Organic acid lithium amino acid salt, crystal form, composition and application

An amino acid salt crystal, organic acid lithium technology, applied in the field of medicine, can solve the problems of insufficient drug efficacy, large toxic and side effects, and achieve the effects of reducing clinical dosage, enhancing curative effect, and uniquely preventing suicide risk.

Active Publication Date: 2022-02-25
ANYUAN BIOTECHNOLOGY (HANGZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Technical problem to be solved: the purpose of the present invention is to provide a novel lithium amino acid salt of organic acid, which is used to solve the problems of insufficient drug efficacy and large toxic and side effects of existing lithium preparations

Method used

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  • Organic acid lithium amino acid salt, crystal form, composition and application
  • Organic acid lithium amino acid salt, crystal form, composition and application
  • Organic acid lithium amino acid salt, crystal form, composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1: single solvent crystallization method prepares lithium isobutyrate-L-proline salt

[0060] Add an appropriate amount of good solvent n-butanol to lithium isobutyrate (500mg) and L-proline (612mg) of equal chemical equivalents, make it just dissolve under heating and reflux and record the amount of solvent used (n-butanol added volume 55ml), stirred for about 3h, filtered while hot, cooled and crystallized naturally, filtered the solid, and vacuum-dried to constant weight to obtain 589.3mg of white solid (lithium isobutyrate-L-proline salt obtained by single-solvent crystallization method) , the mass yield is 53.06%. Carry out XRD and proton spectrum inspection (deuterium reagent: CD 3 OD).

[0061] Figure 1 to Figure 4 They are the hydrogen spectrum of a single compound of lithium isobutyrate, the hydrogen spectrum of a single compound of L-proline, the hydrogen spectrum of a chemically equivalent physical mixture such as lithium isobutyrate and L-prol...

Embodiment 2

[0072] Embodiment 2: mixed solvent crystallization method prepares lithium isobutyrate-L-proline salt

[0073] Add an appropriate amount of 50ml of good solvent (ethanol) to equivalent chemical equivalents of lithium isobutyrate (500mg) and L-proline (612mg), heat to reflux to make it just dissolve, and then add an appropriate amount of 30ml of poor solvent (tetrahydrofuran) to just The solid was precipitated, and a good solvent (7ml) was added to make it redissolved, refluxed for 3h, cooled and crystallized naturally, filtered the solid, and dried in vacuo to constant weight to obtain 374.8 mg of white solid (lithium isobutyrate prepared by mixed solvent crystallization method- L-proline salt), the mass yield is 33.75%. Carry out XRD and proton spectrum respectively (deuterium reagent: CD 3 OD) test.

[0074] Figure 9 It is the hydrogen spectrum of the solid precipitated from the mixed solvent of ethanol and tetrahydrofuran in Example 2.

[0075] comprehensive Figure 9...

Embodiment 3

[0078] Example 3: Characterization of Salt Structure

[0079] According to the results of XRD and hydrogen spectrum, the n-propanol and n-butanol systems were selected for single crystal cultivation, and the structure of the formed solid product was confirmed. The quality of crystals precipitated under the final n-butanol condition meets the test requirements, and its single crystal structure is as follows: Figure 11 Shown:

[0080] Use Mercury software to measure the C-O bond length of L-proline in the single crystal lattice, and its C-O bond length is respectively and The ratio is 1.028. The C-O bond length of L-proline is basically the same, which proves that the proton transfer of L-proline in the solid product leads to the same carboxylate C-O bond length, confirming that the prepared product is lithium isobutyrate-L-pro Amino acid salt.

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Abstract

The invention discloses an organic acid lithium amino acid salt. An organic acid lithium is one or more of lithium isobutyrate, lithium n-butyrate, lithium lactate, lithium citrate or lithium cholesterol; an amino acid is one of L-proline, valine, lysine or artificially synthesized amino acid; and the organic acid lithium amino acid salt is a salt formed by the organic acid lithium and the amino acid. The invention also discloses a crystal form, a preparation method and application of the salt. The organic acid lithium amino acid salt has a positive curative effect and a prevention effect on repeated attack of mania and depression in bipolar affective disorders, can delay degenerative diseases of a central nervous system to achieve better distribution of the central nervous system, and reduces the clinical dosage of the lithium salt while enhancing the curative effect of the central nervous system diseases, so as to avoid the occurrence of peripheral adverse reaction.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a novel organic acid lithium amino acid salt, a crystal form, a composition, a preparation process thereof and an application in the field of neuropsychiatric diseases. Background technique [0002] Lithium salt can be used in the field of mental illness, and has good curative effect and preventive effect on recurrent episodes of mania and depression in bipolar disorder, and has a unique effect of preventing suicide risk. Recent studies have also found that lithium salts can exert neuroprotective effects by acting on GSK-3, WNT, AKT and neurotransmitters. Lithium salts have selective activity on GSK-3β. There are two main modes of action for lithium salts to inhibit GSK-3β. : (1) as Mg 2+ Competitive inhibitors directly inhibit the activity of GSK-3β; (2) indirectly inhibit the activity of GSK-3β by increasing the expression of phosphorylated AKT, phosphorylated GSK-3β (ser9)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/401A61K31/19A61P25/00C07D207/16C07C53/124C07C51/41C07C51/43
CPCA61K31/401A61K31/19A61P25/00C07D207/16C07C53/124C07C51/412C07C51/43C07B2200/13A61K2300/00Y02E60/10C07C227/14C07C227/42C07F1/02C12P13/24
Inventor 谭骏陈斌辉李崧唐勤敏陈江
Owner ANYUAN BIOTECHNOLOGY (HANGZHOU) CO LTD
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