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目的:制备κ-卡拉胶-壳聚糖聚电解质凝胶微丸,考察处方工艺因素对其体外释药的影响。方法:以黄芩苷为模型药物,采用离子胶凝法制备κ-卡拉胶-壳聚糖微丸;通过κ-卡拉胶与壳聚糖形成复合物条件研究,确定微丸中κ-卡拉胶与壳聚糖质量比;通过体外释放度测定,考察κ-卡拉胶浓度、药物与κ-卡拉胶比例、胶凝液氯化钾浓度、胶凝时间和干燥方式等处方工艺因素对微丸药物释放的影响。结果:κ-卡拉胶-壳聚糖凝胶微丸中κ-卡拉胶与壳聚糖质量比为6∶4;微丸在0.1 mol.L-1盐酸溶液中2 h仅释放约10%,在PBS液中药物释放加快,具有缓慢释药特性;随κ-卡拉胶浓度、氯化钾浓度和药物与κ-卡拉胶比例提高,微丸释药速度减慢;随胶凝时间延长,微丸释药速度减慢,当胶凝时间延长至1 h后,影响不显著;冷冻干燥法制得微丸释药速度明显快于烘箱常压干燥和真空干燥,后两者对微丸释药速度影响不显著。结论:κ-卡拉胶-壳聚糖聚电解质凝胶微丸具有缓慢释药特性,通过其处方工艺可调节微丸释药速度。
OBJECTIVE: To prepare κ-carrageenan-chitosan polyelectrolyte gel pellets and investigate the effect of prescription factors on drug release in vitro. Methods: With baicalin as a model drug, κ-carrageenan-chitosan pellets were prepared by ionic gelation method. The condition of complex formation of κ-carrageenan and chitosan was studied to determine the relationship between κ-carrageenan and Chitosan mass ratio. The drug release of pellets was determined by in vitro release test, such as the concentration of κ-carrageenan, the ratio of drug to κ-carrageenan, the concentration of potassium chloride in the gel, the gelation time and the drying method Impact. RESULTS: The mass ratio of κ-carrageenan to chitosan in κ-carrageenan-chitosan gel pellets was 6: 4. The pellets released only about 10% in 0.1 mol·L-1 hydrochloric acid solution for 2 h, The drug release in PBS solution accelerated with sustained release characteristics. With the increase of κ-carrageenan concentration, potassium chloride concentration and the ratio of drug to κ-carrageenan, the release rate of the pellets slowed down. With the prolongation of gel time The release rate of pellets slowed down. When the gelation time was prolonged to 1 h, the effect was insignificant. The release rate of pellets prepared by freeze-drying was significantly faster than that of oven under atmospheric pressure and vacuum drying. The effect is not significant. Conclusion: The κ-carrageenan-chitosan polyelectrolyte gelled pellets have the characteristics of slow release, and the release rate of the pellets can be regulated by the prescription process.