1种寡糖胶囊剂的制备及升高白细胞作用的研究  

The study of oligosaccharide capsule preparation and increasing leukocytes effect

作　　者：赵帅[1] 刘文晶 李红健 刘欢 许美杰 王世欣[1,2] 李春霞 ZHAO Shuai;LIU Wen-jing;LI Hong-jian;LIU Huan;XU Mei-jie;WANG Shi-xin;LI Chun-xia(Key Laboratory of Marine Drugs,Ministry of Education,Shandong Provincial Key Laboratory of Glycoscience and Glycotechnology,School of Medicine and Pharmacy,Ocean University of China,Qingdao 266003,China;Marine Biomedical Research Institute of Qingdao,Qingdao 266071,China;Laboratory for Marine Drugs and Bioproducts of Qingdao Pilot National Laboratory for Marine Science and Technology,Qingdao 266237,China)

机构地区：[1]中国海洋大学海洋药物教育部重点实验室,山东省糖科学与糖工程重点实验室医药学院,山东青岛266003 [2]青岛海洋生物医药研究院,山东青岛266071 [3]青岛海洋科学与技术试点国家实验室,海洋药物与生物制品功能实验室,山东青岛266237

出　　处：《中国海洋药物》2022年第6期41-48,共8页Chinese Journal of Marine Drugs

基　　金：国家自然科学基金项目(82104058);山东省重大科技创新专项(2018SDKJ0404)资助。

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,以休止角、吸湿性、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》(2020年版)等相关规定,对胶囊剂的水分含量、装量差异、活性药物成分含量、溶出度等进行测定。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质量比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《中国药典》(2020年版)规定。在小鼠灌胃给药5 d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。Objective To prepare oligomannuronic acid sodium(DPM207)capsule and evaluate its quality and effect on leukopenia.Methods According to the angle of repose and particle yield,hygroscopicity,the type and content of excipients were investigated to optimize the preparation process of the capsules by wet granulation.According to the Chinese Pharmacopoeia(2020),the water content,packing amount divergence,active pharmaceutical ingredient content and dissolution rate 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 weight 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(2020).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 capsule had the potential to be a drug delivery system for increasing leukocytes.

关 键 词：低聚甘露糖醛酸钠 胶囊剂 制备工艺 质量考察 升高白细胞 

分 类 号：R931.77[医药卫生—生药学]