Novel lamotrigine pharmaceutical co-crystal and preparation method thereof

Abstract

The invention relates to a novel lamotrigine pharmaceutical co-crystal and a preparation method thereof. A PXRD (Powder X Ray Diffractio) of the lamotrigine pharmaceutical co-crystal shows a series of characteristic peaks in 8.3+ / -0.2, 9.7+ / -0.2, 12.4+ / -0.2, 13.5+ / -0.2, 14.0+ / -0.2, 14.5+ / -0.2, 17.0+ / -0.2, 17.5+ / -0.2, 18.2+ / -0.2, 20.0+ / -0.2, 23.0+ / -0.2, 24.6+ / -0.2, 25.0+ / -0.2, 25.6+ / -0.2, 27.0+ / -0.2, and 28.5+ / -0.2. The lamotrigine pharmaceutical co-crystal is prepared through a solution mediate transformation or a grinding method. The prepared pharmaceutical co-crystal remains the characteristic of the traditional raw medicine on treating refractory epilepsy and also shows remarkable improvement on solubility, stability and bioavailability.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystals, and in particular relates to a drug co-crystal of lamotrigine and a preparation method thereof. Background technique [0002] For pharmaceutical active ingredients, its crystalline form can affect many of its physical properties, such as melting point, solubility, stability, bioavailability, etc. The latest research has found that drug co-crystals can use hydrogen bonds or other non-covalent bonds to generate supramolecular compounds through intermolecular recognition, thereby effectively improving the crystallization properties, physicochemical properties and efficacy of the drug itself, and becoming a solid drug formulation. new selection. Since the formation of pharmaceutical co-crystals will not destroy the covalent bonds of active pharmaceutical ingredients, it can provide a better means of changing the physical and chemical properties of active pharmaceutical ingredients. Therefo...

AI Technical Summary

Problems solved by technology

For solvates, the reported solvates of lamotrigine include 1:2 lamotrigine methanol solvate and 1:1:1 lamotrigine ethanol monohydrate, and there are few types of pharmaceutically acceptable solvents at present. , so sometimes the solvate is not the ideal dosage form

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