Piracetam pharmaceutical co-crystal taking 3,4-dihydroxy-benzoic acid as precursor and preparation method of piracetam pharmaceutical co-crystal

A technology of dihydroxybenzoic acid and piracetam, applied in organic chemistry and other fields, can solve the problem of ineffectiveness in patients with severe dementia, and achieve the effect of improving stability and bioavailability

Inactive Publication Date: 2013-05-01
吉林三善恩科技开发有限公司
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AI Technical Summary

Problems solved by technology

[0005] Piracetam is a drug for improving brain metabolism, which belongs to the cyclic derivative of γ-aminobutyric acid. It is used fo

Method used

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  • Piracetam pharmaceutical co-crystal taking 3,4-dihydroxy-benzoic acid as precursor and preparation method of piracetam pharmaceutical co-crystal
  • Piracetam pharmaceutical co-crystal taking 3,4-dihydroxy-benzoic acid as precursor and preparation method of piracetam pharmaceutical co-crystal
  • Piracetam pharmaceutical co-crystal taking 3,4-dihydroxy-benzoic acid as precursor and preparation method of piracetam pharmaceutical co-crystal

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Experimental program
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Embodiment 1

[0028] Synthesis of co-crystals using piracetam and 3,4-dihydroxybenzoic acid:

[0029] Weighing:

[0030] The reactants were fed with 20.00 mg of piracetam and 30.00 mg of 3,4-dihydroxybenzoic acid. Accurately weigh 20.00 mg of piracetam and 30.00 mg of 3,4-dihydroxybenzoic acid with an analytical balance, and add them into a transparent glass vial.

[0031] Dissolution of API:

[0032] Use a 5ml pipette to accurately measure 5ml of methanol into a 20ml transparent glass vial, and stir on a stirrer for 1h to dissolve all the solids, and the solution becomes a colorless clear liquid.

[0033] Solvent room temperature volatilization heat method:

[0034] 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 precipitated in the bottle, that is, piracetam co-crystal.

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Abstract

The invention belongs to the technical field of pharmaceutical co-crystals, and particularly relates to a piracetam pharmaceutical co-crystal taking 3,4-dihydroxy-benzoic acid as a precursor and a preparation method of the piracetam pharmaceutical co-crystal. A space group of the pharmaceutical co-crystal is a monoclinic system, and three 3,4-dihydroxy-benzoic acid molecules (1) and a piracetam molecule (2) are combined through hydrogen bonds to form a basic structural unit of the piracetam pharmaceutical co-crystal. In a pharmaceutical co-crystal preparation process, a selected solvent is methanol; an adopted method is a solvent room-temperature volatilization method; and as a boiling point of the selected organic solvent is lower, a crystal is precipitated in a solvent volatilization process. The prepared pharmaceutical co-crystal inherits the characteristic of the traditional bulk pharmaceutical for repairing nerve cells of a brain function injured patient, and the dissolvability, the stability and the bioavailability of the pharmaceutical co-crystal are improved obviously.

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 3,4-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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IPC IPC(8): C07D207/27C07C65/03
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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