盐酸溴己新的晶型表征及其在颗粒和分散片中的晶型稳定性

Crystal Form of Bromhexine Hydrochloride and Its Crystal Stability in Granules and Dispersible Tablets

盐酸溴己新(1)是一种常用祛痰药,存在多晶型现象,晶型转变可能影响其药效。该研究采用红外光谱(IR)法、粉末X射线衍射(PXRD)分析和差示扫描量热(DSC)法对1颗粒和1分散片进行晶型表征,探究了其在制备和贮存过程中1的晶型稳定性。通过IR法和PXRD法可鉴别出1的3种不同晶型;而DSC法对不同晶型的特征区分不明显,不可用于1晶型表征。IR法和PXRD法分析结果显示,在颗粒、分散片的制备过程中,以及在高温、光照、高湿条件下贮存,晶型A均未发生晶型转变,稳定性良好。该研究为产品质量控制水平的提高和生产过程的监测提供了试验数据。

Bromhexine hydrochloride(1)is a commonly used expectorant,showing a polycrystalline phenomenon.Crystal transformation might affect its efficacy.Infrared spectroscopy(IR),powder X-ray diffraction(PXRD),and differential scanning calorimetry(DSC)analyses were adopted to characterize crystal patterns of 1 in its granules and dispersible tablets,and the crystal stability of 1 during the preparation and storage processes was studied.Through IR and PXRD analyses,three different crystal forms of 1 could be identified,while the characterization results of three different crystal forms by DSC were not remarkable.The results indicated that crystal form A of 1 showed good crystal stability and did not undergo crystal transformation during the preparation processes of granules and dispersible tablets or storage under high temperature,light,and high humidity conditions.This paper provided data for improving quality control levels and monitoring the production process.