Oral colon-targeting preparation can achieve targeted drug release in the lesion site and have a great application prospect. In this study, we presented the principle of particle design in the field of materials science into the preparation of colon-targeting preparation. Enzymatic Pulsatilla saponins Colon-targeting composite Microparticles (EPCM) were prepared by mechanical grinding without any organic solvent. Firstly, Response Surface Methodology (RSM) designed by Box-Behnken was used to optimize the preparation process of EPCM, and the structure of EPCM was characterized. All-Atomic and Molecular Dynamics (AAMD) was used to calculate the compatibility between drugs and coating materials before and after release, so as to explain the principle of colon- targeted drug release in this method. Then, colon-targeting characteristics of EPCM in vitro and in vivo were investigated by experiments. Finally, the pharmacodynamics effects of this composite microparticles on Ulcerative Colitis (UC) induced by DSS in C57BL/6 mice were evaluated. The results demonstrated that the colon-targeting composite microparticles could be prepared by mechanical grinding based on particle design principle. The composite microparticles have appropriate colon-targeting drug release performance in vitro and in vivo, and have good anti-ulcerative colitis effect. This study provides a new idea for the preparation of oral colon-targeting preparation of Traditional Chinese medicine, and has evident reference value for the study of coating isolation and powder modification of traditional Chinese medicine for other purposes.

口服结肠靶向制剂可在病灶部位实现靶向药物释放，具有很大的应用前景。在这项研究中，我们将材料科学领域的粒子设计原理引入结肠靶向制剂的制备中。酶促白头翁皂苷结肠靶向复合微粒（EPCM）通过机械研磨制备，不使用任何有机溶剂。首先，利用Box-Behnken设计的响应面法（RSM）对EPCM的制备工艺进行优化，并对EPCM的结构进行了表征。利用全原子分子动力学（AAMD）计算药物与包衣材料在释放前后的相容性，从而解释该方法中结肠靶向药物释放的原理。然后，通过实验研究了EPCM在体外和体内的结肠靶向特性。最后，评估了这种复合微粒对 DSS 在 C57BL/6 小鼠中诱导的溃疡性结肠炎 (UC) 的药效学影响。结果表明，基于颗粒设计原理，可以通过机械研磨制备结肠靶向复合微粒。该复合微粒在体外和体内均具有适当的结肠靶向药物释放性能，具有良好的抗溃疡性结肠炎作用。本研究为中药口服结肠靶向制剂的制备提供了新思路，对其他用途的中药包衣分离和粉体改性研究具有明显的参考价值。最后，评估了这种复合微粒对 DSS 在 C57BL/6 小鼠中诱导的溃疡性结肠炎 (UC) 的药效学影响。结果表明，基于颗粒设计原理，可以通过机械研磨制备结肠靶向复合微粒。该复合微粒在体外和体内均具有适当的结肠靶向药物释放性能，具有良好的抗溃疡性结肠炎作用。本研究为中药口服结肠靶向制剂的制备提供了新思路，对其他用途的中药包衣分离和粉体改性研究具有明显的参考价值。最后，评估了这种复合微粒对 DSS 在 C57BL/6 小鼠中诱导的溃疡性结肠炎 (UC) 的药效学影响。结果表明，基于颗粒设计原理，可以通过机械研磨制备结肠靶向复合微粒。该复合微粒在体外和体内均具有适当的结肠靶向药物释放性能，具有良好的抗溃疡性结肠炎作用。本研究为中药口服结肠靶向制剂的制备提供了新思路，对其他用途的中药包衣分离和粉体改性研究具有明显的参考价值。结果表明，基于颗粒设计原理，可以通过机械研磨制备结肠靶向复合微粒。该复合微粒在体外和体内均具有适当的结肠靶向药物释放性能，具有良好的抗溃疡性结肠炎作用。本研究为中药口服结肠靶向制剂的制备提供了新思路，对其他用途的中药包衣分离和粉体改性研究具有明显的参考价值。结果表明，基于颗粒设计原理，可以通过机械研磨制备结肠靶向复合微粒。该复合微粒在体外和体内均具有适当的结肠靶向药物释放性能，具有良好的抗溃疡性结肠炎作用。本研究为中药口服结肠靶向制剂的制备提供了新思路，对其他用途的中药包衣分离和粉体改性研究具有明显的参考价值。并具有良好的抗溃疡性结肠炎作用。本研究为中药口服结肠靶向制剂的制备提供了新思路，对其他用途的中药包衣分离和粉体改性研究具有明显的参考价值。并具有良好的抗溃疡性结肠炎作用。本研究为中药口服结肠靶向制剂的制备提供了新思路，对其他用途的中药包衣分离和粉体改性研究具有明显的参考价值。