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Salt of gabapentin and 2, 6-pyridine dicarboxylic acid as well as preparation method and application thereof

A technology of dipicolinic acid and gabapentin is applied in the fields of medical application and crystallization technology, which can solve problems such as chemical instability, and achieve the effects of high purity, simple and feasible preparation method and good reproducibility.

Active Publication Date: 2021-02-05
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, the main problems faced by gabapentin raw materials in the process of preparation production and storage are chemical instability induced by thermochemistry and mechanical force, and itself has good water solubility and bioavailability, so chemical stability is the limit gabapentin Main cause of druggability

Method used

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  • Salt of gabapentin and 2, 6-pyridine dicarboxylic acid as well as preparation method and application thereof
  • Salt of gabapentin and 2, 6-pyridine dicarboxylic acid as well as preparation method and application thereof
  • Salt of gabapentin and 2, 6-pyridine dicarboxylic acid as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Under room temperature conditions, gabapentin (34.2g) and 2,6-pyridinedicarboxylic acid (33.4g) bulk drug are completely dissolved in 500ml ethanol solution, the solution is filtered and slowly volatilized to remove the solvent at room temperature to obtain gabapentin and 2 , the salt of 6-pyridinedicarboxylic acid (65.8 g).

[0060] The prepared salt was subjected to solid-state characterization, Figure 1-Figure 4 Respectively show embodiment 1 gabapentin and 2, the X-ray single crystal diffraction pattern (SCXRD), X-ray powder diffraction pattern (XRPD), differential scanning calorimetry (DSC), thermal TGA.

Embodiment 2

[0062] Under room temperature conditions, gabapentin (34.2g) and 2,6-pyridinedicarboxylic acid (33.4g) were added into ethanol solvent according to the molar ratio of 1:1, until it was stirred into a suspended state at room temperature, reaction 3 day, filtered, and dried at room temperature to obtain a salt of gabapentin and 2,6-pyridinedicarboxylic acid (68.0 g).

Embodiment 3

[0064] At room temperature, gabapentin (34.2g) and 2,6-pyridinedicarboxylic acid (33.4g) were added into methanol solvent at a molar ratio of 1:1 until they were stirred into a suspension at room temperature. Reaction 3 day, filtered, and dried at room temperature to obtain a salt of gabapentin and 2,6-pyridinedicarboxylic acid (65.8 g).

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Abstract

The invention relates to a salt of gabapentin and 2, 6-pyridine dicarboxylic acid as well as a preparation method and application thereof. The salt of gabapentin and 2, 6-pyridine dicarboxylic acid has the advantages of being high in purity, small in hygroscopicity, simple in preparation method and good in reproducibility, the chemical stability is remarkably improved, the production process of amedicine is optimized, and the druggability of the medicine is improved.

Description

technical field [0001] The invention belongs to the technical field of medical application and crystallization technology, and specifically relates to a salt of gabapentin and 2,6-pyridinedicarboxylic acid, a preparation method and application. Background technique [0002] The basic requirements of pharmaceutical preparations are safe, effective and stable. If the drug is degraded during the production or storage process, it will not only affect the efficacy of the drug, but also may produce dangerous toxic degradation products, which pose a huge threat to human physical and mental health and life safety. At the same time, the degradation of drugs can also lead to the failure of the development of new compounds or the risk of withdrawal of marketed drugs. Therefore, how to control and reduce the chemical degradation of drugs plays an important role not only in the development of drug candidates, but also in maintaining the quality, safety and efficacy of approved drug prod...

Claims

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Application Information

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IPC IPC(8): C07C229/28C07C227/18C07D213/79C07D213/803A61K31/195A61P25/08A61P25/04A61P25/02
CPCC07C229/28C07C227/18C07D213/79C07D213/803A61P25/08A61P25/04A61P25/02C07B2200/13C07C2601/14
Inventor 蔡挺郭敏珊孙晓杰
Owner CHINA PHARM UNIV
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