Novel lloperidone pharmaceutical co-crystal 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: 2012-09-12
吉林三善恩科技开发有限公司
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  • Abstract
  • Description
  • 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 the

Method used

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  • Novel lloperidone pharmaceutical co-crystal and preparation method thereof
  • Novel lloperidone pharmaceutical co-crystal and preparation method thereof
  • Novel lloperidone pharmaceutical co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0028] Example 1:

[0029] Synthesize a co-crystal using imperidone and 2,3-dihydroxybenzoic acid:

[0030] Weighing:

[0031] The reactants are fed in a mass ratio of iloperidone: 2,3-dihydroxybenzoic acid = 1:1. Use an analytical balance to accurately weigh out 20.00 mg of iloperidone and 20.00 mg of 2,3-dihydroxybenzoic acid.

[0032] Dissolution of API:

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

[0034] Reflux-steam heating method:

[0035] Put the magnetic stirrer into the round-bottomed flask with the uniformly dissolved medicine after weighing, set up the reflux device, reflux time is 2h, reflux temperature 90℃, turn on the magnetic stirrer and condensed water.

[0036] After refluxing, the reaction solution was filtered, and the filtrate was placed in a 25ml transparent glass vial. After the solvent was slowly volatilized for 6 hours, transparent massive crystals were formed. The weight of the obtained eutectic was 0.0...

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Abstract

The invention belongs to the technical field of pharmaceutical co-crystals, in particular to a novel lloperidone pharmaceutical co-crystal and a preparation method thereof. The pharmaceutical co-crystal takes lloperidone as an active pharmaceutical ingredient and takes 2, 3-dihydroxy-benzoic acid as a precursor; one lloperidone molecule, one 2, 3-dihydroxy-benzoic acid molecule and one water molecule commonly form a basic structural unit of the lloperidone pharmaceutical co-crystal under the hydrogen bond and accumulation actions. A solvent selected by the pharmaceutical co-crystal is ethanol and is prepared by adopting a backflow-diffused evaporation method; and as the selected organic solvent is lower in boiling point, the crystal is crystallized out in the solvent evaporation process after backflow filtering. The pharmaceutical co-crystal prepared by the invention not only inherits the characteristic of traditional raw medicine in treating schizophrenia, but also is remarkably improved on dissolubility, stability and bioavailability of the pharmaceutical co-crystal.

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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