盐酸小檗碱树脂复合物冻干口崩片的制备及质量评价  

Preparation and Quality Evaluation of Berberine Hydrochloride Resin Complex Lyophilized Oral Disintegration Tablets

作　　者：朱笑颜 戴俊东[1] 郭鹏川 吴师月 周琦人 ZHU Xiaoyan;DAI Jundong;GUO Pengchuan;WU Shiyue;ZHOU Qiren(School of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 102488,China)

机构地区：[1]北京中医药大学中药学院,北京102488

出　　处：《中国药学杂志》2024年第8期724-731,共8页Chinese Pharmaceutical Journal

摘　　要：目的以盐酸小檗碱为模型药物,Kyron-T114为载药树脂,制备盐酸小檗碱树脂复合物以实现对冻干口崩片的良好掩味效果。方法采用静态制备法,制备药物树脂复合物,绘制吸附等温线、吸附动力学曲线研究树脂的吸附机理,通过扫描电镜(SEM)、差示扫描量热法(DSC)、X射线衍射法(XRD)和傅立叶红外光谱法(FTIR)对制得的树脂复合物进行物性表征。采用冻干赋型技术,制备盐酸小檗碱与树脂复合物口腔崩解片,对其体外溶出度研究与掩味效果进行评价。结果制得的盐酸小檗碱树脂复合物载药量为43.04%,药物在树脂上的吸附为多分子层的化学吸附。盐酸小檗碱粉末的溶出主要受溶解度的影响,其溶出机制以Fick扩散为主。树脂复合物粉末的溶出主要受溶液pH和离子浓度及种类影响,人工胃液中,药物从树脂中快速解离,薄膜扩散成为溶出的限速步骤;水、人工唾液、pH 4.5和pH 6.8的人工肠液中药物解离速度较慢,粒子扩散成为溶出的限速步骤。树脂复合物冻干口崩片在人工唾液中的溶出显著低于盐酸小檗碱冻干口崩片,经感官评价与电子舌检测,证明其具有良好的矫味效果。结论盐酸小檗碱树脂复合物冻干口崩片掩味效果较好,且弱阳离子交换树脂Kyron-T114制备的树脂复合物有利于改善难溶性药物在人工胃液中的溶出,进而改善其口服生物利用度,为中药的掩味提供新的思路。OBJECTIVE To prepare berberinehydrochloride resincomplex for good taste-masking effectof lyophilized oraldisintegration tablets using berberine hydrochloride as a model drug and using Kyron-T114 as the drug-loaded resin.METHODS The drug-resin composites were prepared by using the static method.Then drawn the adsorption isotherm and adsorption kinetic curves to study the adsorption mechanism of the resin.Afterwards,the characteristic of the berberine hydrochloride resin complex was studied by using the SEM,DSC,XRD and FTIR.Finally,prepared the oral disintegration tablets of berberine hydrochloride and its resin complex by using the lyophilized extrusion technology.Next,studied the in vitro release experiments and evaluated the effect of masking taste.RESULTS According to the research,a berberine hydrochloride-resin complex with the drug loaded of 43.04%was prepared.And the analysis showed that the adsorption of the drug on the resin was the multilayered chemical adsorption.The dissolution of berberine hydrochloride′s powder is mainly affected by the solubility of berberine hydrochloride.Moreover,the dissolution mechanism is mainly based on Fick diffusion.The dissolution of berberine hydrochloride′s powder is mainly affected by the pH of the solution,along with the concentration and the type of the ion in the solution.In artificial gastric juice,the drug dissociates rapidly from the resin.So the film diffusion was the rate-limiting step for dissolution.On the contrary,the drug dissociated slowly in the water,artificial saliva,artificial intestinal fluids including pH 4.5 and pH 6.8.So the particle diffusion was the rate-limiting step for dissolution.Besides,the dissolution of lyophilized oral disintegration tablets of drug-resin complexes in artificial saliva was significantly lower than that of berberine hydrochloride oral disintegration tablets.Lastly,the results from sensory evaluation and electronic tongue detection proved that the lyophilized oral disintegration tablets of berberine hydrochloride-resin com

关 键 词：盐酸小檗碱 离子交换树脂 Kyron-T114 掩味作用 药物树脂复合物 

分 类 号：R944[医药卫生—药剂学]