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Novel paliperidone medicinal eutectic and preparation method thereof

A paliperidone and drug technology, applied in the field of novel paliperidone drug co-crystal and preparation thereof, to achieve the effect of improving stability and bioavailability

Inactive Publication Date: 2012-07-18
吉林三善恩科技开发有限公司
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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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  • Novel paliperidone medicinal eutectic and preparation method thereof
  • Novel paliperidone medicinal eutectic and preparation method thereof
  • Novel paliperidone medicinal eutectic and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Synthesis of co-crystals using paliperidone and p-aminobenzoic acid:

[0025] Weighing:

[0026] The reactant is fed according to the mass ratio of paliperidone:p-aminobenzoic acid=1:1. Accurately weigh 40.00 mg of paliperidone and 40.00 mg of p-aminobenzoic acid with an analytical balance in a transparent glass bottle.

[0027] Dissolution of API:

[0028] Accurately measure 2ml of dichloromethane, 2ml of ethanol and 2ml of ether into the transparent glass bottle container with a 5ml pipette, put a magnetic stirring bar, and spread a layer of tinfoil on the glass bottle mouth. The above glass container was placed on a magnetic stirrer and stirred for 3 h.

[0029] Solvent room temperature volatilization heat method:

[0030] After the powder is completely dissolved, quickly take out the stirring bar, cover the glass container with tinfoil, and then slowly volatilize the solvent at room temperature. After 160 hours, transparent long rod-shaped crystals are formed, w...

Embodiment 2

[0032] Weighing:

[0033] The reactant is fed according to the mass ratio of paliperidone:p-aminobenzoic acid=1:1. Accurately weigh 40.00 mg of paliperidone and 40.00 mg of p-aminobenzoic acid with an analytical balance in a transparent glass bottle.

[0034] Use a 5ml pipette to accurately measure 2ml of dichloromethane and 2ml of ethanol into the transparent glass bottle container, put a magnetic stirring bar, and spread a layer of tin foil on the glass bottle mouth. The above-mentioned glass bottle was placed on a magnetic stirrer and stirred for 3 h.

[0035] Gas phase diffusion method:

[0036] After the powder is completely dissolved, take out the stirring bar quickly, cover the glass bottle with tinfoil paper and put it into a beaker containing a certain amount of ether, seal the beaker with plastic wrap and sealing film, and then pass the low boiling point ether solvent in the beaker slowly Diffusion into the glass bottle, after 60 hours, transparent long rod-shaped c...

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Abstract

The invention belongs to the technical field of medicinal eutectics, and particularly relates to a novel paliperidone medicinal eutectic and a preparation method thereof. According to the paliperidone medicinal eutectic, two paliperidone molecules and a para aminobenzoic acid molecule are bonded by two hydrogen bonds to form a basic structural unit of the paliperidone medicinal eutectic, an N atom on a piperidine ring in one paliperidone molecule, which serves as a hydrogen bond donor, and an H atom on carboxyl in the para aminobenzoic acid, which serves as a hydrogen bond receptor form a first hydrogen bond; and a hydrogen atom on amino of the para aminobenzoic acid, which serves as a hydrogen bond donor, and an oxygen atom on pyrimidine-4-keto-carbonyl of the other paliperidone molecule, which serves as a hydrogen bond receptor form a second hydrogen bond. According to the medicinal eutectic, the characteristic of the conventional Chinese herbal medicines in the treatment of dementia praecox is inherited, and the dissolubility, stability and bioavailability of the medicinal eutectic are improved obviously.

Description

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

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04
Inventor 韩冰张婷刘磊赵晓君罗亚楠
Owner 吉林三善恩科技开发有限公司
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