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目的优选脑得生有效部位的固体分散体制备工艺,并考察脑得生固体分散体胶囊质量。方法分别以聚乙二醇(PEG6000)、交联聚乙烯吡咯烷酮(PVP-K30)和葡萄糖-PEG4000为载体,采用熔融法制备药粉-载体不同比例(2:1、1:1、1:2、1:3、1:5)的固体分散体。采用差热分析法对脑得生固体分散体进行验证,并采用UV法比较脑得生固体分散体胶囊、物理混合物胶囊及普通胶囊的体外溶出度。此外,对脑得生固体分散体胶囊进行装量差异、水分、崩解时限及分散均匀度检查。结果脑得生固体分散体的最佳载体为PEG6000;药粉与PEG6000的最佳比例为1:2。差热分析法测定结果表明,熔融法制备的脑得生-PEG6000固体分散体形成了低共熔物。UV法测定结果表明,与普通胶囊及物理混合物胶囊相比,脑得生制成固体分散体胶囊后体外溶出速度提高更大,溶出效果最好。此外,所制脑得生固体分散体胶囊经检测符合中国药典项(2015年版)下胶囊剂和固体分散体的各项检查和质量评定。结论将脑得生制备成固体分散体能提高其体外溶出度,为复方脑得生的二次开发提供实验依据。
Objective To optimize the process of preparation of solid dispersions in effective part of brain and investigate the quality of solid dispersions capsules. Methods Polyethylene glycol (PEG6000), cross-linked polyvinylpyrrolidone (PVP-K30) and glucose-PEG4000 were respectively used as carriers to prepare powder-carriers with different ratios of 2: 1, 1: 3, 1: 5). Differential thermal analysis of brain solid dispersion was validated, and UV solid-state dispersion of solid dispersion capsules, physical mixture capsules and capsules in vitro dissolution. In addition, the brain solid dispersion of solid capsules were loaded volume differences, moisture, disintegration time and dispersion uniformity inspection. Results The best carrier of brain-derived solid dispersion was PEG6000; the optimal ratio of powder to PEG6000 was 1: 2. The results of differential thermal analysis showed that the eutectic-PEG6000 solid dispersion prepared by the melt method formed a eutectic. UV results show that, compared with ordinary capsules and physical mixture capsules, the brain produced a solid dispersion capsule dissolution rate increased more in vitro dissolution the best. In addition, the resulting solid-solid dispersion capsules were tested to conform to the inspections and quality evaluations of capsules and dispersions under the Chinese Pharmacopoeia (2015 edition). Conclusion The preparation of the brain into a solid dispersion can improve its in vitro dissolution rate, and provide experimental evidence for the secondary development of compound brain.