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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 improved stability and improved bioavailability

Inactive Publication Date: 2012-08-15
吉林三善恩科技开发有限公司
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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 European and American pharmaceutical industry, but they are still in their infancy in the domestic pharmaceutical industry

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

[0030] Synthesis of co-crystals using iloperidone and 3-hydroxybenzoic acid:

[0031] Weighing:

[0032] The reactant is fed according to iloperidone: 3-hydroxybenzoic acid=1:1 mass ratio. Accurately weigh 20.00 mg each of iloperidone and 3-hydroxybenzoic acid with an analytical balance.

[0033] Dissolution of API:

[0034] Use a 5ml pipette to accurately measure 5ml of ethanol into a 25ml single-necked round bottom flask.

[0035] Reflux-room temperature volatilization heat method:

[0036] Put a magnetic stirrer in the above-mentioned round-bottomed flask of uniformly dissolved medicine, set up a reflux device, set the reflux time to 2 hours, and turn on the magnetic stirrer and condensate at a temperature of 90°C.

[0037] After reflux, the reaction solution was filtered, and the filtrate was placed in a 25ml transparent glass vial and placed at room temperature. After the solvent was slowly volatilized for 3 hours, transparent massive crystals were formed, and the weig...

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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-hydroxybenzoic acid is taken as the former, and an iloperidone molecule, a 3-hydroxybenzoic 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 吉林三善恩科技开发有限公司
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