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目的:对盐酸美金刚缓释微丸进行处方优化,并考察其体外释放。方法:采用流化床技术制备盐酸美金刚缓释微丸,以进风温度、雾化压力和喷液流速为考察因素,以上药百分率为评价指标,采用正交试验优选微丸上药工艺参数。采用Box-Behnken效应面法优化缓释包衣处方及包衣增重。以乙基纤维素水分散体的含量、聚乙二醇6000(PEG 6000)含量及包衣增重为因素,以盐酸美金刚2,6,12 h的累计释放度为响应值,采用Box-Behnken效应面法优化盐酸美金刚缓释微丸的包衣处方及包衣增重,对盐酸美金刚缓释微丸进行释放度考察。结果:最佳的微丸上药工艺参数为:进风温度45℃,雾化压力1.0 bar,喷液流速1.5 r·min~(-1)。最佳缓释包衣处方为:乙基纤维素水分散体含量为8.4%,PEG 6000含量为2.3%,缓释层包衣增重16.7%。盐酸美金刚缓释微丸具有良好的缓释效果。结论:正交试验和Box-Behnken效应面法可用于盐酸美金刚缓释微丸处方工艺的优化,所建立的拟合模型具有较好的预测性。
Objective: To optimize the formulation of memantine hydrochloride sustained-release pellets and investigate its in vitro release. Methods: The fluidized bed technique was used to prepare memantine hydrochloride sustained-release pellets. The inlet air temperature, atomization pressure and jet flow rate were used as the investigation factors. Taking the percentage of the above drugs as the evaluation index, orthogonal test was used to optimize the process parameters . Optimization of sustained-release coating and weight gain by Box-Behnken effect surface method. Taking the content of ethyl cellulose aqueous dispersion, the content of PEG 6000 and the weight gain of the coating as the factors, the cumulative release of memantine hydrochloride for 2, 6, 12 h was taken as the response value, Behnken effect surface method was used to optimize the coating prescription and coating weight gain of memantine hydrochloride sustained-release pellets, and the release rate of memantine hydrochloride sustained-release pellets was investigated. Results: The optimal parameters of the pellets were as follows: air inlet temperature 45 ℃, atomization pressure 1.0 bar, jet velocity 1.5 r · min -1. The best prescription for sustained-release coating is as follows: the content of ethyl cellulose aqueous dispersion is 8.4%, the content of PEG 6000 is 2.3% and the weight of sustained-release coating is 16.7%. Memantine hydrochloride sustained-release pellets have a good sustained-release effect. Conclusion: Orthogonal test and Box-Behnken effect surface method can be used to optimize the prescription of memantine hydrochloride sustained-release pellets. The fitted model has good predictability.