Novel iloperidone pharmaceutical cocrystal and preparation method thereof

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

Inactive Publication Date: 2012-08-15
CHANGCHUN LICHENG BICHENG NEW MEDICINE TECHDEV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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

Method used

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  • Novel iloperidone pharmaceutical cocrystal and preparation method thereof
  • Novel iloperidone pharmaceutical cocrystal and preparation method thereof
  • Novel iloperidone pharmaceutical cocrystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Synthesis of co-crystals using iloperidone and 3,5-dihydroxybenzoic acid:

[0030] Weighing:

[0031] The reactant is fed according to iloperidone:3,5-dihydroxybenzoic acid=1:1 mass ratio. Accurately weigh 20.00 mg of iloperidone and 20 mg of 3,5-dihydroxybenzoic acid in a 25 ml single-necked round bottom flask with an analytical balance.

[0032] Dissolution of API:

[0033] Use a 5ml pipette to accurately measure 5ml of ethanol into 25ml single-necked round bottom flasks.

[0034] Reflux-volatilization heat method:

[0035] Put the stirring bar in the round-bottomed flask of iloperidone and 3,5-dihydroxybenzoic acid dissolved uniformly above, set up the reflux device, the reflux time is 2h, the reflux temperature is 90°C, turn on the magnetic stirrer and condense water.

[0036] After reflux, the reaction solution was filtered, and the filtrate was placed in a 25ml transparent glass vial and placed at room temperature. After 6 hours of slow volatilization of the...

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Abstract

The invention belongs to the technical field of pharmaceutical cocrystals and in particular relates to a novel iloperidone pharmaceutical cocrystal and a preparation method thereof. The pharmaceutical cocrystal is characterized in that iloperidone is taken as the active pharmaceutical ingredient, 3,5-dihydroxy-benzoic acid is taken as the former, and an iloperidone molecule, a 3,5-dihydroxy-benzoic acid molecule and a water molecule jointly form a basic structural unit of the iloperidone pharmaceutical cocrystal through hydrogen bonds and deposition. The pharmaceutical cocrystal is prepared by taking ethanol as the solvent and adopting the method of reflux-room temperature diffusion and volatilization. As the selected organic solvent has lower boiling point, crystals are prepared in the process of solvent volatilization after reflux and filtration. The prepared pharmaceutical cocrystal carries forward the characteristic of the traditional active pharmaceutical ingredients in treating schizophrenia and the dissolubility, stability and bioavailability of the pharmaceutical cocrystal are also obviously improved.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to a novel 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 science that stud...

Claims

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Application Information

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IPC IPC(8): C07D413/04
Inventor 张婷婷赵晓君罗亚楠刘磊韩冰朱广山
Owner CHANGCHUN LICHENG BICHENG NEW MEDICINE TECHDEV
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