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A kind of lamotrigine drug co-crystal and its preparation method and application

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

Active Publication Date: 2021-04-09
GUANGXI UNIV FOR NATITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, no polymorphic forms of lamotrigine have been reported, but there are related reports on lamotrigine salts, lamotrigine solvates, and lamotrigine cocrystals:

Method used

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  • A kind of lamotrigine drug co-crystal and its preparation method and application
  • A kind of lamotrigine drug co-crystal and its preparation method and application
  • A kind of lamotrigine drug co-crystal and its preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Lamotrigine and succinimide are synthesized into co-crystals by room temperature solution evaporation, and the steps are as follows:

[0038] (1) Weigh 0.0019g lamotrigine and put it into a beaker, take 10mL ethyl propionate in the beaker with a pipette gun, and dissolve the lamotrigine;

[0039] (2) The mass ratio of lamotrigine and succinimide is 1:1.89, weigh 0.0036g of succinimide, and add it to the above-mentioned beaker to dissolve;

[0040] (3) Seal the solution with a plastic wrap, poke a few holes in the plastic wrap with an acupuncture needle, and volatilize the solution at room temperature, and the obtained crystal is the drug eutectic of lamotrigine.

Embodiment 2

[0042] Lamotrigine and succinimide are synthesized into co-crystals by room temperature solution evaporation, and the steps are as follows:

[0043] (1) Weigh 0.0019g lamotrigine and put it into a beaker, take 10mL isobutanol in the beaker with a pipette gun, and dissolve the lamotrigine;

[0044] (2) The mass ratio of lamotrigine and succinimide is 1:1.89, weigh 0.0036g of succinimide, and add it to the above-mentioned beaker to dissolve;

[0045] (3) Seal the solution with a plastic wrap, poke a few holes in the plastic wrap with an acupuncture needle, and volatilize the solution at room temperature, and the obtained crystal is the drug eutectic of lamotrigine.

Embodiment 3

[0047] The co-crystals of lamotrigine and succinimide were synthesized by wet grinding as follows:

[0048] (1) Lamotrigine and succinimide are fed at a material ratio of 1:3. Weigh 0.1036g of lamotrigine and 0.1223g of succinimide and place them in a ball mill jar, and then add 200 micrograms of liter isobutanol;

[0049] (2) Add grinding balls, put the ball mill jar into a ball mill, and grind for 30 minutes to obtain the lamotrigine drug eutectic.

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Abstract

The invention discloses a lamotrigine drug co-crystal and its preparation method and application. The lamotrigine drug co-crystal is a lamotrigine and succinimide co-crystal, and the 2θ of its XRPD spectrum is at 10.44° There are characteristic peaks at ±0.2°, 12.96°±0.2°, 14.44°±0.2°, 16.44°±0.2°, 18.28°±0.2°, 21.88°±0.2° and 22.30°±0.2°. The solubility, stability and bioavailability of the lamotrigine drug co-crystal of the invention are all improved.

Description

technical field [0001] The invention relates to a lamotrigine drug co-crystal, in particular to a lamotrigine drug co-crystal and a preparation method and application thereof. Background technique [0002] Pharmaceutical co-crystal refers to the combination of active pharmaceutical ingredient (API, Active pharmaceutical ingredient) and other physiologically acceptable acids, bases, salts, and non-ionic compounds in the same crystal lattice through non-covalent bonds such as hydrogen bonds. At least one of the pharmaceutical co-crystal components is a molecular or ionic API, and any component is solid at room temperature. Drug co-crystals can improve drug stability, solubility, dissolution and other related properties. Since the formation of drug co-crystals will not destroy the covalent bonds of drug active ingredients, it can provide a better means of changing the physical and chemical properties of drug active ingredients, so drug co-crystal research has become an importa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D253/075C07D207/404A61K31/53A61P25/08
CPCA61P25/08C07D207/404C07D253/075
Inventor 张金彦匡雯婕吉绍长曹小雪许海棠蓝平廖安平王小芳
Owner GUANGXI UNIV FOR NATITIES
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