belongs to the technical field of new crystal forms of organic drugs, and particularly relates to an iloperidone drug cocrystal and a preparation method of the iloperidone drug cocrystal. The method comprises the steps that iloperidone is taken as an active drug ingredient; 4-aminobenzoic acid is taken as a precursor; a three-dimensional net structure is formed by iloperidone and 4-aminobenzoic acid through hydrogen bonds and by the action of pi-pi accumulation; on a YZ plane, 4-aminobenzoic acid molecules stretch in a wave manner in a Y direction on the YZ plane through N-H...O hydrogen bonds; iloperidone molecules conduct the pi-pi accumulation on the YZ plane in an end-to-end accumulation manner and stretch in the Y direction; in an X direction, the iloperidone molecules and 4-aminobenzoic acid molecules form the hydrogen bonds through O-H...N, and the iloperidone molecules conduct the pi-pi accumulation in the X direction in an end-to-end accumulation manner. A crystal space group is a monoclinic system. The drug cocrystal carries on the characteristics of a traditional raw material drug in treating schizophrenia, and has obvious improvement in solubility, stability and bioavailability.

Description

technical field [0001] The invention belongs to the technical field of new crystal forms of organic drugs, and in particular relates to an iloperidone drug co-crystal and a preparation method thereof. Background technique [0002] In 1894, E. Fischer of Germany proposed the "lock-key" model based on the idea of ​​"selective interaction between molecules", which was the prototype of modern supramolecular science theory. In 1937, German K.L.Wolf et al. created the term "supramolecular" to describe highly ordered entities formed by the association of molecules. In a general sense, any collection of molecules has interactions, so people often refer to them as The structural level of matter aggregation state is called "supramolecular". It was not until 1978 that Professor J.M.Lehn of France finally proposed the complete concept of "supramolecular chemistry" based on the traditional research on the host-guest system rooted in organic chemistry. Supramolecular chemistry is a scie...

Claims

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Application Information

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IPC IPC(8): C07D413/04
Inventor 张婷贾江涛赵晓君韩冰苏红敏
Owner 苏州纳埃净化科技有限公司
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