摘要
目的制备伪麻黄碱树脂复合物,考察其处方工艺参数,并评价伪麻黄碱树脂复合物的防潮性能。方法采用批式离子交换法制备伪麻黄碱树脂复合物,通过考察离子交换树脂对药物的利用率和树脂复合物的载药量的相互关系来优选最佳药物浓度、最佳树脂用量以及最佳反应温度;通过光学显微镜观察药物树脂复合物的形态外观;通过X-ray衍射分析、差示扫描量热分析探讨药物树脂复合物的形成机制;通过吸湿平衡曲线评价伪麻黄碱树脂复合物的防潮性能。结果离子交换树脂、盐酸伪麻黄碱和纯化水三者的用量对所得伪麻黄碱树脂复合物的载药量以及离子交换树脂对药物的利用率有着直接影响,从节约成本考虑,三者的质量投料比为10:2:100是比较合适的。经X-ray衍射和DSC分析,伪麻黄碱树脂复合物是以化学键的形式结合药物的。伪麻黄碱树脂复合物具有良好的防潮性能,当外界相对湿度增加时,也不会导致吸潮液化问题。结论以离子交换树脂为载体制备的伪麻黄碱树脂复合物具有良好的防潮性能。
OBJECTIVE To prepare the pseudoephedrine-resinate complex, and assess its moistureproofcapability. METHODS Using an ion exchange resin （IER） as a cartier, the pseudoephedrine-resinate complex was prepared by a batch process. The drug concentration, drug/IER ratio and reactive temperature for the pseudoephedrine-resinate complex was optimized according to the drug-loading capacity of the pseudoephedrine-resinate complex and the drug adsorption efficiency of the IER. The pseudoephedrine-resinate complex was characterized by the morphology which was observed using a optical microscope. X-ray diffraction analysis and differential scanning calorimetry analysis were employed to confirm the formation mechanism of the pseudoephedrine-resinate complex. The moistureproof capability of the pseudoephedrine-resinate complex under different humidity environments was investigated. RESULTS The amount of IRE, pseudoephedrine hydrochloride and purified water showed a direct impact on the drug-loading capacity of the pseudoephedrine-resinate complex and the drug adsorption efficiency of the IER. From the prospective of saving industrial production costs, the ratio of the three materials was reasonable for 10 ： 2 ： 100. By X-ray diffraction analysis and differential scanning calorimetry analysis, the drug in pseudoephedrine-resinate complex was combined with ion-exchange resins by chemical bond. The moisture absorption- liquefaction problem of the capsules containing pseudoephedrine hydrochloride was successfully solved by the pseudoephedrine-resinate complex. CONCLUSION The pseudoephedrine-resinate complex could be prepared by batch method of ion exchange and had good moistureproof capability under high humidity environment.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2009年第18期1395-1399,共5页
Chinese Pharmaceutical Journal
关键词
伪麻黄碱
离子交换树脂
药物树脂复合物
制备
防潮
pseudoephedrine
ion exchange resin
drug-resinate complex
preparation
moistureproof capability
