一种卡马西平共晶的合成及表征

Synthesis and Characterization of a New Pharmaceutical Cocrystal of Carbamazepine

以卡马西平（CBZ）为药物活性成分,以没食子酸甲酯（MTG）为共晶形成物,在室温下制得一种卡马西平药物共晶CBZ-MTG。通过XRD测得了其晶体结构,并采用FTIR、X射线粉末衍射仪、热重分析仪和差示扫描量热仪对共晶进行了表征。此外,利用HPLC法测试了其溶解性及稳定性。结果表明,共晶CBZ-MTG的熔点为116.4℃,较单一组分CBZ和MTG有了大幅下降;CBZ-MTG在溶解性上也有明显的改观,其在室温下于水和乙醇中的溶解度达到了1.482 6 mmol/L和0.501 2 mol/L,较单一的卡马西平药物分别提高了2.3倍和3.9倍。

A new pharmaceutical cocrystal of carbamazepine（CBZ）,CBZ-MTG,was synthesized using methyl gallate（MTG） as a cocrystal coformer at room temperature.Its structure was identified by means of X-ray single crystal diffraction.The CBZ-MTG cocrystal was characterized by Fourier transform infrared spectroscopy（FTIR）,X-ray powder diffraction（XRD）,thermogravimetric analysis（TGA） and differential scanning calorimetry（DSC）.In addition,the solubility and stability were measured by HPLC.The results showed that the melting point of CBZ-MTG cocrystal was 116.4 ℃,which was significantly lower than that of single component.The solubility of CBZ-MTG crystal in water was 1.482 6 mmol/L,and that in ethanol was 0.501 2 mol/L,which was 2.3 times and 3.9 times higher than that of single carbamazepine,respectively.