基于电子舌技术的盐酸左西替利嗪掩味研究

Research on taste masking of levocetirizine dihydrochloride based on electronic tongue technology

目的研究不同种类及用量的矫味剂对盐酸左西替利嗪口味的改善情况,以达到掩盖其苦味的目的。方法以盐酸小檗碱作为参比制剂,通过人工口尝的方式确定盐酸左西替利嗪待测中间体溶液浓度;通过对电子舌测定信号值进行主成分分析及计算标准化欧式距离确定甜味剂种类及环糊精的种类及用量;采用傅里叶红外光谱法、差示扫描量热法(DSC)、扫描电子显微镜(SEM)技术对冻干干燥后的环糊精包合物粉末进行表征;对添加三氯蔗糖、β-环糊精掩味之后的盐酸左西替利嗪溶液进行口尝,对掩味效果进行验证。结果盐酸左西替利嗪待测中间体溶液质量浓度为1.25 mg·mL-1;三氯蔗糖掩味效果较好且更为安全,中间体溶液中的添加量为0.3%;8倍量的β-环糊精可以掩盖药物的苦味;表征结果显示,盐酸左西替利嗪β-环糊精包合物制备成功;志愿者口尝结果表明,添加了三氯蔗糖、β-环糊精掩味之后的盐酸左西替利嗪溶液苦味已完全被掩盖。结论利用电子舌技术可以对盐酸左西替利嗪进行掩味研究,且操作简单、耗时短,客观性较强,结果可行性好。

Objective The improvement of the taste of levocetirizine dihydrochloride by different types and dosages of taste masking agents was studied in order to mask the bitter taste of levocetirizine dihydrochloride.Methods The concentration of levocetirizine dihydrochloride intermediate solution to be tested was determined by manual oral tasting using berberine hydrochloride as the reference formulation.The type of sweetener and the type and amount of cyclodextrin were determined by principal component analysis and calculation of standardized Euclidean distances for the electron tongue measurement signal values.Fourier transform infrared spectroscopy,differential scanning calorimetry(DSC),and scanning electron microscopy(SEM)were used to characterize the freeze-dried cyclodextrin inclusion complex powder.After masking the taste withβ-cyclodextrin and sucralose,the levocetirizine hydrochloride solution was orally tasted to verify the masking effect.Results The concentration of levocetirizine dihydrochloride intermediate solution to be tested was 1.25 mg·mL−1.Of the five sweeteners,sucralose was more effective and safer in masking the taste,the addition amount in the intermediate solution is 0.3%.Totally 8 times the amount ofβ-cyclodextrin was sufficient to mask the bitter taste of the drug during the use of cyclodextrin.The characterization results show that the cyclodextrin inclusion complex was successfully prepared.The results of oral tasting by volunteers showed that the bitter taste was completely masked.Conclusion The use of electronic tongue technology allows for taste masking studies of levocetirizine dihydrochloride and is simple,time consuming,objective and provides realistic and reliable results.