一种寡糖胶囊剂的制备及升高白细胞作用的研究

摘要：目的：制备低聚甘露糖醛酸钠（DPM207）胶囊剂，对其质量进行考察，并初步评价其改善白细胞减少的效果。方法：采用湿法制粒，以辅料的种类、用量为考察因素，以吸湿性、休止角、颗粒得率等为评价指标，优化胶囊剂的制备工艺。根据《中国药典》等相关规定，对胶囊剂的水分含量、装量差异、溶出度、含量等进行测定。采用辐照所致白细胞减少的动物模型对DPM207升高白细胞的效果进行评价。结果：DPM207胶囊剂的最佳成型工艺为：低聚甘露糖醛酸钠与微晶纤维素按照1:1混合，添加70%乙醇进行湿法制粒，制备的胶囊水分、装量差异、溶出度等均符合2020版《中国药典》规定。在小鼠灌胃给药5日后，DPM207不同剂量组均显著提高血液中白细胞的数量。结论：DPM207胶囊剂成型工艺稳定，胶囊质量可控，具有作为升高白细胞药物的潜力。

The study of oligosaccharide capsules preparation and increasing leukocytes effect

Abstract: Objective: To prepare oligomannuronic acid sodium (DPM207) capsules and evaluate its quality and effect on leukopenia. Methods: According to the hygroscopicity, angle of repose and particle yield, the type and content of excipients were investigated to optimize the preparation process of the capsules by wet granulation. According to the Chinese Pharmacopoeia, the water content, packing amount divergence, dissolution rate, and API content of the capsules were examined. The effect on leukopenia was evaluated by animal model induced by cyclophosphamide. Results: The optimal preparation process for DPM207 capsules was oligomannuronic acid sodium mixed with microcrystalline cellulose in a ratio of 1:1, and 70% ethanol by wet granulation. The moisture content, packing amount divergence, and dissolution rate of DPM207 capsules met the criterion of the Chinese Pharmacopoeia. The different dose groups of DPM207 could significantly increase the number of leukocytes after intragastric irradiation administration for 5 days. Conclusion: The preparation process of DPM207 capsules was stable, and the quality of the capsules was controllable. DPM207 had the potential to be a drug for increasing leukocytes.