目的 研究不同種類及用量的矯味劑對鹽酸左西替利嗪口味的改善情況，以達(dá)到掩蓋其苦味的目的。方法 以鹽酸小檗堿作為參比制劑，通過人工口嘗的方式確定鹽酸左西替利嗪待測中間體溶液濃度；通過對電子舌測定信號值進(jìn)行主成分分析及計算標(biāo)準(zhǔn)化歐式距離確定甜味劑種類及環(huán)糊精的種類及用量；采用傅里葉紅外光譜法、差示掃描量熱法（DSC）、掃描電子顯微鏡（SEM）技術(shù)對凍干干燥后的環(huán)糊精包合物粉末進(jìn)行表征；對添加三氯蔗糖、β-環(huán)糊精掩味之后的鹽酸左西替利嗪溶液進(jìn)行口嘗，對掩味效果進(jìn)行驗證。結(jié)果 鹽酸左西替利嗪待測中間體溶液質(zhì)量濃度為1.25 mg·mL^-1；三氯蔗糖掩味效果較好且更為安全，中間體溶液中的添加量為0.3%；8倍量的β-環(huán)糊精可以掩蓋藥物的苦味；表征結(jié)果顯示，鹽酸左西替利嗪β-環(huán)糊精包合物制備成功；志愿者口嘗結(jié)果表明，添加了三氯蔗糖、β-環(huán)糊精掩味之后的鹽酸左西替利嗪溶液苦味已完全被掩蓋。結(jié)論 利用電子舌技術(shù)可以對鹽酸左西替利嗪進(jìn)行掩味研究，且操作簡單、耗時短，客觀性較強，結(jié)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 with β-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 of β-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.

R943

國家科技重大專項研發(fā)項目（2011ZX09201-201-15）；北京市科技計劃專項研發(fā)項目（Z16010101390）