盐酸小檗碱结晶水及其稳定性研究

Study on Berberine Hydrochloride Water of Crystallization and Its Stability

目的研究盐酸小檗碱原料药中的结晶水类型及含水量,以及盐酸小檗碱片制剂工艺对原料药结晶水的影响,为完善盐酸小檗碱片制剂质量控制提供依据。方法采用热重分析法(TGA)、差示扫描量热法(DSC)、X-射线粉末衍射法(XRPD)对盐酸小檗碱原料药中的结晶水进行研究,并考察盐酸小檗碱片生产过程及稳定性考察期间结晶水的变化情况。结果盐酸小檗碱以二水物为主,并含有少量的四水物和游离水;盐酸小檗碱片生产过程及稳定性考察期间原料药结晶水基本无明显变化。结论明确了盐酸小檗碱原料药中的结晶水,并做好盐酸小檗碱片生产过程质量控制,有助于确保其制剂质量均一、稳定、可控。

Objective To study the type and water content of water of crystallization in berberine hydrochloride bulk drug and the influence of berberine hydrochloride tablet preparation technology on the water of crystallization of active pharmaceutical ingredient,and to provide basis for improving the quality control of berberine hydrochloride tablets.Methods Thermogravimetric analysis(TGA),differential scanning calorimetry(DSC)and X-ray powder diffraction(XRPD)were used to study the water of crystallization in berberine hydrochloride,the production process of berberine hydrochloride tablets and the change of water of crystallization during the stability investigation were also investigated.Results Berberine hydrochloride is mainly dihydrate and contains a small amount of tetrahydrate and free water,during the production process and stability investigation of berberine hydrochloride tablets,there was basically unchanged in water of crystallization of active pharmaceutical ingredient.Conclusion Defined the water of crystallization in berberine hydrochloride active pharmaceutical ingredient and controlling the quality of berberine hydrochloride tablets in the production process are helpful to ensure the uniform,stable and controllable quality of its preparation.