摘要
目的制备氢溴酸右美沙芬树脂复合物,初步考察药物树脂复合物体外释放的影响因素。方法本研究起止时间为2018年9月至2019年6月,以树脂载药量和药物利用率为指标,通过单因素考察法,筛选了树脂型号、交换温度、药物浓度、药物与树脂的配比、交换时间、交换介质的离子强度等因素对药物树脂复合物制备的影响。采用场发射扫描电子显微镜(FESEM),差示扫描热分析法(DSC)对树脂结构及药物与树脂的结合方式进行剖析。结果成功制备了氢溴酸右美沙芬树脂复合物,优选AMBERLITE IRP 69树脂,交换温度为40℃,药物浓度为3.0%,药物与树脂的配比为1∶1,交换时间为480min,交换介质为水。药物树脂复合物在pH1.0盐酸溶液(含0.4 mol/L氯化钾)中8 h的释放达到99.40%,在pH4.0醋酸盐缓冲液(含0.4 mol/L氯化钾)中8 h的释放达到100.14%,在pH6.8磷酸盐缓冲液(含0.4 mol/L氯化钾)中8 h的释放达到97.98%。结论最优制备工艺下,树脂载药量达到933.2 mg/g,药物利用率为93.30%。药物与树脂的结合方式为离子键结合,药物树脂复合物的释放受离子强度的影响。
Objective To prepare Dextromethorphan Hydrobromide resin complex and to make a preliminary study on factors influ encing the in vitro release of drug resin complex.Methods The study was conducted from September 2018 to June 2019.With res in exchange capacity and drug utilization rate as indicators,the effects of resin type,exchange temperature,drug concentration,drug resin ratio,exchange time and ion strength of exchange medium on the preparation of drug resin composite were screened by single factor method.Field emission scanning electron microscopy(FESEM)and differential scanning calorimetry(DSC)were used to an alyze the structure of the resin complex and the binding mode of the drug with the resin.Results Dextromethorphan hydrobromide resin complex was successfully prepared.AMBERLITE IRP 69 resin was selected.The exchange temperature was 40℃,the concen tration of drug was 3.0%,the ratio of drug to resin was 1:1,the exchange time was 480 minutes,and the exchange medium was wa ter.The release of drug resin complex reached 99.40%,100.14%and 97.98%respectively in pH 1.0 hydrochloric acid solution(containing 0.4mol/L KCl),pH 4.0 acetate buffer(containing 0.4 mol/L KCl),and pH 6.8 phosphate buffer(containing 0.4 mol/L KCl)at 8h.Conclusions Under the optimum preparation process,drug loading of resin reached 933.2mg/g and drug utilization rate was 93.30%.The binding mode of drug and resin is ion bonding.The release of drug resin complex is influenced by ionic strength.
作者
严家丽
苏峰
李颖
鲁胜男
桂双英
何广卫
YAN Jiali;SU Feng;LI Ying;LU Shengnan;GUI Shuangying;HE Guangwei(Anhui University of Chinese Medicine,Hefei,Anhui 230012,China;Hefei Industrial Pharmaceutical Institute Co.,Hefei,Anhui 230088,China)
出处
《安徽医药》
CAS
2020年第4期661-665,共5页
Anhui Medical and Pharmaceutical Journal
关键词
迟效制剂/化学合成
氢溴酸
右美沙芬
树脂类
合成
分析样品制备方法
制备工艺
Delayed action preparations/chemical synthesis
Hydrobromic acid
Dextromethorphan
Resins
synthetic
Ana lytic sample preparation methods
Preparation technology
