Objective To optimize the prescription and preparation process of rapidly disintegrating oral tablets of levoceririzine,and to establish the method of content analysis by HPCE.Methods ① The best preparation process of the tablet was screened by observing the wetting time and disintegration time through the following three methods:direct powder compression,adding disintegrants inside,and adding inside and outside.②The amount of the disintegrants,taste masking agent,taste correcting agents and fillers was screened by orthogonal experiment to optimize the process conditions.③The effect of chiral selector type and concentration,buffer,pH,separation voltage and other factors on the separation was investigated by using HPCE method to analyze the content of levocetirizine in orally disintegrating tablets.Results ①The optimized preparation of rapidly disintegrating oral tablets of levocetirizine was direct powder compression method,and the best prescription was:levocetirizine (2.06 ％),β-CD (8.24 ％),mixtures of MCC + L-HPC (4∶1) (40％),PVPP (10％),mannifol (28.7％),aspartame (5％),and citric acid (6％).②The linear relationship between peak area (Y) and concentration (X) in the range of 1 ～50 μg/mL was good.The RSDs of precision test,stability test and recovery test were 0.69％,0.69％ and 0.53 ％,respectively.Conclusion This process for preparing a product has good appearance,rapid disintegration and good taste,with low production costs and technical requirements,which is suitable for industrial mass production.%目的 对左旋西替利嗪口腔速崩片的工艺处方进行优化,并建立其HPCE含量分析方法.方法 ①考察粉末直接压片法、内加崩解剂法、内外加崩解剂法3种制备工艺条件下各片剂的润湿时间及崩解时间,筛选最佳制备工艺;②采用正交试验对崩解剂、掩味剂、矫味剂和填充剂用量进行筛选,优化工艺条件;③采用HPCE法对口腔速崩片中的左旋西替利嗪进行含量分析,考察手性选择剂类型及浓度、缓冲液pH、分离电压等因素对分离的影响.结果 ①左旋西替利嗪口腔速崩片的最佳制备工艺为粉末直接压片法,最佳处方:左旋西替利嗪用量2.06％,β-CD用量8.24％,MCC+ L-HPC最佳配比为4∶1的混合物用量为40％,PVPP用量10％,甘露醇用量28.7％,阿斯巴甜用量5％,柠檬酸用量6％;②左旋西替利嗪溶液在1～ 50 μg/mL范围内,峰面积Y与浓度X呈良好线性关系,精密度RSD为0.69％,稳定性RSD为0.69％,回收率RSD为0.53％.结论 利用该工艺制备的成品具有较好的外观,崩解迅速,口感佳,且生产成本和技术要求不高,适合工业化大生产.
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