Piracetam pharmaceutical co-crystal using 2,4-dihydroxy-benzoic acid as precursor and preparation method of co-crystal

A technology of dihydroxybenzoic acid and piracetam, applied in the field of drug co-crystals, can solve problems such as ineffectiveness in patients with severe dementia, and achieve the effect of improving stability and bioavailability

Inactive Publication Date: 2013-04-17
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

[0005] Piracetam is a drug for improving brain metabolism, which belongs to the cyclic derivative of Y-aminobutyric acid. It is used for the treatment of cerebrovascular disease and peripheral vascular disease. Cognitive abilities, but not in people with severe dementia

Method used

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  • Piracetam pharmaceutical co-crystal using 2,4-dihydroxy-benzoic acid as precursor and preparation method of co-crystal
  • Piracetam pharmaceutical co-crystal using 2,4-dihydroxy-benzoic acid as precursor and preparation method of co-crystal
  • Piracetam pharmaceutical co-crystal using 2,4-dihydroxy-benzoic acid as precursor and preparation method of co-crystal

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Synthesis of co-crystals using piracetam and 2,4-dihydroxybenzoic acid:

[0028] Weighing:

[0029] The reactants were fed with 20.00 mg of piracetam and 22.00 mg of 2,4-dihydroxybenzoic acid. Accurately weigh 20.00 mg of piracetam and 22.00 mg of 2,4-dihydroxybenzoic acid with an analytical balance, and then put them into a glass vial;

[0030] Dissolution of API:

[0031] Use a 5ml pipette to accurately measure 5ml of methanol into a 20ml transparent glass vial container, stir on a stirrer for 1 hour to dissolve all the solids, fully react Piracetam with 2,4-dihydroxybenzoic acid, and the solution becomes It is a colorless clear liquid.

[0032] Solvent room temperature volatilization heat method:

[0033] After the solid is completely dissolved, take out the stirring bar, seal the mouth of the bottle with tinfoil, prick a few small holes with a needle, and let it stand for volatilization. After about 6 days, a colorless and transparent block crystal was precipit...

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Abstract

The invention belongs to the technical field of pharmaceutical co-crystals and in particular relates to a piracetam pharmaceutical co-crystal and a preparation method thereof. The space group of the prepared piracetam pharmaceutical co-crystal is a monoclinic system; one piracetam moleculre (1) and one 2,4-dihydroxy-benzoic acid molecule (2) are combined together by a hydrogen bond to form a basic structure unit of the piracetam pharmaceutical co-crystal, wherein the O atom on the hydroxyl group of the 2,4-dihydroxy-benzoic acid molecule is uses as a hydrogen bond donator, and the O atom on the hydroxyl group of the piracetam molecule is used a hydrogen bond acceptor. The solvent selected in the preparation process of the pharmaceutical co-crystal is methanol; and the adopted method is a solvent room-temperature evaporation method. The boiling point of the selected organic solvent is relatively low, and so crystals are separated out in the evaporation process of the solvent. According to the pharmaceutical co-crystal prepared by the preparation method disclosed by the invention, the characteristics of the traditional material medicines for restoring nerve cells are inherited for treating a patient with brain damages; and the solubility, stability and bioavailability of the pharmaceutical co-crystal are remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to a piracetam drug co-crystal with 2,4-dihydroxybenzoic acid as a precursor 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. Supramole...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/27C07C65/03C07C51/43
Inventor 罗亚楠张婷苏红敏
Owner 吉林三善恩科技开发有限公司
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