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目的应用表面降解溶蚀释药模型,指导他克莫司缓释微丸的处方设计,提高设计的准确性和针对性。方法采用单纯形重心设计法,确立处方配比与表面降解速率常数K值的关系,建立起释药模型释放度预测与制剂处方的关联,根据预期的释放度要求,实现对处方设计的指导。并采用热熔包衣技术制备他克莫司缓释微丸,对模型预测和实验测定的释放曲线进行比较。结果测定和预测的释放曲线相似因子f2>75,释放度单点误差<5%。结论本实验所建模型,可根据释放度要求,快速、准确地指导他克莫司缓释微丸的处方设计。
Objective To study the prescription design of tacrolimus sustained-release pellets and to improve the accuracy and pertinence of the design by applying the dissolution-release model of surface degradation and dissolution. Methods The simplex centroid design method was used to establish the relationship between the prescription ratio and the rate constant K of the surface degradation. The correlation between the release rate prediction of drug release model and formulation prescription was established. According to the expected release requirement, the prescription design guidance was achieved. Tacrolimus sustained-release pellets were prepared by hot-melt coating technique, and the release curves of the model prediction and experiment were compared. The results of the determination and prediction of the release curve similarity factor f2> 75, single point error of release <5%. Conclusion The model of this experiment can be used to guide the formulation of tacrolimus sustained-release pellets quickly and accurately according to the requirements of release.