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A kind of novel iloperidone medicine co-crystal and preparation method thereof

A technology of iloperidone and piperidine in perperidone is applied in the field of novel iloperidone drug co-crystal and its preparation, and achieves the effects of improved stability and improved bioavailability

Active Publication Date: 2011-12-14
JILIN UNIV
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  • Summary
  • 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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  • A kind of novel iloperidone medicine co-crystal and preparation method thereof
  • A kind of novel iloperidone medicine co-crystal and preparation method thereof
  • A kind of novel iloperidone medicine co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0030] Weighing:

[0031] The reactants are fed according to the mass ratio of iloperidone:3,5-pyridinedicarboxylic acid=1:1. Accurately weigh 40.00 mg of iloperidone and 40.00 mg of 3,5-pyridinedicarboxylic acid with an analytical balance.

[0032] Dissolution of API:

[0033] Use a 5ml pipette to accurately measure 4ml of ethanol into a 25ml single-necked round bottom flask.

[0034] Reflux-solvent room temperature volatilization heat method:

[0035]Put a magnetic stirring bar in the round bottom flask, set up the reflux device. Set the reflux temperature to 90°C, turn on stirring and condensing water, reflux for 3 hours, filter, and place the filtrate in a 25ml beaker at room temperature. Afterwards, the solvent was slowly volatilized at room temperature, and after 30 hours, transparent strip-shaped crystals were formed. After the solvent volatilized, the weight of the obtained ilop...

Embodiment 2

[0037] Synthesis of co-crystals using iloperidone and 3,5-pyridinedicarboxylic acid:

[0038] Weighing:

[0039] The reactant is fed according to the mass ratio of iloperidone:3,5-pyridinedicarboxylic acid=3:1. Accurately weigh 30.00 mg of iloperidone and 10.00 mg of 3,5-pyridinedicarboxylic acid with an analytical balance.

[0040] Dissolution of API:

[0041] Use a 5ml pipette to accurately measure 4ml of ethanol into a 25ml single-necked round bottom flask.

[0042] Reflux-solvent room temperature volatilization heat method:

[0043] Put a magnetic stirring bar in the round bottom flask, set up the reflux device. Set the reflux temperature to 90°C, turn on stirring and condensing water, reflux for 3 hours, filter, and place the filtrate in a 25ml beaker at room temperature. Afterwards, the solvent was slowly volatilized at room temperature. After 30 hours, transparent strip-shaped and thin-sheet two-phase crystals were formed. After the solvent volatilized, the weight ...

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Abstract

The invention belongs to the technical field of medicinal cocrystal, and particularly relates to a novel iloperidone medicinal cocrystal and a preparation method thereof. An N atom in a piperidine ring of iloperidone is used as a hydrogen bond donor, and an H atom on a carboxyl group in 3,5-pyridine dicarboxylic acid is used as a hydrogen bond receptor to form a hydrogen bond; an iloperidone molecule is combined with a 3,5-pyridine dicarboxylic acid molecule through the hydrogen bond to form a basic structural unit of the iloperidone medicinal cocrystal; and a space group of the medicinal cocrystal is a triclinic system. The preparation method of the iloperidone medicinal cocrystal is a reflux-room temperature volatilization method. The medicinal cocrystal prepared by using the preparation method disclosed by the invention has the characteristics of inheriting the conventional raw material medicament on treatment of schizophrenia; and the dissolubility, the stability and the bioavailability of the medicinal cocrystal are 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 "supramolecule" 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): C07D413/04C07D213/80A61P25/18
Inventor 张婷朱广山邢娇娇韩冰苏红敏
Owner JILIN UNIV
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