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Two novel paliperidone drug eutectics and preparation method of the novel paliperidone drug eutectics

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

Inactive Publication Date: 2011-08-17
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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  • Two novel paliperidone drug eutectics and preparation method of the novel paliperidone drug eutectics
  • Two novel paliperidone drug eutectics and preparation method of the novel paliperidone drug eutectics
  • Two novel paliperidone drug eutectics and preparation method of the novel paliperidone drug eutectics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Synthesis of co-crystal CC-1 using paliperidone and p-hydroxybenzoic acid:

[0040] Weighing:

[0041] The reactant is fed according to the mass ratio of paliperidone:p-hydroxybenzoic acid=1:1. Accurately weigh 40.00 mg of paliperidone and 40.00 mg of p-hydroxybenzoic acid with an analytical balance into a transparent glass vial, and then put it into a magnetic stirring bar.

[0042] Dissolution of API:

[0043] Use a 5ml pipette to accurately measure 2ml of dichloromethane, 2ml of ethanol and 2ml of ether into a transparent glass vial container, put in a magnetic stirring bar, and spread a layer of tin foil on the top of the glass container. The above glass container was placed on a magnetic stirrer and stirred for 3 h.

[0044] Solvent room temperature evaporation heat method:

[0045] After the powder is completely dissolved in water, quickly take out the stirring bar, cover and seal the glass container, and its internal pressure is 101KPa. Afterwards, the solve...

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Abstract

The invention belongs to the technical field of drug eutectics, and particularly relates to two novel paliperidone drug eutectics and a preparation method of the novel paliperidone drug eutectics, wherein one paliperidone molecule and one p-hydroxybenzoic acid molecule are combined together by a hydrogen bond to form the basic structure unit of a paliperidone drug eutectic CC-1; and two paliperidone molecules are respectively combined with one p-hydroxybenzoic acid molecule by a hydrogen bond to form the basic structure unit of a paliperidone drug eutectic CC-2. The preparation method of the paliperidone drug eutectics CC-1 and CC-2 is a solvent room-temperature volatilization method. The prepared paliperidone drug eutectics in the invention inherits the characteristic of the traditional bulk drug in treating dementia praecox, in addition, the dissolubility, the stability and the bioavailability of the prepared paliperidone drug eutectics are improved obviously.

Description

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

Claims

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Application Information

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IPC IPC(8): C07D471/04C07C65/03C07C51/347
Inventor 张婷朱广山
Owner JILIN UNIV
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